47 CFR 25.262 - Licensing and domestic coordination requirements for 17/24 GHz BSS space stations.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 2 2010-10-01 2010-10-01 false Licensing and domestic coordination requirements for 17/24 GHz BSS space stations. 25.262 Section 25.262 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) COMMON CARRIER SERVICES SATELLITE COMMUNICATIONS Technical Standards § 25.262...

Comparative study of CD4 and CD45RO T cells and CD20 B cells in cerebrospinal fluid of syphilitic meningitis and tuberculous meningitis patients.

Science.gov (United States)

Yu, Nian; Zhang, Qiao-Quan; Zhang, Kang; Xie, Yuan; Zhu, Hai-Qing; Lin, Xing-Jian; Di, Qing

2016-09-01

This study was to investigate the differences of lymphocyte in the cerebrospinal fluid (CSF) of patients with syphilis meningitis (SM) and tuberculous meningitis (TBM) for new diagnostic insights. Totally, 79 cases of SM and 45 cases of TBM were enrolled. In the CSF, the CD4, CD45RO or CD20 positive lymphocytes were detected by immunohistochemistry. The proportion of CD4 T cells in the CSF lymphocytes in patients with SM was significantly higher than that in patients with TBM (p CD4 T-cell proportion in both groups (p CD45RO T cells in CSF lymphocytes of patients with SM was less than that of patients with TBM (p CD45RO T cells was increased in the CSF of both group patients (p cells in the CSF lymphocytes was not obviously different between the two groups during every stage. In conclusion, there are strong differences of CD4 and CD45RO T-cell ratio, but not the CD20 B cells in the meningitis. CD4 and CD45RO T cells in CSF are a useful complement in differentially diagnosing SM and TBM; it contributes to further understand the pathogenesis and prognosis of SM and TBM. © 2016 APMIS. Published by John Wiley & Sons Ltd.

47 CFR 25.224 - Protection of receive-only earth stations in the 17/24 GHz BSS.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 2 2010-10-01 2010-10-01 false Protection of receive-only earth stations in the 17/24 GHz BSS. 25.224 Section 25.224 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) COMMON CARRIER SERVICES SATELLITE COMMUNICATIONS Technical Standards § 25.224 Protection of...

Application Side Casing on Open Deck RoRo to Improve Ship Stability

Science.gov (United States)

Hasanudin; K. A. P Utama, I.; Chen, Jeng-Horng

2018-03-01

RoRo is a vessel that can transport passengers, cargo, container and cars. Open Car Deck is favourite RoRo Vessel in developing countries due to its small GT, small tax and spacious car deck, but it has poor survival of stability. Many accident involve Open Car Deck RoRo which cause fatalities and victim. In order to ensure the safety of the ship, IMO had applied intact stability criteria IS Code 2008 which adapted from Rahola’s Research, but since 2008 IMO improved criteria become probabilistic damage stability SOLAS 2009. The RoRo type Open Car Deck has wide Breadth (B), small Draft (D) and small freeboard. It has difficulties to satisfy the ship’s stability criteria. Side Casings which has been applied in some RoRo have be known reduce freeboard or improve ship’s safety. In this paper investigated the effect side casings to survival of intact dan damage ship’s stability. Calculation has been conducted for four ships without, existing and full side casings. The investigation results shows that defect stability of Open Deck RoRo can be reduce with fitting side casing.

Ilves osaleb ÜRO Peaassamblee 62. istungjärgul

Index Scriptorium Estoniae

2007-01-01

President Toomas Hendrik Ilves osaleb New Yorgis ÜRO peaassamblee 62. istungjärgu töös. Eesti riigipea osaleb ka ÜRO korraldatud kliimamuutuste konverentsil, kohtub ÜRO peasekretäri ja Makedoonia, Slovakkia ning Bosnia ja Hertsegoviina presidendiga, samuti filantroop George Sorosega ning osaleb Baltimaade riigipeade kohtumisel. T.H. Ilves külastab ka Columbia Ülikooli ning osaleb New Yorgi Eesti haridusseltsi korraldatud vastuvõtul New Yorgi Eesti Majas. Vabariigi President töövisiidil Ameerika Ühendriikides 20.-26.09.2007

Inhibitory Effects of Cytosolic Ca2+ Concentration by Ginsenoside Ro Are Dependent on Phosphorylation of IP3RI and Dephosphorylation of ERK in Human Platelets

Directory of Open Access Journals (Sweden)

Hyuk-Woo Kwon

2015-01-01

Full Text Available Intracellular Ca2+ ([Ca2+]i is platelet aggregation-inducing molecule and is involved in activation of aggregation associated molecules. This study was carried out to understand the Ca2+-antagonistic effect of ginsenoside Ro (G-Ro, an oleanane-type saponin in Panax ginseng. G-Ro, without affecting leakage of lactate dehydrogenase, dose-dependently inhibited thrombin-induced platelet aggregation, and the half maximal inhibitory concentration was approximately 155 μM. G-Ro inhibited strongly thrombin-elevated [Ca2+]i, which was strongly increased by A-kinase inhibitor Rp-8-Br-cAMPS compared to G-kinase inhibitor Rp-8-Br-cGMPS. G-Ro increased the level of cAMP and subsequently elevated the phosphorylation of inositol 1, 4, 5-triphosphate receptor I (IP3RI (Ser1756 to inhibit [Ca2+]i mobilization in thrombin-induced platelet aggregation. Phosphorylation of IP3RI (Ser1756 by G-Ro was decreased by PKA inhibitor Rp-8-Br-cAMPS. In addition, G-Ro inhibited thrombin-induced phosphorylation of ERK 2 (42 kDa, indicating inhibition of Ca2+ influx across plasma membrane. We demonstrate that G-Ro upregulates cAMP-dependent IP3RI (Ser1756 phosphorylation and downregulates phosphorylation of ERK 2 (42 kDa to decrease thrombin-elevated [Ca2+]i, which contributes to inhibition of ATP and serotonin release, and p-selectin expression. These results indicate that G-Ro in Panax ginseng is a beneficial novel Ca2+-antagonistic compound and may prevent platelet aggregation-mediated thrombotic disease.

Effect of the scale inhibitor on ion content in reverse osmosis system for seawater desalination

Science.gov (United States)

Gao, Yuhua; Liu, Zhenfa; Zhang, Lihui; Li, Haihua

2017-09-01

A scale inhibitor was synthesized from polysuccinimide with 2-aminoethanesulfonic acid and aspartic acid. The effect of scale inhibitor on ion content in reverse osmosis system for seawater desalination was studied. The results showed that the ion content of permeate water is lower with the scale inhibitor added in RO system for seawater desalination than without scale inhibitor. On the contrary, the ion content of concentrate water is higher when with scale inhibitor in RO system.

Probabilistic Analysis of Collision Damages with Application to ro-Ro Passenger Vessels

DEFF Research Database (Denmark)

Pedersen, Preben Terndrup; Hansen, Peter Friis; Nielsen, Lars Peter

1997-01-01

To quantify the risks involved in Ro-ro passenger vessel traffic, rational criteria for prediction and evaluation of collision accidents have to be developed. This implies that probabilities as well as the inherent consequences have to be analyzed and assessed.The present report outlines a method...... for evaluation of the probability of a Ro-Ro passenger vessel on a given route being struck by another ship. Given a collision has taken place the spatial distribution of the collision damages is calculated. Results are presented in terms of probability distributions, for indentation depth, length and height...... of the holes and for the vertical location. The main benefit of the formulated procedure is that it allows comparisons of various navigation routes by assessing the relative frequencies of collisions. The derived procedure is applied to two typical Ro-Ro passenger vessel routes....

Environmental Performance Evaluation of Ro-Ro Passenger Ferry Transportation

DEFF Research Database (Denmark)

Kristensen, Hans Otto Holmegaard; Hagemeister, Constantin

2012-01-01

/or emissions per transport unit, is related to the same unit for the different transport forms. For Ro-Ro passenger ferries it can be difficult to find a suitable common transport unit, as they often transport a mix of cargo, such as passengers, passenger cars, trucks, lorries, busses and other rolling...

123I-labeling and evaluation of Ro 43-0463, a SPET tracer for MAO-B imaging

International Nuclear Information System (INIS)

Beer, H.-F.; Rossetti, I.; Frey, L.D.; Hasler, P.H.; Schubiger, P.A.

1995-01-01

Using the copper assisted halogen exchange the MAO-B inhibitor Ro 43-0463, N-(2-aminoethyl)-5-iodo-2-pyridinecarboxamide, was labelled with 123 I as well as with 125 I to allow in vitro and in vivo investigations including SPET with healthy volunteers. Ro 43-0463 is known to inhibit reversibly and specifically MAO-B, having an ic 50 of 3 x 10 -8 Mol/L. The labeling in the presence of CuSO 4 and ascorbic acid was optimised, varying time (30 to 105 min), precursor concentration (1-3.5 mg) and temperature (130-200 deg. C). The labeling yield ranged between 60 and 70%. Purification was achieved with Lichrosorb RP-18 (5 μm, 250 x 8 mm) and 1.5 mL/min 0.36 M H 3 PO 4 /EtOH (97(3)) [0.01 M (NH 4 ) 2 HPO 4 ]. After neutralisation and sterile filtration the final activity concentration ranged between 18.5 and 37 MBq/mL. Biodistribution studies showed a brain to blood ratio greater than 1 within 1 h p.i. The main radiation burden calculated from these animal data is to alimentary and excretory organs and the ovaries. Autoradiography was performed using rat brain slices and 5 nM [ 125 I]Ro 43-0463 in TRIS-buffer pH 7.4 for 90 min at 20 deg. C. Its radioactivity pattern corresponds to the known distribution of MAO-B in the rat brain. By displacement with L-deprenyl the highly specific binding of Ro 43-0463 was proven in vitro. SPECT studies with normal volunteers corresponded with the pattern found in autoradiography

The Assessment of the Ultimate Hull Girder Strength of RO-RO Ship after Damages

Science.gov (United States)

Zubair Muis Alie, Muhammad; Sitepu, Ganding; Izaak Latumahin, Samuel

2018-03-01

Many accidents of Ro-Ro ships happen in Indonesia such as collision and grounding. When the collision or grounding takes place on the Ro-Ro ship, the ultimate strength of hull structure after damage becomes decrease. Car and passenger decks are critical location since collision and/or grounding occur. In the present study, the assessment of the ultimate hull girder strength is conducted. The cross section of Ro-Ro ship is taken to be analyzed. The collision and grounding damages are assumed to be palced on the side and bottom area, respectively. The damages are created by removing the element from the side shell and bottom part. Finally, the result obtained is compared with one another.

Retroviral proteinases and their inhibitors

Czech Academy of Sciences Publication Activity Database

Sedláček, Juraj

2000-01-01

Roč. 3, 3,4 (2000), s. 23-24 [ Proteolytic enzymes and their inhibitors in physiology and pathogenesis. 14.09.2000, Plzen] Institutional research plan: CEZ:AV0Z5052915 Subject RIV: EB - Genetics ; Molecular Biology

ps-ro Fuzzy Open(Closed Functions and ps-ro Fuzzy Semi-Homeomorphism

Directory of Open Access Journals (Sweden)

Pankaj Chettri

2015-11-01

Full Text Available The aim of this paper is to introduce and characterize some new class of functions in a fuzzy topological space termed as ps-ro fuzzy open(closed functions, ps-ro fuzzy pre semiopen functions and ps-ro fuzzy semi-homeomorphism. The interrelation among these concepts and also their relations with the parallel existing concepts are established. It is also shown with the help of examples that these newly introduced concepts are independent of the well known existing allied concepts.

Vabariigi President esines ÜRO Peaassambleel

Index Scriptorium Estoniae

2007-01-01

ÜRO Peaassamblee 62. istungjärgul kõneles president Toomas Hendrik Ilves kliimamuutuse, küberjulgeoleku, kriiside reguleerimise ja rahvusvaheliste organisatsioonide koostöö teemadel. Ilmunud ka: Koit 29. sept. 2007, lk. 6; Eesti Elu 28. sept. 2007, lk. 2; ingl. k. Vaba Eesti Sõna 4. okt. 2007, lk. 12, pealk.: The President of the Republic Spoke to the UN General Assembly. Vabariigi President töövisiidil Ameerika Ühendriikides 20.-26.09.2007

47 CFR 25.223 - Off-axis EIRP spectral density limits for feeder link earth stations in the 17/24 GHz BSS.

Science.gov (United States)

2010-10-01

... 47 Telecommunication 2 2010-10-01 2010-10-01 false Off-axis EIRP spectral density limits for feeder link earth stations in the 17/24 GHz BSS. 25.223 Section 25.223 Telecommunication FEDERAL COMMUNICATIONS COMMISSION (CONTINUED) COMMON CARRIER SERVICES SATELLITE COMMUNICATIONS Technical Standards § 25...

Preclinical Evaluation of 18F-RO6958948, 11C-RO6931643, and 11C-RO6924963 as Novel PET Radiotracers for Imaging Tau Aggregates in Alzheimer Disease.

Science.gov (United States)

Honer, Michael; Gobbi, Luca; Knust, Henner; Kuwabara, Hiroto; Muri, Dieter; Koerner, Matthias; Valentine, Heather; Dannals, Robert F; Wong, Dean F; Borroni, Edilio

2018-04-01

Tau aggregates and amyloid-β (Aβ) plaques are key histopathologic features in Alzheimer disease (AD) and are considered targets for therapeutic intervention as well as biomarkers for diagnostic in vivo imaging agents. This article describes the preclinical in vitro and in vivo characterization of 3 novel compounds-RO6958948, RO6931643, and RO6924963-that bind specifically to tau aggregates and have the potential to become PET tracers for future human use. Methods: RO6958948, RO6931643, and RO6924963 were identified as high-affinity competitors at the 3 H-T808 binding site on native tau aggregates in human late-stage AD brain tissue. Binding of tritiated compounds to brain tissue sections of AD patients and healthy controls was analyzed by macro- and microautoradiography and by costaining of tau aggregates and Aβ plaques on the same tissue section using specific antibodies. All 3 tracer candidates were radiolabeled with a PET nuclide and tested in vivo in tau-naïve baboons to assess brain uptake, distribution, clearance, and metabolism. Results: 3 H-RO6958948, 3 H-RO6931643, and 3 H-RO6924963 bound with high affinity and specificity to tau aggregates, clearly lacking affinity for concomitant Aβ plaques in human AD Braak V tissue sections. The specificity of all 3 radioligands for tau aggregates was supported, first, by binding patterns in AD sections comparable to the tau-specific radioligand 3 H-T808; second, by very low nonspecific binding in brain tissue devoid of tau pathology, excluding significant radioligand binding to any other central nervous system target; and third, by macroscopic and microscopic colocalization and quantitative correlation of radioligand binding and tau antibody staining on the same tissue section. RO6958948, RO6931643, and RO6924963 were successfully radiolabeled with a PET nuclide at high specific activity, radiochemical purity, and yield. After intravenous administration of 18 F-RO6958948, 11 C-RO6931643, and 11 C-RO6924963 to

Fast response, 2.5K psi (17.24 MPa) transducer for measurement of gas pressure in PWR fuel rods

International Nuclear Information System (INIS)

Piper, T.C.

1976-09-01

A strain gage pressure transducer of 2,500 psi (17.24 MPa) range for operation in a 650 0 F environment is described. Specific design parameters are given along with the calibration results obtained from typical transducers. Appendices delineate the bridge output to be expected and the actual open circuit value of a strain gage calculated from measurements taken with the bridge completed

Decision Making Model for Ro-Ro Short Sea Shipping Operations in Archipelagic Southeast Asia

Directory of Open Access Journals (Sweden)

Aminuddin Md Arof

2018-03-01

Full Text Available This study aims to develop a decision-making model for determining the potential of interstate Ro-Ro Short Sea Shipping (SSS operations in Archipelagic Southeast Asia (ASEA. It is expected to assist SSS authorities, private investors and financial institutions focus their limited resources on several key factors that could ensure the success of their undertakings. This study will begin with identifying the relevant factors that have contributed towards successful SSS operations through a process of literature review. Subsequently, a Delphi survey was conducted with sub-regional experts to identify any new determinants and assess their opinions on the relative importance of all the determinants involved. Finally the weightages of the determinants were ascertained through the Analytic Hierarchy Process (AHP. Twenty expert respondents from Brunei Darussalam. Indonesia, Malaysia and the Philippines were involved in the Delphi survey while 18 expert respondents continue to participate in the AHP survey. This study concludes with the development of a decision-making model that was tested on three interstate Ro-Ro SSS routes within the ASEA sub-region. Keywords: Archipelagic Southeast Asia, Analytic Hierarchy Process (AHP, ASEAN, Delphi, Ro-Ro, Short Sea Shipping (SSS

CoRoT 101186644 : A transiting low-mass dense M-dwarf on an eccentric 20.7-day period orbit around a late F-star. Discovered in the CoRoT lightcurves

NARCIS (Netherlands)

Tal-Or, L.; Mazeh, T.; Alonso, R.; Bouchy, F.; Cabrera, J.; Deeg, H.; Deleuil, M.; Faigler, S.; Fridlund, M.; Hébrard, G.; Moutou, C.; Santerne, A.; Tingley, B.

2013-01-01

We present the study of the CoRoT transiting planet candidate 101186644, also named LRc01_E1_4780. Analysis of the CoRoT lightcurve and the HARPS spectroscopic follow-up observations of this faint (m$_V$ = 16) candidate revealed an eclipsing binary composed of a late F-type primary (T$_{eff}$ = 6090

Exploration of the brown dwarf regime around solar-like stars by CoRoT

OpenAIRE

Csizmadia, Szilárd

2016-01-01

Aims. A summary of the CoRoT brown dwarf investigations are presented. Methods. Transiting brown dwarfs around solar like stars were studied by using the photometric time-series of CoRoT, and ground based radial velocity measurements. Results. CoRoT detected three transiting brown dwarfs around F and G dwarf stars. The occurence rate of brown dwarfs was found to be 0.20 +/- 0.15% around solar-like stars which is compatible with the value obtained by Kepler-data.

Structure of a Kunitz-type potato cathepsin D inhibitor

Czech Academy of Sciences Publication Activity Database

Guo, J.; Erskine, P. T.; Coker, A. R.; Wood, S. P.; Cooper, J. B.; Mareš, Michael; Baudyš, Miroslav

2015-01-01

Roč. 192, č. 3 (2015), s. 554-560 ISSN 1047-8477 R&D Projects: GA ČR GA15-18929S; GA MŠk LO1302 Institutional support: RVO:61388963 Keywords : potato cathepsin D inhibitor * Kunitz-type protease inhibitor * protein X-ray structure * reactive-site loop * docking Subject RIV: CE - Biochemistry Impact factor: 2.570, year: 2015

Analysis of the influence of tectonics on the evolution of valley networks based on SRTM DEM, Jemma River basin, Ethiopia

Czech Academy of Sciences Publication Activity Database

Kusák, Michal; Kropáček, J.; Vilímek, V.; Schillaci, C.

2016-01-01

Roč. 39, č. 1 (2016), 37-50 ISSN 1724-4757 Institutional support: RVO:67985891 Keywords : valley network * tectonic lineaments * Jemma River basin * Ethiopian Highlands Subject RIV: DE - Earth Magnetism, Geodesy, Geography

Argument ÜRO vastu / Joshua Muravchik

Index Scriptorium Estoniae

Muravchik, Joshua

2004-01-01

ÜRO rollist Somaalias, Rwandas ja Bosnias, Iisraeli eristaatusest. ÜRO silmakirjalikkusest inimõiguste alal, terrorismi legaliseerimisest, Kofi Annani juhtimisstiilist. Maailmas on pärast 1945. aastat valitsenud suhteline rahu mitte tänu ÜRO-le, vaid peamiselt USA tegevusele, leiab autor

Novel antidepressant candidate RO-05 modulated glucocorticoid receptors activation and FKBP5 expression in chronic mild stress model in rats.

Science.gov (United States)

Xing, Y; Hou, J; Meng, Q; Yang, M; Kurihara, H; Tian, J

2015-04-02

In this study, a novel TRI (triple reuptake inhibitors) antidepressant candidate RO-05 (4-[1-[1-(benzoyloxy)cyclohexyl]-2-(dimethylamino)ethyl]-phenyl benzoate) was investigated in TST (tail suspension test), FST (forced swimming test) and CMS (chronic mild stress) model. Results showed RO-05 significantly decreased the immobility time in FST and TST at 4.5-, 9-, 18-mg/kg in rats and 9-, 18-, 36-mg/kg in mice. Chronic administration of 18-mg/kg RO-05 improved the behavioral index, anhedonia and normalized the hyperactivity of HPA (hypothalamic-pituitary-adrenal axis) of CMS rats. We further investigated the possible mechanisms of RO-05 in the CMS model. Eighteen milligrams per kilogram of RO-05 chronic administration significantly reversed the increase of mRNA and protein expression of FKBP5 in the CMS rat hippocampus, which facilitated the activation of GR- (glucocorticoid receptor) and GR-responsive gene Foxo1 expression. RO-05 also elevated the expression of BDNF (brain-derived neurotrophic factor) in CMS rat hippocampus. In summary, our results indicated that RO-05 is a promising antidepressant candidate. The possible antidepressant mechanisms of RO-05 were the modulation of FKBP5 expression, GR activation, corresponding inhibition of HPA axis hyperactivity, and the increase of BDNF expression. Copyright © 2015 IBRO. Published by Elsevier Ltd. All rights reserved.

Forest reclamation of fly ash deposit: a field study on appraisal of mycorrhizal inoculation

Czech Academy of Sciences Publication Activity Database

Sýkorová, Z.; Rydlová, J.; Slavíková, Renata; Ness, T.; Kohout, P.; Püschel, David

2016-01-01

Roč. 24, č. 2 (2016), s. 184-193 ISSN 1061-2971 Institutional support: RVO:61388971 Keywords : arbuscular mycorrhiza * ectomycorrhiza * inoculum tracing Subject RIV: EE - Microbiology, Virology Impact factor: 1.724, year: 2016

Pharmacological caspase inhibitors: Research towards therapeutic perspectives

Czech Academy of Sciences Publication Activity Database

Kudělová, J.; Fleischmannová, Jana; Adamová, Eva; Matalová, Eva

2015-01-01

Roč. 66, č. 4 (2015), s. 473-482 ISSN 0867-5910 R&D Projects: GA ČR GB14-37368G Institutional support: RVO:67985904 Keywords : caspase * caspase inhibitor * apoptosis Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.804, year: 2015

Elements of Risk Analysis for Collision and Grounding of a RoRo Passenger Ferry

DEFF Research Database (Denmark)

Otto, S.; Pedersen, Preben Terndrup; Samuelidis, M.

2002-01-01

Newly developed software was applied to study the effects of damages due to collision and grounding. The annual risk of collision and grounding was computed for an example RoRo passenger ferry. Collision frequency was evaluated for a specified route taking into account traffic data. Grounding...

Pharmacological caspase inhibitors: Research towards therapeutic perspectives

Czech Academy of Sciences Publication Activity Database

Kudělová, J.; Fleischmannová, J.; Adamová, E.; Matalová, Eva

2015-01-01

Roč. 66, č. 4 (2015), s. 473-482 ISSN 0867-5910 R&D Projects: GA ČR(CZ) GA14-28254S Institutional support: RVO:68081715 Keywords : caspase * caspase inhibitor * apoptosis Subject RIV: CB - Analytical Chemistry, Separation Impact factor: 2.804, year: 2015

Histone deacetylase inhibitors for the treatment of cancer stem cells

Czech Academy of Sciences Publication Activity Database

Dvořáková, Marcela; Vaněk, Tomáš

2016-01-01

Roč. 7, č. 12 (2016), s. 2217-2231 ISSN 2040-2503 R&D Projects: GA MŠk LD14128 Institutional support: RVO:61389030 Keywords : acute myeloid-leukemia * epithelial-mesenchymal transition * acute myelogenous leukemia * tumor-initiating cells * human aml cells * breast-cancer * hdac inhibitors * sirtuin inhibitors * colorectal-cancer * anticancer agents Subject RIV: CC - Organic Chemistry Impact factor: 2.608, year: 2016

Několik poznámek k výročí 20 let od rozsudku Bosman

Czech Academy of Sciences Publication Activity Database

Hamerník, Pavel

2015-01-01

Roč. 5, č. 3 (2015), s. 26-30 ISSN 1338-5569 Institutional support: RVO:68378122 Keywords : EU Law * transfer fee * football Subject RIV: AG - Legal Sciences http://www.magisterofficiorum.sk/vydania-rocnik-v-2015/cislo-3-2015/

SU-E-T-218: The IHE-RO Helper Tool: Demonstrating the Connectivity Issues Solved by IHE-RO.

Science.gov (United States)

Kapoor, Rishabh; Yeung, Daniel; Kumar, Sabari Ajay; Alex, Daley; Kapur, Priyanka; Palta, Jatinder

2012-06-01

To develop a Web-based application (IHE-RO Helper) to allow comprehensive review of the interconnectivity and interoperability of various radiotherapy devices established through testing sanctioned by the Integrating Healthcare Enterprise-Radiation Oncology (IHE-RO). IHE-RO is an initiative sponsored by ASTRO to improve the way computer based systems in radiation oncology share information using well-defined data exchange standards (DICOM / HL7). At the IHE-RO Connectathon events over the last 4 years, 11 vendors with 14 different products have successfully tested and identified solutions to connectivity problems in treatment planning, simulation and delivery. Because the test results are highly technical, the interconnectivity issues amongst the RT devices may get overlooked by the end users. The IHE-RO helper tool is designed to operate in simple clinical terms with queries and presentations organized based on treatment techniques and clinical features that are familiar to the practitioners. For example, if you are planning to purchase a treatment planning system capable of generating plans (e.g. Stereotactic treatments) and are concerned whether the TPS can successfully transfer such data to your treatment management system (TMS) and subsequently to your treatment delivery system (TDS), the IHE-RO Helper can identify the connectivity requirements and list vendors that have successfully passed an IHE-RO Connectathon and validated their solution to the specific requirements. The IHE-RO helper tool provides a graphical and textual user interface to effectively demonstrate the solved interconnectivity problems between TPS, TMS and TDS. A report is also provided that explains the interconnectivity problems and its solutions. The IHE-RO helper is an effective tool to clearly identify vendor products that are IHE-RO compliant, thereby encourages vendor participation in testing and validation. Such a tool will be invaluable in procurement of new equipment to ensure a

Screening of protein kinase inhibitors identifies PKC inhibitors as inhibitors of osteoclastic acid secretion and bone resorption

Directory of Open Access Journals (Sweden)

Boutin Jean A

2010-10-01

Full Text Available Abstract Background Bone resorption is initiated by osteoclastic acidification of the resorption lacunae. This process is mediated by secretion of protons through the V-ATPase and chloride through the chloride antiporter ClC-7. To shed light on the intracellular signalling controlling extracellular acidification, we screened a protein kinase inhibitor library in human osteoclasts. Methods Human osteoclasts were generated from CD14+ monocytes. The effect of different kinase inhibitors on lysosomal acidification in human osteoclasts was investigated using acridine orange for different incubation times (45 minutes, 4 and 24 hours. The inhibitors were tested in an acid influx assay using microsomes isolated from human osteoclasts. Bone resorption by human osteoclasts on bone slices was measured by calcium release. Cell viability was measured using AlamarBlue. Results Of the 51 compounds investigated only few inhibitors were positive in both acidification and resorption assays. Rottlerin, GF109203X, Hypericin and Ro31-8220 inhibited acid influx in microsomes and bone resorption, while Sphingosine and Palmitoyl-DL-carnitine-Cl showed low levels of inhibition. Rottlerin inhibited lysosomal acidification in human osteoclasts potently. Conclusions In conclusion, a group of inhibitors all indicated to inhibit PKC reduced acidification in human osteoclasts, and thereby bone resorption, indicating that acid secretion by osteoclasts may be specifically regulated by PKC in osteoclasts.

DNA-linked Inhibitor Antibody Assay (DIANA) for sensitive and selective enzyme detection and inhibitor screening

Czech Academy of Sciences Publication Activity Database

Navrátil, Václav; Schimer, Jiří; Tykvart, Jan; Knedlík, Tomáš; Vik, V.; Majer, Pavel; Konvalinka, Jan; Šácha, Pavel

2017-01-01

Roč. 45, č. 2 (2017), č. článku e10. ISSN 0305-1048 R&D Projects: GA MŠk LO1302 Institutional support: RVO:61388963 Keywords : quantitative PCR * enzyme detection * inhibitor screening Subject RIV: CE - Biochemistry OBOR OECD: Biochemical research methods Impact factor: 10.162, year: 2016 https:// academic .oup.com/nar/article-lookup/doi/10.1093/nar/gkw853

Premier numéro bilingue

Directory of Open Access Journals (Sweden)

Esther Cloutier

2008-05-01

Full Text Available Nous sommes heureux de vous présenter ce nouveau numéro bilingue de la revue PISTES. Nous espérons ainsi faire connaître les travaux francophones sur la santé au travail dans le monde anglo-saxon. Nous vous rappelons que la traduction de ce numéro a été rendu possible grâce à une subvention du CRSH (Conseil de la recherche en sciences humaines du Canada ainsi qu’à la contribution de certains auteurs que nous tenons à remercier. Ce numéro aborde plusieurs thèmes de recherche reliés au travail...

Structural Basis for Inhibitor-Induced Hydrogen Peroxide Production by Kynurenine 3-Monooxygenase.

Science.gov (United States)

Kim, Hyun Tae; Na, Byeong Kwan; Chung, Jiwoung; Kim, Sulhee; Kwon, Sool Ki; Cha, Hyunju; Son, Jonghyeon; Cho, Joong Myung; Hwang, Kwang Yeon

2018-04-19

Kynurenine 3-monooxygenase (KMO) inhibitors have been developed for the treatment of neurodegenerative disorders. The mechanisms of flavin reduction and hydrogen peroxide production by KMO inhibitors are unknown. Herein, we report the structure of human KMO and crystal structures of Saccharomyces cerevisiae (sc) and Pseudomonas fluorescens (pf) KMO with Ro 61-8048. Proton transfer in the hydrogen bond network triggers flavin reduction in p-hydroxybenzoate hydroxylase, but the mechanism triggering flavin reduction in KMO is different. Conformational changes via π-π interactions between the loop above the flavin and substrate or non-substrate effectors lead to disorder of the C-terminal α helix in scKMO and shifts of domain III in pfKMO, stimulating flavin reduction. Interestingly, Ro 61-8048 has two different binding modes. It acts as a competitive inhibitor in scKMO and as a non-substrate effector in pfKMO. These findings provide understanding of the catalytic cycle of KMO and insight for structure-based drug design of KMO inhibitors. Copyright © 2018 Elsevier Ltd. All rights reserved.

El violón de Domingo Román (Valladolid, 1724

Directory of Open Access Journals (Sweden)

Reula Baquero, Pedro

2009-12-01

Full Text Available Domingo Roman’s cello is one of the very few surviving Spanish bowed instruments from the eighteenth century. This article basically pretends to present and describe this recently rediscovered instrument by analising it’s very peculiar way of construction, comparing it with the informations we have about the Spanish school of making from sixteen till eighteenth century and other contemporary schools like the fl amish and the german one.

El violón de Domingo Román (Valladolid, 1724 viene a enriquecer la escasa nómina de instrumentos de arco españoles conservados del siglo XVIII. Este artículo pretende ser, básicamente, una presentación y descripción del violón. El análisis del contexto estilístico trata de poner en relación sus peculiares características constructivas con las de la escuela española de los violeros de los siglos XVI a XVIII y con otras europeas como la fl amenca y alemana.

Anomalous structural evolution and √ 3 x√ 3 reconstruction of a clean Si(111) surface observed after thermal desorption of thallium

Czech Academy of Sciences Publication Activity Database

Kocán, P.; Krejčí, Ondřej; Tochihara, H.

2015-01-01

Roč. 33, č. 2 (2015), "021408-1"-"021408-8" ISSN 0734-2101 Institutional support: RVO:68378271 Keywords : surface structure * Si(111) * thallium * LEED * STM Subject RIV: BM - Solid Matter Physics ; Magnetism Impact factor: 1.724, year: 2015

Current and Novel Inhibitors of HIV Protease

Czech Academy of Sciences Publication Activity Database

Pokorná, Jana; Machala, L.; Řezáčová, Pavlína; Konvalinka, Jan

2009-01-01

Roč. 1, č. 3 (2009), s. 1209-1239 ISSN 1999-4915 R&D Projects: GA MŠk 1M0508 Grant - others:GA AV ČR(CZ) IAAX00320901 Program:IA Institutional research plan: CEZ:AV0Z40550506 Keywords : HIV protease * protease inhibitor * HAART Subject RIV: CE - Biochemistry

Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors

Czech Academy of Sciences Publication Activity Database

Šebestík, Jaroslav; Marques, S. M.; Falé, P. L.; Santos, S.; Arduíno, D. M.; Cardoso, S. M.; Oliveira, S. M.; Serralheiro, M. L. M.; Santos, A. M.

Roč. 26, č. 4 (485), s. 497 ISSN 1475-6366 Institutional research plan: CEZ:AV0Z40550506 Keywords : acetylcholinesterase inhibitors * antioxidants * hybrid ligands * anti-neurodegeneratives * Alzheimer´s disease Subject RIV: CC - Organic Chemistry

Find selv fred og ro

DEFF Research Database (Denmark)

Juelskjær, Malou

2010-01-01

I klasseværelset er det lærerens ansvar at skabe ro. Men i de nye skolebygninger er det den enkelte elevs ansvar at finde frem til fredfyldte steder.......I klasseværelset er det lærerens ansvar at skabe ro. Men i de nye skolebygninger er det den enkelte elevs ansvar at finde frem til fredfyldte steder....

Genetic analysis of possibly the oldest greyhound remains within the territory of the Czech Republic as a proof of a local elite presence at Chotěbuz-Podobora hillfort in the 8th–9th century AD

Czech Academy of Sciences Publication Activity Database

Svobodová, H.; Bartoš, M.; Nývltová Fišáková, Miriam; Kouřil, Pavel

2015-01-01

Roč. 71, 1-2 (2015), s. 17-24 ISSN 0036-5343 Institutional research plan: CEZ:AV0Z80010507 Institutional support: RVO:68081758 Keywords : greyhound * mtDNA * Control region * Great Moravia * Middle Ages Subject RIV: AC - Archeology, Anthropology, Ethnology

The Modified Fouling Index Ultrafiltration constant flux for assessing particulate/colloidal fouling of RO systems

KAUST Repository

Salinas-Rodriguez, Sergio G.

2015-02-18

Reliable methods for measuring and predicting the fouling potential of reverse osmosis (RO) feed water are important in preventing and diagnosing fouling at the design stage, and for monitoring pre-treatment performance during plant operation. The Modified Fouling Index Ultrafiltration (MFI-UF) constant flux is a significant development with respect to assessing the fouling potential of RO feed water. This research investigates (1) the variables influencing the MFI-UF test at constant flux filtration (membrane pore size, membrane material, flux rate); and (2) the application of MFI-UF into pre-treatment assessment and RO fouling estimation. The dependency of MFI on flux, means that to assess accurately particulate fouling in RO systems, the MFI should be measured at a flux similar to a RO system (close to 20 L/m2/h) or extrapolated from higher fluxes. The two studied membrane materials showed reproducible results; 10% for PES membranes and 6.3% for RC membranes. Deposition factors (amount of particles that remain on the surface of membrane) were measured in a full-scale plant ranging between 0.2 and 0.5. The concept of “safe MFI” is presented as a guideline for assessing pre-treatment for RO systems.

New inhibitors of HDAC to purge latent HIV-1 reservoir

Czech Academy of Sciences Publication Activity Database

Hejnar, Jiří; Hirsch, I.

2010-01-01

Roč. 2, č. 4 (2010), s. 505-506 ISSN 1750-1911 Institutional research plan: CEZ:AV0Z50520514 Keywords : HAART * HIV latency * HDAC inhibitor Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 3.429, year: 2010

Aurora kinase inhibitors: Progress towards the clinic

Czech Academy of Sciences Publication Activity Database

Kollareddy, M.; Zheleva, D.; Dzubak, P.; Brahmkshatriya, Pathik; Lepšík, Martin; Hajduch, M.

2012-01-01

Roč. 30, č. 6 (2012), s. 2411-2432 ISSN 0167-6997 Grant - others:GA ČR(CZ) GA301/08/1649; GA ČR(CZ) GD303/09/H048 Program:GA; GD Institutional research plan: CEZ:AV0Z40550506 Keywords : Aurora kinases * cancer * inhibitors Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 3.498, year: 2012

Cyclin-dependent kinase inhibitors as anticancer drugs

Czech Academy of Sciences Publication Activity Database

Kryštof, Vladimír; Uldrijan, S.

2010-01-01

Roč. 11, č. 3 (2010), s. 291-302 ISSN 1389-4501 R&D Projects: GA ČR GA204/08/0511; GA ČR GA301/08/1649; GA MŠk(CZ) LC06077 Institutional research plan: CEZ:AV0Z50380511 Keywords : CDK * protein kinase * inhibitor Subject RIV: CE - Biochemistry Impact factor: 3.061, year: 2010

Novel arylazopyrazole inhibitors of cyclin-dependent kinases

Czech Academy of Sciences Publication Activity Database

Jorda, Radek; Schütznerová, E.; Cankař, P.; Brychtová, Veronika; Navrátilová, Jana; Kryštof, Vladimír

2015-01-01

Roč. 23, č. 9 (2015), s. 1975-1981 ISSN 0968-0896 R&D Projects: GA ČR GAP305/12/0783; GA ČR GA14-19590S; GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Cyclin-dependent kinases * Inhibitor * Cell cycle Subject RIV: CE - Biochemistry Impact factor: 2.923, year: 2015

The Chicken - a Laboratory Animal of the Class "Aves"

Czech Academy of Sciences Publication Activity Database

Plachý, Jiří

2000-01-01

Roč. 46, č. 1 (2000), s. 17-24 ISSN 0015-5500 R&D Projects: GA ČR GA524/99/0366 Institutional research plan: CEZ:AV0Z5052915 Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 0.351, year: 2000

A single episode of neonatal seizures alters the cerebellum of immature rats

Czech Academy of Sciences Publication Activity Database

Lomoio, S.; Necchi, D.; Mareš, Vladislav; Scherini, E.

2011-01-01

Roč. 93, č. 1 (2011), s. 17-24 ISSN 0920-1211 Institutional research plan: CEZ:AV0Z50110509 Keywords : metrazol seizures * cerebellum * Purkinje cells * GluR2/3 * GLT1 Subject RIV: FH - Neurology Impact factor: 2.290, year: 2011

RoMo

DEFF Research Database (Denmark)

Pedersen, Esben Warming; Hornbæk, Kasper

2011-01-01

In TUIs, physical/digital conflicts can occur when the digital model does not match the model implied by the spatial lay- out of tangibles. We show how tangible tabletop interfaces (TTI) can be modified to allow robot movement of tangi- bles, thereby avoiding conflicts. We present RoMo, an open...... source Java library that allow existing TTI applications to perform robot movement, and demonstrate its functionality with three applications....

Inhibitors of plant hormone transport

Czech Academy of Sciences Publication Activity Database

Klíma, Petr; Laňková, Martina; Zažímalová, Eva

2016-01-01

Roč. 253, č. 6 (2016), s. 1391-1404 ISSN 0033-183X R&D Projects: GA MŠk(CZ) LD15088 Institutional support: RVO:61389030 Keywords : polar auxin transport * acid-binding protein * gnom arf-gef * equilibrative nucleoside transporter * efflux carrier polarity * plasma-membrane-protein * cultured tobacco cells * arabidopsis-thaliana * gravitropic response * brefeldin-a * Plant hormones * Transport * Inhibitors * Auxin * Cytokinins * Strigolactones * Abscisic acid * Cell biology Subject RIV: ED - Physiology Impact factor: 2.870, year: 2016

Development of first inhibitors for betaine-homocysteine S-methyltransferase 2

Czech Academy of Sciences Publication Activity Database

Mládková, J.; Vaněk, Václav; Elbert, Tomáš; Buděšínský, Miloš; Jiráček, Jiří

2012-01-01

Roč. 106, - (2012), s894-s894 ISSN 0009-2770. [EuCheMS Chemistry Congress /4./. 26.08.2012-30.08.2012, Prague] Institutional research plan: CEZ:AV0Z40550506 Keywords : enzyme catalysis * inhibitors * alkylation Subject RIV: CC - Organic Chemistry

Magnetic field sensor based on asymmetric inverse Wiedemann effect

Czech Academy of Sciences Publication Activity Database

Kraus, Luděk; Malátek, M.; Dvořák, M.

2008-01-01

Roč. 142, č. 2 (2008), s. 468-473 ISSN 0924-4247 Institutional research plan: CEZ:AV0Z10100520 Keywords : magnetic field sensor * inverse Wiedemann effect * off-diagonal magnetoimpedance * amorphous ribbon Subject RIV: BM - Solid Matter Physics ; Magnetism Impact factor: 1.724, year: 2008

Secondary eclipses in the CoRoT light curves

Directory of Open Access Journals (Sweden)

Belmonte Juan Antonio

2013-04-01

Full Text Available We identify and characterize secondary eclipses in the original light curves of published CoRoT planets using uniform detection and evaluation criteria. Our analysis is based on a Bayesian statistics: the eclipse search is carried out using Bayesian model selection, and the characterization of the plausible eclipse candidates using Bayesian parameter estimation. We discover statistically significant eclipse events for two planets, CoRoT-6b and CoRoT-11b, and for one brown dwarf, CoRoT-15b. We also find marginally significant eclipse events passing our plausibility criteria for CoRoT-3b, 13b, 18b, and 21b, and confirm the previously published CoRoT-1b and CoRoT-2b eclipses.

Acrosin inhibitor detecting along the boar epididymis

Czech Academy of Sciences Publication Activity Database

Maňásková-Postlerová, Pavla; Cozlová, Nina; Dorosh, Andriy; Šulc, Miroslav; Guyonet, B.; Jonáková, Věra

2016-01-01

Roč. 82, Jan 2016 (2016), s. 733-739 ISSN 0141-8130 R&D Projects: GA ČR(CZ) GAP503/12/1834; GA MŠk(CZ) ED1.1.00/02.0109; GA ČR GA14-05547S Institutional support: RVO:86652036 ; RVO:61388971 Keywords : Acrosin inhibitor * Boar epididymis * Spermatozoa Subject RIV: CE - Biochemistry Impact factor: 3.671, year: 2016

FAITH - Fast Assembly Inhibitor Test for HIV

Czech Academy of Sciences Publication Activity Database

Hadravová, Romana; Rumlová, Michaela; Ruml, T.

2015-01-01

Roč. 486, Dec (2015), s. 78-87 ISSN 0042-6822 R&D Projects: GA ČR(CZ) GA14-15326S; GA MŠk LO1302; GA MŠk(CZ) LO1304 Institutional support: RVO:61388963 Keywords : retrovirus * HIV * assembly * assay * inhibitor Subject RIV: EE - Microbiology, Virology Impact factor: 3.200, year: 2015 http://www.sciencedirect.com/science/article/pii/S0042682215003864

Luminometric method for screening retroviral protease inhibitors

Czech Academy of Sciences Publication Activity Database

Horáková, D.; Rumlová, Michaela; Pichová, Iva; Ruml, Tomáš

2005-01-01

Roč. 345, č. 1 (2005), s. 96-101 ISSN 0003-2697 R&D Projects: GA AV ČR(CZ) IAA4055304; GA MŠk(CZ) 1M0508; GA MŠk(CZ) 1M0520 Institutional research plan: CEZ:AV0Z40550506 Keywords : retroviral protease * inhibitors * luminescent assay Subject RIV: CE - Biochemistry Impact factor: 2.670, year: 2005

Oncogenic Kinase Bcr-Abl and Its Resistance to Pharmacological Inhibitors

Czech Academy of Sciences Publication Activity Database

Kryštof, Vladimír

2008-01-01

Roč. 102, č. 9 (2008), s. 795-800 E-ISSN 1213-7103 Institutional research plan: CEZ:AV0Z50380511 Keywords : imatinib * inhibitor * chronic myeloid leukaemia * kinase * cancer Subject RIV: CE - Biochemistry www.chemicke-listy.cz/docs/full/2008_09_795-800.pdf

Sketching the historical development of pyrimidones as the inhibitors of the HIV integrase

Czech Academy of Sciences Publication Activity Database

Patel, Rahul V.; Keum, Y.S.; Park, S.W.

2015-01-01

Roč. 97, JUN 5 (2015), s. 649-663 ISSN 0223-5234 Institutional support: RVO:61389030 Keywords : Pyrimidones * Anti-HIV * Integrase inhibitors Subject RIV: CE - Biochemistry Impact factor: 3.902, year: 2015

Development of a Rapid Fluorescence-Based High-Throughput Screening Assay to Identify Novel Kynurenine 3-Monooxygenase Inhibitor Scaffolds.

Science.gov (United States)

Jacobs, K R; Guillemin, G J; Lovejoy, D B

2018-02-01

Kynurenine 3-monooxygenase (KMO) is a well-validated therapeutic target for the treatment of neurodegenerative diseases, including Alzheimer's disease (AD) and Huntington's disease (HD). This work reports a facile fluorescence-based KMO assay optimized for high-throughput screening (HTS) that achieves a throughput approximately 20-fold higher than the fastest KMO assay currently reported. The screen was run with excellent performance (average Z' value of 0.80) from 110,000 compounds across 341 plates and exceeded all statistical parameters used to describe a robust HTS assay. A subset of molecules was selected for validation by ultra-high-performance liquid chromatography, resulting in the confirmation of a novel hit with an IC 50 comparable to that of the well-described KMO inhibitor Ro-61-8048. A medicinal chemistry program is currently underway to further develop our novel KMO inhibitor scaffolds.

Larvicidal activity of extracts from Ammi visnaga Linn. (Apiaceae) seeds against Culex quinquefasciatus Say. (Diptera: Culicidae)

Czech Academy of Sciences Publication Activity Database

Pavela, R.; Vrchotová, Naděžda; Tříska, Jan

2016-01-01

Roč. 165, mar (2016), s. 51-57 ISSN 0014-4894 R&D Projects: GA MŠk(CZ) ED1.1.00/02.0073 Institutional support: RVO:67179843 Keywords : botanical larvicide * Furanochromenes * Visnagin * Khellin * Sublethal effect * Mosquito Subject RIV: GC - Agronomy Impact factor: 1.724, year: 2016

Biomass of Speckled Alder on an Air-Polluted Mountain Site and its Response to Fertilization

Czech Academy of Sciences Publication Activity Database

Kuneš, I.; Baláš, M.; Koňasová, T.; Špulák, O.; Balcar, V.; Bednářová Millerová, K.; Kacálek, D.; Jakl, M.; Zahradník, D.; Vítámvás, J.; Šťastná, J.; Jaklová Dytrtová, Jana

2014-01-01

Roč. 54, č. 6 (2014), s. 1421-1433 ISSN 0364-152X Grant - others:GA MZe(CZ) QH92087 Institutional support: RVO:61388963 Keywords : Alnus incana * site amelioration * biological amelioration * slow-acting amendments * ecosystem restoration Subject RIV: GK - Forestry Impact factor: 1.724, year: 2014

Geochemie a zirkonové U-Pb stáří derflického granodioritu z dyjského masivu

Czech Academy of Sciences Publication Activity Database

Svojtka, Martin; Breiter, Karel; Ďurišová, Jana; Ackerman, Lukáš; Veselovský, F.; Šmerda, J.

2017-01-01

Roč. 50, č. 1 (2017), s. 17-24 ISSN 0514-8057 R&D Projects: GA ČR GA13-15390S Institutional support: RVO:67985831 Keywords : Bohemian Massif * Cadomian granitoids * Thaya (Dyje) Massif * zircon U-Pb dating Subject RIV: DB - Geology ; Mineralogy OBOR OECD: Geology

Infrared spectroscopy of Ba.sub.2./sub.NaNb.sub.5./sub.O.sub.15./sub. single crystal and thin films

Czech Academy of Sciences Publication Activity Database

Buixaderas, Elena; Kamba, Stanislav; Petzelt, Jan; Wada, M.; Shitzutoshi, A.; Tsukamoto, T.

2000-01-01

Roč. 239, - (2000), s. 17-24 ISSN 0015-0193 R&D Projects: GA ČR GA202/98/1282; GA AV ČR IAA1010828 Institutional research plan: CEZ:AV0Z1010914 Subject RIV: BM - Solid Matter Physics ; Magnetism Impact factor: 0.547, year: 2000

UWB Propagation through Walls

Czech Academy of Sciences Publication Activity Database

Schejbal, V.; Bezoušek, P.; Čermák, D.; NĚMEC, Z.; Fišer, Ondřej; Hájek, M.

2006-01-01

Roč. 15, č. 1 (2006), s. 17-24 ISSN 1210-2512 R&D Projects: GA MPO(CZ) FT-TA2/030 Institutional research plan: CEZ:AV0Z30420517 Keywords : Ultra wide band * UWB antennas * UWB propagation * multipath effects Subject RIV: JB - Sensors, Measurment, Regulation

The interaction of quaternary reversible acetylcholinesterase inhibitors with the nicotinic receptor

Czech Academy of Sciences Publication Activity Database

Šepsová, V.; Krůšek, Jan; Zdarová Karasová, J.; Zemek, F.; Musílek, K.; Kuča, K.; Soukup, O.

2014-01-01

Roč. 63, č. 6 (2014), s. 771-777 ISSN 0862-8408 R&D Projects: GA ČR(CZ) GBP304/12/G069 Institutional support: RVO:67985823 Keywords : acetylcholinesterase inhibitor * nicotin receptor Subject RIV: ED - Physiology Impact factor: 1.293, year: 2014

A role for CD4+ but not CD8+ T cells in immunity to Schistosoma mansoni induced by 20 krad-irradiated and Ro 11-3128-terminated infections

International Nuclear Information System (INIS)

Vignali, D.A.A.; Bickle, Q.D.; Taylor, M.G.; Crocker, P.; Cobbold, S.; Waldmann, H

1989-01-01

The role of CD4 + (L3/T4 + ) and CD8 + (Lyt-2 + ) T cells in immunity to Schistosoma mansoni induced by 20 krad-irradiated and Ro 11-terminated infections in mice was investigated directly by in vivo depletion of these subsets with cytotoxic rat monoclonal antibodies (mAb). Effective physical depletion was demonstrated by flow cytometric analysis and immunohistochemical staining. Functional depletion of helper activity following anti-CD4 treatment was indicated by an abrogation of concanavalin A(Con A)-induced colony-stimulating factor (CSF) release, while anti-CD8 treatment had no effect in these assays. Pre-existing S. mansoni-specific antibody levels were unaffected by anti-CD4 and anti-CD8 treatment. In vivo depletion of CD4 + T cells resulted in a dramatic reduction in immunity induced by one (up to 100%) and two (up to 70%) vaccinations with 20 krad-irradiated cercariae and also of resistance induced by Ro 11-attenuated infections (up to 100%). Depletion of CD8 + T cells had no effect on resistance induced by any of the vaccination protocols investigated. A correlation was observed between resistance and T cell-induced, macrophage-mediated killing of schistosomula in vitro, both of which were abrogated following anti-CD4 treatment but were unaffected by CD8 + T-cell depletion. The possible role of CD4 + T cells in vivo and the implications for vaccine development are discussed. (author)

Serine proteinases and their inhibitors in fertilization

Czech Academy of Sciences Publication Activity Database

Jonáková, Věra

2000-01-01

Roč. 3, 3,4 (2000), s. 23 [ Proteolytic enzymes and their inhibitors in physiology and pathogenesis. 14.09.2000, Plzen] R&D Projects: GA ČR GV524/96/K162; GA ČR GA303/99/0357; GA MŠk VS96141 Grant - others:GA UK(CZ) 12/1998 Institutional research plan: CEZ:AV0Z5052915 Subject RIV: EB - Genetics ; Molecular Biology

Pile-up correction for coincidence counting using a CAEN 1724 digitizer

Energy Technology Data Exchange (ETDEWEB)

Ribeiro Junior, Iberê S.; Zahn, Guilherme S.; Genezini, Frederico A., E-mail: gzahn@ipen.br [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil)

2017-07-01

In conventional gamma-ray spectrometry, the probability of pile-up effects is considered to be proportional to the dead-time, and is usually neglected for low dead-times (below 4-5%). In gamma-gamma coincidence spectrometry, though, while the dead time takes into account only events that are actually digitized, the pile-up effects are proportional to the actual gamma-ray detection rate in each detector, not only to the ones that trigger the coincidence gate. Thus, the pile-up corrections may not be so easy to assess as in single spectrometry systems. In this work, a system composed of two HPGe detectors coupled to a CAEN v1724 digitizer is studied. A 3kBq {sup 60}Co source was analyzed, both alone and in the presence of other radioactive sources ({sup 137}Cs, {sup 133}Ba and {sup 152}Eu), and the resulting coincidence peak areas were compared to assess the effectiveness of two distinct corrections: a simple normalization by the live time of acquisition and the normalization by the count rate obtained using a pulse generator. The results obtained stress the need to use the pulse generator in this specific setup in order to get accurate results. (author)

The CoRoT Exoplanet program: status & results

Directory of Open Access Journals (Sweden)

Moutou C.

2011-02-01

Full Text Available The CoRoT satellite is the first instrument hunting for planets from space. We will review the status of the CoRoT/Exoplanet program. We will then present the CoRoT exoplanetary systems and how they widen the range of properties of the close-in population and contribute to our understanding of the properties of planets.

IAEA Theory Summary 1998 IAEA Meeting, Yokohama, Japan - Oct. 17-24, 1998

International Nuclear Information System (INIS)

Tang, W.M.

2000-01-01

This is a summary of the advances in magnetic fusion energy theory research presented at the 17th International Atomic Energy Agency Fusion Energy Conference from 17--24 October, 1998 in Yokohama, Japan. Theory and simulation results from this conference provided encouraging evidence of significant progress in understanding the physics of thermonuclear plasmas. Indeed, the grand challenge for this field is to acquire the basic understanding that can readily enable the innovations which would make fusion energy practical. In this sense, as depicted in Fig. 1, research in fusion energy is increasingly able to be categorized as fitting well the ''Pasteur's Quadrant'' paradigm, where the research strongly couples basic science (''Bohr's Quadrant'') to technological impact (''Edison's Quadrant''). As supported by some of the work presented at this conference, this trend will be further enhanced by advanced simulations. Eventually, realistic three-dimensional modeling capabilities, when properly combined with rapid and complete data interpretation of results from both experiments and simulations, can contribute to a greatly enhanced cycle of understanding and innovation. Plasma science theory and simulation have provided reliable foundations for this improved modeling capability, and the exciting advances in high-performance computational resources have further accelerated progress

An integrative study to identify novel scaffolds for sphingosine kinase 1 inhibitors

Czech Academy of Sciences Publication Activity Database

Vettorazzi, M.; Angelina, E.; Lima, S.; Goněc, T.; Otevřel, J.; Marvanová, P.; Padrtová, T.; Mokrý, P.; Bobáľ, P.; Acosta, L. M.; Palma, A.; Cobo, J.; Bobálová, Janette; Csollei, J.; Malik, I.; Alvarez, S.; Spiegel, S.; Jampílek, J.; Enriz, R. D.

2017-01-01

Roč. 139, OCT (2017), s. 461-481 ISSN 0223-5234 Institutional support: RVO:68081715 Keywords : sphingosine kinase 1 inhibitors * bioassays * molecular modelling * virtual screening Subject RIV: CB - Analytical Chemistry, Separation OBOR OECD: Analytical chemistry Impact factor: 4.519, year: 2016

Cryptosporidium parvum and Enterocytozoon bieneusi in American Mustangs and Chincoteague ponies

Czech Academy of Sciences Publication Activity Database

Wagnerová, Pavla; Sak, Bohumil; McEvoy, J.; Rost, M.; Sherwood, D.; Holcomb, K.; Kváč, Martin

2016-01-01

Roč. 162, MAR (2016), s. 24-27 ISSN 0014-4894 R&D Projects: GA ČR GA15-01090S Institutional support: RVO:60077344 Keywords : feral horses * Cryptosporidium * SSU * gp60 * Microsporidia * ITS Subject RIV: GJ - Animal Vermins ; Diseases, Veterinary Medicine Impact factor: 1.724, year: 2016

Root and Eruption Defects in c-Fos Mice Are Driven by Loss of Osteoclasts

Czech Academy of Sciences Publication Activity Database

Alfaqeeh, S.; Oralová, Veronika; Foxworthy, M.; Matalová, Eva; Grigoriadis, A. E.; Tucker, A. S.

2015-01-01

Roč. 94, č. 12 (2015), s. 1724-1731 ISSN 0022-0345 R&D Projects: GA ČR GCP302/12/J059; GA ČR GB14-37368G Institutional support: RVO:67985904 Keywords : tooth * bone * rescue Subject RIV: EA - Cell Biology Impact factor: 4.602, year: 2015

Haitilased süüdistavad kooleras ÜRO rahuvalvajaid

Index Scriptorium Estoniae

2010-01-01

Paljud kohalikud elanikud on veendunud, et Haiti kooleraepideemia vallandamises on süüdi ÜRO stabilisatsioonimission MINUSTAH. Riigis on puhkenud ÜRO-vastased rahutused. ÜRO arvates on protestilaine algatatud presidendivalimisi nurjata soovivate poliitiliste liikumiste poolt

Structure-based drug design of selective 5´-nucleotidases inhibitors

Czech Academy of Sciences Publication Activity Database

Pachl, Petr; Brynda, Jiří; Rosenberg, Ivan; Fábry, Milan; Řezáčová, Pavlína

2011-01-01

Roč. 18, č. 1 (2011), s. 33-34 ISSN 1211-5894. [Discussions in Structural Molecular Biology /9./. 24.03.2011-26.03.2011, Nové Hrady] Institutional research plan: CEZ:AV0Z40550506; CEZ:AV0Z50520701 Keywords : inhibitor design * nucleotidase * Xray crystalography Subject RIV: EB - Genetics ; Molecular Biology

Adsorption, Mobility, and Self-Association of Naphthalene and 1-Methylnaphthalene at the Water-Vapor Interface

Czech Academy of Sciences Publication Activity Database

Gladich, Ivan; Habartová, Alena; Roeselová, Martina

2014-01-01

Roč. 118, č. 6 (2014), s. 1052-1066 ISSN 1089-5639 R&D Projects: GA ČR(CZ) GAP208/10/1724 Institutional support: RVO:61388963 Keywords : polycyclic aromatic hydrocarbons * atmospheric air /ice interfaces * molecular dynamics method Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 2.693, year: 2014

Forest reclamation of fly ash deposit: a field study on appraisal of mycorrhizal inoculation

Czech Academy of Sciences Publication Activity Database

Sýkorová, Zuzana; Rydlová, Jana; Slavíková, Renata; Ness, T.; Kohout, Petr; Püschel, David

2016-01-01

Roč. 24, č. 2 (2016), s. 184-193 ISSN 1061-2971 R&D Projects: GA MŠk 1M0571; GA ČR GPP504/10/P021 Institutional support: RVO:67985939 Keywords : arbuscular mycorrhiza * ectomycorrhiza * inoculum tracing Subject RIV: EH - Ecology, Behaviour Impact factor: 1.724, year: 2016

Rhomboid protease inhibitors: Emerging tools and future therapeutics

Czech Academy of Sciences Publication Activity Database

Stříšovský, Kvido

2016-01-01

Roč. 60, Dec (2016), s. 52-62 ISSN 1084-9521 R&D Projects: GA MŠk(CZ) LK11206; GA MŠk LO1302 EU Projects: European Commission(XE) 304154 - Rhomboid substrates Institutional support: RVO:61388963 Keywords : rhomboid protease * inhibitor * disease * mechanism * substrate specificity Subject RIV: CE - Biochemistry Impact factor: 6.614, year: 2016 http://www.sciencedirect.com/science/article/pii/S1084952116302592

Ku-pa-ro en las tablillas de Cnoso

Directory of Open Access Journals (Sweden)

José L. Melena

1974-12-01

Full Text Available This paper is intended to be a comprehensive analysis of the evidence of ku-pa-ro in the Knossos Linear B tablets. Its main purpose is to set up the importance of such aromatic plant in the Mycenaean economy at Knossos and to identify what kind of sedge was concealed under the name ku-pa-ro and what part of the plant was used and for what purposes. What it is stressed is the usage of the Cyperus rotundus L. (i. e. the ku-pa-ro in the industry of perfumes and as a food additive as well. What is inferred from the discussion on the evidence of ku-pa-ro issues a series of valuable data concerning the localization of certain place-names in the map of Crete, and concerning the explanation of ideogram *171. The high qualities of ku-pa-ro preserved in the tablets lead the author to assume that such a plant was cultivated in Crete and was one of the main aromatic plants used by the Mycenaeans in the making of perfumes.

Short Review on Predicting Fouling in RO Desalination

Directory of Open Access Journals (Sweden)

Alejandro Ruiz-García

2017-10-01

Full Text Available Reverse Osmosis (RO membrane fouling is one of the main challenges that membrane manufactures, the scientific community and industry professionals have to deal with. The consequences of this inevitable phenomenon have a negative effect on the performance of the desalination system. Predicting fouling in RO systems is key to evaluating the long-term operating conditions and costs. Much research has been done on fouling indices, methods, techniques and prediction models to estimate the influence of fouling on the performance of RO systems. This paper offers a short review evaluating the state of industry knowledge in the development of fouling indices and models in membrane systems for desalination in terms of use and applicability. Despite major efforts in this field, there are gaps in terms of effective methods and models for the estimation of fouling in full-scale RO desalination plants. In existing models applied to full-scale RO desalination plants, neither the spacer geometry of membranes, nor the efficiency and frequency of chemical cleanings are considered.

Identification and Mechanistic Analysis of a Novel Tick-Derived Inhibitor of Thrombin

Czech Academy of Sciences Publication Activity Database

Jablonka, W.; Kotsyfakis, Michalis; Mizurini, D.M.; Monteiro, R.Q.; Lukszo, J.; Drake, S.K.; Ribeiro, J.M.C.; Andersen, J. F.

2015-01-01

Roč. 10, č. 8 (2015), e0133991 E-ISSN 1932-6203 R&D Projects: GA ČR GAP502/12/2409 Institutional support: RVO:60077344 Keywords : Haemaphysalis longicornis * binding inhibitor * crystal structure Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 3.057, year: 2015

The implications of the new sulphur limits on the European Ro-Ro sector

DEFF Research Database (Denmark)

Zis, Thalis; Psaraftis, Harilaos N.

-based alternatives. The exact repercussions of the new sulphur limits are difficult to identify in the wake of significant recent reductions of the fuel prices for both low-sulphur and heavy fuel oil. This paper presents a modal split model that estimates modal shifts vis-a-vis competing maritime and land......In an effort to reduce the environmental impacts of maritime transportation, the International Maritime Organization (IMO) designated special Sulphur Emission ControlAreas (SECAs) where ships are required to use low-sulphur fuel. In January 2015, the sulphur limit within SECAs was lowered to 0.......1%, which can only be achieved if vessels are using pricier ultra-low sulphur fuel, or invest in abatement technologies. The increased operating costs borne by Ro-Ro operators in SECAs due to the stricter limits can result in the shutting down of some routes and a redistribution of cargo flows with land...

Serine proteinases and their inhibitors in fertilization

Czech Academy of Sciences Publication Activity Database

Jonáková, Věra; Jelínková-Slavíčková, Petra

2004-01-01

Roč. 8, 3,4 (2004), s. 108-110 ISSN 1211-8869. [Central European Conference on Human Tumor Markers /5./. Praha, 01.10.2004-03.10.2004] R&D Projects: GA ČR GA303/02/0433; GA ČR GP303/02/P069; GA ČR GP303/04/P070; GA MZd NJ7463 Institutional research plan: CEZ:AV0Z5052915 Keywords : serine proteinase * proteinase inhibitors * fertilization Subject RIV: CE - Biochemistry

RO-PRO desalination: An integrated low-energy approach to seawater desalination

International Nuclear Information System (INIS)

Prante, Jeri L.; Ruskowitz, Jeffrey A.; Childress, Amy E.; Achilli, Andrea

2014-01-01

Highlights: • In the novel RO-PRO system, the energy produced by PRO is utilized to offset the energy consumed by the RO. • The specific energy consumption of a RO-PRO system was modeled for the first time. • A novel module-based PRO model for full-scale applications was developed. • The minimum net specific energy consumption of the modeled RO-PRO system was 1.2 kW h/m 3 at 50% RO recovery. • A sensitivity analysis showed a min RO-PRO specific energy consumption of 1.0 kW h/m 3 and a max power density of 10 W/m 2 . - Abstract: Although reverse osmosis (RO) is currently the most energy efficient desalination technology, it still requires a great deal of energy to create the high pressures necessary to desalinate seawater. An opposite process of RO, called pressure retarded osmosis (PRO), utilizes the salinity gradient between a relatively fresh impaired water source and seawater to produce pressure and hence, energy. In this paper, PRO is evaluated in conjunction with RO, in a system called RO-PRO desalination, to reduce the energy requirement of seawater RO desalination. RO-PRO specific energy consumption was modeled using RO conditions at the thermodynamic restriction and a newly developed module-based PRO model. Using a well-characterized cellulose triacetate (CTA) membrane, the minimum net specific energy consumption of the system was found to be approximately 40% lower than state-of-the-art seawater RO. A sensitivity analysis was performed to determine the effects of membrane characteristics on the specific energy production of the PRO process in the RO-PRO system. The sensitivity analysis showed that the minimum specific energy consumption using virtual membranes is approximately 1.0 kW h per m 3 of RO permeate at 50% RO recovery and that a maximum power density of approximately 10 W/m 2 could be achieved

Potential Clinical Uses of CDK Inhibitors: Lessons from Synthetic Lethality Screens

Czech Academy of Sciences Publication Activity Database

Vymětalová, Ladislava; Kryštof, Vladimír

2015-01-01

Roč. 35, č. 6 (2015), s. 1156-1174 ISSN 0198-6325 R&D Projects: GA MŠk(CZ) LO1204; GA ČR(CZ) GA15-15264S Institutional support: RVO:61389030 Keywords : cyclin-dependent kinase * inhibitor * cancer Subject RIV: FR - Pharmacology ; Medidal Chemistry Impact factor: 9.135, year: 2015

The refined 2.0 A X-ray crystal structure of the complex formed between bovine beta-trypsin and CMTI-I, a trypsin inhibitor from squash seeds (Cucurbita maxima). Topological similarity of the squash seed inhibitors with the carboxypeptidase A inhibitor from potatoes.

Science.gov (United States)

Bode, W; Greyling, H J; Huber, R; Otlewski, J; Wilusz, T

1989-01-02

The stoichiometric complex formed between bovine beta-trypsin and the Cucurbita maxima trypsin inhibitor I (CMTI-I) was crystallized and its X-ray crystal structure determined using Patterson search techniques. Its structure has been crystallographically refined to a final R value of 0.152 (6.0-2.0 A). CMTI-I is of ellipsoidal shape; it lacks helices or beta-sheets, but consists of turns and connecting short polypeptide stretches. The disulfide pairing is CYS-3I-20I, Cys-10I-22I and Cys-16I-28I. According to the polypeptide fold and disulfide connectivity its structure resembles that of the carboxypeptidase A inhibitor from potatoes. Thirteen of the 29 inhibitor residues are in direct contact with trypsin; most of them are in the primary binding segment Val-2I (P4)-Glu-9I (P4') which contains the reactive site bond Arg-5I-Ile-6I and is in a conformation observed also for other serine proteinase inhibitors.

SS-A/Ro52 promotes apoptosis by regulating Bcl-2 production

Energy Technology Data Exchange (ETDEWEB)

Jauharoh, Siti Nur Aisyah [Department of Clinical Pathology and Immunology, Kobe University Graduate School of Medicine, Hyogo 650-0017 (Japan); Faculty of Medicine and Health Science, Syarif Hidayatullah State Islamic University, Jakarta 15412 (Indonesia); Saegusa, Jun; Sugimoto, Takeshi [Department of Clinical Pathology and Immunology, Kobe University Graduate School of Medicine, Hyogo 650-0017 (Japan); Ardianto, Bambang [Department of Clinical Pathology and Immunology, Kobe University Graduate School of Medicine, Hyogo 650-0017 (Japan); Department of Child Health, Faculty of Medicine, Gadjah Mada University, Yogyakarta 55282 (Indonesia); Kasagi, Shimpei; Sugiyama, Daisuke; Kurimoto, Chiyo [Department of Clinical Pathology and Immunology, Kobe University Graduate School of Medicine, Hyogo 650-0017 (Japan); Tokuno, Osamu; Nakamachi, Yuji [Department of Laboratory Medicine, Kobe University Hospital, Hyogo 650-0017 (Japan); Kumagai, Shunichi [Department of Clinical Pathology and Immunology, Kobe University Graduate School of Medicine, Hyogo 650-0017 (Japan); Kawano, Seiji, E-mail: sjkawano@med.kobe-u.ac.jp [Department of Clinical Pathology and Immunology, Kobe University Graduate School of Medicine, Hyogo 650-0017 (Japan); Department of Laboratory Medicine, Kobe University Hospital, Hyogo 650-0017 (Japan)

2012-01-06

Highlights: Black-Right-Pointing-Pointer Ro52{sup low} HeLa cells are resistant to apoptosis upon various stimulations. Black-Right-Pointing-Pointer Ro52 is upregulated by IFN-{alpha}, etoposide, or IFN-{gamma} and anti-Fas Ab. Black-Right-Pointing-Pointer Ro52-mediated apoptosis is independent of p53. Black-Right-Pointing-Pointer Ro52 selectively regulates Bcl-2 expression. -- Abstract: SS-A/Ro52 (Ro52), an autoantigen in systemic autoimmune diseases such as systemic lupus erythematosus and Sjoegren's syndrome, has E3 ligase activity to ubiquitinate proteins that protect against viral infection. To investigate Ro52's role during stress, we transiently knocked it down in HeLa cells by siRo52 transfection. We found that Ro52{sup low} HeLa cells were significantly more resistant to apoptosis than wild-type HeLa cells when stimulated by H{sub 2}O{sub 2}- or diamide-induced oxidative stress, IFN-{alpha}, IFN-{gamma} and anti-Fas antibody, etoposide, or {gamma}-irradiation. Furthermore, Ro52-mediated apoptosis was not influenced by p53 protein level in HeLa cells. Depleting Ro52 in HeLa cells caused Bcl-2, but not other Bcl-2 family molecules, to be upregulated. Taken together, our data showed that Ro52 is a universal proapoptotic molecule, and that its proapoptotic effect does not depend on p53, but is exerted through negative regulation of the anti-apoptotic protein Bcl-2. These findings shed light on a new physiological role for Ro52 that is important to intracellular immunity.

SS-A/Ro52 promotes apoptosis by regulating Bcl-2 production

International Nuclear Information System (INIS)

Jauharoh, Siti Nur Aisyah; Saegusa, Jun; Sugimoto, Takeshi; Ardianto, Bambang; Kasagi, Shimpei; Sugiyama, Daisuke; Kurimoto, Chiyo; Tokuno, Osamu; Nakamachi, Yuji; Kumagai, Shunichi; Kawano, Seiji

2012-01-01

Highlights: ► Ro52 low HeLa cells are resistant to apoptosis upon various stimulations. ► Ro52 is upregulated by IFN-α, etoposide, or IFN-γ and anti-Fas Ab. ► Ro52-mediated apoptosis is independent of p53. ► Ro52 selectively regulates Bcl-2 expression. -- Abstract: SS-A/Ro52 (Ro52), an autoantigen in systemic autoimmune diseases such as systemic lupus erythematosus and Sjögren’s syndrome, has E3 ligase activity to ubiquitinate proteins that protect against viral infection. To investigate Ro52’s role during stress, we transiently knocked it down in HeLa cells by siRo52 transfection. We found that Ro52 low HeLa cells were significantly more resistant to apoptosis than wild-type HeLa cells when stimulated by H 2 O 2 - or diamide-induced oxidative stress, IFN-α, IFN-γ and anti-Fas antibody, etoposide, or γ-irradiation. Furthermore, Ro52-mediated apoptosis was not influenced by p53 protein level in HeLa cells. Depleting Ro52 in HeLa cells caused Bcl-2, but not other Bcl-2 family molecules, to be upregulated. Taken together, our data showed that Ro52 is a universal proapoptotic molecule, and that its proapoptotic effect does not depend on p53, but is exerted through negative regulation of the anti-apoptotic protein Bcl-2. These findings shed light on a new physiological role for Ro52 that is important to intracellular immunity.

CoRoT’s first seven planets: An overview*

Directory of Open Access Journals (Sweden)

Barge P.

2011-07-01

Full Text Available The up to 150 day uninterrupted high-precision photometry of about 100000 stars – provided so far by the exoplanet channel of the CoRoT space telescope – gave a new perspective on the planet population of our galactic neighbourhood. The seven planets with very accurate parameters widen the range of known planet properties in almost any respect. Giant planets have been detected at low metallicity, rapidly rotating and active, spotted stars. CoRoT-3 populated the brown dwarf desert and closed the gap of measured physical properties between standard giant planets and very low mass stars. CoRoT extended the known range of planet masses down-to 5 Earth masses and up to 21 Jupiter masses, the radii to less than 2 Earth radii and up to the most inflated hot Jupiter found so far, and the periods of planets discovered by transits to 9 days. Two CoRoT planets have host stars with the lowest content of heavy elements known to show a transit hinting towards a different planet-host-star-metallicity relation then the one found by radial-velocity search programs. Finally the properties of the CoRoT-7b prove that terrestrial planets with a density close to Earth exist outside the Solar System. The detection of the secondary transit of CoRoT-1 at the 10−5-level and the very clear detection of the 1.7 Earth radii of CoRoT-7b at 3.5 10−4 relative flux are promising evidence of CoRoT being able to detect even smaller, Earth sized planets.

Techno-economic investigation of alternative propulsion plants for Ferries and RoRo ships

International Nuclear Information System (INIS)

Livanos, George A.; Theotokatos, Gerasimos; Pagonis, Dimitrios-Nikolaos

2014-01-01

Highlights: • Alternative Diesel and Gas engine propulsion plants of Ferries and RoRos were studied. • Special focus on marine Natural Gas burning engines and ship waste heat recovery systems. • Significant savings in annual operating costs were predicted in the case of Natural Gas engines. • Environmental and economic optimum propulsion plant alternative was proposed in a specific case study. - Abstract: In this paper, the main alternative propulsion plants based on reciprocating internal combustion engines of a ferry or RoRo ship operating in routes that include Emission Control Areas (ECAs) are comparatively assessed. Specifically, a dual fuel engine propulsion plant is compared with a conventional Diesel engine plant. For both cases, the installation of a waste heat recovery system, which covers a part of the ship electric energy demand, is also considered. The ship main DF engines are assumed to operate using LNG and a small amount of MDO for initiating combustion, whereas low sulphur MDO was regarded as the fuel for the case of the Diesel engine plant. The installation of Selective Catalytic Reduction (SCR) after-treatment unit for reducing the NOx emissions for the case of Diesel engines plant is also taken into account. The propulsion plants were modelled under steady state conditions, and the simulation results were analysed in order to compare the alternative configurations. Furthermore, the Energy Efficiency Design Index (EEDI) values were calculated and the two examined propulsion system cases were compared on EEDI basis. Finally, the Life Cycle Cost for each alternative propulsion plant was calculated and used for completing an economic evaluation of the Dual fuel propulsion plant versus the conventional designs applied in ferries

The reversible N-oxidation of the nitroimidazole radiosensitizer Ro 03-8799

International Nuclear Information System (INIS)

Walton, M.I.; Bleehen, N.M.; Workman, P.; Cambridge Univ.

1985-01-01

The nitroimidazole radiosensitizer Ro 03-8799 and the N-oxide Ro 31-0313 were dissolved in buffered solution and given i.v. to inbred male mice. Drug concentrations in whole blood, blood plasma and urine were determined by MPLC. Ro 03 8799 is rapidly cleared and extensively metabolised. Ro 31-0313 is reduced back to Ro 03-8799 by whole blood. The pharmacological and toxicological consequences of this are unknown. (UK)

Alcohols are inhibitors of Saccharomyces cerevisiae multidrug-resistance pumps Pdr5p and Snq2p

Czech Academy of Sciences Publication Activity Database

Gášková, D.; Plášek, J.; Zahumenský, J.; Benešová, I.; Buriánková, I.; Sigler, Karel

2013-01-01

Roč. 13, č. 8 (2013), s. 782-795 ISSN 1567-1356 Institutional support: RVO:61388971 Keywords : alcohols * yeast MDR pump * pump inhibitor Subject RIV: EE - Microbiology, Virology Impact factor: 2.436, year: 2013

Abnormal clinical pharmacokinetics of the developmental radiosensitizers pimonidazole (Ro 03-8799) and etanidazole (SR 2508)

International Nuclear Information System (INIS)

Maughan, T.S.; Newman, H.F.; Bleehen, N.M.; Ward, R.; Workman, P.

1990-01-01

The hypoxic cell radiosensitizers Ro 03-8799 (pimonidazole) and SR 2508 (etanidazole) are under evaluation as single agents (Phase III) and in combination (Phase I). Ro 03-8799 produces an acute, transient central nervous system syndrome, whereas SR 2508 causes cumulative, peripheral neurotoxicity; both effects are dose-limiting. Pharmacokinetic studies have shown the importance of area under the plasma drug concentration versus time curve (AUC) in predicting the risk of peripheral neuropathy. Most patients have very similar pharmacokinetic parameters. This study reports 2/25 patients receiving 0.75 g/m2 Ro 03-8799 plus 2.0 g/m2 SR 2508 who showed significant discrepancies in drug handling. One patient exhibited a markedly elevated AUC and prolonged t1/2 beta for SR 2508 and this was associated with an unusually rapid onset of peripheral neuropathy. A second patient showed normal handling of SR 2508 but prolonged values for both t1/2 alpha and t1/2 beta for Ro 03-8799 and unusually low levels of its N-oxide metabolite. In addition a low peak Ro 03-8799 concentration combined with a very high volume of distribution was found in this patient, leading to a normal AUC value and toxicity profile. Both patients exhibited a relatively low creatinine clearance. The mechanisms which may underlie these findings are discussed, and the importance of pharmacokinetic monitoring in the use of these agents is emphasized

The feasibility of nanofiltration membrane bioreactor (NF-MBR)+reverse osmosis (RO) process for water reclamation: Comparison with ultrafiltration membrane bioreactor (UF-MBR)+RO process.

Science.gov (United States)

Tay, Ming Feng; Liu, Chang; Cornelissen, Emile R; Wu, Bing; Chong, Tzyy Haur

2018-02-01

This study examines the feasibility of a novel nanofiltration membrane bioreactor (NF-MBR) followed by reverse osmosis (RO) process for water reclamation at 90% recovery and using an ultrafiltration MBR (UF-MBR)+RO as baseline for comparison. Both MBRs adopted the same external hollow fiber membrane configurations and operating conditions. The collected permeates of the MBRs were subsequently fed to the respective RO systems. The results showed that the NF-MBR (operated at a constant flux of 10 L/m 2 h) achieved superior MBR permeate quality due to enhanced biodegradation and high rejection capacity of the NF membrane, leading to lower RO fouling rates (∼3.3 times) as compared to the UF-MBR. Further analysis indicated that the cake layer fouling that caused the cake-enhanced osmotic pressure (CEOP) effect contributed predominantly to the transmembrane pressure (TMP) increase in the NF-MBR, while irreversible pore fouling was the major reason for UF membrane fouling. Furthermore, it was found that the biopolymers (i.e., organics with MW > 10 kDa) were the main components present in the foulants of the NF/UF membranes and RO membranes. The analysis indicated that the NF-MBR + RO system at recovery of 90% has comparable energy consumption as the UF-MBR + RO system at recovery of 75%. Our findings proved the feasibility of the NF-MBR + RO for water reclamation at a high recovery rate. Copyright © 2017 Elsevier Ltd. All rights reserved.

Disseminated Infections with Talaromyces marneffei in Non-AIDS Patients Given Monoclonal Antibodies against CD20 and Kinase Inhibitors

OpenAIRE

Chan, Jasper F.W.; Chan, Thomas S.Y.; Gill, Harinder; Lam, Frank Y.F.; Trendell-Smith, Nigel J.; Sridhar, Siddharth; Tse, Herman; Lau, Susanna K.P.; Hung, Ivan F.N.; Yuen, Kwok-Yung; Woo, Patrick C.Y.

2015-01-01

Infections with the fungus Talaromyces (formerly Penicillium) marneffei are rare in patients who do not have AIDS. We report disseminated T. marneffei infection in 4 hematology patients without AIDS who received targeted therapy with monoclonal antibodies against CD20 or kinase inhibitors during the past 2 years. Clinicians should be aware of this emerging complication, especially in patients from disease-endemic regions.

Rebound increase in seizure susceptibility but not isolation-induced calls after single administration of clonazepam and Ro 19-8022 in infant rats

Czech Academy of Sciences Publication Activity Database

Mikulecká, Anna; Mareš, Pavel; Kubová, Hana

2011-01-01

Roč. 20, č. 1 (2011), s. 12-19 ISSN 1525-5050 R&D Projects: GA ČR(CZ) GA305/09/0846 Institutional research plan: CEZ:AV0Z50110509 Keywords : Pentylenetetrazole-induced seizure * ultrasonic vocalization * motor performance * Clonazepam * Ro 19-8022 * immature rats Subject RIV: FH - Neurology Impact factor: 2.335, year: 2011

Trisubstituted purine inhibitors of PDGFR alpha and their antileukemic activity in the human eosinophilic cell line EOL-1

Czech Academy of Sciences Publication Activity Database

Malínková, Veronika; Řezníčková, Eva; Jorda, Radek; Gucký, T.; Kryštof, Vladimír

2017-01-01

Roč. 25, č. 24 (2017), s. 6523-6535 ISSN 0968-0896 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : dependent kinase inhibitors * src tyrosine kinase * 2,6,9-trisubstituted purines * therapeutic target * potent inhibitor * imatinib * leukemia * mutations * mutant * domain Subject RIV: EB - Genetics ; Molecular Biology OBOR OECD: Hematology Impact factor: 2.930, year: 2016

Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP

Directory of Open Access Journals (Sweden)

Hsueh Chung-Tsen

2011-04-01

Full Text Available Abstract We reviewed preclinical data and clinical development of MDM2 (murine double minute 2, ALK (anaplastic lymphoma kinase and PARP (poly [ADP-ribose] polymerase inhibitors. MDM2 binds to p53, and promotes degradation of p53 through ubiquitin-proteasome degradation. JNJ-26854165 and RO5045337 are 2 small-molecule inhibitors of MDM2 in clinical development. ALK is a transmembrane protein and a member of the insulin receptor tyrosine kinases. EML4-ALK fusion gene is identified in approximately 3-13% of non-small cell lung cancer (NSCLC. Early-phase clinical studies with Crizotinib, an ALK inhibitor, in NSCLC harboring EML4-ALK have demonstrated promising activity with high response rate and prolonged progression-free survival. PARPs are a family of nuclear enzymes that regulates the repair of DNA single-strand breaks through the base excision repair pathway. Randomized phase II study has shown adding PARP-1 inhibitor BSI-201 to cytotoxic chemotherapy improves clinical outcome in patients with triple-negative breast cancer. Olaparib, another oral small-molecule PARP inhibitor, demonstrated encouraging single-agent activity in patients with advanced breast or ovarian cancer. There are 5 other PARP inhibitors currently under active clinical investigation.

Expression and localization of acrosin inhibitor in boar reproductive tract

Czech Academy of Sciences Publication Activity Database

Davidová, Nina; Jonáková, Věra; Maňásková-Postlerová, Pavla

2009-01-01

Roč. 338, č. 2 (2009), s. 303-311 ISSN 0302-766X R&D Projects: GA ČR GA303/09/1285; GA MŠk 1M06011; GA ČR GD523/08/H064 Institutional research plan: CEZ:AV0Z50520701 Keywords : Acrosin inhibitor * Reproductive tract * Spermatozoa * Boar Subject RIV: CE - Biochemistry Impact factor: 2.308, year: 2009

Study of acrosin inhibitor along the boar epididymis

Czech Academy of Sciences Publication Activity Database

Davidová, Nina; Dorosh, Andriy; Jonáková, Věra; Postlerová, Pavla

2010-01-01

Roč. 33, Supplement 1 (2010), s. 70-71 ISSN 0105-6263. [6th European Congress of And rology. 29.09.2010-01.10.2010, Athens] R&D Projects: GA ČR(CZ) GA303/09/1285; GA MŠk(CZ) 1M06011; GA ČR(CZ) GD523/08/H064 Institutional research plan: CEZ:AV0Z50520701 Keywords : spermatozoa * acrosin inhibitor * proteolytic enzymes * glycosidic enzyme * glycoproteins * antibody Subject RIV: CE - Biochemistry

Ab initio ro-vibronic spectroscopy of SiCCl (X{sup ~2}Π)

Energy Technology Data Exchange (ETDEWEB)

Brites, Vincent [Université d’Evry Val d’Essonne, Laboratoire Analyse et Modélisation pour la Biologie et l’Environnement, LAMBE CNRS UMR 8587, Boulevard F. Mitterrand, 91025 Evry Cedex (France); Mitrushchenkov, Alexander O.; Léonard, Céline, E-mail: celine.leonard@u-pem.fr [Université Paris-Est, Laboratoire Modélisation et Simulation Multi Echelle, MSME UMR 8208 CNRS, 5 bd Descartes, 77454 Marne-la-Vallée (France); Peterson, Kirk A. [Department of Chemistry, Washington State University, Pullman, Washington 99164 (United States)

2014-07-21

The full dimensional potential energy surfaces of the {sup 2}A{sup ′} and {sup 2}A{sup ′′} electronic components of X{sup ~2}Π SiCCl have been computed using the explicitly correlated coupled cluster method, UCCSD(T)-F12b, combined with a composite approach taking into account basis set incompleteness, core-valence correlation, scalar relativity, and higher order excitations. The spin-orbit and dipole moment surfaces have also been computed ab initio. The ro-vibronic energy levels and absorption spectrum at 5 K have been determined from variational calculations. The influence of each correction on the fundamental frequencies is discussed. An assignment is proposed for bands observed in the LIF experiment of Smith et al. [J. Chem. Phys. 117, 6446 (2002)]. The overall agreement between the experimental and calculated ro-vibronic levels is better than 7 cm{sup −1} which is comparable with the 10–20 cm{sup −1} resolution of the emission spectrum.

Methyl and Pentyl Chloride in a Microhydrated Environment and at the Liquid Water-Vapor Interface: A Theoretical Study

Czech Academy of Sciences Publication Activity Database

Pašalič, H.; Roeselová, Martina; Lischka, H.

2011-01-01

Roč. 115, č. 8 (2011), s. 1807-1816 ISSN 1520-6106 R&D Projects: GA MŠk ME09064; GA MŠk LC512; GA ČR(CZ) GAP208/10/1724 Institutional research plan: CEZ:AV0Z40550506 Keywords : alkyl halides * air-water interface Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 3.696, year: 2011

Effect of Piper betle on Giardia intestinalis infection in vivo

Czech Academy of Sciences Publication Activity Database

Pecková, R.; Doležal, Karel; Sak, Bohumil; Květoňová, Dana; Kváč, Martin; Nurcahyo, W.; Foitová, I.

2018-01-01

Roč. 184, JAN (2018), s. 39-45 ISSN 0014-4894 R&D Projects: GA ČR(CZ) GAP505/11/1163 Institutional support: RVO:61389030 ; RVO:60077344 Keywords : Antigiardial activity * Drug of choice * Giardia intestinalis * Natural antiparasitics * Parasites * Piper betle Subject RIV: EF - Botanics OBOR OECD: Plant sciences, botany Impact factor: 1.724, year: 2016

Cream and albinotic – two new mutations affecting body colour in Pyrrhocoris apterus (Heteroptera: Pyrrhocoridae)

Czech Academy of Sciences Publication Activity Database

Socha, Radomír

2011-01-01

Roč. 108, č. 1 (2011), s. 17-24 ISSN 1210-5759 R&D Projects: GA ČR GAP501/10/1215 Institutional research plan: CEZ:AV0Z50070508 Keywords : firebug * body- colour mutants * albinotic Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 1.061, year: 2011 http://www.eje.cz/scripts/viewabstract.php?abstract=1582

Effects of selected Indonesian plant extracts on E. cuniculi infection in vivo

Czech Academy of Sciences Publication Activity Database

Sak, Bohumil; Jandova, Anna; Doležal, Karel; Kváč, Martin; Květoňová, Dana; Hlásková, Lenka; Rost, M.; Olšanský, M.; Nurcahyo, W.; Foitová, I.

2017-01-01

Roč. 181, OCT (2017), s. 94-101 ISSN 0014-4894 R&D Projects: GA ČR(CZ) GAP505/11/1163; GA ČR GA14-20684S Institutional support: RVO:60077344 ; RVO:61389030 Keywords : molecular detection * antifungal * plant extract * Encephalitozoon cuniculi * in vivo Subject RIV: EG - Zoology OBOR OECD: Zoology Impact factor: 1.724, year: 2016

Combining combinatorial chemistry and affinity chromatography: highly selective inhibitors of human betaine:homocysteine S-methyltransferase

Czech Academy of Sciences Publication Activity Database

Collinsová, Michaela; Castro, C.; Garrow, T. A.; Yiotakis, A.; Dive, V.; Jiráček, Jiří

2003-01-01

Roč. 10, - (2003), s. 113-122 ISSN 1074-5521 R&D Projects: GA AV ČR IAB4055003 Institutional research plan: CEZ:AV0Z4055905 Keywords : BHMT * inhibitor * phosphinic Subject RIV: CE - Biochemistry Impact factor: 6.129, year: 2003

Simple, mammalian cell-based assay for identification of inhibitors of the Erk MAP kinase pathway

Czech Academy of Sciences Publication Activity Database

Krejčí, Pavel; Pejchalová, K.; Wilcox, W.R.

2007-01-01

Roč. 25, č. 4 (2007), s. 391-395 ISSN 0167-6997 Institutional research plan: CEZ:AV0Z50040507; CEZ:AV0Z50040702 Keywords : Erk * inhibitor * FGFR3 Subject RIV: BO - Biophysics Impact factor: 2.806, year: 2007

AstRoMap European Astrobiology Roadmap.

Science.gov (United States)

Horneck, Gerda; Walter, Nicolas; Westall, Frances; Grenfell, John Lee; Martin, William F; Gomez, Felipe; Leuko, Stefan; Lee, Natuschka; Onofri, Silvano; Tsiganis, Kleomenis; Saladino, Raffaele; Pilat-Lohinger, Elke; Palomba, Ernesto; Harrison, Jesse; Rull, Fernando; Muller, Christian; Strazzulla, Giovanni; Brucato, John R; Rettberg, Petra; Capria, Maria Teresa

2016-03-01

The European AstRoMap project (supported by the European Commission Seventh Framework Programme) surveyed the state of the art of astrobiology in Europe and beyond and produced the first European roadmap for astrobiology research. In the context of this roadmap, astrobiology is understood as the study of the origin, evolution, and distribution of life in the context of cosmic evolution; this includes habitability in the Solar System and beyond. The AstRoMap Roadmap identifies five research topics, specifies several key scientific objectives for each topic, and suggests ways to achieve all the objectives. The five AstRoMap Research Topics are • Research Topic 1: Origin and Evolution of Planetary Systems • Research Topic 2: Origins of Organic Compounds in Space • Research Topic 3: Rock-Water-Carbon Interactions, Organic Synthesis on Earth, and Steps to Life • Research Topic 4: Life and Habitability • Research Topic 5: Biosignatures as Facilitating Life Detection It is strongly recommended that steps be taken towards the definition and implementation of a European Astrobiology Platform (or Institute) to streamline and optimize the scientific return by using a coordinated infrastructure and funding system.

Cancer Cell Resistance to Aurora Kinase Inhibitors: Identification of Novel Targets for Cancer Therapy

Czech Academy of Sciences Publication Activity Database

Hrabáková, Rita; Kollaredy, M.; Tylečková, Jiřina; Halada, Petr; Hajdúch, M.; Gadher, S. J.; Kovářová, Hana

2013-01-01

Roč. 12, č. 1 (2013), s. 455-469 ISSN 1535-3893 R&D Projects: GA MŠk LC07017 Institutional support: RVO:67985904 ; RVO:61388971 Keywords : Aurora kinase inhibitors * resistance * p53 * apoptosis Subject RIV: CE - Biochemistry Impact factor: 5.001, year: 2013

The development of a new class of inhibitors for betaine-homocysteine S-methyltransferase

Czech Academy of Sciences Publication Activity Database

Pícha, Jan; Vaněk, Václav; Buděšínský, Miloš; Mládková, Jana; Garrow, T. A.; Jiráček, Jiří

2013-01-01

Roč. 65, July (2013), s. 256-275 ISSN 0223-5234 R&D Projects: GA ČR(CZ) GAP207/10/1277 Institutional support: RVO:61388963 Keywords : BHMT * inhibitor * homocysteine * phosphonate * phosphinate * amino acid derivative * bioisostere * S-alkylated homocysteine Subject RIV: CE - Biochemistry Impact factor: 3.432, year: 2013

Konstruiranje ročaja hidravličnih klešč

OpenAIRE

Žižek, Tomaž

2015-01-01

V diplomskem delu je opisan potek konstruiranja ročaja hidravličnih klešč za odstranjevanje ločnega podporja v Premogovniku Velenje. Predstavljeni so vsi pomembnejši koraki, in sicer modeliranje klešč, modeliranje ročaja, numerični rezultati, izbira najustreznejše oblike ročaja ter predstavitev rezultatov ustreznega modela. Diplomsko delo zajema tudi izbiro ustreznega materiala, postopek izdelave ter podatke za pravilno varjenje ročaja na ohišje klešč. Numerični preračuni so opravljeni v pro...

Detection of small-size planetary candidates with CoRoT data

Directory of Open Access Journals (Sweden)

Moutou C.

2011-02-01

Full Text Available With the discovery of CoRoT-7b, the first transiting super-Earth, the CoRoT space mission has shown the capability to detect short-period rocky planets around solar-like stars. By performing a blind test with real CoRoT light curves, we want to establish the detection threshold of small-size planets in CoRoT data. We investigate the main obstacles to the detection of transiting super-Earths in CoRoT data, notably the presence of short-time scale variability and hot pixels.

USA uus ÜRO saadik alustas pealetungi / Neeme Raud

Index Scriptorium Estoniae

Raud, Neeme, 1969-

2005-01-01

Ameerika Ühendriikide uus ÜRO suursaadik John Bolton nõuab 190 liikmesriigile saadetud kirjas ÜRO reformikavades suurte ja oluliste muudatuste tegemist: reformikavast peaks USA arvates kustutama vähemalt 400 paragrahvi

Staurosporine, but not Ro 31-8220, induces interleukin 2 production and synergizes with interleukin 1alpha in EL4 thymoma cells.

Science.gov (United States)

Mahon, T M; Matthews, J S; O'Neill, L A

1997-07-01

Protein kinase C (PKC) has been implicated in interleukin 1 (IL1) signal transduction in a number of cellular systems, either as a key event in IL1 action or as a negative regulator. Here we have examined the effects of two PKC inhibitors, staurosporine and the more selective agent Ro 31-8220, on IL1 responses in the murine thymoma line EL4.NOB-1. A 1 h pulse of staurosporine was found to strongly potentiate the induction of IL2 by IL1alpha in these cells. In contrast, neither a pulse nor prolonged incubation with Ro 31-8220 affected the response to IL1alpha. Both agents blocked the response to PMA, however. A 1 h pulse of staurosporine was also found to induce IL2 production on its own, activate the transcription factor nuclear factor kappaB (NFkappaB) and increase the expression of a NFkappaB-linked reporter gene. It synergized with IL1alpha in all of these responses. Ro 31-8220 was again without effect, although both staurosporine and Ro 31-8220 blocked the activation of NFkappaB by PMA. Finally, staurosporine caused the translocation of PKC-alpha and -epsilon, and to a lesser extent PKC-beta, but not PKC-θ or -zeta, from the cytosol to the membrane, although a similar effect was observed with Ro 31-8220. The results suggest that PKC is not involved in IL1alpha signalling in EL4 cells. Furthermore, the potentiating effect of staurosporine on IL1alpha action does not involve PKC inhibition, and is likely to be at the level of NFkappaB activation.

Removal of Pharmaceutical and Personal Care Products (PPCPs) from Municipal Waste Water with Integrated Membrane Systems, MBR-RO/NF.

Science.gov (United States)

Wang, Yonggang; Wang, Xu; Li, Mingwei; Dong, Jing; Sun, Changhong; Chen, Guanyi

2018-02-05

This study focuses on the application of combining membrane bioreactor (MBR) treatment with reverse osmosis (RO) or nanofiltration (NF) membrane treatment for removal of pharmaceuticals and personal care products (PPCPs) in municipal wastewater. Twenty-seven PPCPs were measured in real influent with lowest average concentration being trimethoprim (7.12 ng/L) and the highest being caffeine (18.4 ng/L). The results suggest that the MBR system effectively removes the PPCPs with an efficiency of between 41.08% and 95.41%, and that the integrated membrane systems, MBR-RO/NF, can achieve even higher removal rates of above 95% for most of them. The results also suggest that, due to the differences in removal mechanisms of NF/RO membrane, differences of removal rates exist. In this study, the combination of MBR-NF resulted in the removal of 13 compounds to below detection limits and MBR-RO achieved even better results with removal of 20 compounds to below detection limits.

Protease Inhibitors in Tick Saliva: The Role of Serpins and Cystatins in Tick-host-Pathogen Interaction

Czech Academy of Sciences Publication Activity Database

Chmelař, J.; Kotál, Jan; Langhansová, Helena; Kotsyfakis, Michalis

2017-01-01

Roč. 7, MAY 29 (2017), č. článku 276. ISSN 2235-2988 Institutional support: RVO:60077344 Keywords : tick-host interaction * immunomodulation * protease inhibitors * serpins * cystatins Subject RIV: EC - Immunology OBOR OECD: Immunology Impact factor: 4.300, year: 2016

The Dushak–Erekdag Survey of roAp Stars

Indian Academy of Sciences (India)

2016-01-27

Jan 27, 2016 ... The search of roAp stars at Mt. Dushak–Erekdag Observatory was started in 1992 using the 0.8m Odessa telescope equipped with a two-star high-speed photometer. We have observed more than a dozen stars so far and discovered HD 99563 as roAp star while BD+8087 is suspected to have rapid ...

Characterization of the insulin-sensitive low Km cAMP phosphodiesterase from rat adipose tissue

International Nuclear Information System (INIS)

Degerman, E.; Belfrage, P.; Manganiello, V.C.

1986-01-01

Particulate, but not soluble, low K/sub m/ cAMP phosphodiesterase (PDE) activity of rat adipocytes was increased 50-100% during incubation (10 min) of intact cells with 1-3 nM insulin; activation was less with higher or lower insulin concentrations. Activation was maintained during solubilization with an alkyl polyoxyethylene non-ionic detergent C 13 , E 12 and NaBr and chromatography on DEAE. Enzyme from DEAE was further purified by chromatography on Sepahadex G-200 and Blue-Sepharose. Activity (with 0.5 μM [ 3 H]cAMP) was rather sensitive to inhibition by p-chloromercuribenzoate (IC 50 , 1 μM) and less so by 2,2'-dithiobis-(5-nitropyridine) (160 μM), N-ethylmaleimide (525 μM) and iodoacetamide (750 μM). PDE activity was also rather sensitive to inhibition by cilostamide (IC 50 , ∼40 nM) and the cardiotonic drugs CI 930 (450 nM) and milrinone (630 nM) but rather insensitive to RO 20-1724 (190 μM). Based on effects of these inhibitors, the hormone-sensitive low K/sub m/ particulate cAMP PDE from rat adipocytes seems to be analogous to the insulin-activated particulate PDE from 3T3-L1 adipocytes and the cilostamide-sensitive soluble low K/sub m/ cAMP PDE from bovine liver (designated as III-C), platelets, heart, and other tissues

Fungal Gene-Encoded Peptidase Inhibitors

Czech Academy of Sciences Publication Activity Database

Bauerová, Václava; Pichová, Iva; Hrušková-Heidingsfeldová, Olga

2013-01-01

Roč. 20, č. 25 (2013), s. 3041-3048 ISSN 0929-8673 Institutional support: RVO:61388963 Keywords : AFUEI * Avr2 * cystatin * fungi * IA3 * IAPs * I2B Subject RIV: CE - Biochemistry Impact factor: 3.715, year: 2013

Design of Plasmodium vivax Hypoxanthine-Guanine Phosphoribosyltransferase Inhibitors as Potential Antimalarial Therapeutics

Czech Academy of Sciences Publication Activity Database

Keough, D. T.; Rejman, Dominik; Pohl, Radek; Zborníková, Eva; Hocková, Dana; Croll, T.; Edstein, M. D.; Birrell, G. W.; Chavchich, M.; Naesens, L. M. J.; Pierens, G. K.; Brereton, I. M.; Guddat, L. W.

2018-01-01

Roč. 13, č. 1 (2018), s. 82-90 ISSN 1554-8929 R&D Projects: GA ČR(CZ) GA16-06049S; GA ČR GA15-11711S Institutional support: RVO:61388963 Keywords : plasmodium vivax * inhibitor * pyrrolidine nucleotide bisphosphonate * HXGPRT Subject RIV: CC - Organic Chemistry OBOR OECD: Organic chemistry Impact factor: 4.995, year: 2016

Radiosensitization of mouse spermatogenic stem cells by Ro-07-0582

International Nuclear Information System (INIS)

Suzuki, N.; Withers, R.; Hunter, N.

1977-01-01

The hypoxic character of the spermatogenic stem cells of the mouse testis was investigated by measuring the effect on radiosensitivity of treatment with the hypoxic cell radiosensitizer, Ro-07-0582 or hyperbaric oxygen (30 psi). The D 0 values obtained were 181 (161-207) rad for irradiation alone, 140 (133-148) rad for irradiation after treatment with Ro-07-0582, and about 100 rad for irradiation in the presence of hyperbaric oxygen. Ro-07-0582 alone was slightly cytotoxic. The results demonstrate that mouse spermatogenic stem cells are radiosensitized by Ro-07-0582 or hyperbaric oxygen and are not as well oxygenated as other normal tissues

Design of Highly Potent Urea-Based, Exosite-Binding Inhibitors Selective for Glutamate Carboxypeptidase II

Czech Academy of Sciences Publication Activity Database

Tykvart, Jan; Schimer, Jiří; Jančařík, Andrej; Bařinková, Jitka; Navrátil, Václav; Starková, Jana; Šrámková, Karolína; Konvalinka, Jan; Majer, Pavel; Šácha, Pavel

2015-01-01

Roč. 58, č. 10 (2015), s. 4357-4363 ISSN 0022-2623 R&D Projects: GA ČR GBP208/12/G016; GA MŠk LO1302 Institutional support: RVO:61388963 Keywords : GCPII selective inhibitors * GCPIII * GCPII Subject RIV: CE - Biochemistry Impact factor: 5.589, year: 2015

The course of infection caused by Encephalitozoon cuniculi genotype III in immunocompetent and immunodeficient mice

Czech Academy of Sciences Publication Activity Database

Kotková, Michaela; Sak, Bohumil; Hlásková, Lenka; Kváč, Martin

2017-01-01

Roč. 182, November (2017), s. 16-21 ISSN 0014-4894 R&D Projects: GA ČR GA17-12871S; GA ČR GA14-20684S Institutional support: RVO:60077344 Keywords : albendazole * BALB/C * Encephalitozoon cuniculi genotypes II and III * microsporidiosis * SCID Subject RIV: FN - Epidemiology, Contagious Diseases ; Clinical Immunology OBOR OECD: Infectious Diseases Impact factor: 1.724, year: 2016

Antimalarial activity of prodrugs of N-branched acyclic nucleoside phosphonate inhibitors of 6-oxopurine phosphoribosyltransferases

Czech Academy of Sciences Publication Activity Database

Hocková, Dana; Janeba, Zlatko; Naesens, L.; Edstein, M. D.; Chavchich, M.; Keough, D. T.; Guddat, L. W.

2015-01-01

Roč. 23, č. 17 (2015), s. 5502-5510 ISSN 0968-0896 R&D Projects: GA ČR GAP207/11/0108 Institutional support: RVO:61388963 Keywords : nucleotide analogues * enzyme inhibitors * malaria * HG(X)PRT * ANP Subject RIV: CC - Organic Chemistry Impact factor: 2.923, year: 2015

DSP-based CSO cancellation technique for RoF transmission system implemented by using directly modulated laser.

Science.gov (United States)

Kim, Byung Gon; Bae, Sung Hyun; Kim, Hoon; Chung, Yun C

2017-05-29

We propose and demonstrate a simple composite second-order (CSO) cancellation technique based on the digital signal processing (DSP) for the radio-over-fiber (RoF) transmission system implemented by using directly modulated lasers (DMLs). When the RoF transmission system is implemented by using DMLs, its performance could be limited by the CSO distortions caused by the interplay between the DML's chirp and fiber's chromatic dispersion. We present the theoretical analysis of these nonlinear distortions and show that they can be suppressed at the receiver by using a simple DSP. To verify the effectiveness of the proposed technique, we demonstrate the transmission of twenty-four 100-MHz filtered orthogonal frequency-division multiplexing (f-OFDM) signals in 64 quadrature amplitude modulation (QAM) format over 20 km of the standard single-mode fiber (SSMF). The results show that, by using the proposed technique, we can suppress the CSO distortion components by >10 dB and achieve the error-vector magnitude performance better than 6% even after the 20-km long SSMF transmission.

RoMPS concept review automatic control of space robot

Science.gov (United States)

1991-01-01

The Robot operated Material Processing in Space (RoMPS) experiment is being performed to explore the marriage of two emerging space commercialization technologies: materials processing in microgravity and robotics. This concept review presents engineering drawings and limited technical descriptions of the RoMPS programs' electrical and software systems.

U-61,431F, a stable prostacyclin analogue, inhibits the proliferation of bovine vascular smooth muscle cells with little antiproliferative effect on endothelial cells

International Nuclear Information System (INIS)

Shirotani, M.; Yui, Y.; Hattori, R.; Kawai, C.

1991-01-01

The effects of U-61,431F, ciprostene, a stable prostacyclin analogue, were examined on the proliferation of cultured quiescent bovine aortic endothelial cells (EC) and smooth muscle cells (SMC). After stimulation with 5% fetal calf serum, U-61,431F suppressed both the DNA synthesis and proliferation of SMC dose-dependently at the concentration of 3-100 microM, but had no effect on either of them in EC at a concentration of up to 30 microM. The inhibitory effect on DNA synthesis was greater in SMC than in EC at 3-50 microM. When SMC were stimulated with platelet-derived growth factor (PDGF) for 2 hrs followed by a 22-hr incubation with insulin, U-61,431F (1-50 microM) administered at the time of PDGF stimulation did not inhibit DNA synthesis. SMC initiated and terminated DNA synthesis at about 15-18 h and 24 h after stimulation with serum, respectively. Inhibition of DNA synthesis in serum-stimulated SMC as a function of the addition time of U-61,431F reduced at 3-12 h after the stimulation. U-61,431F raised the cyclic AMP (cAMP) content in SMC. Moreover, a phosphodiesterase inhibitor, 3-isobutyl-1-methylxanthine, and a more specific cAMP phosphodiesterase inhibitor, Ro 20-1724, augmented the inhibition of DNA synthesis in SMC concomitant with further elevation of cAMP level. These results suggest that U-61,431F inhibits DNA synthesis of SMC acting in the progression stage rather than in the competence stage, with little antiproliferative effect on EC. cAMP may play an important role in its antiproliferative action in SMC

Structure-activity study of new inhibitors of human betaine-homocysteine S-methyltransferase

Czech Academy of Sciences Publication Activity Database

Vaněk, Václav; Buděšínský, Miloš; Kabeleová, Petra; Šanda, Miloslav; Kožíšek, Milan; Hančlová, Ivona; Mládková, Jana; Brynda, Jiří; Rosenberg, Ivan; Koutmos, M.; Garrow, T. A.; Jiráček, Jiří

2009-01-01

Roč. 52, č. 12 (2009), s. 3652-3665 ISSN 0022-2623 R&D Projects: GA MŠk 1M0508 Grant - others:GA MŠk(CZ) LC06077; NIH(US) R01TW0052501 Program:LC Institutional research plan: CEZ:AV0Z40550506 Keywords : BHMT * betain * homocysteine * methionine * inhibitor Subject RIV: CE - Biochemistry Impact factor: 4.802, year: 2009

S-alkylated homocysteine derivatives: New inhibitors of human betaine-homocysteine S-methyltransferase

Czech Academy of Sciences Publication Activity Database

Jiráček, Jiří; Collinsová, Michaela; Rosenberg, Ivan; Buděšínský, Miloš; Protivínská, Eva; Netušilová, Hana; Garrow, T. A.

2006-01-01

Roč. 49, č. 13 (2006), s. 3982-3989 ISSN 0022-2623 R&D Projects: GA AV ČR(CZ) IAA4055302 Grant - others:NIH(US) DK52501; NIH(US) R01TW0052501; IARS(US) 50-352 Institutional research plan: CEZ:AV0Z40550506 Keywords : BHMT * S-alkylated homocystein e * inhibitor Subject RIV: CE - Biochemistry Impact factor: 5.115, year: 2006

Reduced Levels of Tissue Inhibitors of Metalloproteinases in UVB-Irradiated Corneal Epithelium

Czech Academy of Sciences Publication Activity Database

Ardan, Taras; Němcová, Lucie; Bohuslavová, Božena; Klezlová, A.; Popelka, Štěpán; Studenovská, Hana; Hrnčiarová, Eva; Čejková, Jitka; Motlík, Jan

2016-01-01

Roč. 92, č. 5 (2016), s. 720-727 ISSN 0031-8655 R&D Projects: GA ČR GPP302/10/P155; GA MŠk(CZ) LO1609 Institutional support: RVO:67985904 ; RVO:61389013 ; RVO:68378041 Keywords : tissue inhibitors of metalloproteinases * matrix metalloproteinases Subject RIV: EB - Genetics ; Molecular Biology; CD - Macromolecular Chemistry (UMCH-V) Impact factor: 2.121, year: 2016

Transiting exoplanets from the CoRoT space mission. VIII. CoRoT-7b: the first super-Earth with measured radius

Science.gov (United States)

Léger, A.; Rouan, D.; Schneider, J.; Barge, P.; Fridlund, M.; Samuel, B.; Ollivier, M.; Guenther, E.; Deleuil, M.; Deeg, H. J.; Auvergne, M.; Alonso, R.; Aigrain, S.; Alapini, A.; Almenara, J. M.; Baglin, A.; Barbieri, M.; Bruntt, H.; Bordé, P.; Bouchy, F.; Cabrera, J.; Catala, C.; Carone, L.; Carpano, S.; Csizmadia, Sz.; Dvorak, R.; Erikson, A.; Ferraz-Mello, S.; Foing, B.; Fressin, F.; Gandolfi, D.; Gillon, M.; Gondoin, Ph.; Grasset, O.; Guillot, T.; Hatzes, A.; Hébrard, G.; Jorda, L.; Lammer, H.; Llebaria, A.; Loeillet, B.; Mayor, M.; Mazeh, T.; Moutou, C.; Pätzold, M.; Pont, F.; Queloz, D.; Rauer, H.; Renner, S.; Samadi, R.; Shporer, A.; Sotin, Ch.; Tingley, B.; Wuchterl, G.; Adda, M.; Agogu, P.; Appourchaux, T.; Ballans, H.; Baron, P.; Beaufort, T.; Bellenger, R.; Berlin, R.; Bernardi, P.; Blouin, D.; Baudin, F.; Bodin, P.; Boisnard, L.; Boit, L.; Bonneau, F.; Borzeix, S.; Briet, R.; Buey, J.-T.; Butler, B.; Cailleau, D.; Cautain, R.; Chabaud, P.-Y.; Chaintreuil, S.; Chiavassa, F.; Costes, V.; Cuna Parrho, V.; de Oliveira Fialho, F.; Decaudin, M.; Defise, J.-M.; Djalal, S.; Epstein, G.; Exil, G.-E.; Fauré, C.; Fenouillet, T.; Gaboriaud, A.; Gallic, A.; Gamet, P.; Gavalda, P.; Grolleau, E.; Gruneisen, R.; Gueguen, L.; Guis, V.; Guivarc'h, V.; Guterman, P.; Hallouard, D.; Hasiba, J.; Heuripeau, F.; Huntzinger, G.; Hustaix, H.; Imad, C.; Imbert, C.; Johlander, B.; Jouret, M.; Journoud, P.; Karioty, F.; Kerjean, L.; Lafaille, V.; Lafond, L.; Lam-Trong, T.; Landiech, P.; Lapeyrere, V.; Larqué, T.; Laudet, P.; Lautier, N.; Lecann, H.; Lefevre, L.; Leruyet, B.; Levacher, P.; Magnan, A.; Mazy, E.; Mertens, F.; Mesnager, J.-M.; Meunier, J.-C.; Michel, J.-P.; Monjoin, W.; Naudet, D.; Nguyen-Kim, K.; Orcesi, J.-L.; Ottacher, H.; Perez, R.; Peter, G.; Plasson, P.; Plesseria, J.-Y.; Pontet, B.; Pradines, A.; Quentin, C.; Reynaud, J.-L.; Rolland, G.; Rollenhagen, F.; Romagnan, R.; Russ, N.; Schmidt, R.; Schwartz, N.; Sebbag, I.; Sedes, G.; Smit, H.; Steller, M. B.; Sunter, W.; Surace, C.; Tello, M.; Tiphène, D.; Toulouse, P.; Ulmer, B.; Vandermarcq, O.; Vergnault, E.; Vuillemin, A.; Zanatta, P.

2009-10-01

Aims: We report the discovery of very shallow (Δ F/F ≈ 3.4× 10-4), periodic dips in the light curve of an active V = 11.7 G9V star observed by the CoRoT satellite, which we interpret as caused by a transiting companion. We describe the 3-colour CoRoT data and complementary ground-based observations that support the planetary nature of the companion. Methods: We used CoRoT colours information, good angular resolution ground-based photometric observations in- and out- of transit, adaptive optics imaging, near-infrared spectroscopy, and preliminary results from radial velocity measurements, to test the diluted eclipsing binary scenarios. The parameters of the host star were derived from optical spectra, which were then combined with the CoRoT light curve to derive parameters of the companion. Results: We examined all conceivable cases of false positives carefully, and all the tests support the planetary hypothesis. Blends with separation >0.40´´or triple systems are almost excluded with a 8 × 10-4 risk left. We conclude that, inasmuch we have been exhaustive, we have discovered a planetary companion, named CoRoT-7b, for which we derive a period of 0.853 59 ± 3 × 10-5 day and a radius of Rp = 1.68 ± 0.09 R_Earth. Analysis of preliminary radial velocity data yields an upper limit of 21 M_Earth for the companion mass, supporting the finding. Conclusions: CoRoT-7b is very likely the first Super-Earth with a measured radius. This object illustrates what will probably become a common situation with missions such as Kepler, namely the need to establish the planetary origin of transits in the absence of a firm radial velocity detection and mass measurement. The composition of CoRoT-7b remains loosely constrained without a precise mass. A very high surface temperature on its irradiated face, ≈1800-2600 K at the substellar point, and a very low one, ≈50 K, on its dark face assuming no atmosphere, have been derived. The CoRoT space mission, launched on 27

News Agency Website Agenda on Religion. Comparative Analysis on Mediafax.ro and Agerpres.ro

Directory of Open Access Journals (Sweden)

Aurelia Ana Vasile

2016-06-01

Full Text Available According to the “Global Index of Religiosity and Atheism” (WIN-Gallup International, 27 July 2012, retrieved 24 August 2012, which was a global 2012 poll, the reports label 59% of the world's population as “religious” and 36% as not religious, including 13% who are atheists, with a 9% decrease in religious belief from 2005. Thereto, religion is an important issue of inherent influence in the media nowadays. Despite the ongoing secularization process that we are facing these days, humans still feel the need to refer to religion within their attempt to construct one’s own outlook on life, and to make some sense out of existence in general (Max Weber, 19202. A comparative content analysis on Mediafax.ro and Agerpres.ro, performed for an almost nine-and-a-half-month time span (1st January to 13th October 2015, showed interesting facts on how press agency journalists relate to religion as a media topic, both in terms of quality (key words and key topics and in terms of quantity. A comparison between the Orthodox religion of the majority of the Romanians, and other denominations, also accounted for intriguing research findings.

Contribution of HIV minority variants to drug resistance in an integrase strand transfer inhibitor-based therapy

Czech Academy of Sciences Publication Activity Database

Weber, Jan; Gibson, R. M.; Meyer, A. M.; Winner, D.; Robertson, D. L.; Miller, M. D.; Quinones-Mateu, M. E.

2013-01-01

Roč. 18, Suppl. 1 (2013), A66-A66 ISSN 1359-6535. [International Workshop on HIV & Hepatitis Virus Drug Resistance Curative Strategies. 04.06.2013-08.06.2013, Toronto] Institutional support: RVO:61388963 Keywords : HIV minority variants * integrase inhibitor * replicative fitness Subject RIV: CE - Biochemistry

Evaluation of RO modules for the SSP ETC/LSS.

Science.gov (United States)

Jasionowski, W. J.; Bambenek, R. A.

1973-01-01

During the past eight years the NASA Manned Spacecraft Center has supported the development of an Integrated Water and Waste Management System for use in the Space Station Prototype (SSP) Environmental Thermal Control/Life-Support System (ETC/LSS). This system includes the reverse osmosis (RO) process for recycling wash water and the compression distillation process for recovering useable water from urine, urinal flush water, humidity condensate, commode flush water and the wash water concentrated by RO. This paper summarizes the experimental work performed during the past four years to select the best commercially available RO module for this system and to also define which surfactants and germicides are most compatible with the selected module.

Planetary transit candidates in CoRoT LRa01 field

DEFF Research Database (Denmark)

Carone, L.; Gandolfi, D.; Cabrera, J.

2012-01-01

We present the list of planetary transit candidates from the CoRoT LRa01 star field in the Monoceros constellation toward the Galactic anti-center direction. The CoRoT observations of LRa01 lasted from 24 October 2007 to 3 March 2008. We acquired and analyzed 7470 chromatic and 3938 monochromatic...... lightcurves. Instrumental noise and stellar variability were treated with several filtering tools by different teams from the CoRoT community. Different transit search algorithms were applied to the lightcurves. (2 data files)....

Validation of Robotic Surgery Simulator (RoSS).

Science.gov (United States)

Kesavadas, Thenkurussi; Stegemann, Andrew; Sathyaseelan, Gughan; Chowriappa, Ashirwad; Srimathveeravalli, Govindarajan; Seixas-Mikelus, Stéfanie; Chandrasekhar, Rameella; Wilding, Gregory; Guru, Khurshid

2011-01-01

Recent growth of daVinci Robotic Surgical System as a minimally invasive surgery tool has led to a call for better training of future surgeons. In this paper, a new virtual reality simulator, called RoSS is presented. Initial results from two studies - face and content validity, are very encouraging. 90% of the cohort of expert robotic surgeons felt that the simulator was excellent or somewhat close to the touch and feel of the daVinci console. Content validity of the simulator received 90% approval in some cases. These studies demonstrate that RoSS has the potential of becoming an important training tool for the daVinci surgical robot.

Double-Headed Sulfur-Linked Amino Acids As First Inhibitors for Betaine-Homocysteine S-Methyltransferase 2

Czech Academy of Sciences Publication Activity Database

Mládková, Jana; Vaněk, Václav; Buděšínský, Miloš; Elbert, Tomáš; Demianova, Zuzana; Garrow, T. A.; Jiráček, Jiří

2012-01-01

Roč. 55, č. 15 (2012), s. 6822-6831 ISSN 0022-2623 R&D Projects: GA ČR GA203/09/1919; GA ČR(CZ) GAP207/10/1277 Institutional support: RVO:61388963 Keywords : betaine * homocysteine * methionine * BHMT * inhibitor Subject RIV: CE - Biochemistry Impact factor: 5.614, year: 2012

Cuentos ashaninka del r??o Peren??

OpenAIRE

Plasencia Soto, Rommel; S??nchez V??squez, Melisa

2009-01-01

La memoria ind??gena de los pueblos amaz??nicos del Per?? de hoy, es mostrada en cuatro relatos registrados en la comunidad de Mariscal C??ceres en el valle del r??o Peren?? de la selva central peruana.

Growth and characterization of thin oriented Co3O4 (111) films obtained by decomposition of layered cobaltates NaxCoO2

Czech Academy of Sciences Publication Activity Database

Buršík, Josef; Soroka, Miroslav; Kužel, R.; Mika, Filip

2015-01-01

Roč. 227, JUL (2015), s. 17-24 ISSN 0022-4596 R&D Projects: GA ČR GA13-03708S; GA ČR(CZ) GA14-18392S Institutional support: RVO:61388980 ; RVO:68081731 Keywords : Cobalt oxides * Spinels * Layered cobaltates * Chemical solution deposition * Thin films Subject RIV: CA - Inorganic Chemistry; JA - Electronics ; Optoelectronics, Electrical Engineering (UPT-D) Impact factor: 2.265, year: 2015

Transforming Anion Instability into Stability: Contrasting Photoionization of Three Protonation Forms of the Phosphate Ion upon Moving into Water

Czech Academy of Sciences Publication Activity Database

Pluhařová, Eva; Ončák, M.; Seidel, R.; Schroeder, C.; Schroeder, W.; Winter, B.; Bradforth, S. E.; Jungwirth, Pavel; Slavíček, P.

2012-01-01

Roč. 116, č. 44 (2012), s. 13254-13264 ISSN 1520-6106 R&D Projects: GA ČR(CZ) GAP208/10/1724; GA ČR GA203/08/0114 Institutional research plan: CEZ:AV0Z40550506 Keywords : multiply-charged anions * ab-initio calculations * aqueous-solution * photoelectron-spectroscopy * ionization energies * emission-spectroscopy Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 3.607, year: 2012

Radical chemistry at a rural site (Wangdu) in the North China Plain: observation and model calculations of OH, HO2 and RO2 radicals

Science.gov (United States)

Tan, Zhaofeng; Fuchs, Hendrik; Lu, Keding; Hofzumahaus, Andreas; Bohn, Birger; Broch, Sebastian; Dong, Huabin; Gomm, Sebastian; Häseler, Rolf; He, Lingyan; Holland, Frank; Li, Xin; Liu, Ying; Lu, Sihua; Rohrer, Franz; Shao, Min; Wang, Baolin; Wang, Ming; Wu, Yusheng; Zeng, Limin; Zhang, Yinsong; Wahner, Andreas; Zhang, Yuanhang

2017-01-01

A comprehensive field campaign was carried out in summer 2014 in Wangdu, located in the North China Plain. A month of continuous OH, HO2 and RO2 measurements was achieved. Observations of radicals by the laser-induced fluorescence (LIF) technique revealed daily maximum concentrations between (5-15) × 106 cm-3, (3-14) × 108 cm-3 and (3-15) × 108 cm-3 for OH, HO2 and RO2, respectively. Measured OH reactivities (inverse OH lifetime) were 10 to 20 s-1 during daytime. The chemical box model RACM 2, including the Leuven isoprene mechanism (LIM), was used to interpret the observed radical concentrations. As in previous field campaigns in China, modeled and measured OH concentrations agree for NO mixing ratios higher than 1 ppbv, but systematic discrepancies are observed in the afternoon for NO mixing ratios of less than 300 pptv (the model-measurement ratio is between 1.4 and 2 in this case). If additional OH recycling equivalent to 100 pptv NO is assumed, the model is capable of reproducing the observed OH, HO2 and RO2 concentrations for conditions of high volatile organic compound (VOC) and low NOx concentrations. For HO2, good agreement is found between modeled and observed concentrations during day and night. In the case of RO2, the agreement between model calculations and measurements is good in the late afternoon when NO concentrations are below 0.3 ppbv. A significant model underprediction of RO2 by a factor of 3 to 5 is found in the morning at NO concentrations higher than 1 ppbv, which can be explained by a missing RO2 source of 2 ppbv h-1. As a consequence, the model underpredicts the photochemical net ozone production by 20 ppbv per day, which is a significant portion of the daily integrated ozone production (110 ppbv) derived from the measured HO2 and RO2. The additional RO2 production from the photolysis of ClNO2 and missing reactivity can explain about 10 % and 20 % of the discrepancy, respectively. The underprediction of the photochemical ozone

Coupling of RO-MSF hybrid desalination plants with nuclear reactors

International Nuclear Information System (INIS)

Al-Sulaiman, Khalil; Al-Mutaz, Ibrahim S.

1999-01-01

Full text.Reverse osmosis (RO) and multistage flash (MSF) desalination are the most widely commercial available processes. MSF utilizes stream in the brine heater as a primary source of energy. RO is derived mainly by electricity that pumps the feed water against the mambranes. Steam and electricity and be produced easily by nuclear reactors. Nuclear reactors may be coupled with deslination plants (MSF, RO or combined (hybrid) RO/MSF configuration). This integrated plant will be capable of producing power and water at reasonable cost. The capital and operating cost will be reduced and the excess power can be efficiently utilized. Maintenance and operating cost will drop significantly. In this paper, a techno-economic study of hybrid reverses osmosis /multistage flash desalination will be carried. The proposed configuration (hybrid RO/MSF) coupled with nuclear reactor is considered the most appropriate candidate system for the application of dual-purpose nuclear desalination plants. the design parameters for such a desalination hybrid system will be the applied pressure and recovery for reverse osmosis plant and the number of stages and the heat transfer areas for multistage flash plant

Diagnostic and prognostic significance of measuring antibodies to alpha-fodrin compared to anti-Ro-52, anti-Ro-60, and anti-La in primary Sjogren's syndrome

DEFF Research Database (Denmark)

Pelck, R.; Manthorpe, R.; Locht, Henning

2008-01-01

OBJECTIVE: To compare sensitivity and specificity of autoantibodies to alpha-fodrin with conventional anti-Ro and anti-La antibodies in patients with primary Sjogren's syndrome (pSS). Data on internal organ manifestations were correlated with presence of autoantibodies. METHODS: We collected...... clinical and laboratory data from 321 patients with pSS (Copenhagen criteria), of which 205 fulfilled the new American-European 2002 consensus criteria. Sera were tested for autoantibodies against alpha-fodrin and recombinant Ro-52, Ro-60, and La proteins. RESULTS: Antibodies to alpha-fodrin were...

Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine

Czech Academy of Sciences Publication Activity Database

Jorda, Radek; Dušek, J.; Řezníčková, Eva; Pauk, K.; Magar, P. P.; Imramovský, A.; Kryštof, Vladimír

2017-01-01

Roč. 135, JUL 28 (2017), s. 142-158 ISSN 0223-5234 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Apoptosis * Inhibitor * Proteasome * Salicylamide * Ubiquitin Subject RIV: EB - Genetics ; Molecular Biology OBOR OECD: Biochemical research methods Impact factor: 4.519, year: 2016

Inhibition of Post-Transcriptional RNA Processing by CDK Inhibitors and Its Implication in Anti-Viral Therapy

Czech Academy of Sciences Publication Activity Database

Holčáková, J.; Müller, P.; Tomasec, P.; Hrstka, R.; Nekulová, M.; Kryštof, Vladimír; Strnad, Miroslav; Wilkinson, G. W. G.; Vojtěšek, B.

2014-01-01

Roč. 9, č. 2 (2014) E-ISSN 1932-6203 R&D Projects: GA ČR GBP206/12/G151 Institutional support: RVO:61389030 Keywords : IMMUNODEFICIENCY-VIRUS TYPE-1 * DEPENDENT KINASE INHIBITORS * LARGE T-ANTIGEN Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 3.234, year: 2014

Douglas R.O. Morrison

CERN Multimedia

2001-01-01

Douglas R.O. Morrison 1929 - 2001 Douglas' friends and colleagues are warmly invited to join in a memorial gathering on Friday, 23 March 2001 at 16.00 hours in the CERN Main Auditorium Some colleagues will pay tribute to Douglas' scientific achievements and to his role in leading the collaborations:   Welcome, short CV The 'hadron times' The 'neutrino times' Recent activities Collaborations The 'social environment' A book of condolence will be available. The gathering will conclude with refreshments in the Salle des Pas Perdus.

Identification of anti-proliferative kinase inhibitors as potential therapeutic agents to treat canine osteosarcoma.

Science.gov (United States)

Mauchle, Ulrike; Selvarajah, Gayathri T; Mol, Jan A; Kirpensteijn, Jolle; Verheije, Monique H

2015-08-01

Osteosarcoma is the most common primary bone tumour in dogs but various forms of therapy have not significantly improved clinical outcomes. As dysregulation of kinase activity is often present in tumours, kinases represent attractive molecular targets for cancer therapy. The purpose of this study was to identify novel compounds targeting kinases with the potential to induce cell death in a panel of canine osteosarcoma cell lines. The ability of 80 well-characterized kinase inhibitor compounds to inhibit the proliferation of four canine osteosarcoma cell lines was investigated in vitro. For those compounds with activity, the mechanism of action and capability to potentiate the activity of doxorubicin was further evaluated. The screening showed 22 different kinase inhibitors that induced significant anti-proliferative effects across the four canine osteosarcoma cell lines investigated. Four of these compounds (RO 31-8220, 5-iodotubercidin, BAY 11-7082 and an erbstatin analog) showed significant cell growth inhibitory effects across all cell lines in association with variable induction of apoptosis. RO 31-8220 and 5-iodotubercidin showed the highest ability to potentiate the effects of doxorubicin on cell viability. In conclusion, the present study identified several potent kinase inhibitors targeting the PKC, CK1, PKA, ErbB2, mTOR and NF-κB pathways, which may warrant further investigations for the treatment of osteosarcoma in dogs. Copyright © 2014 Elsevier Ltd. All rights reserved.

Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models

Czech Academy of Sciences Publication Activity Database

Tavares, M. T.; Shen, S.; Knox, T.; Hadley, M.; Kutil, Zsofia; Bařinka, Cyril; Villagra, A.; Kozikowski, A. P.

2017-01-01

Roč. 8, č. 10 (2017), s. 1031-1036 ISSN 1948-5875 R&D Projects: GA ČR GA15-19640S; GA MŠk(CZ) ED1.1.00/02.0109 Institutional support: RVO:86652036 Keywords : HDAC6 inhibitors * nexturastat A * melanoma Subject RIV: FR - Pharmacology ; Medidal Chemistry OBOR OECD: Biochemistry and molecular biology Impact factor: 3.746, year: 2016

Sõjaraport õõnestab ÜRO usaldusväärsust / Jürgen Tamme

Index Scriptorium Estoniae

Tamme, Jürgen

2011-01-01

ÜRO Gaza sõda puudutavas raportis kritiseeritakse nii Iisraeli kui ka Palestiina islamistlikku äärmusrühmitust Hamas. ÜRO inimõiguste uurija Richard Goldstone leiab, et raport on siiski puudulik, kuna praegu omab ÜRO juba rohkem infot Gaza sõja kohta

Fellow's Apéro

CERN Multimedia

Staff Association

2017-01-01

Let's get together, meet each other, exchange experiences and ideas, and share useful information on CERN and the Staff Association. Join us for Fellow's Apéro, organised by the Staff Association on Tuesday 21 February at 16.30 in Restaurant 1. There will be drinks and snacks for everybody! We look forward to seeing you there! Please confirm your participation on Doodle http://doodle.com/poll/skvm7ucm2z78i6bt or alternatively on Facebook https://www.facebook.com/events/1862757017340069/. Your delegates in the Staff Association, Barbora & Jiri

Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor

Czech Academy of Sciences Publication Activity Database

Kryštof, Vladimír; McNae, I. W.; Walkinshaw, M. D.; Fischer, P.M.; Müller, P.; Vojtešek, B.; Orság, Martin; Havlíček, Libor; Strnad, Miroslav

2005-01-01

Roč. 62, č. 15 (2005), s. 1763-1771 ISSN 1420-682X R&D Projects: GA ČR GP204/03/D231 Institutional research plan: CEZ:AV0Z50380511 Keywords : olomoucine II * roscovitine * cyclin-dependent kinase inhibitor Subject RIV: CE - Biochemistry Impact factor: 4.582, year: 2005

Clinical and Pathological Roles of Ro/SSA Autoantibody System

Directory of Open Access Journals (Sweden)

Ryusuke Yoshimi

2012-01-01

Full Text Available Anti-Ro/SSA antibodies are among the most frequently detected autoantibodies against extractable nuclear antigens and have been associated with systemic lupus erythematosus (SLE and Sjögren's syndrome (SS. Although the presence of these autoantibodies is one of the criteria for the diagnosis and classification of SS, they are also sometimes seen in other systemic autoimmune diseases. In the last few decades, the knowledge of the prevalence of anti-Ro/SSA antibodies in various autoimmune diseases and symptoms has been expanded, and the clinical importance of these antibodies is increasing. Nonetheless, the pathological role of the antibodies is still poorly understood. In this paper, we summarize the milestones of the anti-Ro/SSA autoantibody system and provide new insights into the association between the autoantibodies and the pathogenesis of autoimmune diseases.

De novo design of alpha-amylase inhibitor: A small linear mimetic of macromolecular proteinaceous ligands

Czech Academy of Sciences Publication Activity Database

Marešová, Lucie; Pavlík, Manfred; Horn, Martin; Mareš, Michael

2005-01-01

Roč. 12, č. 12 (2005), 1349-1357 ISSN 1074-5521 R&D Projects: GA ČR(CZ) GP203/02/P081; GA MŠk(CZ) OC D16.001 Institutional research plan: CEZ:AV0Z40550506 Keywords : amylase * peptide inhibitor * combinatorial chemistry Subject RIV: CE - Biochemistry Impact factor: 6.138, year: 2005

Expression of BAFF receptors in muscle tissue of myositis patients with anti-Jo-1 or anti-Ro52/anti-Ro60 autoantibodies.

Science.gov (United States)

Kryštůfková, Olga; Barbasso Helmers, Sevim; Venalis, Paulius; Malmström, Vivianne; Lindroos, Eva; Vencovský, Jiří; Lundberg, Ingrid E

2014-10-10

Anti-Jo-1 and anti-Ro52 autoantibodies are common in patients with myositis, but the mechanisms behind their production are not known. Survival of autoantibody-producing cells is dependent on B-cell-activating factor of the tumour necrosis factor family (BAFF). BAFF levels are elevated in serum of anti-Jo-1-positive myositis patients and are influenced by type-I interferon (IFN). IFN-producing cells and BAFF mRNA expression are present in myositis muscle. We investigated expression of the receptors for BAFF in muscle tissue in relation to anti-Jo-1 and anti-Ro52/anti-Ro60 autoantibodies and type-I IFN markers. Muscle biopsies from 23 patients with myositis selected based on autoantibody profile and 7 healthy controls were investigated for expression of BAFF receptor (BAFF-R), B-cell maturation antigen (BCMA) and transmembrane activator and calcium modulator and cyclophilin ligand interactor (TACI). Nineteen samples were assessed for plasma (CD138) and B-cell (CD19) markers. The numbers of positive cells per area were compared with the expression of plasmacytoid dendritic cell (pDC) marker blood dendritic cell antigen-2 (BDCA-2) and IFNα/β-inducible myxovirus resistance-1 protein (MX-1). BAFF-R, BCMA and TACI were expressed in five, seven and seven patients, respectively, and more frequently in anti-Jo-1-positive and/or anti-Ro52/anti-Ro60-positive patients compared to controls and to patients without these autoantibodies (P = BAFF-R: 0.007, BCMA: 0.03 and TACI: 0.07). A local association of receptors with B and plasma cells was confirmed by confocal microscopy. The numbers of CD138-positive and BCMA-positive cells were correlated (r = 0.79; P = 0.001). Expression of BDCA-2 correlated with numbers of CD138-positive cells and marginally with BCMA-positive cells (r = 0.54 and 0.42, respectively; P = 0.04 and 0.06, respectively). There was a borderline correlation between the numbers of positively stained TACI cells and MX-1 areas (r = 0.38, P = 0.08). The expression

Magnetic fields in proton solar flare of X17.2/4B class according to data of simultaneous measurements in a few spectral lines

Science.gov (United States)

Lozitsky, V.; Lozitska, N.

2017-06-01

Spectral-polarized magnetic field measurements in solar flare of 28 October 2003 of X17.2/4B class are compared in six FeI lines and in Hα line. Observations were carried out on Echelle spectrograph of horizontal solar telescope of Astronomical Observatory of Taras Shevchenko National University of Kyiv. Presented data relate to peak phase of flare and a place of photosphere outside sunspots where effective (average) magnetic field in FeI 6302.5 line was about 100 G and had S polarity. Measured splitting of emissive peaks in cores of strong FeI lines of 15th multiplet correspond to stronger fields, in range 550-700 G and S polarity too. Noticeablre splitting of emissive peaks (11-20 mÅ) were found also in Fe I 5434.527 line with effective Lande factor geff = -0.014. Value of this splitting and its sign indicate the existence of extremely strong fields of 25-50 kG of opposite (N) polarity which had negative Doppler velocities (lifting of plasma) on level of 1.7-2.2 km/sec. Magnetic field according to Hα line was 300 G and N polarity. Presented results indicate the essential inhomogeneity of magnetic field in flare volume which include the opposite polarities along the line of sight and wide range of effective magnetic fields.

Identification of a novel A20-binding inhibitor of nuclear factor-kappa B activation termed ABIN-2.

Science.gov (United States)

Van Huffel, S; Delaei, F; Heyninck, K; De Valck, D; Beyaert, R

2001-08-10

The nuclear factor kappaB (NF-kappaB) plays a central role in the regulation of genes implicated in immune responses, inflammatory processes, and apoptotic cell death. The zinc finger protein A20 is a cellular inhibitor of NF-kappaB activation by various stimuli and plays a critical role in terminating NF-kappaB responses. The underlying mechanism for NF-kappaB inhibition by A20 is still unknown. A20 has been shown to interact with several proteins including tumor necrosis factor (TNF) receptor-associated factors 2 and 6, as well as the inhibitory protein of kappaB kinase (IKK) gamma protein. Here we report the cloning and characterization of ABIN-2, a previously unknown protein that binds to the COOH-terminal zinc finger domain of A20. NF-kappaB activation induced by TNF and interleukin-1 is inhibited by overexpression of ABIN-2. The latter also inhibits NF-kappaB activation induced by overexpression of receptor-interacting protein or TNF receptor-associated factor 2. In contrast, NF-kappaB activation by overexpression of IKKbeta or direct activators of the IKK complex, such as Tax, cannot be inhibited by ABIN-2. These results indicate that ABIN-2 interferes with NF-kappaB activation upstream of the IKK complex and that it might contribute to the NF-kappaB-inhibitory function of A20.

Acyclic Nucleoside Phosphonates Containing a Second Phosphonate Group Are Potent Inhibitors of 6-Oxopurine Phosphoribosyltransferases and Have Antimalarial Activity

Czech Academy of Sciences Publication Activity Database

Keough, D. T.; Špaček, Petr; Hocková, Dana; Tichý, Tomáš; Vrbková, S.; Slavětínská, Lenka; Janeba, Zlatko; Naesens, L.; Edstein, M. D.; Chavchich, M.; Wang, T. H.; de Jersey, J.; Guddat, L. W.

2013-01-01

Roč. 56, č. 6 (2013), s. 2513-2526 ISSN 0022-2623 R&D Projects: GA ČR GAP207/11/0108 Institutional support: RVO:61388963 Keywords : enzyme inhibitors * ANPs * malaria * bisphosphonates Subject RIV: CC - Organic Chemistry Impact factor: 5.480, year: 2013

Treatment and Prevention of Breast Cancer Using Multifunctional Inhibitors of Cholesterol Biosynthesis

Science.gov (United States)

2015-08-01

suggesting an allosteric modification of estrogen receptor  RO blocks the production of an estrogen regulated gene ( progesterone receptor) in...alternative targets in the pathway leading to the production of cholesterol, which might be regulated with less toxic inhibitors to control the progression of...to effectively treat and prevent cancers of the breast. Our goal was to identify alternative targets in the pathway leading to the production of

Sensitive Detection of the Natural Killer Cell-Mediated Cytotoxicity of Anti-CD20 Antibodies and Its Impairment by B-Cell Receptor Pathway Inhibitors

Directory of Open Access Journals (Sweden)

Floyd Hassenrück

2018-01-01

Full Text Available The antibody-dependent cell-mediated cytotoxicity (ADCC of the anti-CD20 monoclonal antibodies (mAbs rituximab and obinutuzumab against the cell line Raji and isolated CLL cells and its potential impairment by kinase inhibitors (KI was determined via lactate dehydrogenase release or calcein retention, respectively, using genetically modified NK92 cells expressing CD16-176V as effector cells. Compared to peripheral blood mononuclear cells, recombinant effector cell lines showed substantial alloreactivity-related cytotoxicity without addition of mAbs but afforded determination of ADCC with reduced interassay variability. The cytotoxicity owing to alloreactivity was less susceptible to interference by KI than the ADCC of anti-CD20 mAbs, which was markedly diminished by ibrutinib, but not by idelalisib. Compared to rituximab, the ADCC of obinutuzumab against primary CLL cells showed approximately 30% higher efficacy and less interference with KI. Irreversible BTK inhibitors at a clinically relevant concentration of 1 μM only weakly impaired the ADCC of anti-CD20 mAbs, with less influence in combinations with obinutuzumab than with rituximab and by acalabrutinib than by ibrutinib or tirabrutinib. In summary, NK cell line-based assays permitted the sensitive detection of ADCC of therapeutic anti-CD20 mAbs against CLL cells and of the interference of KI with this important killing mechanism.

CoRoT-2b: a Tidally Inflated, Young Exoplanet?

Science.gov (United States)

Guillot, Tristan; Havel, M.

2009-09-01

CoRoT-2b is among the most anomalously large transiting exoplanet known. Due to its large mass (3.3 Mjup), its large radius ( 1.5 Rjup) cannot be explained by standard evolution models. Recipes that work for other anomalously large exoplanets (e.g. HD209458b), such as invoking kinetic energy transport in the planetary interior or increased opacities, clearly fail for CoRoT-2b. Interestingly, the planet's parent star is an active star with a large fraction (7 to 20%) of spots and a rapid rotation (4.5 days). We first model the star's evolution to accurately constrain the planetary parameters. We find that the stellar activity has little influence on the star's evolution and inferred parameters. However, stellar evolution models point towards two kind of solutions for the star-planet system: (i) a very young system (20-40 Ma) with a star still undergoing pre-main sequence contraction, and a planet which could have a radius as low as 1.4 Rjup, or (ii) a young main-sequence star (40 to 500 Ma) with a planet that is slightly more inflated ( 1.5 Rjup). In either case, planetary evolution models require a significant added internal energy to explain the inferred planet size: from a minimum of 3x1028 erg/s in case (i), to up to 1.5x1029 erg/s in case (ii). We find that evolution models consistently including planet/star tides are able to reproduce the inferred radius but only for a short period of time ( 10 Ma). This points towards a young age for the star/planet system and dissipation by tides due to either circularization or synchronization of the planet. Additional observations of the star (infrared excess due to disk?) and of the planet (precise Rossiter effect, IR secondary eclispe) would be highly valuable to understand the early evolution of star-exoplanet systems.

Impact of RO-desalted water on distribution water qualities.

Science.gov (United States)

Taylor, J; Dietz, J; Randall, A; Hong, S

2005-01-01

A large-scale pilot distribution study was conducted to investigate the impacts of blending different source waters on distribution water qualities, with an emphasis on metal release (i.e. corrosion). The principal source waters investigated were conventionally treated ground water (G1), surface water processed by enhanced treatment (S1), and desalted seawater by reverse osmosis membranes (RO). Due to the nature of raw water quality and associated treatment processes, G1 water had high alkalinity, while S1 and RO sources were characterized as high sulfate and high chloride waters, respectively. The blending ratio of different treated waters determined the quality of finished waters. Iron release from aged cast iron pipes increased significantly when exposed to RO and S1 waters: that is, the greater iron release was experienced with alkalinity reduced below the background of G1 water. Copper release to drinking water, however, increased with increasing alkalinity and decreasing pH. Lead release, on the other hand, increased with increasing chloride and decreasing sulfate. The effect of pH and alkalinity on lead release was not clearly observed from pilot blending study. The flat and compact corrosion scales observed for lead surface exposed to S1 water may be attributable to lead concentration less than that of RO water blends.

Structure-Aided Design of Novel Inhibitors of HIV Protease Based on a Benzodiazepine Scaffold

Czech Academy of Sciences Publication Activity Database

Schimer, Jiří; Cígler, Petr; Veselý, J.; Grantz Šašková, Klára; Lepšík, Martin; Brynda, Jiří; Řezáčová, Pavlína; Kožíšek, Milan; Císařová, I.; Oberwinkler, H.; Kraeusslich, H. G.; Konvalinka, Jan

2012-01-01

Roč. 55, č. 22 (2012), s. 10130-10135 ISSN 0022-2623 R&D Projects: GA ČR GBP208/12/G016; GA ČR GAP207/11/1798 Institutional research plan: CEZ:AV0Z40550506; CEZ:AV0Z50520514 Keywords : HIV protease inhibitor * rational drug design * 1,4-benzodiazepines Subject RIV: CE - Biochemistry Impact factor: 5.614, year: 2012

Quantitative comparison of simulated and measured signals in the STEM mode of a SEM

Czech Academy of Sciences Publication Activity Database

Walker, Christopher; Konvalina, Ivo; Mika, Filip; Frank, Luděk; Müllerová, Ilona

2018-01-01

Roč. 415, JAN (2018), s. 17-24 ISSN 0168-583X R&D Projects: GA TA ČR(CZ) TE01020118; GA MŠk(CZ) LO1212; GA MŠk ED0017/01/01 EU Projects: European Commission(XE) 606988 - SIMDALEE2 Institutional support: RVO:68081731 Keywords : low-energy electrons * multiple scattering * elastic-scattering * transmission Subject RIV: JA - Electronics ; Optoelectronics, Electrical Engineering Impact factor: 1.109, year: 2016

Comparison of selected polarizable and nonpolarizable water models in molecular dynamics simulations of ice I-h

Czech Academy of Sciences Publication Activity Database

Gladich, Ivan; Roeselová, Martina

2012-01-01

Roč. 14, č. 32 (2012), s. 11371-11385 ISSN 1463-9076 R&D Projects: GA ČR(CZ) GAP208/10/1724; GA MŠk ME09064; GA ČR GBP208/12/G016 Grant - others:NSF(US) 0909227 Institutional support: RVO:61388963 Keywords : particle mesh ewald * quasi-liquid layer * melting-point * atmospheric chemistry * surface Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 3.829, year: 2012

Partial hydration of n-alkyl halides at the water-vapor interface: a molecular simulation study with atmospheric implications

Czech Academy of Sciences Publication Activity Database

Habartová, Alena; Obisesan, A.; Minofar, Babak; Roeselová, Martina

2014-01-01

Roč. 133, č. 3 (2014), 1455/1-1455/15 ISSN 1432-881X R&D Projects: GA ČR(CZ) GAP208/10/1724; GA MŠk ME09064 Grant - others:GA ČR(CZ) GA13-08651S Institutional support: RVO:61388963 ; RVO:67179843 Keywords : haloalkanes * adsorption * interfacial solvation * halogenated organics * interfacial partitioning * surface orientation * heterogeneous chemistry Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 2.233, year: 2014

ÜRO rahuvalvemissiooni juhtinud brasiillane leiti Haiti hotellist surnult / Heiki Suurkask

Index Scriptorium Estoniae

Suurkask, Heiki, 1972-

2006-01-01

ÜRO Haiti rahuvalvemissiooni juht Urano Teixeira da Matta Bacellar sooritas enesetapu. ÜRO rahuvalvemissioon MINUSTAH on Haitil 2005. aastast pärast nelja-aastast eemalolekut, samas jätkub seal vägivald

The Dushak–Erekdag Survey of roAp Stars Tatyana Dorokhova ...

Indian Academy of Sciences (India)

South-African Astronomical Observatory (SAAO). Details of the discovery and further studies are given in Kurtz (1990) and Kurtz & Martinez (2000). Some roAp stars have multiple modes of pulsations and they are valuable for asteroseismological studies. Out of the 32 known roAp stars so far, about 84% were discovered in ...

Transiting exoplanets from the CoRoT space mission . VI. CoRoT-Exo-3b: the first secure inhabitant of the brown-dwarf desert

Science.gov (United States)

Deleuil, M.; Deeg, H. J.; Alonso, R.; Bouchy, F.; Rouan, D.; Auvergne, M.; Baglin, A.; Aigrain, S.; Almenara, J. M.; Barbieri, M.; Barge, P.; Bruntt, H.; Bordé, P.; Collier Cameron, A.; Csizmadia, Sz.; de La Reza, R.; Dvorak, R.; Erikson, A.; Fridlund, M.; Gandolfi, D.; Gillon, M.; Guenther, E.; Guillot, T.; Hatzes, A.; Hébrard, G.; Jorda, L.; Lammer, H.; Léger, A.; Llebaria, A.; Loeillet, B.; Mayor, M.; Mazeh, T.; Moutou, C.; Ollivier, M.; Pätzold, M.; Pont, F.; Queloz, D.; Rauer, H.; Schneider, J.; Shporer, A.; Wuchterl, G.; Zucker, S.

2008-12-01

Context: The CoRoT space mission routinely provides high-precision photometric measurements of thousands of stars that have been continuously observed for months. Aims: The discovery and characterization of the first very massive transiting planetary companion with a short orbital period is reported. Methods: A series of 34 transits was detected in the CoRoT light curve of an F3V star, observed from May to October 2007 for 152 days. The radius was accurately determined and the mass derived for this new transiting, thanks to the combined analysis of the light curve and complementary ground-based observations: high-precision radial-velocity measurements, on-off photometry, and high signal-to-noise spectroscopic observations. Results: CoRoT-Exo-3b has a radius of 1.01 ± 0.07 R_Jup and transits around its F3-type primary every 4.26 days in a synchronous orbit. Its mass of 21.66 ± 1.0 M_Jup, density of 26.4 ± 5.6 g cm-3, and surface gravity of logg = 4.72 clearly distinguish it from the regular close-in planet population, making it the most intriguing transiting substellar object discovered so far. Conclusions: With the current data, the nature of CoRoT-Exo-3b is ambiguous, as it could either be a low-mass brown-dwarf or a member of a new class of “superplanets”. Its discovery may help constrain the evolution of close-in planets and brown-dwarfs better. Finally, CoRoT-Exo-3b confirms the trend that massive transiting giant planets (M ≥ 4 M_Jup) are found preferentially around more massive stars than the Sun. The CoRoT space mission, launched on December 27th 2006, has been developed and is operating by CNES, with the contribution of Austria, Belgium, Brasil, ESA, Germany and Spain. The first CoRoT data will be available to the public in February 2009 from the CoRoT archive: http://idoc-corot.ias.u-psud.fr/ Table of the COROT photometry is only available in electronic form at the CDS via anonymous ftp to cdsarc.u-strasbg.fr (130.79.128.5) or via http

High-efficient full-duplex WDM-RoF system with sub-central station

Science.gov (United States)

Liu, Anliang; Yin, Hongxi; Wu, Bin

2018-05-01

With an additional sub-central station (S-CS), a high-efficient full-duplex radio-over-fiber (RoF) system compatible with the wavelength-division-multiplexing technology is proposed and experimentally demonstrated in this paper. To improve the dispersion tolerance of the RoF system, the baseband data format for the downlink and an all-optical down-conversion approach for the uplink are employed. In addition, this RoF system can not only make full use of the fiber link resources but also realize the upstream transmission without any local light sources at remote base stations (BSs). A 10-GHz RoF experimental system with a 1.25-Gb/s rate bidirectional transmission is established based on the S-CS structure. The feasibility and reliability of this RoF system are verified through eye diagrams and bit error rate (BER) curves experimentally obtained.

[Expression and clinical significance of CD45RO in laryngeal carcinoma tissue].

Science.gov (United States)

Li, Manyi; Liu, Jishengi; Zhou, Hui; Wu, Wenying; Xiao, Gensheng; Yu, Yafeng; Guo, Lingchuan

2014-03-01

To investigate the role and significance of CD45RO in occurance and development in laryngeal squamous carcinoma, and to provide some valuable clues for searching new approaches to assess prognosis and theoretical basis for tumor biotherapy. The expression of CD45RO protein in 50 cases of laryngeal squamous carcinoma and 10 cases normal mucos was detected by immunohistochemical S-P method. The positive rate of CD45RO was 30% and 86% respectively in normal tissue and laryngeal squamous cell carcinoma tissue. The expresion of CD45RO was significantly and negatively associated with local metastatic of lymph nodes 0.713, P < 0.05) and tumor sites (r = -0.750, P < 0.05), but it have no notable difference with pathology differentiation, age, infiltrating depth and clinical stages in 50 cases of laryngeal squamous cell cancer. (1) The expresion of CD45RO in laryngeal squamous cell cancer is more than that in normal tissue. (2) It is possible that overexpresion of CD45RO in laryngeal squamous cell carcinoma cut local metastatic lymph nodes. (3) It is probable that overexpresion of CD45RO in laryngeal squamous cell cancer made for prognosis of patients. (4) Other than UICC-TNM stage, pathology differentiation, it provide valuable clues for searching new approaches to assess prognosis of laryngeal squamous cell carcinoma.

Serum matrix metalloproteinase-9 and tissue inhibitor of metalloproteinase-1 levels in patients with tick-borne encephalitis

Czech Academy of Sciences Publication Activity Database

Palus, Martin; Žampachová, E.; Elsterová, Jana; Růžek, Daniel

2014-01-01

Roč. 68, č. 2 (2014), s. 165-169 ISSN 0163-4453 R&D Projects: GA ČR GAP502/11/2116 Institutional support: RVO:60077344 Keywords : tick-borne encephalitis * matrix metalloproteinase-9 * tissue inhibitor of metalloproteinase-1 * bloodebrain barrier Subject RIV: EC - Immunology Impact factor: 4.441, year: 2014

ÜRO asesekretäri kriitika USA suunal ajas viimase marru / Liise Lehtsalu

Index Scriptorium Estoniae

Lehtsalu, Liise

2006-01-01

ÜRO asesekretär Malloch Brown kritiseeris oma kõnes USA tahtmatust teavitada ameeriklasi ÜRO osast USA välispoliitikas. USA ÜRO-suursaadiku John Boltoni reageering Browni märkustele. Lisa: Rikaste ja vaeste riikide vastuolud

RoHS Compliance - Is the Global Electronics Industry Ready?

OpenAIRE

Head, Marieke; Hróarsson, Hallur

2006-01-01

RoHS is an EU directive that was proposed along with the WEEE Directive in 2002 as a part of a plan to promote extended producer responsibility within the electronics industry. Together, these two directives seek to make electrical and electronic equipment easier to manage both in terms of environmental impacts and recycling. The RoHS Directive seeks to remove lead, cadmium, mercury, hexavalent chromium and two brominated flame retardants from all consumer electrical equipment. This paper dea...

Isatin derivatives as a non-toxic corrosion inhibitor for mild steel in 20% H2SO4

International Nuclear Information System (INIS)

Ansari, K.R.; Quraishi, M.A.; Singh, Ambrish

2015-01-01

Highlights: • Mild steel protection in 20% H 2 SO 4 by TZs. • Potentiodynamic polarization curves reveal that the actions of TZs are mixed type but cathodically predominant. • The adsorption of TZs obeys the Langmuir adsorption isotherm. • Examination of surface morphology by SEM and EDX. • Correlation between experimental and quantum chemical results. - Abstract: The corrosion inhibition action of Isatin-β-thiosemicarbzone derivatives namely 1-Benzylidene-5-(2-oxoindoline-3-ylidene) Thiocarbohydrazone (TZ-1) and 1-(4-Methylbenzylidene)-5-(2-oxoindolin-3-ylidene) Thiocarbohydrazone (TZ-2) was studied on mild steel surface in 20% H 2 SO 4 by gravimetric measurements, Electrochemical measurements (EIS and Tafel), SEM, EDX and quantum chemical methods. Potentiodynamic polarization curves reveal that the TZs act as mixed type inhibitors exhibiting predominantly cathodic behavior. The adsorption of TZs obeys the Langmuir adsorption isotherm. The thermodynamic parameters (E a , K ads , ΔG° ads ) were also computed and discussed

Planetary transit candidates in the CoRoT-SRc01 field

DEFF Research Database (Denmark)

Erikson, A.; Santerne, A.; Renner, S.

2012-01-01

Context. CoRoT is a pioneering space mission whose primary goals are stellar seismology and extrasolar planets search. Its surveys of large stellar fields generate numerous planetary candidates whose lightcurves have transit-like features. An extensive analytical and observational follow-up effort...... is undertaken to classify these candidates. Aims. We present the list of planetary transit candidates from the CoRoT LRa01 star field in the Monoceros constellation toward the Galactic anti-center direction. The CoRoT observations of LRa01 lasted from 24 October 2007 to 3 March 2008. Methods. We acquired...... and analyzed 7470 chromatic and 3938 monochromatic lightcurves. Instrumental noise and stellar variability were treated with several filtering tools by different teams from the CoRoT community. Different transit search algorithms were applied to the lightcurves. Results. Fifty-one stars were classified...

Characterization of the insulin-sensitive low Km cAMP phosphodiesterase from rat adipose tissue

Energy Technology Data Exchange (ETDEWEB)

Degerman, E.; Belfrage, P.; Manganiello, V.C.

1986-05-01

Particulate, but not soluble, low K/sub m/ cAMP phosphodiesterase (PDE) activity of rat adipocytes was increased 50-100% during incubation (10 min) of intact cells with 1-3 nM insulin; activation was less with higher or lower insulin concentrations. Activation was maintained during solubilization with an alkyl polyoxyethylene non-ionic detergent C/sub 13/, E/sub 12/ and NaBr and chromatography on DEAE. Enzyme from DEAE was further purified by chromatography on Sepahadex G-200 and Blue-Sepharose. Activity (with 0.5 ..mu..M (/sup 3/H)cAMP) was rather sensitive to inhibition by p-chloromercuribenzoate (IC/sub 50/, 1 ..mu..M) and less so by 2,2'-dithiobis-(5-nitropyridine) (160 ..mu..M), N-ethylmaleimide (525 ..mu..M) and iodoacetamide (750 ..mu..M). PDE activity was also rather sensitive to inhibition by cilostamide (IC/sub 50/, approx.40 nM) and the cardiotonic drugs CI 930 (450 nM) and milrinone (630 nM) but rather insensitive to RO 20-1724 (190 ..mu..M). Based on effects of these inhibitors, the hormone-sensitive low K/sub m/ particulate cAMP PDE from rat adipocytes seems to be analogous to the insulin-activated particulate PDE from 3T3-L1 adipocytes and the cilostamide-sensitive soluble low K/sub m/ cAMP PDE from bovine liver (designated as III-C), platelets, heart, and other tissues.

Transiting exoplanets from the CoRoT space mission. IV. CoRoT-Exo-4b: a transiting planet in a 9.2 day synchronous orbit

Science.gov (United States)

Aigrain, S.; Collier Cameron, A.; Ollivier, M.; Pont, F.; Jorda, L.; Almenara, J. M.; Alonso, R.; Barge, P.; Bordé, P.; Bouchy, F.; Deeg, H.; de La Reza, R.; Deleuil, M.; Dvorak, R.; Erikson, A.; Fridlund, M.; Gondoin, P.; Gillon, M.; Guillot, T.; Hatzes, A.; Lammer, H.; Lanza, A. F.; Léger, A.; Llebaria, A.; Magain, P.; Mazeh, T.; Moutou, C.; Paetzold, M.; Pinte, C.; Queloz, D.; Rauer, H.; Rouan, D.; Schneider, J.; Wuchter, G.; Zucker, S.

2008-09-01

CoRoT, the first space-based transit search, provides ultra-high-precision light curves with continuous time-sampling over periods of up to 5 months. This allows the detection of transiting planets with relatively long periods, and the simultaneous study of the host star's photometric variability. In this Letter, we report the discovery of the transiting giant planet CoRoT-Exo-4b and use the CoRoT light curve to perform a detailed analysis of the transit and determine the stellar rotation period. The CoRoT light curve was pre-processed to remove outliers and correct for orbital residuals and artefacts due to hot pixels on the detector. After removing stellar variability about each transit, the transit light curve was analysed to determine the transit parameters. A discrete autocorrelation function method was used to derive the rotation period of the star from the out-of-transit light curve. We determine the periods of the planetary orbit and star's rotation of 9.20205 ± 0.00037 and 8.87 ± 1.12 days respectively, which is consistent with this being a synchronised system. We also derive the inclination, i = 90.00_-0.085+0.000 in degrees, the ratio of the orbital distance to the stellar radius, a/Rs = 17.36-0.25+0.05, and the planet-to-star radius ratio R_p/R_s=0.1047-0.0022+0.0041. We discuss briefly the coincidence between the orbital period of the planet and the stellar rotation period and its possible implications for the system's migration and star-planet interaction history. The CoRoT space mission, launched on December 27th 2006, has been developed and is operated by CNES, with the contribution of Austria, Belgium, Brazil, ESA, Germany, and Spain. The first CoRoT data will be available to the public in February 2009 from the CoRoT archive: http://idoc-corot.ias.u-psud.fr/ Figures 1, 4 and 5 are only available in electronic form at http://www.aanda.org

MO-AB-204-01: IHE RO Overview

International Nuclear Information System (INIS)

Hadley, S.

2016-01-01

You’ve experienced the frustration: vendor A’s device claims to work with vendor B’s device, but the practice doesn’t match the promise. Getting devices working together is the hidden art that Radiology and Radiation Oncology staff have to master. To assist with that difficult process, the Integrating the Healthcare Enterprise (IHE) effort was established in 1998, with the coordination of the Radiological Society of North America. Integrating the Healthcare Enterprise (IHE) is a consortium of healthcare professionals and industry partners focused on improving the way computer systems interconnect and exchange information. This is done by coordinating the use of published standards like DICOM and HL7. Several clinical and operational IHE domains exist in the healthcare arena, including Radiology and Radiation Oncology. The ASTRO-sponsored IHE Radiation Oncology (IHE-RO) domain focuses on radiation oncology specific information exchange. This session will explore the IHE Radiology and IHE RO process for; IHE solicitation process for new profiles. Improving the way computer systems interconnect and exchange information in the healthcare enterprise Supporting interconnectivity descriptions and proof of adherence by vendors Testing and assuring the vendor solutions to connectivity problems. Including IHE profiles in RFPs for future software and hardware purchases. Learning Objectives: Understand IHE role in improving interoperability in health care. Understand process of profile development and implantation. Understand how vendors prove adherence to IHE RO profiles. S. Hadley, ASTRO Supported Activity

Radial velocity follow-up of CoRoT transiting exoplanets

Directory of Open Access Journals (Sweden)

Deleuil M.

2011-02-01

Full Text Available We report on the results from the radial-velocity follow-up program performed to establish the planetary nature and to characterize the transiting candidates discovered by the space mission CoRoT. We use the SOPHIE at OHP, HARPS at ESO and the HIRES at Keck spectrographs to collect spectra and high-precision radial velocity (RV measurements for several dozens different candidates from CoRoT. We have measured the Rossiter-McLaughlin effect of several confirmed planets, especially CoRoT-1b which revealed that it is another highly inclined system. Such high-precision RV data are necessary for the discovery of new transiting planets. Furthermore, several low mass planet candidates have emerged from our Keck and HARPS data.

WE-B-Exhibit Hall-01: Ask the RO-ILS Experts

Energy Technology Data Exchange (ETDEWEB)

Ezzell, G [Mayo Clinic Arizona, Phoenix, AZ (United States); Sanscrainte, E [Clarity PSO, Chicago, IL (United States); Tomlinson, C [ASTRO, Fairfax, VA (United States)

2015-06-15

Have a question about RO-ILS: Radiation Oncology Incident Learning System™, or interested in learning more? Sponsored by the American Society for Radiation Oncology (ASTRO) and AAPM, RO-ILS is the only medical specialty society-sponsored incident learning system for radiation oncology. It facilitates safer and higher quality care in radiation oncology by providing a mechanism for shared learning in a secure and non-punitive environment. Please join our RO-ILS experts for a question and answer session on Wednesday, July 15th at 8:30 in the Partners in Solutions Room in Exhibit Hall C. Our experts include: Gary Ezzell, PhD, Mayo Clinic Arizona, [Brett Miller, Phillip Beron, and Derek Brown], Emily Sanscrainte from Clarity PSO and Cindy Tomlinson, MPP, ASTRO.

ÜRO teatel peavad toidukriisi eest vastutama rikkad riigid / Liisi Poll

Index Scriptorium Estoniae

Poll, Liisi, 1980-

2008-01-01

ÜRO peasekretär Ban Ki-Moon kutsus ÜRO põllumajandus- ja toiduorganisatsiooni erakorralisel toidukriisi-teemalisel tippkohtumisel Roomas riike üles vähendama ekspordipiiranguid ja imporditariife, et toiduvarude nappust vähendada. Vt. samas: Kohtumise poliitilised häbiplekid

Thematic trip: "Save Roşia MontanÄă"

Science.gov (United States)

Eugenia, Marcu

2015-04-01

The name Roşia Montană, situated in Transylvania, became well known after a Romanian-Canadian company, Roşia Montană Gold Company (RMGC), obtained the concession license on exploitation for gold and silver minerals in the Roşia Montană area. The project consists of opening the largest surface gold mines in Europe using cyanide, which will include four open pits and a processing plant for gold and silver in The Roşia Valley and a tailings facility with an area of 367 hectares in the Corna Valley. One of the main fears is related to a possible ecological accident like the one in Baia Mare in 2000, when a tailing facility dam break led to cyanide pollution of Tisa and Danube rivers that resulted in the death of 1,200 tons of fish and contamination of water resources for 2 million people. This thematic trip is important for the scientific preparation of students and an opportunity to educate them in the spirit of environmental protection. The training and education of students will require assimilation and understanding, actively and consciously, using the knowledge acquired during the compulsory curriculum and training skills. REASON: The continuous degradation of the environment is a major crisis due to human intervention in nature, and the proposed Roşia Montană mining project will continue this trend. The company proposes to extract gold from mines by using the gold separation technique using cyanide, a process that involves destroying a total area of 16 km² which includes 5 mountains, 7 churches, 11 cemeteries and the ruins of Alburnus Maior Citadel, as well as creating pollution that would last for hundreds of years. The extraction of gold from low-grade ores using cyanide processes was estimated to result in a worldwide emission of 45,300 tons of hydrogen cyanide. Environmental education for a healthy life has children as target group, because they are the trustees and beneficiaries of tomorrow's natural resources and can influence the attitudes of

Protease inhibitor from insect silk - activities of derivatives expressed in vitro and in transgenic potato

Czech Academy of Sciences Publication Activity Database

Kodrík, Dalibor; Kludkiewicz, Barbara; Navrátil, Oldřich; Skoková Habuštová, Oxana; Horáčková, V.; Svobodová, Z.; Vinokurov, Konstantin; Sehnal, František

2013-01-01

Roč. 171, č. 1 (2013), s. 209-224 ISSN 0273-2289 R&D Projects: GA MZe QI91A229 Institutional support: RVO:60077344 ; RVO:61389030 Keywords : genetically modified organism * silk protease inhibitor * protease Subject RIV: ED - Physiology Impact factor: 1.687, year: 2013 http://link.springer.com/content/pdf/10.1007%2Fs12010-013-0325-9.pdf

Amidate prodrugs of 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA) as inhibitors of adenylate cyclase toxin from Bordetella pertussis

Czech Academy of Sciences Publication Activity Database

Šmídková, Markéta; Dvořáková, Alexandra; Tloušťová, Eva; Česnek, Michal; Janeba, Zlatko; Mertlíková-Kaiserová, Helena

2014-01-01

Roč. 281, Suppl S1 (2014), s. 729 ISSN 1742-464X. [FEBS EMBO 2014 Conference. 30.08.2014-04.09.2014, Paris] R&D Projects: GA MŠk LO1302; GA MV VG20102015046 Institutional support: RVO:61388963 Keywords : Bordetella pertussis * adenylyl cyclase toxin * inhibitors Subject RIV: CE - Biochemistry

Human Ro60 (SSA2) genomic organization and sequence alterations, examined in cutaneous lupus erythematosus.

Science.gov (United States)

Millard, T P; Ashton, G H S; Kondeatis, E; Vaughan, R W; Hughes, G R V; Khamashta, M A; Hawk, J L M; McGregor, J M; McGrath, J A

2002-02-01

The Ro 60 kDa protein (Ro60 or SSA2) is the major component of the Ro ribonucleoprotein (Ro RNP) complex, to which an immune response is a specific feature of several autoimmune diseases. The genomic organization and any sequence variation within the DNA encoding Ro60 are unknown. To characterize the Ro60 gene structure and to assess whether any sequence alterations might be associated with serum anti-Ro antibody in subacute cutaneous lupus erythematosus (SCLE), thus potentially providing new insight into disease pathogenesis. The cDNA sequence for Ro60 was obtained from the NCBI database and used for a BLAST search for a clone containing the entire genomic sequence. The intron-exon borders were confirmed by designing intronic primer pairs to flank each exon, which were then used to amplify genomic DNA for automated sequencing from 36 caucasian patients with SCLE (anti-Ro positive) and 49 with discoid LE (DLE, anti-Ro negative), in addition to 36 healthy caucasian controls. Heteroduplex analysis of polymerase chain reaction (PCR) products from patients and controls spanning all Ro60 exons (1-8) revealed a common bandshift in the PCR products spanning exon 7. Sequencing of the corresponding PCR products demonstrated an A > G substitution at nucleotide position 1318-7, within the consensus acceptor splice site of exon 7 (GenBank XM001901). The allele frequencies were major allele A (0.71) and minor allele G (0.29) in 72 control chromosomes, with no significant differences found between SCLE patients, DLE patients and controls. The genomic organization of the DNA encoding the Ro60 protein is described, including a common polymorphism within the consensus acceptor splice site of exon 7. Our delineation of a strategy for the genomic amplification of Ro60 forms a basis for further examination of the pathological functions of the Ro RNP in autoimmune disease.

Differential effect of detergents on [3H]Ro 5-4864 and [3H]PK 11195 binding to peripheral-type benzodiazepine-binding sites

International Nuclear Information System (INIS)

Awad, M.; Gavish, M.

1988-01-01

The present study demonstrates a differential effect of various detergent treatments on [ 3 H]Ro 5-4864 and [ 3 H]PK 11195 binding to peripheral benzodiazepine binding sites (PBS). Triton X-100 caused a decrease of about 70% in [ 3 H]Ro 5-4864 binding to membranes from various peripheral tissues of rat, but had only a negligible effect on [ 3 H]PK 11195 binding. A similar effect of Triton X-100 was observed on guinea pig and rabbit kidney membranes. The decrease in [ 3 H]Ro 5-4864 binding after treatment with Triton X-100 was apparently due to a decrease in the density of PBS, since the affinity remained unaltered. The detergents 3-[(3-cholamidopropyl)-dimethylammonio]-1-propane sulfonate (CHAPS), Tween 20, deoxycholic acid, or digitonin (0.0125%) caused only a minor change in [ 3 H]Ro 5-4864 and [ 3 H]PK 11195 binding to rat kidney membranes; but when concentrations were substantially increased (0.1%), all detergents caused a decrease of at least 50% in [ 3 H]Ro 5-4864 binding, while [ 3 H]PK 11195 binding to rat kidney membranes remained unaffected by the first three detergents, with only a minor decrease (15%) after treatment with digitonin

Transiting exoplanets from the CoRoT space mission . XIX. CoRoT-23b: a dense hot Jupiter on an eccentric orbit

DEFF Research Database (Denmark)

Rouan, D.; Parviainen, H.; Moutou, C.

2012-01-01

We report the detection of CoRoT-23b, a hot Jupiter transiting in front of its host star with a period of 3.6314 ± 0.0001 days. This planet was discovered thanks to photometric data secured with the CoRoT satellite, combined with spectroscopic radial velocity (RV) measurements. A photometric search...... to be 7 Gyr, not far from the transition to subgiant, in agreement with the rather large stellar radius. The two features of a significant eccentricity of the orbit and of a fairly high density are fairly uncommon for a hot Jupiter. The high density is, however, consistent with a model of contraction...... is more than a few 105, a value that is the lower bound of the usually expected range. Even if CoRoT-23b  features a density and an eccentricity that are atypical of a hot Jupiter, it is thus not an enigmatic object....

Experimental Study of Advanced Treatment of Coking Wastewater Using MBR-RO Combined Process

Science.gov (United States)

Zhang, Lei; Hwang, Jiannyang; Leng, Ting; Xue, Gaifeng; Chang, Hongbing

A membrane bioreactor-reverse osmosis (MBR-RO) combined process was used for advanced treatment of coking wastewater from secondary biological treatment. MBR and RO units' treatment efficiency for the pollution removal were conducted, and effects of raw water conductivity and trans-membrane pressure on water yield and desalination rate in RO unit were investigated in detail. The experimental results proved that MBR-RO combined process ran steadily with good treatment effect, which could obtain stable effluent water quality and met the requirement of "Design Criterion of the Industrial Circulating Cooling Water Treatment" (GB 50050-2007).

Acyclic Nucleoside Phosphonates Containing 9-Deazahypoxanthine and a Five-Membered Heterocycle as Selective Inhibitors of Plasmodial 6-Oxopurine Phosphoribosyltransferases

Czech Academy of Sciences Publication Activity Database

Kaiser, Martin Maxmilian; Baszczyňski, Ondřej; Hocková, Dana; Poštová Slavětínská, Lenka; Dračínský, Martin; Keough, D. T.; Guddat, L. W.; Janeba, Zlatko

2017-01-01

Roč. 12, č. 14 (2017), s. 1133-1141 ISSN 1860-7179 R&D Projects: GA ČR(CZ) GA16-06049S Institutional support: RVO:61388963 Keywords : inhibitors * nucleosides * malaria * phosphonates * purine salvage Subject RIV: CC - Organic Chemistry OBOR OECD: Organic chemistry Impact factor: 3.225, year: 2016

Synthesis, evaluation, and mechanism of N,N,N-trimethyl-D-glucosamine-(1→4)-chitooligosaccharides as selective inhibitors of glycosyl hydrolase family 20 β-N-acetyl-D-hexosaminidases.

Science.gov (United States)

Yang, You; Liu, Tian; Yang, Yongliang; Wu, Qingyue; Yang, Qing; Yu, Biao

2011-02-11

GH20 β-N-acetyl-D-hexosaminidases are enzymes involved in many vital processes. Inhibitors that specifically target GH20 enzymes in pests are of agricultural and economic importance. Structural comparison has revealed that the bacterial chitindegrading β-N-acetyl-D-hexosaminidases each have an extra +1 subsite in the active site; this structural difference could be exploited for the development of selective inhibitors. N,N,Ntrimethyl-D-glucosamine (TMG)-chitotriomycin, which contains three GlcNAc residues, is a natural selective inhibitor against bacterial and insect β-N-acetyl-D-hexosaminidases. However, our structural alignment analysis indicated that the two GlcNAc residues at the reducing end might be unnecessary. To prove this hypothesis, we designed and synthesized a series of TMG-chitotriomycin analogues containing one to four GlcNAc units. Inhibitory kinetics and molecular docking showed that TMG-(GlcNAc)(2), is as active as TMG-chitotriomycin [TMG-(GlcNAc)(3)]. The selective inhibition mechanism of TMG-chitotriomycin was also explained. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Assessing the consistency of optical properties measured in four integrating spheres

Czech Academy of Sciences Publication Activity Database

Lukeš, Petr; Homolová, Lucie; Navrátil, M.; Hanuš, Jan

2017-01-01

Roč. 38, č. 13 (2017), s. 3817-3830 ISSN 0143-1161 R&D Projects: GA MŠk(CZ) LO1415; GA MŠk(CZ) LM2015061 Institutional support: RVO:67179843 Keywords : Artificial material * Canopy radiative transfer * Directional hemispherical reflectances * Integrating spheres * Leaf optical property * Measurement protocol * Standard deviation * Statistically significant difference Subject RIV: EH - Ecology, Behaviour OBOR OECD: Environmental sciences (social aspects to be 5.7) Impact factor: 1.724, year: 2016

Regional specific binding of [11C]RO 15 1788 to central type benzodiazepine receptors in human brain: quantitative evaluation by PET

International Nuclear Information System (INIS)

Pappata, S.; Samson, Y.; Chavoix, C.; Prenant, C.; Maziere, M.; Baron, J.C.

1988-01-01

The central type benzodiazepine receptors were studied in 17 healthy human subjects with 11 C-RO 15 1788 and positron emission tomography (PET). The brain regional distribution of the tracer in eight control studies performed after injection of trace doses of 11 C-RO 15 1788 was consistent with that of benzodiazepine receptors. Saturation studies with co-injected cold RO 15 1788 in the remaining subjects showed a dose-dependent decrease of brain radiotracer until full inhibition of specific binding was achieved with doses above 0.1 mg/kg (four studies). Based on the results, a simple method to estimate the specifically bound 11 C-RO 15 1788 regionally in a single PET study is proposed, using the data from the full-saturation studies as a stable estimate of the nondisplaceable radioligand concentration. Using this method, it was found that quasiequilibrium between the estimated specifically bound and nondisplaceable components was achieved at times equal to or longer than 20 min after tracer administration. The validity of this method was partly supported by further results, showing a good agreement between the regional specific binding so calculated and postmortem data of receptor density

Sensitization by SR-2508 plus Ro 03-8799

International Nuclear Information System (INIS)

Stone, H.B.; Luu, Y.H.; Lam, K.N.

1986-01-01

The primary toxicity of Ro 03-8799 is a central nervous system toxicity, whereas that of SR-2508 is a peripheral neuropathy. The feasibility of reducing overall toxicity while maintaining maximal radiosensitization by using the two sensitizers together was tested. The LD50/2 of Ro 03-8799 was 0.68 mg/g body wt (mg/gbw) after intravenous (i.v.) administration, and that of SR-2508 was 4.4 mg/gbw after i.v. administration. When both drugs were given together in equitoxic proportions, the LD50/2 was 0.45 mg of Ro 03-8799 plus 2.9 mg of SR-2508/gbw. These doses are 66% of the respective LD50/2 values of the drugs when given separately. Radiosensitization was evaluated using in vivo-in vitro assays with EMT6/SF tumors in BALB/c mice. At drug doses between 10 and 60% of the LD50/2, sensitization was generally maximal and similar to that from misonidazole, but there was less sensitization below this dose, both with the drugs given separately and together. If chronic toxicities of these drugs overlap as do the acute toxicities there will be little or no additional benefit from using these drugs in combination, compared to using them separately

Potential inhibitors of dapE and argE enzymes as the new antimicrobial agents: Synthesis and characterization

Czech Academy of Sciences Publication Activity Database

Hlaváček, Jan; Pícha, Jan; Vaněk, Václav; Jiráček, Jiří; Slaninová, Jiřina; Fučík, Vladimír; Holz, R. C.

2008-01-01

Roč. 14, č. 8 (2008), s. 83-84 ISSN 1075-2617. [European Peptide Symposium /30./. 31.08.2008-05.09.2008, Helsinki] R&D Projects: GA AV ČR IAA400550614 Institutional research plan: CEZ:AV0Z40550506 Keywords : antimicrobial agents * dapE and argE inhibitors * synthesis and activity Subject RIV: CC - Organic Chemistry

Amidate Prodrugs of 9-[2-(Phosphonomethoxy)Ethyl]Adenine as Inhibitors of Adenylate Cyclase Toxin from Bordetella pertussis

Czech Academy of Sciences Publication Activity Database

Šmídková, Markéta; Dvořáková, Alexandra; Tloušťová, Eva; Česnek, Michal; Janeba, Zlatko; Mertlíková-Kaiserová, Helena

2014-01-01

Roč. 58, č. 2 (2014), s. 664-671 ISSN 0066-4804 R&D Projects: GA MV VG20102015046 Grant - others:OPPC(XE) CZ.2.16/3.1.00/24016 Institutional support: RVO:61388963 Keywords : Bordetella pertussis * adenylate cyclase toxin * ACT * inhibitors * PMEA * amidate prodrugs Subject RIV: CC - Organic Chemistry Impact factor: 4.476, year: 2014

Malonate-based inhibitors of mammalian serine racemase: Kinetic characterization and structure-based computational study

Czech Academy of Sciences Publication Activity Database

Vorlová, Barbora; Nachtigallová, Dana; Jirásková-Vaníčková, Jana; Ajani, Haresh; Jansa, Petr; Řezáč, Jan; Fanfrlík, Jindřich; Otyepka, M.; Hobza, Pavel; Konvalinka, Jan; Lepšík, Martin

2015-01-01

Roč. 89, Jan 7 (2015), s. 189-197 ISSN 0223-5234 R&D Projects: GA ČR GBP208/12/G016 Grant - others:GA MŠk(CZ) ED2.1.00/03.0058 Program:ED Institutional support: RVO:61388963 Keywords : NMDA receptor * pyridoxal-5 '-phosphate-dependent enzyme * human/mouse serine racemase * malonate-based inhibitors * semiempirical quantum mechanical calculations Subject RIV: CE - Biochemistry Impact factor: 3.902, year: 2015

Apoptosis inhibitor 5 (API-5; AAC-11; FIF) is upregulated in human carcinomas in vivo

Czech Academy of Sciences Publication Activity Database

Kočí, Lenka; Chlebová, K.; Hýžďalová, Martina; Hofmanová, Jiřina; Jíra, M.; Kysela, P.; Kozubík, Alois; Kala, Z.; Krejčí, Pavel

2012-01-01

Roč. 3, č. 4 (2012), s. 913-916 ISSN 1792-1074 R&D Projects: GA ČR(CZ) GA305/09/1526; GA ČR(CZ) GD303/09/H048; GA ČR(CZ) GAP301/11/1730 Institutional research plan: CEZ:AV0Z50040702 Keywords : apoptosis inhibitor 5 * apoptosis * human carcinoma Subject RIV: BO - Biophysics Impact factor: 0.237, year: 2012

Geografická výročí

Czech Academy of Sciences Publication Activity Database

Martínek, Jiří

2017-01-01

Roč. 36, č. 2 (2017), s. 69-72 ISSN 1213-1075 Institutional support: RVO:67985963 Keywords : Czech geography * personalities * anniversaries Subject RIV: AB - History OBOR OECD: History (history of science and technology to be 6.3, history of specific sciences to be under the respective headings)

Dual-Targeting Small-Molecule Inhibitors of the Staphylococcus aureus FMN Riboswitch Disrupt Riboflavin Homeostasis in an Infectious Setting.

Science.gov (United States)

Wang, Hao; Mann, Paul A; Xiao, Li; Gill, Charles; Galgoci, Andrew M; Howe, John A; Villafania, Artjohn; Barbieri, Christopher M; Malinverni, Juliana C; Sher, Xinwei; Mayhood, Todd; McCurry, Megan D; Murgolo, Nicholas; Flattery, Amy; Mack, Matthias; Roemer, Terry

2017-05-18

Riboswitches are bacterial-specific, broadly conserved, non-coding RNA structural elements that control gene expression of numerous metabolic pathways and transport functions essential for cell growth. As such, riboswitch inhibitors represent a new class of potential antibacterial agents. Recently, we identified ribocil-C, a highly selective inhibitor of the flavin mononucleotide (FMN) riboswitch that controls expression of de novo riboflavin (RF, vitamin B2) biosynthesis in Escherichia coli. Here, we provide a mechanistic characterization of the antibacterial effects of ribocil-C as well as of roseoflavin (RoF), an antimetabolite analog of RF, among medically significant Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus faecalis. We provide genetic, biophysical, computational, biochemical, and pharmacological evidence that ribocil-C and RoF specifically inhibit dual FMN riboswitches, separately controlling RF biosynthesis and uptake processes essential for MRSA growth and pathogenesis. Such a dual-targeting mechanism is specifically required to develop broad-spectrum Gram-positive antibacterial agents targeting RF metabolism. Copyright © 2017 Elsevier Ltd. All rights reserved.

Phase I study of the combination of two hypoxic cell radiosensitizers, Ro 03-8799 and SR-2508: toxicity and pharmacokinetics

International Nuclear Information System (INIS)

Newman, H.F.; Bleehen, N.M.; Workman, P.

1986-01-01

The hypoxic cell radiosensitizer Ro 03-8799 produces acute central nervous system toxicity which limits repeated doses of the drug to 0.75 g/m 2 , but peripheral neuropathy does not occur. SR-2508 causes no acute effects at doses greater than 3.0 g/m 2 , but causes peripheral neuropathy at cumulative doses of 30 g/m 2 . By combining maximum tolerated doses of each agent, it may be possible to increase efficacy, but not toxicity. Escalating single doses of Ro 03-8799 and SR-2508 were administered to 10 patients. The drugs were infused together in 50 ml of 0.9% saline over 10 min, beginning at 0.5 g/m 2 of each agent, and proceeding to a fixed dose of 0.75 g/m 2 Ro 03-8799 with 0.5, 1.0, 2.0, and 3.0 g/m 2 SR-2508. Four patients experienced the expected acute syndrome related to Ro 03-8799, but the incidence was not increased by escalating doses of SR-2508, and no peripheral neuropathy was seen. Plasma and urine pharmacokinetic studies showed that no drug interaction occurred. Six patients have been given a 9-dose regime over a 3 week period, using 0.75 g/m 2 Ro 03-8799 and escalating doses of 0.5, 1.0, and 1.5 g/m2 SR-2508. All exhibited the expected acute side effects related to Ro 03-8799, but with no increase at the higher doses of SR-2508. No other toxicity was seen. Plasma pharmacokinetics performed at the beginning and end of the schedule were similar. Biopsies were taken from six superficial tumors following combined radiosensitizer administration. Mean tumor concentrations over the 30 min following the end of infusion were 30 and 72 micrograms/g for Ro 03-8799 and SR-2508, respectively. These values would be expected to translate into an approximate single dose sensitizer enhancement ratio of 1.5 to 1.6, offering a significant gain over the enhancement possible with the drugs given alone

Med-Ro Hybrid desalination as option to supply fresh water in BABEL Islands Province

International Nuclear Information System (INIS)

Siti Alimah; Sudi Ariyanto; June Mellawati; Budiarto

2011-01-01

Med-Ro hybrid desalination systems are combining both thermal (Med) and membrane (Ro) desalination processes with power generation systems. This configuration has more economical and operational benefits in comparison with single desalination plant. Hybrid configurations are characterized by flexibility in operation, specific energy consumption (33.50 kWh/m 3 ) is lower than Med (36.54 kWh/m 3 ) and high plant availability. The objective of study is to analyze the Med-Ro hybrid desalination as an option to add supply fresh water in Babel Islands Province, in terms of technology and economy aspects. The result of study showed that adopting nuclear power plants as dual-purpose for power generation and producing fresh water is has economic competitiveness than fossil-fired generation plants. Med-Ro hybrid configuration, with feed Ro from heat rejection of Med system is suitable as fresh water supply add option because increase of Ro feed temperature will increase flux. Economic analysis of water cost are performed using the Deep-3.2. Water cost of hybrid Med-Ro desalination with energy of NPP (0.581 $/m ) is lower than that of Med water cost (0.752 $/m ) . Water cost of hybrid Med-Ro with energy of NPP (0.581 $/m ) is lower than that of water cost of energy with fossil-fired generation plants (0.720 $/m 3 ). (author)

Cardiac fibroblast transcriptome analyses support a role for interferogenic, profibrotic, and inflammatory genes in anti-SSA/Ro-associated congenital heart block.

Science.gov (United States)

Clancy, Robert M; Markham, Androo J; Jackson, Tanisha; Rasmussen, Sara E; Blumenberg, Miroslav; Buyon, Jill P

2017-09-01

The signature lesion of SSA/Ro autoantibody-associated congenital heart block (CHB) is fibrosis and a macrophage infiltrate, supporting an experimental focus on cues influencing the fibroblast component. The transcriptomes of human fetal cardiac fibroblasts were analyzed using two complementary approaches. Cardiac injury conditions were simulated in vitro by incubating human fetal cardiac fibroblasts with supernatants from macrophages transfected with the SSA/Ro-associated noncoding Y ssRNA. The top 10 upregulated transcripts in the stimulated fibroblasts reflected a type I interferon (IFN) response [e.g., IFN-induced protein 44-like (IFI44L), of MX dynamin-like GTPase (MX)1, MX2, and radical S -adenosyl methionine domain containing 2 (Rsad2)]. Within the fibrotic pathway, transcript levels of endothelin-1 (EDN1), phosphodiesterase (PDE)4D, chemokine (C-X-C motif) ligand (CXCL)2, and CXCL3 were upregulated, while others, including adenomedullin, RAP guanine nucleotide exchange factor 3 (RAPGEF3), tissue inhibitor of metalloproteinase (TIMP)1, TIMP3, and dual specificity phosphatase 1, were downregulated. Agnostic Database for Annotation, Visualization and Integrated Discovery analysis revealed a significant increase in inflammatory genes, including complement C3A receptor 1 (C3AR1), F2R-like thrombin/trypsin receptor 3, and neutrophil cytosolic factor 2. In addition, stimulated fibroblasts expressed high levels of phospho-MADS box transcription enhancer factor 2 [a substrate of MAPK5 (ERK5)], which was inhibited by BIX-02189, a specific inhibitor of ERK5. Translation to human disease leveraged an unprecedented opportunity to interrogate the transcriptome of fibroblasts freshly isolated and cell sorted without stimulation from a fetal heart with CHB and a matched healthy heart. Consistent with the in vitro data, five IFN response genes were among the top 10 most highly expressed transcripts in CHB fibroblasts. In addition, the expression of matrix-related genes

Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl) methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1

Czech Academy of Sciences Publication Activity Database

Šimon, Petr; Baszczyňski, Ondřej; Šaman, David; Stepan, G.; Hu, E.; Lansdon, E. B.; Jansa, P.; Janeba, Zlatko

2016-01-01

Roč. 122, Oct 21 (2016), s. 185-195 ISSN 0223-5234 Institutional support: RVO:61388963 Keywords : diarylpyrimidine (DAPY) * etravirine * human immunodeficiency virus ( HIV ) * non-nucleoside reverse transcriptase inhibitors * NNRTIs * rilpivirine Subject RIV: CC - Organic Chemistry Impact factor: 4.519, year: 2016

VizieR Online Data Catalog: CoRoT observation log (N2-4.4) (CoRoT, 2009-2016)

Science.gov (United States)

COROT Team

2014-03-01

CoRoT is a space astronomy mission devoted to the study of the variability with time of stars brightness, with an extremely high accuracy (100 times better than from the ground), on very long durations (up to 150 days) and a very high duty cycle (more than 90%). The mission was led by CNES in association with four french laboratories, and 7 participating countries and agencies (Austria, Belgium, Brazil, Germany, Spain, and the ESA Science Programme). The satellite is composed of a PROTEUS platform (the 3rd in the serie), and a unique instrument: a stellar photometer. It has been launched on December 27th 2006 by a Soyuz Rocket, from Baikonour. The mission has lasted almost 6 years (the nominal 3 years duration and a 3 years extension) and has observed more than 160 000 stars. It stopped to send data suddenly on November 2nd 2012. CoRoT is performing Ultra High Precision Photomery of Stars to detect and characterise the variability of their luminosity with two main directions: - variability of the object itself: oscillations, rotation, magnetic activity - variability due to external causes as bodies in orbit around the star: planets and stars The original scientific objectives were focussed on the study of stellar pulsations (asteroseismology) to probe the internal structure of stars, and the detection of small exoplanets through their "transit in front of their host star, and the measurement of their size. This lead to introduce two modes of observations, working simultaneously: - The bright star mode dedicated to very precise seismology of a small sample of bright and closeby stars (data presented in file momentarily named "astero.dat", but should change in the near future to to "bright star.dat") - The faint star mode, observing a very large number of stars at the same time, to detect transits, which are rare events, as they imply the alignment of the star, the planet and the observer (data presented in momentarily named "exo.dat" but should change in the near

S1 pocket fingerprints of human and bacterial methionine aminopeptidases determined using fluorogenic libraries of substrates and phosphorus based inhibitors

Czech Academy of Sciences Publication Activity Database

Poreba, M.; Gajda, A.; Pícha, Jan; Jiráček, Jiří; Marschner, A.; Klein, Ch. D.; Salvesen, G. S.; Drag, M.

2012-01-01

Roč. 94, č. 3 (2012), s. 704-710 ISSN 0300-9084 R&D Projects: GA MŠk(CZ) LC06077 Institutional research plan: CEZ:AV0Z40550506 Keywords : methionine aminopeptidase * substrate library * protease * enzyme * inhibitor * substrate specificity Subject RIV: CC - Organic Chemistry Impact factor: 3.142, year: 2012

Anisotropic attenuation in rocks: Theory, modelling and lab measurements

Czech Academy of Sciences Publication Activity Database

Vavryčuk, Václav; Svitek, Tomáš; Lokajíček, Tomáš

2017-01-01

Roč. 208, č. 3 (2017), s. 1724-1739 ISSN 0956-540X R&D Projects: GA ČR(CZ) GAP210/12/1491; GA ČR(CZ) GC16-19751J; GA MŠk LH13102 Institutional support: RVO:67985530 ; RVO:67985831 Keywords : elasticity and anelasticity * body waves * seismic anisotropy * seismic attenuation Subject RIV: DC - Siesmology, Volcanology, Earth Structure; DB - Geology ; Mineralogy (GLU-S) OBOR OECD: Volcanology; Geology (GLU-S) Impact factor: 2.414, year: 2016

Natural inhibitors of tumor-associated proteases

International Nuclear Information System (INIS)

Magdolen, U.; Krol, J.; Sato, S.; Schmitt, M.; Magdolen, V.; Krueger, A.; Mueller, M.M.; Sperl, S.

2002-01-01

The turnover and remodelling of extracellular matrix (ECM) is an essential part of many normal biological processes including development, morphogenesis, and wound healing. ECM turnover also occurs in severe pathological situations like artherosclerosis, fibrosis, tumor invasion and metastasis. The major proteases involved in this turnover are serine proteases (especially the urokinase-type plasminogen activator/plasmin system), matrix metalloproteases (a family of about 20 zinc-dependent endopeptidases including collagenases, gelatinases, stromelysins, and membrane-type metalloproteases), and cysteine proteases. In vivo, the activity of these proteases is tightly regulated in the extracellular space by zymogen activation and/or controlled inhibition. In the present review, we give an overview on the structure and biochemical properties of important tumor-associated protease inhibitors such as plasminogen activator inhibitor type 1 and type 2 (PAI-1, PAI-2), tissue inhibitors of metalloproteinases (TIMP-1, -2, -3, and -4), and the cysteine protease inhibitor cystatin C. Interestingly, some of these inhibitors of tumor-associated proteases display multiple functions which rather promote than inhibit tumor progression, when the presence of inhibitors in the tumor tissue is not balanced. (author)

Inhibitors of NADPH oxidase decrease endotoxin mediated induction of inducible nitric oxide expression in mouse macrophages

Czech Academy of Sciences Publication Activity Database

Krejčová, Daniela; Okénková, Kateřina; Konopka, Roman; Lojek, Antonín; Kubala, Lukáš

2007-01-01

Roč. 101, č. 14 (2007), s203-s204 E-ISSN 1213-7103. [Mezioborová česko-slovenská toxikologická konference /12./. Praha, 11.06.2007-13.06.2007] R&D Projects: GA ČR(CZ) GA524/06/1197 Institutional research plan: CEZ:AV0Z50040507; CEZ:AV0Z50040702 Keywords : lipopolysaccharide * inhibitors of NADPH oxidase * macrophage s Subject RIV: BO - Biophysics

Unprecedented Binding Mode of Hydroxamate-Based Inhibitors of Glutamate Carboxypeptidase II: Structural Characterization and Biological Activity

Czech Academy of Sciences Publication Activity Database

Nováková, Zora; Wozniak, K.; Jančařík, Andrej; Rais, R.; Wu, Y.; Pavlíček, Jiří; Ferraris, D.; Havlínová, Barbora; Ptáček, Jakub; Vávra, Jan; Hin, N.; Rojas, C.; Majer, Pavel; Slusher, B. S.; Tsukamoto, T.; Bařinka, Cyril

2016-01-01

Roč. 59, č. 10 (2016), s. 4539-4550 ISSN 0022-2623 R&D Projects: GA MŠk(CZ) ED1.1.00/02.0109; GA ČR GAP301/12/1513 Institutional support: RVO:86652036 ; RVO:61388963 Keywords : LINKED ACIDIC DIPEPTIDASE * N-ACETYLASPARTYLGLUTAMATE NAAG * THIOL-BASED INHIBITORS Subject RIV: FR - Pharmacology ; Medidal Chemistry ; CC - Organic Chemistry (UOCHB-X) Impact factor: 6.259, year: 2016

RO-75, Reverse Osmosis Plant Design Optimization and Cost Optimization

International Nuclear Information System (INIS)

Glueckstern, P.; Reed, S.A.; Wilson, J.V.

1999-01-01

1 - Description of problem or function: RO75 is a program for the optimization of the design and economics of one- or two-stage seawater reverse osmosis plants. 2 - Method of solution: RO75 evaluates the performance of the applied membrane module (productivity and salt rejection) at assumed operating conditions. These conditions include the site parameters - seawater salinity and temperature, the membrane module operating parameters - pressure and product recovery, and the membrane module predicted long-term performance parameters - lifetime and long flux decline. RO75 calculates the number of first and second stage (if applied) membrane modules needed to obtain the required product capacity and quality and evaluates the required pumping units and the power recovery turbine (if applied). 3 - Restrictions on the complexity of the problem: The program does not optimize or design the membrane properties and the internal structure and flow characteristics of the membrane modules; it assumes operating characteristics defined by the membrane manufacturers

Simple, Accurate, Low-cost RO Science with the Iridium-NEXT Satellite Constellation

Science.gov (United States)

Meehan, T.; Mannucci, A. J.

2011-12-01

Over the last decade, a disparate collection of GNSS-RO instruments have been measuring the refractivity of the Earth's ionosphere and atmosphere. These measurements have proven to be robust and precise data sets for operational weather, climate and geospace sciences. Future GNSS-RO weather and science will most benefit from a large number of profiles (10000+/day), with lower latency and greater accuracy in the lowest 5 km altitude. For weather, latencies below 90 minutes are required, 30 minutes desired. Space weather latency requirements are more stringent, with 15 minutes being a long sought goal. Climate studies benefit from averaging measurements uniformly distributed over the Earth, acquired over decades, with local time sampling errors minimized by dense coverage or well designed orbits. There's much more of course, because space GNSS science is still nascent but with gathering momentum among the international community. Although individual GNSS-RO instruments are relatively cheap as space hardware goes, growing the measurement density can be costly when a dozen or more are required for a single program. In this presentation, we propose a novel technique for greatly reducing the cost of a constellation of GNSS-RO instruments and discuss the science trade-offs of this approach versus the more traditional GNSS-RO designs.

Radioprotective effect of misonidazole (Ro-07-0582) on normal canine rectum

Energy Technology Data Exchange (ETDEWEB)

Stryker, J.A.; Albert, A.; Abt, A.B.

1980-10-01

A single 1500 rad (=15 Gy) dose of 10-MeV X-rays was administered to the pelvis of 20 mongrel dogs. Ten received misonidazole (Ro-07-0582), 100 mg/kg p.o., 4 hours pre-irradiation. Serum misonidazole levels immediately pre-irradiation were 43 +- 10 ..mu..g/ml (mean +- SD). The dogs were euthanized within 3 months post-irradiation. Each rectal specimen was studied for anatomic and histologic pathology and was assigned a Pathologic Alteration Score (PAS) of 1, 2, or 3 in order of increasing severity. The PAS of the rectal specimens from the drug group was 1.6 +- 0.7, and that of the controls 2.3 +- 0.8. The PAS of the drug group was significantly lower than the control group (P = 0.008). The data suggest that misonidazole is a radioprotector for normal tissue.

Glu-Ureido-Based Inhibitors of Prostate-Specific Membrane Antigen: Lessons Learned During the Development of a Novel Class of Low-Molecular-Weight Theranostic Radiotracers

Czech Academy of Sciences Publication Activity Database

Kopka, K.; Benesova, M.; Bařinka, Cyril; Haberkorn, U.; Babich, J.

2017-01-01

Roč. 58, Suppl. 2 (2017), s. 17-26 ISSN 0161-5505 Institutional support: RVO:86652036 Keywords : small-molecule PSMA inhibitors * theranostic PSMA radioligands * PSMA radiotracers Subject RIV: EB - Genetics ; Molecular Biology OBOR OECD: Cell biology Impact factor: 6.646, year: 2016

Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.

Science.gov (United States)

Bagley, Mark C; Davis, Terence; Dix, Matthew C; Murziani, Paola G S; Rokicki, Michal J; Kipling, David

2008-07-01

5-Aminopyrazol-4-yl ketones are prepared rapidly and efficiently using microwave dielectric heating from beta-ketonitriles by treatment with N,N'-diphenylformamidine followed by heterocyclocondensation by irradiation with a hydrazine. The inhibitory activity of RO3201195 prepared by this methodology was confirmed in hTERT-immortalized HCA2 and WS dermal fibroblasts at 200nM concentration, both by ELISA and immunoblot assay, and displays excellent kinase selectivity for p38alpha MAPK over the related stress-activated kinase JNK.

Utilization of reverse osmosis (RO) for reuse of MBR-treated wastewater in irrigation-preliminary tests and quality analysis of product water.

Science.gov (United States)

Bunani, Samuel; Yörükoğlu, Eren; Sert, Gökhan; Kabay, Nalan; Yüksel, Ümran; Yüksel, Mithat; Egemen, Özdemir; Pek, Taylan Özgür

2018-02-01

Membrane bioreactor (MBR) effluent collected from a wastewater treatment plant installed at an industrial zone was used for reverse osmosis (RO) membrane tests in the laboratory. For this, two different GE Osmonics RO membranes (AK-BWRO and AD-SWRO) were employed. The results showed that AK-brackish water reverse osmosis (AK-BWRO) and AD-seawater reverse osmosis (AD-SWRO) membranes have almost similar rejection performances regarding analyzed parameters such as conductivity, salinity, color, chemical oxygen demand (COD), and total organic carbon (TOC). On the other hand, these membranes behaved quite differently considering their permeate water flux at the same applied pressure of 10 bar. AD-SWRO membrane was also tested at 20 bar. The results revealed that AD-SWRO membrane had almost the same rejections either at 10 or at 20 bar of applied pressure. Compared with irrigation water standards, AK-BWRO and AD-SWRO gave an effluent with low salinity value and sodium adsorption ratio (SAR) which makes it unsuitable for irrigation due to the infiltration problems risi0ng from unbalanced values of salinity and SAR. Combination of MBR effluent and RO effluent at respective proportions of 0.3:0.7 and 0.4:0.6 for AK-BWRO and AD-SWRO, respectively, are the optimum mixing ratios to overcome the infiltration hazard problem. Choice of less-sensitive crops to chloride and sodium ions is another strategy to overcome all hazards which may arise from above suggested mixing proportions.

RO5: proposal of a relevant facility in nuclear fusion research

International Nuclear Information System (INIS)

Pouzo, J.

1987-01-01

The RO5 project is a proposal of an experiment in nuclear fusion research based in a plasma focus device. The main research scopes of the experiment, with respect to the scaling law foundations and the identification of the main nuclear reaction mechanisms, are discussed. A practical aim of the experiment is to reach 10 14 - 10 15 neutrons/pulse from D-D reactions in the plasma focus using a 3 MJ capacitor bank. It represents an energy efficience of around a 5% when D-T mixture is used as filling gas in the reactor (RO5 = Reactor of 5% in energy efficience). A first RO5 design obtained with a 2D snowplow model and taken into account the operation limits recently found, is presented. (author) [pt

Glucocorticoids and Polyamine Inhibitors Synergize to Kill Human Leukemic CEM Cells

Directory of Open Access Journals (Sweden)

Aaron L. Miller

2002-01-01

Full Text Available Glucocorticoids are well-known apoptotic agents in certain classes of lymphoid cell malignancies. Reduction of intracellular polyamine levels by use of inhibitors that block polyamine synthesis slows or inhibits growth of many cells in vitro. Several such inhibitors have shown efficacy in clinical trials, though the toxicity of some compounds has limited their usefulness. We have tested the effects of combinations of the glucocorticoid dexamethasone. (20Dex and two polyamine inhibitors, difluoromethylornithine. (20DFMO and methyl glyoxal bis guanylhydrazone. (20MGBG, on the clonal line of human acute lymphoblastic leukemia cells, CEM-C7-14. Dex alone kills these cells, though only after a delay of at least 24 hours. We also evaluated a partially glucocorticoid-resistant c-Myc-expressing CEM-C7-14 clone. We show that Dex downregulates ornithine decarboxylase. (20ODC, the rate-limiting enzyme in polyamine synthesis. Pretreatment with the ODC inhibitor DFMO, followed by addition of Dex, enhances steroid-evoked kill slightly. The combination of pretreatment with sublethal concentrations of both DFMO and the inhibitor of S-adenosylmethionine decarboxylase, MGBG, followed by addition of Dex, results in strong synergistic cell kill. Both the rapidity and extent of cell kill are enhanced compared to the effects of Dex alone. These results suggest that use of such combinations in vivo may result in apoptosis of malignant cells with lower overall toxicity.

Monoamine depletion by reuptake inhibitors

Directory of Open Access Journals (Sweden)

Hinz M

2011-10-01

Full Text Available Marty Hinz1, Alvin Stein2, Thomas Uncini31Clinical Research, NeuroResearch Clinics Inc, Cape Coral, FL; 2Stein Orthopedic Associates, Plantation, FL; 3DBS Labs Inc, Duluth, MN, USABackground: Disagreement exists regarding the etiology of cessation of the observed clinical results with administration of reuptake inhibitors. Traditionally, when drug effects wane, it is known as tachyphylaxis. With reuptake inhibitors, the placebo effect is significantly greater than the drug effect in the treatment of depression and attention deficit hyperactivity disorder, leading some to assert that waning of drug effects is placebo relapse, not tachyphylaxis.Methods: Two groups were retrospectively evaluated. Group 1 was composed of subjects with depression and Group 2 was composed of bariatric subjects treated with reuptake inhibitors for appetite suppression.Results: In Group 1, 200 subjects with depression were treated with citalopram 20 mg per day. A total of 46.5% (n = 93 achieved relief of symptoms (Hamilton-D rating score ≤ 7, of whom 37 (39.8% of whom experienced recurrence of depression symptoms, at which point an amino acid precursor formula was started. Within 1–5 days, 97.3% (n = 36 experienced relief of depression symptoms. In Group 2, 220 subjects were treated with phentermine 30 mg in the morning and citalopram 20 mg at 4 pm. In this group, 90.0% (n = 198 achieved adequate appetite suppression. The appetite suppression ceased in all 198 subjects within 4–48 days. Administration of an amino acid precursor formula restored appetite suppression in 98.5% (n = 195 of subjects within 1–5 days.Conclusion: Reuptake inhibitors do not increase the total number of monoamine molecules in the central nervous system. Their mechanism of action facilitates redistribution of monoamines from one place to another. In the process, conditions are induced that facilitate depletion of monoamines. The "reuptake inhibitor monoamine depletion theory" of this paper

Hypoxic cell radiosensitizers in the treatment of high grade gliomas: a new direction using combined Ro 03-8799 (pimonidazole) and SR 2508 (etanidazole)

International Nuclear Information System (INIS)

Newman, H.F.; Bleehen, N.M.; Ward, R.; Workman, P.

1988-01-01

The hypoxic cell radiosensitizers Ro 03-8799 (pimonidazole) and SR 2508 (etanidazole) have been evaluated for their simultaneous penetration into human brain tumors and surrounding normal tissue. Thirteen patients received a dose of 1 g of each agent, infused over a 10 minute period during neurosurgery. Samples of glioma (20), brain (10) and cerebrospinal fluid (1) were obtained at a mean time (+/- SD) of 31 +/- 18 min from the end of infusion. A 24 hr plasma time course was measured in six patients. Nitroimidazole concentrations were determined by HPLC. For a mean dose of 0.55 g/m2 of each agent, the mean tumor concentrations (+/- SD) were 17.0 +/- 12.0 micrograms/g for Ro 03-8799 and 13.5 +/- 10.9 micrograms/g for SR 2508. The tumor/plasma ratios were 279 +/- 230% and 47 +/- 34% respectively. For adjacent 'normal' brain tissue, the radiosensitizer concentrations were 29.9 +/- 13.1 micrograms/g for Ro 03-8799, and 4.0 +/- 1.7 micrograms/g for SR 2508, and the brain/plasma ratios were 430 +/- 29% and 14 +/- 8% respectively. There was a significant trend towards increasing accumulation of both agents with time, in both tumor and normal brain. Concentrations in cerebrospinal fluid were very low. Plasma pharmacokinetics for Ro 03-8799 were similar to previous experience, but for SR 2508 the terminal half-life was greater in this series by a factor of 1.3. The results confirm that Ro 03-8799 is distributed widely in the central nervous system, and demonstrate that SR 2508 can achieve high tumor concentrations when the blood-brain barrier is compromised. The concentrations achieved with the combination are indicative of a significant advantage over metronidazole, misonidazole, or either agent alone, and normalized to the therapeutic dose of 0.75 g/m2 plus 2.0 g/m2 SR 2508 are consistent with those giving additive sensitization in an in vivo mouse tumor model

Discovery and Biological Evaluation of Potent and Selective N-Methylene Saccharin-Derived Inhibitors for Rhomboid Intramembrane Proteases

Czech Academy of Sciences Publication Activity Database

Goel, P.; Jumpertz, T.; Mikles, David C.; Tichá, Anežka; Nguyen, M. T. N.; Verhelst, S.; Hubálek, Martin; Johnson, D. C.; Bachovchin, D. A.; Ogorek, I.; Pietrzik, C. U.; Stříšovský, Kvido; Schmidt, B.; Weggen, S.

2017-01-01

Roč. 56, č. 51 (2017), s. 6713-6725 ISSN 0006-2960 R&D Projects: GA MŠk(CZ) LK11206; GA MŠk LO1302 EU Projects: European Commission(XE) 304154 - Rhomboid substrates Grant - others:EMBO(DE) 2329 Institutional support: RVO:61388963 Keywords : intramembrane protease * rhomboid * inhibitor Subject RIV: CE - Biochemistry OBOR OECD: Biochemistry and molecular biology Impact factor: 2.938, year: 2016

Polysubstituted 4,6-bis(hetero)arylpyrimidines as dual inhibitors of nitric oxide and prostaglandin E-2 production

Czech Academy of Sciences Publication Activity Database

Kolman, Viktor; Jansa, Petr; Kalčic, Filip; Janeba, Zlatko; Zídek, Zdeněk

2017-01-01

Roč. 67, Jul 1 (2017), s. 53-57 ISSN 1089-8603 R&D Projects: GA TA ČR(CZ) TE01020028 Institutional support: RVO:61388963 ; RVO:68378041 Keywords : pyrimidine derivatives * nitric oxide * prostaglandin E-2 * dual inhibitors * anti-inflammatory properties Subject RIV: CE - Biochemistry; CC - Organic Chemistry (UEM-P) OBOR OECD: Biochemistry and molecular biology; Organic chemistry (UEM-P) Impact factor: 4.181, year: 2016

Digestive alpha-amylases of the flour moth Ephestia kuehniella - adaptation to alkaline environment and plant inhibitors

Czech Academy of Sciences Publication Activity Database

Pytelková, Jana; Hubert, J.; Lepšík, Martin; Šobotník, Jan; Šindelka, Radek; Křížková, I.; Horn, Martin; Mareš, Michael

2009-01-01

Roč. 276, č. 13 (2009), s. 3531-3546 ISSN 1742-464X R&D Projects: GA AV ČR IAA400550617; GA MŠk LC512; GA ČR GA301/09/1752 Institutional research plan: CEZ:AV0Z40550506; CEZ:AV0Z50520701 Keywords : alkaline adaptation * alpha - amylase * alpha - amylase inhibitor * Ephestia kuehniella * plant-insect interaction Subject RIV: CE - Biochemistry Impact factor: 3.042, year: 2009

Modulation of hypericin photodynamic therapy by pretreatment with 12 various inhibitors of arachidonic acid metabolism in colon adenocarcinoma HT-29 cells

Czech Academy of Sciences Publication Activity Database

Kleban, J.; Mikeš, J.; Szilárdiová, B.; Koval, J.; Sačková, V.; Solár, P.; Horváth, Viktor; Hofmanová, Jiřina; Kozubík, Alois; Fedoročko, P.

2007-01-01

Roč. 83, č. 5 (2007), s. 1174-1185 ISSN 0031-8655 R&D Projects: GA AV ČR(CZ) 1QS500040507 Institutional research plan: CEZ:AV0Z50040507; CEZ:AV0Z50040702 Keywords : hypericin * photodynamic therapy * arachidonic acid inhibitors Subject RIV: BO - Biophysics Impact factor: 2.172, year: 2007

3D visualization of the internal nanostructure of polyamide thin films in RO membranes

KAUST Repository

Pacheco Oreamuno, Federico

2015-11-02

The front and back surfaces of fully aromatic polyamide thin films isolated from reverse osmosis (RO) membranes were characterized by TEM, SEM and AFM. The front surfaces were relatively rough showing polyamide protuberances of different sizes and shapes; the back surfaces were all consistently smoother with very similar granular textures formed by polyamide nodules of 20–50 nm. Occasional pore openings of approximately the same size as the nodules were observed on the back surfaces. Because traditional microscopic imaging techniques provide limited information about the internal morphology of the thin films, TEM tomography was used to create detailed 3D visualizations that allowed the examination of any section of the thin film volume. These tomograms confirmed the existence of numerous voids within the thin films and revealed structural characteristics that support the water permeance difference between brackish water (BWRO) and seawater (SWRO) RO membranes. Consistent with a higher water permeance, the thin film of the BWRO membrane ESPA3 contained relatively more voids and thinner sections of polyamide than the SWRO membrane SWC3. According to the tomograms, most voids originate near the back surface and many extend all the way to the front surface shaping the polyamide protuberances. Although it is possible for the internal voids to be connected to the outside through the pore openings on the back surface, it was verified that some of these voids comprise nanobubbles that are completely encapsulated by polyamide. TEM tomography is a powerful technique for investigating the internal nanostructure of polyamide thin films. A comprehensive knowledge of the nanostructural distribution of voids and polyamide sections within the thin film may lead to a better understanding of mass transport and rejection mechanisms in RO membranes.

3D visualization of the internal nanostructure of polyamide thin films in RO membranes

KAUST Repository

Pacheco Oreamuno, Federico; Sougrat, Rachid; Reinhard, Martin; Leckie, James O.; Pinnau, Ingo

2015-01-01

The front and back surfaces of fully aromatic polyamide thin films isolated from reverse osmosis (RO) membranes were characterized by TEM, SEM and AFM. The front surfaces were relatively rough showing polyamide protuberances of different sizes and shapes; the back surfaces were all consistently smoother with very similar granular textures formed by polyamide nodules of 20–50 nm. Occasional pore openings of approximately the same size as the nodules were observed on the back surfaces. Because traditional microscopic imaging techniques provide limited information about the internal morphology of the thin films, TEM tomography was used to create detailed 3D visualizations that allowed the examination of any section of the thin film volume. These tomograms confirmed the existence of numerous voids within the thin films and revealed structural characteristics that support the water permeance difference between brackish water (BWRO) and seawater (SWRO) RO membranes. Consistent with a higher water permeance, the thin film of the BWRO membrane ESPA3 contained relatively more voids and thinner sections of polyamide than the SWRO membrane SWC3. According to the tomograms, most voids originate near the back surface and many extend all the way to the front surface shaping the polyamide protuberances. Although it is possible for the internal voids to be connected to the outside through the pore openings on the back surface, it was verified that some of these voids comprise nanobubbles that are completely encapsulated by polyamide. TEM tomography is a powerful technique for investigating the internal nanostructure of polyamide thin films. A comprehensive knowledge of the nanostructural distribution of voids and polyamide sections within the thin film may lead to a better understanding of mass transport and rejection mechanisms in RO membranes.

Zonal NePhRO scoring system: a superior renal tumor complexity classification model.

Science.gov (United States)

Hakky, Tariq S; Baumgarten, Adam S; Allen, Bryan; Lin, Hui-Yi; Ercole, Cesar E; Sexton, Wade J; Spiess, Philippe E

2014-02-01

Since the advent of the first standardized renal tumor complexity system, many subsequent scoring systems have been introduced, many of which are complicated and can make it difficult to accurately measure data end points. In light of these limitations, we introduce the new zonal NePhRO scoring system. The zonal NePhRO score is based on 4 anatomical components that are assigned a score of 1, 2, or 3, and their sum is used to classify renal tumors. The zonal NePhRO scoring system is made up of the (Ne)arness to collecting system, (Ph)ysical location of the tumor in the kidney, (R)adius of the tumor, and (O)rganization of the tumor. In this retrospective study, we evaluated patients exhibiting clinical stage T1a or T1b who underwent open partial nephrectomy performed by 2 genitourinary surgeons. Each renal unit was assigned both a zonal NePhRO score and a RENAL (radius, exophytic/endophytic properties, nearness of tumor to the collecting system or sinus in millimeters, anterior/posterior, location relative to polar lines) score, and a blinded reviewer used the same preoperative imaging study to obtain both scores. Additional data points gathered included age, clamp time, complication rate, urine leak rate, intraoperative blood loss, and pathologic tumor size. One hundred sixty-six patients underwent open partial nephrectomy. There were 37 perioperative complications quantitated using the validated Clavien-Dindo system; their occurrence was predicted by the NePhRO score on both univariate and multivariate analyses (P = .0008). Clinical stage, intraoperative blood loss, and tumor diameter were all correlated with the zonal NePhRO score on univariate analysis only. The zonal NePhRO scoring system is a simpler tool that accurately predicts the surgical complexity of a renal lesion. Copyright © 2014 Elsevier Inc. All rights reserved.

Transiting exoplanets from the CoRoT space mission. XVII. The hot Jupiter CoRoT-17b: a very old planet

Science.gov (United States)

Csizmadia, Sz.; Moutou, C.; Deleuil, M.; Cabrera, J.; Fridlund, M.; Gandolfi, D.; Aigrain, S.; Alonso, R.; Almenara, J.-M.; Auvergne, M.; Baglin, A.; Barge, P.; Bonomo, A. S.; Bordé, P.; Bouchy, F.; Bruntt, H.; Carone, L.; Carpano, S.; Cavarroc, C.; Cochran, W.; Deeg, H. J.; Díaz, R. F.; Dvorak, R.; Endl, M.; Erikson, A.; Ferraz-Mello, S.; Fruth, Th.; Gazzano, J.-C.; Gillon, M.; Guenther, E. W.; Guillot, T.; Hatzes, A.; Havel, M.; Hébrard, G.; Jehin, E.; Jorda, L.; Léger, A.; Llebaria, A.; Lammer, H.; Lovis, C.; MacQueen, P. J.; Mazeh, T.; Ollivier, M.; Pätzold, M.; Queloz, D.; Rauer, H.; Rouan, D.; Santerne, A.; Schneider, J.; Tingley, B.; Titz-Weider, R.; Wuchterl, G.

2011-07-01

We report on the discovery of a hot Jupiter-type exoplanet, CoRoT-17b, detected by the CoRoT satellite. It has a mass of 2.43 ± 0.30 MJup and a radius of 1.02 ± 0.07 RJup, while its mean density is 2.82 ± 0.38 g/cm3. CoRoT-17b is in a circular orbit with a period of 3.7681 ± 0.0003 days. The host star is an old (10.7 ± 1.0 Gyr) main-sequence star, which makes it an intriguing object for planetary evolution studies. The planet's internal composition is not well constrained and can range from pure H/He to one that can contain ~380 earth masses of heavier elements. The CoRoT space mission, launched on December 27th 2006, has been developed and is operated by CNES, with the contribution of Austria, Belgium, Brazil, ESA (RSSD and Science Programme), Germany and Spain. Part of the observations were obtained at the Canada-France-Hawaii Telescope (CFHT) which is operated by the National Research Council of Canada, the Institut National des Sciences de l'Univers of the Centre National de la Recherche Scientifique of France, and the University of Hawaii. Based on observations made with HARPS spectrograph on the 3.6-m European Organisation for Astronomical Research in the Southern Hemisphere telescope at La Silla Observatory, Chile (ESO program 184.C-0639). Based on observations made with the IAC80 telescope operated on the island of Tenerife by the Instituto de Astrofísica de Canarias in the Spanish Observatorio del Teide. Part of the data presented herein were obtained at the W.M. Keck Observatory, which is operated as a scientific partnership among the California Institute of Technology, the University of California and the National Aeronautics and Space Administration. The Observatory was made possible by the generous financial support of the W.M. Keck Foundation.

In Vitro Mode of Action and Anti-thrombotic Activity of Boophilin, a Multifunctional Kunitz Protease Inhibitor from the Midgut of a Tick Vector of Babesiosis, Rhipicephalus microplus

Czech Academy of Sciences Publication Activity Database

Assumpção, T.C.; Ma, D.; Mizurini, D.M.; Kini, D.M.; Ribeiro, J.M.C.; Kotsyfakis, Michalis; Monteiro, R.Q.; Francischetti, I.M.B.

2016-01-01

Roč. 10, č. 1 (2016), č. článku e0004298. ISSN 1935-2735 Institutional support: RVO:60077344 Keywords : thrombin inhibitor * salivary gland * anticolagulant protein Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 3.834, year: 2016

Monoamine oxidase B single-photon emission tomography with [123I]Ro 43-0463: imaging in volunteers and patients with temporal lobe epilepsy

International Nuclear Information System (INIS)

Buck, A.; Frey, L.D.; Blaeuenstein, P.; Schubiger, P.; Kraemer, G.; Siegel, A.; Weber, B.; Wieser, H.G.

1998-01-01

Imaging of monoamine oxidase of subtype B (MAO B) is of interest in various neurological diseases. In the past non-invasive assessment of MAO B has only been possible with positron emission tomography (PET) ligands. Given the limited availability of PET, a single-photon emission tomography (SPET) ligand would be desirable. In this study SPET imaging with the new MAO B inhibitor [ 123 I]Ro 43-0463 was performed in five volunteers and nine patients with temporal lobe epilepsy (TLE). In two volunteers a second study was performed 12 h following blockade with deprenyl. In the TLE patients the tracer was administered as bolus (n = 4) or as prolonged infusion (n = 5). The regional uptake pattern correlated well with the known distribution of MAO B. In the two blocking studies ligand uptake was substantially reduced compared with baseline. In the TLE patients increased uptake was found in the ipsilateral mesial temporal lobe and, surprisingly, in the ipsilateral putamen. This study indicates the potential of the new SPET ligand [ 123 I]Ro 43-0463 to map MAO B concentration in the human brain. The new finding of increased MAO B in the putamen of TLE patients needs further studies to elucidate its exact pathophysiology. (orig.)

Inhibitor-induced oxidation of the nucleus and cytosol in Arabidopsis thaliana: implications for organelle to nucleus retrograde signalling.

Science.gov (United States)

Karpinska, Barbara; Alomrani, Sarah Owdah; Foyer, Christine H

2017-09-26

Concepts of organelle-to-nucleus signalling pathways are largely based on genetic screens involving inhibitors of chloroplast and mitochondrial functions such as norflurazon, lincomycin (LINC), antimycin A (ANT) and salicylhydroxamic acid. These inhibitors favour enhanced cellular oxidation, but their precise effects on the cellular redox state are unknown. Using the in vivo reduction-oxidation (redox) reporter, roGFP2, inhibitor-induced changes in the glutathione redox potentials of the nuclei and cytosol were measured in Arabidopsis thaliana root, epidermal and stomatal guard cells, together with the expression of nuclear-encoded chloroplast and mitochondrial marker genes. All the chloroplast and mitochondrial inhibitors increased the degree of oxidation in the nuclei and cytosol. However, inhibitor-induced oxidation was less marked in stomatal guard cells than in epidermal or root cells. Moreover, LINC and ANT caused a greater oxidation of guard cell nuclei than the cytosol. Chloroplast and mitochondrial inhibitors significantly decreased the abundance of LHCA1 and LHCB1 transcripts. The levels of WHY1 , WHY3 and LEA5 transcripts were increased in the presence of inhibitors. Chloroplast inhibitors decreased AOXA1 mRNA levels, while mitochondrial inhibitors had the opposite effect. Inhibitors that are used to characterize retrograde signalling pathways therefore have similar general effects on cellular redox state and gene expression.This article is part of the themed issue 'Enhancing photosynthesis in crop plants: targets for improvement'. © 2017 The Authors.

Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors

Czech Academy of Sciences Publication Activity Database

Baltus, C.B.; Jorda, Radek; Marot, Ch.; Berka, K.; Bazgier, Václav; Kryštof, Vladimír; Prie, G.; Viaud-Massuard, M.C.

2016-01-01

Roč. 108, JAN 27 (2016), s. 701-719 ISSN 0223-5234 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Cyclin-dependent kinase 2 * Kinase inhibitors * Anti-tumor agent Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 4.519, year: 2016

Multiple star systems observed with CoRoT and Kepler

Directory of Open Access Journals (Sweden)

Southworth John

2015-01-01

Full Text Available The CoRoT and Kepler satellites were the first space platforms designed to perform high-precision photometry for a large number of stars. Multiple systems display a wide variety of photometric variability, making them natural benefactors of these missions. I review the work arising from CoRoT and Kepler observations of multiple systems, with particular emphasis on eclipsing binaries containing giant stars, pulsators, triple eclipses and/or low-mass stars. Many more results remain untapped in the data archives of these missions, and the future holds the promise of K2, TESS and PLATO.

On the use of triazines as inhibitors of steel corrosion

International Nuclear Information System (INIS)

Sizaya, O.I.; Andrushko, A.P.

2004-01-01

A possibility of using substandard pesticides as a raw materials for synthesis of a set of triazines and also using them as a inhibitors of acidic corrosion of steel 20, as well as additions to epoxy powder coatings is considered. It is shown that triazines studied are inhibitors of acidic corrosion of steel 20. 2,4-di(ethylamino)-6-phenylhydrazono-1,3,5-triazine (In 4) has a maximum inhibiting effect among the studied compounds [ru

The gene signature in CCAAT-enhancer-binding protein alpha dysfunctional acute myeloid leukemia predicts responsiveness to histone deacetylase inhibitors

Czech Academy of Sciences Publication Activity Database

Liss, A.; Ooi, C.; Zjablovskaja, Polina; Benoukraf, T.; Radomska, H.S.; Ju, C.; Wu, M.C.; Balaštík, Martin; Delwel, R.; Brdička, Tomáš; Tan, P.; Tenen, D.G.; Alberich-Jorda, Meritxell

2014-01-01

Roč. 99, č. 4 (2014), s. 697-705 ISSN 0390-6078 R&D Projects: GA MŠk LK21307; GA MŠk(CZ) LK11213 Grant - others:NIH(US) CA66996; NIH(US) CA118316 Institutional support: RVO:68378050 Keywords : C/EBPa * histone deacetylase inhibitor * acute myeloid leukemia Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 5.814, year: 2014

YSOVAR II: Mapping YSO Inner Disk Structure in NGC 2264 with Simultaneous Spitzer and CoRoT Time Series Photometry

Science.gov (United States)

Stauffer, John; Morales-Calderon, Maria; Rebull, Luisa; Affer, Laura; Alencar, Sylvia; Allen, Lori; Barrado, David; Bouvier, Jerome; Calvet, Nuria; Carey, Sean; Carpenter, John; Ciardi, David; Covey, Kevin; D'Alessio, Paola; Espaillat, Catherine; Favata, Fabio; Flaccomio, Ettore; Forbrich, Jan; Furesz, Gabor; Hartman, Lee; Herbst, William; Hillenbrand, Lynne; Holtzman, Jon; Hora, Joe; Marchis, Franck; McCaughrean, Mark; Micela, Giusi; Mundt, Reinhard; Plavchan, Peter; Turner, Neal; Skrutzkie, Mike; Smith, Howard; Song, Inseok; Szentgyorgi, Andy; Terebey, Susan; Vrba, Fred; Wasserman, Lawrence; Watson, Alan; Whitney, Barbara; Winston, Elaine; Wood, Kenny

2011-05-01

We propose a simultaneous, continuous 30 day observation of the star forming region NGC2264 with Spitzer and CoRoT. NGC2264 is the only nearby, rich star-forming region which can be observed with CoRoT; it is by definition then the only nearby, rich star-forming region where a simultaneous Spitzer/CoRoT campaign is possible. Fortunately, the visibility windows for the two spacecraft overlap, allowing this program to be done in the Nov. 25, 2011 to Jan. 4, 2012 time period. For 10 days, we propose to map the majority of the cluster (a 35'x35' region) to a depth of 48 seconds per point, with each epoch taking 1.7 hours, allowing of order 12 epochs per day. For the other 20 days, we propose to obtaining staring-mode data for two positions in the cluster having a high density of cluster members. We also plan to propose for a variety of other ground and space-based data, most of which would also be simultaneous with the Spitzer and CoRoT observing. These data will allow us to address many astrophysical questions related to the structure and evolution of the disks of young stars and the interaction of those disks with the forming star. The data may also help inform models of planet formation since planets form and migrate through the pre-main sequence disks during the 0.5-5 Myr age range of stars in NGC2264. The data we collect will also provide an archive of the variability properties of young stars that is unmatched in its accuracy, sensitivity, cadence and duration and which therefore could inspire investigation of phenomena which we cannot now imagine. The CoRoT observations have been approved, contingent on approval of a simultaneous Spitzer observing program (this proposal).

Application of indirect immunofluorescent test with an improved HEp-2 substrate tranfected with human Ro60/SSA autoantigens

International Nuclear Information System (INIS)

Lv Liangjing; Chen Shunle; Gu Yueying; Shen Nan; Bao Chunde; Wang Yuan; Xue Feng; Ye Peng; Yu Chongzhao

2006-01-01

To develop an improved substrate for indirect immunofluorescent test (IIF) to detect anti-Ro/SSA autoantibodies, the human 60-kDa Ro/SSA autoantigens (Ro60) cDNAs were obtained from placental cDNA library using PCR and were cloned into the mammalian expression vectorpEGFP-C1. Then the recombinant plasmids were transfected into HEp-2 cells. We con- firmed the overexpression, localization and antigenicity of fusion proteins in transfected cells by means of fluorescence microscopy, immunoblotting and IIF. HEp-2 and HEp-Ro60 was analyzed by IIF using a panel of 10 precipitinpositive anti-Ro human sera simultaneously. Stable expression of Ro60-GFP (green fluorescent protein) fusion proteins maintained ten more generations. And Ro60-GFP kept the antigenicity of Ro and had its own characteristic immunofluorescent pattern in HEp-Ro60 cells. The transfectants dramatically increased the sensitivity of IIF testing (a mean increase of 6.7-fold in endpoint titer, P<0.01). Eight (8/10) positive an- ti-Ro sera showed characteristic immunofluorescent pattern on HEp-Ro60, including two sera which were antinuclear antibodies (ANA) negative on untransfected HEp-2. IIF-ANA in all healthy sera were negative on HEp-Ro60. As a kind of new substrate of IIF, the Ro60 transfectants can be used to detect anti-Ro antibodies. In addition, transfected HEp-2 cells kept the immunofluorescent property of HEp-2 cells in IIF-ANA tests and could be employed as substrate for the routine IIF-ANA detection. The method improved the sensitivity of IIF-ANA. (authors)

Triggering HIV polyprotein processing by light using rapid photodegradation of a tight-binding protease inhibitor

Czech Academy of Sciences Publication Activity Database

Schimer, Jiří; Pávová, Marcela; Anders, M.; Pachl, Petr; Šácha, Pavel; Cígler, Petr; Weber, Jan; Majer, Pavel; Řezáčová, Pavlína; Kräusslich, H. G.; Müller, B.; Konvalinka, Jan

2015-01-01

Roč. 6, Mar (2015), 6461/1-6461/8 ISSN 2041-1723 R&D Projects: GA ČR GBP208/12/G016; GA MŠk LO1302 Grant - others:GA MŠk(CZ) ED1.1.00/02.0109 Program:ED Institutional support: RVO:61388963 Keywords : HIV maturation * HIV PR photodegradable inhibitor * HIV PR caging Subject RIV: CE - Biochemistry Impact factor: 11.329, year: 2015 http://www.nature.com/ncomms/2015/150309/ncomms7461/pdf/ncomms7461.pdf

Aza-acyclic Nucleoside Phosphonates Containing a Second Phosphonate Group As Inhibitors of the Human, Plasmodium falciparum and vivax 6-Oxopurine Phosphoribosyltransferases and Their Prodrugs As Antimalarial Agents

Czech Academy of Sciences Publication Activity Database

Keough, D. T.; Hocková, Dana; Janeba, Zlatko; Wang, T. H.; Naesens, L.; Edstein, M. D.; Chavchich, M.; Guddat, L. W.

2015-01-01

Roč. 58, č. 2 (2015), s. 827-846 ISSN 0022-2623 R&D Projects: GA ČR GAP207/11/0108 Institutional support: RVO:61388963 Keywords : enzyme inhibitors * ANPs * Plasmodium * malaria Subject RIV: CC - Organic Chemistry Impact factor: 5.589, year: 2015

Biodistribution and metabolism of the anti-influenza drug [{sup 11}C]oseltamivir and its active metabolite [{sup 11}C]Ro 64-0802 in mice

Energy Technology Data Exchange (ETDEWEB)

Hatori, Akiko; Arai, Takuya; Yanamoto, Kazuhiko; Yamasaki, Tomoteru; Kawamura, Kazunori; Yui, Joji; Konno, Fujiko; Nakao, Ryuji; Suzuki, Kazutoshi [Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences (NIRS), Inage-ku, Chiba 263-8555 (Japan); Zhang Mingrong [Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences (NIRS), Inage-ku, Chiba 263-8555 (Japan)], E-mail: zhang@nirs.go.jp

2009-01-15

Introduction: Oseltamivir phosphate (Tamiflu) is an orally active anti-influenza drug, which is hydrolyzed by esterase to its carboxylate metabolite Ro 64-0802 with potent activity to inhibit the influenza virus. The abnormal behavior and death associated with the use of oseltamivir have developed into a major problem in Japan where Tamiflu is often prescribed for seasonal influenza. It is critical to determine the amount of oseltamivir and Ro 64-0802 in the human brain and to elucidate the relationship between their amounts and neuropsychiatric side effects. The aim of this study was to evaluate [{sup 11}C]oseltamivir and [{sup 11}C]Ro 64-0802 in mice as promising positron emission tomography (PET) ligands for measuring their amounts in living brains. Methods: Whole-body biodistribution of [{sup 11}C]oseltamivir and [{sup 11}C]Ro 64-0802 was determined in mice using the dissection method and micro-PET. In vitro and in vivo metabolite assay was performed in the plasma and brain of mice. Results: Between 1 and 60 min after injection of [{sup 11}C]oseltamivir and [{sup 11}C]Ro 64-0802, 0.20-0.06% and 0.39-0.03% ID/g were detected in the mouse brains, respectively (dissection method). Radioactivity concentrations in the living brains between 0 and 90 min after injection were measured at standardized uptake values of 0.25-0.05 for [{sup 11}C]oseltamivir and 0.38-0.02 for [{sup 11}C]Ro 64-0802 (micro-PET). In vivo metabolite assay demonstrated the presence of [{sup 11}C]oseltamivir and [{sup 11}C]Ro 64-0802 in the brains after [{sup 11}C]oseltamivir injection. Conclusion: This study determined the distribution and metabolism of [{sup 11}C]oseltamivir and [{sup 11}C]Ro 64-0802 in mice. PET could be used to measure their amounts in the living brain and to elucidate the relationship between the amounts in the brain and the side effects of Tamiflu in the central nervous system.

RO unit for canned coffee drink processing line. Shipped to Tone Coca-Cola Bottling Co. Ltd., Ibaraki plant; Coffee line yo RO sochi. Tone Coca-Cola Bottling (kabu) Ibaraki kojo nonyu

Energy Technology Data Exchange (ETDEWEB)

Nakajima, K. [Ebara Corp., Tokyo (Japan)

1996-01-20

The paper introduces an RO unit (reverse osmotic membrane equipment) for producing water holding for the canned coffee drink processing line introduced to the Ibaraki plant of Tone Coca-Cola Bottling Co. The unit aims at reducing hardness components from city water and producing water holding for the coffee drink processing line. The capacity of the unit is 25m{sup 3}/h and the recovery rate is 80%. The unit is composed of a sand filter, an heat exchanger, a pre-filter, RO modules, a treated water tank, chemicals storage tanks, and an RO cleaning unit, which are all for pretreatment. The treated water, into which chlorine is injected, is sent through the existing activated carbon tower and micro filter to the processing line. The RO unit can remove at the same time ion and trihalomethane, pathogens, organic matters which are substances other than hardness components. The continued water bottling is possible with no need for the usual reproduction process, and the maintenance is easy. Because of the high hardness of the supplied raw water, acid is injected at the primary side of the unit for pH regulation to prevent scale deposition in the RO modules. The quality of the treated water well met the specifications. 2 figs., 2 tabs.

A comparative study of Ro 03-8799: racemic mixture and enantiomers

International Nuclear Information System (INIS)

Newman, H.F.V.; Bleehen, N.M.; Workman, P.; Dunphy, E.P.; Dische, S.; Saunders, M.I.; Des Rochers, C.; Lenox-Smith, I.; Smithen, C.E.

1986-01-01

The maximum single dose of the 2-nitroimidazole hypoxic cell radiosensitiser Ro 03-8799 is limited to 1 g/m 2 by the occurrence of a well characterised acute syndrome of sweating, nausea and mental changes. In an attempt to increase the tolerable dose, the clinical toxicity of the racemic mixture was compared with that of the R- and S-enantiomers of Ro 03-8799. Twelve patients received escalating alternate doses of racemic mixture and R- or S-enantiomer, the dose levels being 0.25 g/m 2 , 0.5 g/m 2 , 0.75 g/m 2 and 1.0 g/m 2 . Careful monitoring of the acute syndrome failed to demonstrate any consistent differences between racemic mixture and either enantiomer. This would suggest that the toxicity is not mediated via any specific central nervous system receptor. It is concluded that separation of Ro 03-8799 into its enantiomers will not enable a clinically useful increase in dosage. (author)

Rožňava ore field - geophysical works

Directory of Open Access Journals (Sweden)

Géczy Július

1998-12-01

Full Text Available The article prowides a review of geophysical works in the ore field Rožňava conducted up to date. Magnetometric and geoelectric methods and gravimetric measurements have been used. Geophysical works were focused to the solving regional problems whose contribution to the prospecting of vein deposits is not essential.

MO-AB-204-01: IHE RO Overview [Health Care

Energy Technology Data Exchange (ETDEWEB)

Hadley, S. [The University of Michigan (United States)

2016-06-15

You’ve experienced the frustration: vendor A’s device claims to work with vendor B’s device, but the practice doesn’t match the promise. Getting devices working together is the hidden art that Radiology and Radiation Oncology staff have to master. To assist with that difficult process, the Integrating the Healthcare Enterprise (IHE) effort was established in 1998, with the coordination of the Radiological Society of North America. Integrating the Healthcare Enterprise (IHE) is a consortium of healthcare professionals and industry partners focused on improving the way computer systems interconnect and exchange information. This is done by coordinating the use of published standards like DICOM and HL7. Several clinical and operational IHE domains exist in the healthcare arena, including Radiology and Radiation Oncology. The ASTRO-sponsored IHE Radiation Oncology (IHE-RO) domain focuses on radiation oncology specific information exchange. This session will explore the IHE Radiology and IHE RO process for; IHE solicitation process for new profiles. Improving the way computer systems interconnect and exchange information in the healthcare enterprise Supporting interconnectivity descriptions and proof of adherence by vendors Testing and assuring the vendor solutions to connectivity problems. Including IHE profiles in RFPs for future software and hardware purchases. Learning Objectives: Understand IHE role in improving interoperability in health care. Understand process of profile development and implantation. Understand how vendors prove adherence to IHE RO profiles. S. Hadley, ASTRO Supported Activity.

ÜRO - tõeliselt üleilmne foorum / Tiina Intelmann

Index Scriptorium Estoniae

Intelmann, Tiina, 1963-

2007-01-01

Eesti Vabariigi alaline esindaja ÜRO juures tutvustab maailmaorganisatsiooni põhikirjalisi eesmärke, globaliseerumise mõjusid tegevusele, raskusi rahvusvaheliste kokkulepete täitmisel, rahuvalve ja kohtupidamisega seotud küsimusi ning igapäevatööd

Transiting exoplanets from the CoRoT space mission

DEFF Research Database (Denmark)

Ollivier, M.; Gillon, M.; Santerne, A.

2012-01-01

Aims. We report the discovery of CoRoT-16b, a low density hot jupiter that orbits a faint G5V star (mV = 15.63) in 5.3523 ± 0.0002 days with slight eccentricity. A fit of the data with no a priori assumptions on the orbit leads to an eccentricity of 0.33 ± 0.1. We discuss this value and also derive......RoT-16b is a 0.535 −0.083/+0.085 MJ, 1.17 −0.14/+0.16 RJ hot Jupiter with a density of 0.44 −0.14/+0.21 g cm-3. Despite its short orbital distance (0.0618 ± 0.0015 AU) and the age of the parent star (6.73 ± 2.8 Gyr), the planet orbit exhibits significantly non-zero eccentricity. This is very uncommon...

On-line dosing of Ammonium Biflouride for reduction of silica scaling on RO membranes

Directory of Open Access Journals (Sweden)

Ehab A. Rashed

2016-08-01

The primary goal of this research is to investigate the effectiveness of using Ammonium Biflouride (ABF as an anti-scaling agent in improving the performance of the RO membranes. ABF was used as on-line dosing with different doses for mitigation of scaling caused by silica (SiO2 on RO membranes. To study the efficiency of the anti-scaling agent, Scanning Electron Microscopy & Energy Dispersive X-ray Spectroscopy (SEM–EDS were performed for all phases before and after using the anti-scaling agent on the used RO membrane surface. The main parameters measured were: silica, TDS. Flux loss was observed for the cross-flow RO membrane after filtration. ABF doses used were: 2, 4, and 6 mg/l at constant pH = 6 and the optimum dose was found to be 4 mg/l.

Large Intergenic Non-coding RNA-RoR Inhibits Aerobic Glycolysis of Glioblastoma Cells via Akt Pathway

Science.gov (United States)

Li, Yong; He, Zhi-Cheng; Liu, Qing; Zhou, Kai; Shi, Yu; Yao, Xiao-Hong; Zhang, Xia; Kung, Hsiang-Fu; Ping, Yi-Fang; Bian, Xiu-Wu

2018-01-01

Reprogramming energy metabolism is a hallmark of malignant tumors, including glioblastoma (GBM). Aerobic glycolysis is often utilized by tumor cells to maintain survival and proliferation. However, the underlying mechanisms of aerobic glycolysis in GBM remain elusive. Herein, we demonstrated that large intergenic non-coding RNA-RoR (LincRNA-RoR) functioned as a critical suppressor to inhibit the aerobic glycolysis and viability of GBM cells. We found that LincRNA-RoR was markedly reduced in GBM tissues compared with adjacent non-tumor tissues from 10 cases of GBM patients. Consistently, LincRNA-RoR expression in GBM cells was significantly lower than that in normal glial cells. The aerobic glycolysis of GBM cells, as determined by the measurement of glucose uptake and lactate production, was impaired by LincRNA-RoR overexpression. Mechanistically, LincRNA-RoR inhibited the expression of Rictor, the key component of mTORC2 (mammalian target of rapamycin complex 2), to suppress the activity of Akt pathway and impair the expression of glycolytic effectors, including Glut1, HK2, PKM2 and LDHA. Finally, enforced expression of LincRNA-RoR reduced the proliferation of GBM cells in vitro, restrained tumor growth in vivo, and repressed the expression of glycolytic molecules in GBM xenografts. Collectively, our results underscore LincRNA-RoR as a new suppressor of GBM aerobic glycolysis with therapeutic potential. PMID:29581766

ÜRO peakorterile otsitakse naabrit / Maria-Kristiina Soomre

Index Scriptorium Estoniae

Soomre, Maria-Kristiina, 1978-

2001-01-01

New Yorki, ÜRO peakorterist lõunasse hakatakse ehitama uut hoonet. Arhitektuurikonkursist on kutsutud osalema: David Childs, Richard Meier ja Peter Eisenmann; Schuman Lichtenstein Claman Efron ja HOK arhitektid; Kohn Pederson Fox, Davis Brody Bond, Toyo Ito ja Rem Koolhaas; Henry Cobb, James Ingo Freed ja Machado & Silvetti Associates; Christian de Portzamparc ja Gary Edward Handel & Associates

A New Method for Detecting and Monitoring Atmospheric Natural Hazards with GPS RO

Science.gov (United States)

Biondi, R.; Steiner, A. K.; Rieckh, T. M.; Kirchengast, G.

2014-12-01

Global Positioning System (GPS) Radio Occultation (RO) allows measurements in any meteorological condition, with global coverage, high vertical resolution, and high accuracy. With more than 13 years of data availability, RO also became a fundamental tool for studying climate change. We present here the application of RO for detecting and monitoring tropical cyclones (TCs), deep convective systems (CSs) and volcanic ash clouds (ACs).Deep CSs and TCs play a fundamental role in atmospheric circulation producing vertical transport, redistributing water vapor and trace gases, changing the thermal structure of the Upper Troposphere and Lower Stratosphere (UTLS) and affecting climate through overshooting into the stratosphere. Explosive volcanic eruptions produce large ACs dangerous for the aviation and they can impact climate when the ash is injected into the UTLS.The detection of cloud top height, the determination of cloud extent, the discrimination of ACs from CSs clouds and the detection of overshooting are main challenges for atmospheric natural hazards study. We created a reference atmosphere with a resolution of 5° in latitude and longitude, sampled on a 1° x 1° grid, and a vertical sampling of 100 m. We then compared RO profiles acquired during TCs, CSs and ACs to the reference atmosphere and computed anomaly profiles.CSs, TCs and the ACs leave a clear signature in the atmosphere which can be detected by RO. Using RO temperature and bending angle profiles we gain insight into the vertical thermal structure and developed a new method for detecting the cloud top altitude with high accuracy.We have characterized the TCs by ocean basins and intensities, showing that they have a different thermal structure and reach to different altitudes according to the basin. We provide statistics on overshooting frequency, achieving results consistent with patterns found in the literature and demonstrating that RO is well suited for this kind of study. We have analyzed the

Overcoming multidrug resistance in Dox-resistant neuroblastoma cell lines via treatment with HPMA copolymer conjugates containing anthracyclines and P-gp inhibitors

Czech Academy of Sciences Publication Activity Database

Koziolová, Eva; Janoušková, Olga; Cuchalová, Lucie; Hvězdová, Zuzana; Hraběta, J.; Eckschlager, T.; Sivák, Ladislav; Ulbrich, Karel; Etrych, Tomáš; Šubr, Vladimír

2016-01-01

Roč. 233, 10 July (2016), s. 136-146 ISSN 0168-3659 R&D Projects: GA ČR(CZ) GAP301/12/1254; GA MŠk(CZ) LO1507 Institutional support: RVO:61389013 ; RVO:61388971 Keywords : N-(2-hydroxypropyl)methacrylamide copolymers * multidrug resistance * P-glycoprotein inhibitors Subject RIV: CD - Macromolecular Chemistry ; FD - Oncology ; Hematology (MBU-M) Impact factor: 7.786, year: 2016

CoRoT and Kepler results: Solar-like oscillators

NARCIS (Netherlands)

Hekker, S.

2013-01-01

The space-borne observatories CoRoT (Convection Rotation and planetary Transits) and Kepler have provided photometric time series data of unprecedented precision for large numbers of stars. These data have revolutionized the fields of transiting exoplanets and asteroseismology. In this review some

EXO-DAT: AN INFORMATION SYSTEM IN SUPPORT OF THE CoRoT/EXOPLANET SCIENCE

International Nuclear Information System (INIS)

Deleuil, M.; Meunier, J. C.; Moutou, C.; Surace, C.; Barbieri, M.; Agneray, F.; Granet, Y.; Guterman, P.; Deeg, H. J.; Almenara, J. M.; Debosscher, J.; Hodgkin, S.

2009-01-01

Exo-Dat is a database and an information system created primarily in support of the exoplanet program of the COnvection ROtation and planetary Transits (CoRoT) mission. In the directions of CoRoT pointings, it provides a united interface to several sets of data: stellar published catalogs, photometric and spectroscopic data obtained during the mission preparation, results from the mission and from follow-up observations, and several mission-specific technical parameters. The new photometric data constitute the subcatalog Exo-Cat, and give consistent 4-color photometry of 14.0 million stars with a completeness to 19th magnitude in the r-filter. It covers several zones in the galactic plane around CoRoT pointings, with a total area of 209 deg 2 . This Exo-Dat information system provides essential technical support to the ongoing CoRoT light-curve analyses and ground-based follow-up by supplying additional complementary information such as the prior knowledge of the star's fundamental parameters or its contamination level inside the large CoRoT photometric mask. The database is fully interfaced with VO tools and thus benefits from existing visualization and analysis tools like TOPCAT or ALADIN. It is accessible to the CoRoT community through the Web, and will be gradually opened to the public. It is the ideal tool to prepare the foreseen statistical studies of the properties of the exoplanetary systems. As a VO-compliant system, such analyses could thus benefit from the most up-to-date classifier tools.

A beta skin dose monitor using an Eberline RO-2 ion chamber

International Nuclear Information System (INIS)

Jester, W.A.; Levine, S.H.; Lin, T.J.; Hock, R.

1994-01-01

The authors have developed a portable beta skin dose monitor that uses an Eberline RO-2trademark ion chamber. The development was based, in part, upon the previous development of a beta skin dose monitor employing silicon detectors. In this current work, the two entrance windows of the RO-2 were replaced by windows having a total mass thickness of 1.74 mg/cm 2 . A two section source-detector holder was constructed. One section fastens to the RO-2 and holds the detector at the right position to determine the contact skin dose from beta emitters located on surfaces. A second section attaches to the first, and provides fixed counting geometry for radioactive samples such as hot particles. The first section also contains a slide mechanism that allows the placement of absorbers of zero (0), 8.38, and 1000 mg/cm 2 between the detector window and the beta source. The detector response to these absorbers allows for the determination of beta skin dose. The system was modeled using a Monte Carlo beta attenuation code computing the beta skin dose to RO-2 detector response as a function of absorber thickness, average beta energy, source diameter and source position. Using the RO-2 reading from each of the three absorber configurations allows the calculation of beta skin dose and the average beta energy. The results of these calculations were confirmed through the use of three massless radioactive beta sources, traceable to the National Institute of Standards and Technology, and several utility-supplied hot particles having well-established contact skin doses. An extrapolation chamber was also used to confirm the results obtained from this monitor. This system is now use at the Pennsylvania Power and Light (PP and L) Company, the project sponsor. ((orig.))

Ninety-nine is not enough: molecular characterization of inhibitor-resistant human immunodeficiency virus type 1 protease mutants with insertions in the flap region

Czech Academy of Sciences Publication Activity Database

Kožíšek, Milan; Grantz Šašková, Klára; Řezáčová, Pavlína; Brynda, Jiří; Maarseveen van, N. M.; De Jongh, D.; Boucher, Ch. A. B.; Kagan, R. M.; Nijhuis, M.; Konvalinka, Jan

2008-01-01

Roč. 82, č. 12 (2008), s. 5869-5878 ISSN 0022-538X R&D Projects: GA MŠk 1M0508; GA MZd NR8571 Institutional research plan: CEZ:AV0Z40550506; CEZ:AV0Z50520514 Keywords : HIV protease inhibitors * aspartic proteases * viral resistance * insertions Subject RIV: CE - Biochemistry Impact factor: 5.308, year: 2008

4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects

Czech Academy of Sciences Publication Activity Database

Kryštof, Vladimír; Cankař, Petr; Fryšová, I.; Slouka, J.; Kontopidis, G.; Džubák, P.; Hajdúch, M.; Srovnal, J.; de Azevedo Jr., W.F.; Orság, Martin; Paprskářová, Martina; Rolčík, Jakub; Látr, Aleš; Fischer, P.M.; Strnad, Miroslav

2006-01-01

Roč. 49, č. 22 (2006), s. 6500-6509 ISSN 0022-2623 R&D Projects: GA ČR GA301/05/0418 Institutional research plan: CEZ:AV0Z50380511 Source of funding: V - iné verejné zdroje Keywords : DEPENDENT KINASE INHIBITORS * POLYMERASE-II TRANSCRIPTION * TUMOR-NECROSIS-FACTOR Subject RIV: CE - Biochemistry Impact factor: 5.115, year: 2006

Synthesis of Novel N-Branched Acyclic Nucleoside Phosphonates As Potent and Selective Inhibitors of Human, Plasmodium falciparum and Plasmodium vivax 6-Oxopurine Phosphoribosyltransferases

Czech Academy of Sciences Publication Activity Database

Hocková, Dana; Keough, D. T.; Janeba, Zlatko; Wang, T.; de Jersey, J.; Guddat, L. W.

2012-01-01

Roč. 55, č. 13 (2012), s. 6209-6223 ISSN 0022-2623 R&D Projects: GA ČR GAP207/11/0108; GA MŠk 1M0508 Grant - others:NHMRC(AU) 569703; NHMRC(AU) 1030353 Institutional support: RVO:61388963 Keywords : enzyme inhibitors * aza-ANPs * malaria Subject RIV: CC - Organic Chemistry Impact factor: 5.614, year: 2012

Effect of Watertight Subdivision on Subdivision Index for Medium Size Ro–Ro Passenger Ferries

Directory of Open Access Journals (Sweden)

M. Pawlowski

2017-09-01

Full Text Available Ro-pax vessels should fulfil the requirements of the current harmonised SOLAS Convention. The study analyses the effect of various ro-pax vessel subdivision arrangements on the subdivision index. A Polish ferry was chosen as a generic ship to perform the study. For illustration of damage survivability, the attained subdivision index A was calculated for a number of modified configurations. The arrangements included single and double sides above and below the car deck, with and without a double buoyant car deck. The conclusions of the study can be used in the design of new ro-pax vessels.

Inhibitors of glutaminyl cyclases against Alzheimer´s disease

Czech Academy of Sciences Publication Activity Database

Kolenko, Petr; Koch, B.; Schilling, S.; Rahfeld, J.-U.; Demuth, H.-U.; Stubbs, M. T.

2013-01-01

Roč. 20, č. 1 (2013), s. 16 ISSN 1211-5894. [Discussions in Structural Molecular Biology /11./. 14.03.2013-16.03.2013, Nové Hrady] R&D Projects: GA MŠk EE2.3.30.0029 Institutional support: RVO:61389013 Keywords : glutaminyl cyclases * Alzheimer ´s disease Subject RIV: CE - Biochemistry

Modulation of neutrophil superoxide generation by inhibitors of protein kinase C, calmodulin, diacylglycerol and myosin light chain kinases, and peptidyl prolyl cis-trans isomerase.

Science.gov (United States)

Bergstrand, H; Eriksson, T; Hallberg, A; Johansson, B; Karabelas, K; Michelsen, P; Nybom, A

1992-12-01

To assess the role of protein kinase C (PKC) in the respiratory burst of adherent human polymorphonuclear leukocytes (PMNL), reduction of ferricytochrome C by cells triggered with a phorbol ester (PMA), ionophore A23187, serum-treated zymosan (STZ) or three lipid derivatives, 3-decanoyl-sn-glycerol (G-3-OCOC9), (R,R)-1,4-diethyl-2-O-decyl-L-tartrate (Tt-2-OC10) and 3-decyloxy-5-hydroxymethylphenol (DHP) was examined in a microtiter plate procedure in the presence of inhibitors of PKC and, for comparison, inhibitors of calmodulin, diacylglycerol and myosin light chain kinases and the peptidyl-prolyl cis-trans isomerase activity of fujiphilin. 1) Of the protein kinase inhibitors examined, Ro 31-7549 and staurosporine reduced responses to all stimuli except possibly STZ; in contrast, K252a and the myosin light chain kinase inhibitors ML-7 and ML-9 blocked responses to A23187 and STZ better than those triggered by PMA. H-7 reduced responses to A23187, DHP and G-3-OCOC9, and calphostin, palmitoyl carnitine, sphingosine and the multifunctional drugs TMB-8 and W-7 reduced A23187; they also, when examined, reduced decane derivative-induced O2- production more effectively than PMA- and STZ-triggered responses. Polymyxin B, 4 alpha-PMA and retinal displayed no inhibitory capacity. 2) Of the selective calmodulin antagonists, CGS 9343B, Ro 22-4839 and calmidazolium did not inhibit the oxidative response irrespective of the stimulus used, whereas metofenazate reduced those evoked by A23187, DHP, G-3-OCOC9 and STZ.(ABSTRACT TRUNCATED AT 250 WORDS)

Complementary genetic screens identify the E3 ubiquitin ligase CBLC, as a modifier of PARP inhibitor sensitivity

Czech Academy of Sciences Publication Activity Database

Frankum, J.; Moudrý, P.; Brough, R.; Hodný, Zdeněk; Ashworth, A.; Bartek, Jiří; Lord, C.J.

2015-01-01

Roč. 6, č. 13 (2015), s. 10746-10758 ISSN 1949-2553 R&D Projects: GA ČR GA13-17555S EU Projects: European Commission HEALTH-F2-2010-259893 Grant - others:Lundbeck Foundation(DK) R93-A8990; Danish Council for Independent Research(DK) DFF-1331-00262 Institutional support: RVO:68378050 Keywords : DNA damage response * ubiquitin-proteasome system * RNA interference screens * PARP inhibitors * CBLC Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 5.008, year: 2015

Studies on terrein as a new class of proteasome inhibitors

International Nuclear Information System (INIS)

Demasi, M.; Felicio, A.L.; Lima, C.; Pacheco, A.O.; Leite, H.G.; Andrade, L.H.

2010-01-01

The proteasome is an intracellular multicatalytic protease involved in the cell cycle regulation, signaling response, antigen presentation and apoptosis. Since proteasome inhibitors promote cell death by apoptosis, they have been proposed as new anti-tumoral drugs. Terrein, a secondary metabolite secreted by the fungus Aspergillus terreus, was firstly described in 1935. In the present work we report that terrein isolated through the screening for inhibitors of the 20S proteasome showed inhibitory effect upon both chymotrypsin- and trypsin-like activities of the multicatalytic core particle, the 20S proteasome. Despite of the high inhibitory concentration determined in vitro, that verified by incubating cells (fibroblasts and a pulmonary tumor cell line) in the presence of terrein was 4-fold lower indicating the proteasome as a selective intracellular target. Moreover, terrein promoted apoptotic cell death on both fibroblasts and pulmonary tumor cell line tested. Although terrein concentrations (mM range) necessary to elicit apoptosis in the cellular models herein tried were high when compared to those (muM and nM range) of other inhibitors recently described, its chemical structure is not correlated to any other inhibitor reported thus far. Therefore, the present results point out for the possibility of exploring terrein as a new molecular fragment for the development of synthetic proteasome inhibitors. (author)

Spectroscopic Properties of Benzene at the Air-Ice Interface: A Combined Experimental-Computational Approach

Czech Academy of Sciences Publication Activity Database

Kania, R.; Malongwe, J. K.; Nachtigallová, Dana; Krousko, J.; Gladich, I.; Roeselová, Martina; Heger, D.; Klán, P.

2014-01-01

Roč. 118, č. 35 (2014), s. 7535-7547 ISSN 1089-5639 R&D Projects: GA ČR GAP208/12/1318; GA ČR(CZ) GAP208/10/1724; GA MŠk(CZ) LH11021 Grant - others:GA ČR(CZ) GAP503/10/0947; GA MŠk(CZ) LO1214; European Social Fund(XE) CZ.1.07/2.3.00/30.0037 Institutional support: RVO:61388963 Keywords : density functional theory * polycyclic aromatic hydrocarbons * atmospheric air/ice interfaces Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 2.693, year: 2014

Self-Organization of 1-Methylnaphthalene on the Surface of Artificial Snow Grains: A Combined Experimental - Computational Approach

Czech Academy of Sciences Publication Activity Database

Heger, D.; Nachtigallová, Dana; Surman, F.; Krausko, J.; Magyarová, B.; Brumovský, M.; Rubeš, M.; Gladich, Ivan; Klán, P.

2011-01-01

Roč. 115, č. 41 (2011), s. 11412-11422 ISSN 1089-5639 R&D Projects: GA MŠk LC512; GA MŠk ME09064; GA ČR(CZ) GAP208/10/1724 Grant - others:CE-TOCOEN(XE) CZ.1.05/2.1.00/01.0001; GA ČR(CZ) GAP503/10/0947; GA ČR(CZ) GP203/09/P445 Institutional research plan: CEZ:AV0Z40550506 Keywords : excimers * fluorescence spectroscopy * CC2 calculations Subject RIV: CF - Physical ; Theoretical Chemistry Impact factor: 2.946, year: 2011

Limits to the presence of transiting circumbinary planets in CoRoT Data

Science.gov (United States)

Klagyivik, P.; Deeg, H. J.; Cabrera, J.; Csizmadia, Sz.; Almenara, J. M.

2017-06-01

Aims: During its flight phase, from 2007-2012, the CoRoT mission delivered light curves for over 2000 eclipsing binaries. Data from the Kepler mission have proven the existence of several transiting circumbinary planets. While light curves from CoRoT typically have lower precision and shorter coverage, the number of CoRoT targets is similar to that of Kepler and some of the known circumbinary planets could potentially be detected in CoRoT data as well. The aim of this work was to reanalyse the entire CoRoT Data set to search for the presence of circumbinary planets and to derive limits on the abundances of such planets. Methods: We developed a code that removes the signatures of eclipsing binaries from the light curves, and searches for quasi-periodic, transit-like features in the light curves after removal of binary eclipses and instrumental features. The code requires little information on sample systems and can also be used for other space missions, such as Kepler, K2, TESS, and PLATO. The code is broad in the requirements leading to detections, but was tuned to deliver an amount of detections that are manageable in a subsequent, mainly visual, assessment of their origin. Results: We identified three planet candidates in the CoRoT sample whose transits would have arisen from a single pass across the central binary; however, no candidates with transit events from multiple planetary orbits remained. We calculated the upper limits for the number of Jupiter, Saturn-, and Neptune-sized planets in co-planar orbits for different orbital period ranges. We found that there are much fewer giant planets in short periodic orbits around close binary systems than around single stars. Full Table 1 is only available at the CDS via anonymous ftp to http://cdsarc.u-strasbg.fr (http://130.79.128.5) or via http://cdsarc.u-strasbg.fr/viz-bin/qcat?J/A+A/602/A117

Characterization of the nociceptin receptor (ORL-1) agonist, Ro64-6198, in tests of anxiety across multiple species.

Science.gov (United States)

Varty, G B; Hyde, L A; Hodgson, R A; Lu, S X; McCool, M F; Kazdoba, T M; Del Vecchio, R A; Guthrie, D H; Pond, A J; Grzelak, M E; Xu, X; Korfmacher, W A; Tulshian, D; Parker, E M; Higgins, G A

2005-10-01

Previous studies have demonstrated behaviors indicative of anxiolysis in rats pretreated with the nociceptin receptor (opioid receptor like-1, ORL-1) agonist, Ro64-6198. The aim of this study was to examine the effects of Ro64-6198 in anxiety models across three species: rat, guinea pig, and mouse. In addition, the receptor specificity of Ro64-6198 was studied, using the ORL-1 receptor antagonist, J-113397, and ORL-1 receptor knockout (KO) mice. Finally, neurological studies examined potential side effects of Ro64-6198 in the rat and mouse. Ro64-6198 (3-10 mg/kg) increased punished responding in a rat conditioned lick suppression test similarly to chlordiazepoxide (6 mg/kg). This effect of Ro64-6198 was attenuated by J-113397 (10 mg/kg), but not the mu opioid antagonist, naltrexone (3 mg/kg). In addition, Ro64-6198 (1-3 mg/kg) reduced isolation-induced vocalizations in rat and guinea pig pups. Ro64-6198 (3 mg/kg) increased the proportion of punished responding in a mouse Geller-Seifter test in wild-type (WT) but not ORL-1 KO mice, whereas diazepam (1-5.6 mg/kg) was effective in both genotypes. In rats, Ro64-6198 reduced locomotor activity (LMA) and body temperature and impaired rotarod, beam walking, and fixed-ratio (FR) performance at doses of 10-30 mg/kg, i.e., three to ten times higher than an anxiolytic dose. In WT mice, Ro64-6198 (3-10 mg/kg) reduced LMA and rotarod performance, body temperature, and FR responding, but these same measures were unaffected in ORL-1 KO mice. Haloperidol (0.3-3 mg/kg) reduced these measures to a similar extent in both genotypes. These studies confirm the potent, ORL-1 receptor-mediated, anxiolytic-like effects of Ro64-6198, extending the findings across three species. Ro64-6198 has target-based side effects, although the magnitude of these effects varies across species.

Long-term analysis of resistance development in HIV-1 positive patients treated with protease and reverse transcriptase inhibitors: Correlation of the genotype and disease progression

Czech Academy of Sciences Publication Activity Database

Prejdová, Jana; Weber, Jan; Machala, L.; Reiniš, Milan; Linka, M.; Brůčková, M.; Vandasová, M.; Staňková, M.; Konvalinka, Jan

2005-01-01

Roč. 49, č. 1 (2005), 29-36 ISSN 0001-723X R&D Projects: GA MZd(CZ) NI6339 Grant - others:5th Framework(XE) QLK2-CT-2001-02360 Institutional research plan: CEZ:AV0Z4055905 Keywords : HIV * protease inhibitors * resistance development Subject RIV: CE - Biochemistry Impact factor: 0.696, year: 2005

Dispersion and nonlinear effects in OFDM-RoF system

Science.gov (United States)

Alhasson, Bader H.; Bloul, Albe M.; Matin, M.

2010-08-01

The radio-over-fiber (RoF) network has been a proven technology to be the best candidate for the wireless-access technology, and the orthogonal frequency division multiplexing (OFDM) technique has been established as the core technology in the physical layer of next generation wireless communication system, as a result OFDM-RoF has drawn attentions worldwide and raised many new research topics recently. At the present time, the trend of information industry is towards mobile, wireless, digital and broadband. The next generation network (NGN) has motivated researchers to study higher-speed wider-band multimedia communication to transmit (voice, data, and all sorts of media such as video) at a higher speed. The NGN would offer services that would necessitate broadband networks with bandwidth higher than 2Mbit/s per radio channel. Many new services emerged, such as Internet Protocol TV (IPTV), High Definition TV (HDTV), mobile multimedia and video stream media. Both speed and capacity have been the key objectives in transmission. In the meantime, the demand for transmission bandwidth increased at a very quick pace. The coming of 4G and 5G era will provide faster data transmission and higher bit rate and bandwidth. Taking advantages of both optical communication and wireless communication, OFDM Radio over Fiber (OFDM-RoF) system is characterized by its high speed, large capacity and high spectral efficiency. However, up to the present there are some problems to be solved, such as dispersion and nonlinearity effects. In this paper we will study the dispersion and nonlinearity effects and their elimination in OFDM-radio-over-fiber system.

Synthesis and evaluation of symmetric acyclic nucleoside bisphosphonates as inhibitors of the Plasmodium falciparum, Plasmodium vivax and human 6-oxopurine phosphoribosyltransferases and the antimalarial activity of their prodrugs

Czech Academy of Sciences Publication Activity Database

Špaček, Petr; Keough, D. T.; Chavchich, M.; Dračínský, Martin; Janeba, Zlatko; Naesens, L.; Edstein, M. D.; Guddat, L. W.; Hocková, Dana

2017-01-01

Roč. 25, č. 15 (2017), s. 4008-4030 ISSN 0968-0896 R&D Projects: GA ČR(CZ) GA16-06049S Institutional support: RVO:61388963 Keywords : enzyme inhibitors * nucleotide analogues * malaria Subject RIV: CC - Organic Chemistry OBOR OECD: Organic chemistry Impact factor: 2.930, year: 2016

Possible role of anti-SSA/Ro antibodies in the pathogenesis of pulmonary hypertension

Directory of Open Access Journals (Sweden)

Kelsey Guerreso

2016-01-01

Conclusion: It is known that pulmonary hypertension has association with autoimmune diseases, however no clear markers yet exist. Anti-SSA/Ro antibodies have been rarely described in cases of pulmonary disease, and less so in pulmonary hypertension. This case describes a unique association between isolated pulmonary hypertension and anti-SSA/Ro antibody, thereby illustrating the need to investigate this autoantibody and others in the pathogenesis of autoimmune pulmonary hypertension.

A Bacterial Biosensor for Oxidative Stress Using the Constitutively Expressed Redox-Sensitive Protein roGFP2

Directory of Open Access Journals (Sweden)

Carlos R. Arias-Barreiro

2010-06-01

Full Text Available A highly specific, high throughput-amenable bacterial biosensor for chemically induced cellular oxidation was developed using constitutively expressed redox-sensitive green fluorescent protein roGFP2 in E. coli (E. coli-roGFP2. Disulfide formation between two key cysteine residues of roGFP2 was assessed using a double-wavelength ratiometric approach. This study demonstrates that only a few minutes were required to detect oxidation using E. coli-roGFP2, in contrast to conventional bacterial oxidative stress sensors. Cellular oxidation induced by hydrogen peroxide, menadione, sodium selenite, zinc pyrithione, triphenyltin and naphthalene became detectable after 10 seconds and reached the maxima between 80 to 210 seconds, contrary to Cd2+, Cu2+, Pb2+, Zn2+ and sodium arsenite, which induced the oxidation maximum immediately. The lowest observable effect concentrations (in ppm were determined as 1.0 x 10−7 (arsenite, 1.0 x 10−4 (naphthalene, 1.0 x 10−4 (Cu2+, 3.8 x 10−4 (H2O2, 1.0 x 10−3 (Cd2+, 1.0 x 10−3 (Zn2+, 1.0 x 10−2 (menadione, 1.0 (triphenyltin, 1.56 (zinc pyrithione, 3.1 (selenite and 6.3 (Pb2+, respectively. Heavy metal-induced oxidation showed unclear response patterns, whereas concentration-dependent sigmoid curves were observed for other compounds. In vivo GSH content and in vitro roGFP2 oxidation assays together with E. coli-roGFP2 results suggest that roGFP2 is sensitive to redox potential change and thiol modification induced by environmental stressors. Based on redox-sensitive technology, E. coli-roGFP2 provides a fast comprehensive detection system for toxicants that induce cellular oxidation.

Application of monochloramine for wastewater reuse: Effect on biostability during transport and biofouling in RO membranes

KAUST Repository

Farhat, Nadia

2018-02-23

The rising demand for clean and safe water has increased the interest in advanced wastewater treatment and reuse. Reverse osmosis (RO) can provide reliable and high-quality water from treated wastewater. Biofouling inevitably occurs, certainly with wastewater effluents, resulting in RO performance decline and operational problems. Chlorination of feed water has been commonly applied to limit biological growth. However, chlorine use may lead to a loss of membrane integrity of RO systems. In this study the potential of monochloramine as an alternative for chlorine was studied by (i) evaluating the biological stability of a full-scale wastewater membrane bioreactor (MBR) effluent during transport over 13 km to a full-scale RO plant and (ii) assessing the biofouling control potential in membrane fouling simulator (MFS) and pilot-scale RO installation. Microbial water analysis was performed on samples taken at several locations in the full-scale water reuse system (MBR effluent, during transport, and at the RO inlet and outlet) using a suite of tools including heterotrophic plate counts (HPC), adenosine triphosphate (ATP), flow cytometry (FCM), and 16 S rRNA gene pyrosequencing. Growth potential tests were used to evaluate the effect of monochloramine presence and absence on bacterial growth. Results showed limited changes in the microbial water quality in the presence of monochloramine. MFS studies showed that membrane biofouling could be effectively repressed by monochloramine over prolonged time periods. The normalized salt passage in a pilot RO system with monochloramine dosage was constant over a one year period (data of last 130 days presented), demonstrating that no membrane damage occurred. From this study, it can be concluded that monochloramine dosage in wastewater applications is effective in controlling biofouling in RO systems and maintaining a monochloramine residual during water transport provides biologically stable water.

Detection of a westward hotspot offset in the atmosphere of hot gas giant CoRoT-2b

Science.gov (United States)

Dang, Lisa; Cowan, Nicolas B.; Schwartz, Joel C.; Rauscher, Emily; Zhang, Michael; Knutson, Heather A.; Line, Michael; Dobbs-Dixon, Ian; Deming, Drake; Sundararajan, Sudarsan; Fortney, Jonathan J.; Zhao, Ming

2018-03-01

Short-period planets exhibit day-night temperature contrasts of hundreds to thousands of kelvin. They also exhibit eastward hotspot offsets whereby the hottest region on the planet is east of the substellar point1; this has been widely interpreted as advection of heat due to eastward winds2. We present thermal phase observations of the hot Jupiter CoRoT-2b obtained with the Infrared Array Camera (IRAC) on the Spitzer Space Telescope. These measurements show the most robust detection to date of a westward hotspot offset of 23 ± 4°, in contrast with the nine other planets with equivalent measurements3-10. The peculiar infrared flux map of CoRoT-2b may result from westward winds due to non-synchronous rotation11 or magnetic effects12,13, or partial cloud coverage, that obscure the emergent flux from the planet's eastern hemisphere14-17. Non-synchronous rotation and magnetic effects may also explain the planet's anomalously large radius12,18. On the other hand, partial cloud coverage could explain the featureless dayside emission spectrum of the planet19,20. If CoRoT-2b is not tidally locked, then it means that our understanding of star-planet tidal interaction is incomplete. If the westward offset is due to magnetic effects, our result represents an opportunity to study an exoplanet's magnetic field. If it has eastern clouds, then it means that a greater understanding of large-scale circulation on tidally locked planets is required.

HIV protease drug resistance and its impact on inhibitor design.

Science.gov (United States)

Ala, P J; Rodgers, J D; Chang, C H

1999-07-01

The primary cause of resistance to the currently available HIV protease inhibitors is the accumulation of multiple mutations in the viral protease. So far more than 20 substitutions have been observed in the active site, dimer interface, surface loops and flaps of the homodimer. While many mutations reduce the protease's affinity for inhibitors, others appear to enhance its catalytic efficiency. This high degree of genetic flexibility has made the protease an elusive drug target. The design of the next generation of HIV protease inhibitors will be discussed in light of the current structural information.

TU-CD-BRD-00: Incident Learning / RO-ILS

International Nuclear Information System (INIS)

2015-01-01

It has long been standard practice in radiation oncology to report internally when a patient’s treatment has not gone as planned and to report events to regulatory agencies when legally required. Most potential errors are caught early and never affect the patient. Quality assurance steps routinely prevent errors from reaching the patient, and these “near misses” are much more frequent than treatment errors. A growing number of radiation oncology facilities have implemented incident learning systems to report and analyze both errors and near misses. Using the term “incident learning” instead of “event reporting” emphasizes the need to use these experiences to change the practice and make future errors less likely and promote an educational, non-punitive environment. There are challenges in making such a system practical and effective. Speakers from institutions of different sizes and practice environments will share their experiences on how to make such a system work and what benefits their clinics have accrued. Questions that will be addressed include: How to create a system that is easy for front line staff to access How to motivate staff to report How to promote the system as positive and educational and not punitive or demeaning How to organize the team for reviewing and responding to reports How to prioritize which reports to discuss in depth How not to dismiss the rest How to identify underlying causes How to design corrective actions and implement change How to develop useful statistics and analysis tools How to coordinate a departmental system with a larger risk management system How to do this without a dedicated quality manager Some speakers’ experience is with in-house systems and some will share experience with the AAPM/ASTRO national Radiation Oncology Incident Learning System (RO-ILS). Reports intended to be of value nationally need to be comprehensible to outsiders; examples of useful reports will be shown. There will be ample time set

TU-CD-BRD-00: Incident Learning / RO-ILS

Energy Technology Data Exchange (ETDEWEB)

NONE

2015-06-15

It has long been standard practice in radiation oncology to report internally when a patient’s treatment has not gone as planned and to report events to regulatory agencies when legally required. Most potential errors are caught early and never affect the patient. Quality assurance steps routinely prevent errors from reaching the patient, and these “near misses” are much more frequent than treatment errors. A growing number of radiation oncology facilities have implemented incident learning systems to report and analyze both errors and near misses. Using the term “incident learning” instead of “event reporting” emphasizes the need to use these experiences to change the practice and make future errors less likely and promote an educational, non-punitive environment. There are challenges in making such a system practical and effective. Speakers from institutions of different sizes and practice environments will share their experiences on how to make such a system work and what benefits their clinics have accrued. Questions that will be addressed include: How to create a system that is easy for front line staff to access How to motivate staff to report How to promote the system as positive and educational and not punitive or demeaning How to organize the team for reviewing and responding to reports How to prioritize which reports to discuss in depth How not to dismiss the rest How to identify underlying causes How to design corrective actions and implement change How to develop useful statistics and analysis tools How to coordinate a departmental system with a larger risk management system How to do this without a dedicated quality manager Some speakers’ experience is with in-house systems and some will share experience with the AAPM/ASTRO national Radiation Oncology Incident Learning System (RO-ILS). Reports intended to be of value nationally need to be comprehensible to outsiders; examples of useful reports will be shown. There will be ample time set

Zinc oxide nanoparticles as novel alpha-amylase inhibitors

Science.gov (United States)

Dhobale, Sandip; Thite, Trupti; Laware, S. L.; Rode, C. V.; Koppikar, Soumya J.; Ghanekar, Ruchika-Kaul; Kale, S. N.

2008-11-01

Amylase inhibitors, also known as starch blockers, contain substances that prevent dietary starches from being absorbed by the body via inhibiting breakdown of complex sugars to simpler ones. In this sense, these materials are projected as having potential applications in diabetes control. In this context, we report on zinc oxide nanoparticles as possible alpha-amylase inhibitors. Zinc oxide nanoparticles have been synthesized using soft-chemistry approach and 1-thioglycerol was used as a surfactant to yield polycrystalline nanoparticles of size ˜18 nm, stabilized in wurtzite structure. Conjugation study and structural characterization have been done using x-ray diffraction technique, Fourier transform infrared spectroscopy, UV-visible spectroscopy, and transmission electron microscopy. Cytotoxicity studies on human fibrosarcoma (HT-1080) and skin carcinoma (A-431) cell lines as well as mouse primary fibroblast cells demonstrate that up to a dose of 20 μg/ml, ZnO nanoparticles are nontoxic to the cells. We report for the first time the alpha-amylase inhibitory activity of ZnO nanoparticles wherein an optimum dose of 20 μg/ml was sufficient to exhibit 49% glucose inhibition at neutral pH and 35 °C temperature. This inhibitory activity was similar to that obtained with acarbose (a standard alpha-amylase inhibitor), thereby projecting ZnO nanoparticles as novel alpha-amylase inhibitors.

Novel dual small-molecule HIV inhibitors: scaffolds and discovery strategies.

Science.gov (United States)

Song, Anran; Yu, Haiqing; Wang, Changyuan; Zhu, Xingqi; Liu, Kexin; Ma, Xiaodong

2015-01-01

Searching for safe and effective treatments for HIV infection is still a great challenge worldwide in spite of the 27 marketed anti-HIV drugs and the powerful highly active antiretroviral therapy (HAART). As a promising prospect for generation of new HIV therapy drugs, multiple ligands (MDLs) were greatly focused on recently due to their lower toxicity, simplified dosing and patient adherence than single-target drugs. Till now, by disrupting two active sites or steps of HIV replications, a number of HIV dual inhibitors, such as CD4-gssucap120 inhibitors, CXCR4-gp20 inhibitors, RT-CXCR4 inhibitors, RT-protease inhibitors, RT-integrase inhibitors, and RTassociated functions inhibitors have been identified. Generally, these dual inhibitors were discovered mainly through screening approaches and design strategies. Of these compounds, the molecules bearing small skeletons exhibited strong anti-HIV activity and aroused great attention recently. Reviewing the progress of the dual small-molecule HIV inhibitors from the point of view of their scaffolds and discovery strategies will provide valuable information for producing more effective anti-HIV drugs. In this regard, novel dual small-molecule HIV inhibitors were illustrated, and their discovery paradigms as the major contents were also summarized in this manuscript.

General and Modular Strategy for Designing Potent, Selective, and Pharmacologically Compliant Inhibitors of Rhomboid Proteases

Czech Academy of Sciences Publication Activity Database

Tichá, Anežka; Stanchev, Stancho; Vinothkumar, K. R.; Mikles, David C.; Pachl, Petr; Began, Jakub; Škerle, Jan; Švehlová, Kateřina; Nguyen, M. T. N.; Verhelst, S. H. L.; Johnson, D. C.; Bachovchin, D. A.; Lepšík, Martin; Majer, Pavel; Stříšovský, Kvido

2017-01-01

Roč. 24, č. 12 (2017), s. 1523-1536 ISSN 2451-9448 R&D Projects: GA MŠk(CZ) LK11206; GA MŠk LO1302; GA MŠk(CZ) LO1304; GA ČR(CZ) GBP208/12/G016 EU Projects: European Commission(XE) 304154 - Rhomboid substrates Grant - others:EMBO(DE) 2329 Institutional support: RVO:61388963 Keywords : alpha-ketoamide inhibitors * activity-based probes * intramembrane protease Subject RIV: CE - Biochemistry OBOR OECD: Biochemistry and molecular biology http://www.sciencedirect.com/science/article/pii/S2451945617303513?via%3Dihub

Solar fired combined RO/MED desalination plant integrated with electrical power grid

International Nuclear Information System (INIS)

Alrobaei, H.

2006-01-01

Currently, there is a strong demand for efficient seawater desalination plants, which can meet the tougher environment regulation and energy saving requirements. From this standpoint the present work was undertaken to include proposed scheme (solar Fired Combined Reverse Osmosis (ROY Multi-Effect Distillation (MED) Seawater desalination Plant (SCDP) integrated with electrical power grid (EPG)) for repowering and modification of the conventional grid connected RO desalination plants. The model of SCDP during sunny periods may be applied to the following modes operation: *Full solar desalination (i.e. solar thermal and electrical power generation in solar plant is elivered to the desalination process and the surplus electricity is fed into EPG). *Hybrid solar desalination (I.e. a small share of the electrical power consumption for desalination process compensated by EPG). During cloudly periods and at night the SCDP operates as a conventional RO desalination plant. To establish the range, in which solar energy for seawater desalination would be competitive to fossil energy and investigates the potential effect of the proposed scheme on the repowering effectiveness, mathematical model has been developed. The repowered effectiveness, mathematical model has been developed.The repowered effectiveness in optaimizing model was characterized by the condition of attaining maximum fuel saving in the EPG. The study result shows the effectiveness of proposed scheme for modification and repowering the RO plant. For the case study. (SCDP with maual share of solar electrical power generation 67.4%) the economical effect amount 138.9 ton fuel/year for each MW design thermal energy of parabolic solar collectors array and the corresponding decrease in exhaust gases emission (Nitrogen oxides (NO x ) 0.55 ton/year.MW, carbon dioxides (CO2) 434.9 ton/year.MW). Moreover, implementation of combined RO/MED design for repowering and modification of conventional grid connected RO plant will

Effect of histone deacetylase inhibitor, trichostatin A, on cartilage ...

African Journals Online (AJOL)

Purpose: To evaluate the effect of histone deacetylase (HDAC) inhibitor, trichostatin A (TCA), on cartilage regeneration in a rabbit perichondrial graft model. Methods: Perichondrial grafts (20 × 20 mm2) were derived from the ears of New Zealand rabbits and transplanted onto the paravertebral muscle of the face of each ...

The driving mechanism of roAp stars

Energy Technology Data Exchange (ETDEWEB)

Dupret, M-A [Observatoire de Paris, LESIA, CNRS UMR 8109, 5 place J. Janssen, 92195 Meudon (France); Theado, S; Noels, A [Institut d' Astrophysique et Geophysique, Universite de Liege (Belgium)], E-mail: MA.dupret@obspm.fr

2008-10-15

We analyse in detail the driving mechanism of roAp stars and present the theoretical instability strip predicted by our models with solar metallicity. A particular attention is given to the interpretation of the role played by the different eigenfunctions in the stabilization of the modes at the red edge of the instability strip. The gradient of temperature in the H{sub I} opacity bump appears to play a major role in this context. We also consider the particular and complex role played by the shape of the eigenfunctions (location of the nodes, ...)

The driving mechanism of roAp stars

International Nuclear Information System (INIS)

Dupret, M-A; Theado, S; Noels, A

2008-01-01

We analyse in detail the driving mechanism of roAp stars and present the theoretical instability strip predicted by our models with solar metallicity. A particular attention is given to the interpretation of the role played by the different eigenfunctions in the stabilization of the modes at the red edge of the instability strip. The gradient of temperature in the H I opacity bump appears to play a major role in this context. We also consider the particular and complex role played by the shape of the eigenfunctions (location of the nodes, ...).

Dinâmica evolutiva em roças de caboclos amazônicos

Directory of Open Access Journals (Sweden)

Paulo Sodero Martins

2005-04-01

Full Text Available AS ROÇAS DE CABOCLOS são unidades de agricultura de derruba e queima de populações tradicionais nas terras firmes dos trópicos brasileiros, geralmente associados com florestas. Elas são derivadas de sistemas indígenas com algumas modificações introduzidas pelos africanos e portugueses. Neste trabalho, analisamos a estrutura de comunidade dessas roças e o papel dos fatores biológicos e culturais em manter e aumentar a variabilidade genética na mais importante espécie plantada nas roças, a mandioca (Manihot esculenta. Há um alto grau de diversidade nas roças e muitas espécies que estão normalmente presentes, como mandioca, batata-doce, inhame, ariá, araruta, cupá, amendoim, apresentam o que tem sido chamado de habilidade de combinação ecológica, o que significa que elas otimizam o uso dos fatores ambientais e recursos, minimizando a sobreposição de suas arquiteturas. A variabilidade de mandioca é ampliada pelo banco de sementes em ��reas previamente ocupadas, cruzamentos interespecíficos e intervarietais, facilitada pelo arranjo das plantações escolhido pelos caboclos. Depois de criada, a variabilidade é fixada através de clonagem vegetativa, o método de reprodução comum não apenas da mandioca, mas também de outras espécies da roça, a maioria perene e apresentando "disjunção agronômica", ou seja, reprodução e produção efetivada por diferentes órgãos da planta.THE "ROÇAS DE CABOCLOS" are the slash-and-burn agricultural units of traditional populations dwelling in the lowlands of the Brazilian Tropics, generally in association with forests. They are derived from the indigenous system with some modifications introduced by the Africans and Portuguese. In this paper we analyse the community structure of the "roças" and the role of biological and cultural factors in maintaining and augmenting the genetic variability in the most important species planted in roças, the cassava (Manihot esculenta. There

Results of a customer-based, post-market surveillance survey of the HeRO access device.

Science.gov (United States)

Fusselman, Maureen

2010-08-01

In order to supplement post-market surveillance data on the HeRO vascular access device, a non-scientific customer survey was conducted to obtain quantitative data from dialysis providers caring for patients implanted with the device. Dialysis nurses involved in the care of HeRO patients were contacted in order to obtain post-implant device performance information for 10% of patients implanted with the device at the time of the survey. Thirty-eight dialysis units with a total of 65 HeRO patients participated in the survey. The total duration of HeRO device use was 348.4 months with an average use of 5.4 months. Thirty-eight of the 65 HeRO patients (58.5%) were reported to not have experienced any performance issues. There were 28 device performance incidents reported for the remaining 27 patients included in the survey. Occlusion was the single most commonly reported device-related performance issue with 18 patients (27.7%) experiencing 25 occlusive episodes. The majority of the patients who had an occlusion (66.7%) only experienced one occlusive event. Infections occurred in 4 patients (6.2%) with an overall infection rate of 0.38 per 1,000 patient days. Post-market clinical experience during the first 18 months of commercialization of the HeRO device were in line with expectations based on the results from initial clinical studies with the device. Device occlusion remains the most commonly reported performance issue with the reported rate in this survey less than that which was reported in earlier published studies with the device.

Unorthodox Inhibitors of HIV Protease: Looking Beyond Active-site-directed Peptidomimetics

Czech Academy of Sciences Publication Activity Database

Schimer, Jiří; Konvalinka, Jan

2014-01-01

Roč. 20, č. 21 (2014), s. 3389-3397 ISSN 1381-6128 R&D Projects: GA ČR GAP207/11/1798 Institutional support: RVO:61388963 Keywords : proteinase * proteolytic processing * virostatic * rational drug design * resistance development Subject RIV: CE - Biochemistry Impact factor: 3.452, year: 2014

Inhibitory effects of a selective Jak2 inhibitor on adrenocorticotropic hormone production and proliferation of corticotroph tumor AtT20 cells

Directory of Open Access Journals (Sweden)

Asari Y

2017-09-01

Full Text Available Yuko Asari, Kazunori Kageyama, Yuki Nakada, Mizuki Tasso, Shinobu Takayasu, Kanako Niioka, Noriko Ishigame, Makoto Daimon Department of Endocrinology and Metabolism, Graduate School of Medicine, Hirosaki University, Hirosaki, Japan Purpose: The primary cause of Cushing’s disease is adrenocorticotropic hormone (ACTH-producing pituitary adenomas. EGFR signaling induces POMC mRNA-transcript levels and ACTH secretion from corticotroph tumors. The Jak–STAT pathway is located downstream of EGFR signaling; therefore, a Jak2 inhibitor could be an effective therapy for EGFR-related tumors. In this study, we determined the effect of a potent and selective Jak2 inhibitor, SD1029, on ACTH production and proliferation in mouse AtT20 corticotroph tumor cells.Materials and methods: AtT20 pituitary corticotroph tumor cells were cultured after transfection with PTTG1- or GADD45β-specific siRNA. Expression levels of mouse POMC, PTTG1, and GADD45β mRNAs were evaluated using quantitative real-time polymerase chain reaction. ACTH levels were measured using ACTH ELISA. Western blot analysis was performed to examine protein expression of phosphorylated STAT3/STAT3. Viable cells and DNA fragmentation were measured using a cell-proliferation assay and cell-death detection ELISA, respectively. Cellular DNA content was analyzed using fluorescence-activated cell sorting.Results: SD1029 decreased POMC and PTTG1 mRNA and ACTH levels, while increasing GADD45β levels. The drug also decreased AtT20-cell proliferation and induced apoptosis, but did not alter cell-cycle progression. SD1029 also inhibited STAT3 phosphorylation. PTTG1 knockdown inhibited POMC mRNA levels and cell proliferation. However, combined treatment with PTTG1 knockdown and SD1029 had no additive effect on POMC mRNA levels or cell proliferation. GADD45β knockdown inhibited the SD1029-induced decrease in POMC mRNA levels and also partially inhibited the decrease in cell proliferation.Conclusion: Both

Membrane fouling and anti-fouling strategies using RO retentate from a municipal water recycling plant as the feed for osmotic power generation

KAUST Repository

Chen, Si Cong

2015-10-25

RO retentate from a municipal water recycling plant is considered as a potential feed stream for osmotic power generation in this paper. The feasibility of using RO retentate from a municipal water recycling plant was examined from two aspects: (a) the membrane fouling propensity of RO retentate, and (b) the efficacy of anti-fouling strategies. The membranes used in this study were the inner selective thin film composite polyethersulfone (TFC/PES) hollow fiber membranes, which possessed a high water permeability and good mechanical strength. Scaling by phosphate salts was found to be one possible inorganic fouling on the innermost layer of the PES membrane, whereas silica fouling was observed to be the governing fouling on the outmost surface of the PES membrane. Two anti-fouling pretreatments, i.e., pH adjustment and anti-scalant pre-treatment for the feed stream, were studied and found to be straightforward and effective. Using RO retentate at pH 7.2 as the feed and 1 M NaCl as the draw solution, the average power density was 7.3 W/m at 20 bar. The average power density increased to 12.6 W/m by modifying RO retentate with an initial pH value of 5.5 using HCl and to 13.4 W/m by adding 1.1 mM ethylenediaminetetraacetic acid (EDTA). Moreover, the flux recovery of the fouled membranes, without the indicated pretreatments, reached 84.9% using deionized (DI) water flushing and 95.0% using air bubbling under a high crossflow velocity of 23.3 cm/s (Re = 2497) for 30 min. After pretreatment by pH adjustment, the flux recovery increased to 94.6% by DI water flushing and 100.0% by air bubbling. After pretreatment by adding 1.1 mM EDTA into RO retentate, flux was almost fully restored by physical cleaning by DI water flushing and air bubbling. These results provide insight into developing an effective pretreatment by either pH adjustment or EDTA addition before PRO and physical cleaning methods by DI water flushing and air bubbling for membrane used in osmotic power

Membrane fouling and anti-fouling strategies using RO retentate from a municipal water recycling plant as the feed for osmotic power generation

KAUST Repository

Chen, Si Cong; Amy, Gary L.; Chung, Neal Tai-Shung

2015-01-01

RO retentate from a municipal water recycling plant is considered as a potential feed stream for osmotic power generation in this paper. The feasibility of using RO retentate from a municipal water recycling plant was examined from two aspects: (a) the membrane fouling propensity of RO retentate, and (b) the efficacy of anti-fouling strategies. The membranes used in this study were the inner selective thin film composite polyethersulfone (TFC/PES) hollow fiber membranes, which possessed a high water permeability and good mechanical strength. Scaling by phosphate salts was found to be one possible inorganic fouling on the innermost layer of the PES membrane, whereas silica fouling was observed to be the governing fouling on the outmost surface of the PES membrane. Two anti-fouling pretreatments, i.e., pH adjustment and anti-scalant pre-treatment for the feed stream, were studied and found to be straightforward and effective. Using RO retentate at pH 7.2 as the feed and 1 M NaCl as the draw solution, the average power density was 7.3 W/m at 20 bar. The average power density increased to 12.6 W/m by modifying RO retentate with an initial pH value of 5.5 using HCl and to 13.4 W/m by adding 1.1 mM ethylenediaminetetraacetic acid (EDTA). Moreover, the flux recovery of the fouled membranes, without the indicated pretreatments, reached 84.9% using deionized (DI) water flushing and 95.0% using air bubbling under a high crossflow velocity of 23.3 cm/s (Re = 2497) for 30 min. After pretreatment by pH adjustment, the flux recovery increased to 94.6% by DI water flushing and 100.0% by air bubbling. After pretreatment by adding 1.1 mM EDTA into RO retentate, flux was almost fully restored by physical cleaning by DI water flushing and air bubbling. These results provide insight into developing an effective pretreatment by either pH adjustment or EDTA addition before PRO and physical cleaning methods by DI water flushing and air bubbling for membrane used in osmotic power

Membrane fouling and anti-fouling strategies using RO retentate from a municipal water recycling plant as the feed for osmotic power generation.

Science.gov (United States)

Chen, Si Cong; Amy, Gary L; Chung, Tai-Shung

2016-01-01

RO retentate from a municipal water recycling plant is considered as a potential feed stream for osmotic power generation in this paper. The feasibility of using RO retentate from a municipal water recycling plant was examined from two aspects: (a) the membrane fouling propensity of RO retentate, and (b) the efficacy of anti-fouling strategies. The membranes used in this study were the inner selective thin film composite polyethersulfone (TFC/PES) hollow fiber membranes, which possessed a high water permeability and good mechanical strength. Scaling by phosphate salts was found to be one possible inorganic fouling on the innermost layer of the PES membrane, whereas silica fouling was observed to be the governing fouling on the outmost surface of the PES membrane. Two anti-fouling pretreatments, i.e., pH adjustment and anti-scalant pre-treatment for the feed stream, were studied and found to be straightforward and effective. Using RO retentate at pH 7.2 as the feed and 1 M NaCl as the draw solution, the average power density was 7.3 W/m(2) at 20 bar. The average power density increased to 12.6 W/m(2) by modifying RO retentate with an initial pH value of 5.5 using HCl and to 13.4 W/m(2) by adding 1.1 mM ethylenediaminetetraacetic acid (EDTA). Moreover, the flux recovery of the fouled membranes, without the indicated pretreatments, reached 84.9% using deionized (DI) water flushing and 95.0% using air bubbling under a high crossflow velocity of 23.3 cm/s (Re = 2497) for 30 min. After pretreatment by pH adjustment, the flux recovery increased to 94.6% by DI water flushing and 100.0% by air bubbling. After pretreatment by adding 1.1 mM EDTA into RO retentate, flux was almost fully restored by physical cleaning by DI water flushing and air bubbling. These results provide insight into developing an effective pretreatment by either pH adjustment or EDTA addition before PRO and physical cleaning methods by DI water flushing and air bubbling for membrane used in

The inhibitor of cyclin-dependent kinases, olomoucine II, exhibits potent antiviral properties

Czech Academy of Sciences Publication Activity Database

Holčáková, J.; Tomašec, P.; Burget, J. J.; Wang, E. C. Y.; Wilkinson, G. W. G.; Hrstka, R.; Kryštof, Vladimír; Strnad, Miroslav; Vojtešek, B.

2010-01-01

Roč. 20, č. 3 (2010), s. 133-142 ISSN 0956-3202 R&D Projects: GA ČR GA301/08/1649 Institutional research plan: CEZ:AV0Z50380511 Keywords : Cyclin-dependent Kinase * Olomoucine II * vaccinia Subject RIV: EE - Microbiology, Virology

Ab initio density functional theory study of non-polar (10-10), (11-20) and semipolar {20-21} GaN surfaces

Czech Academy of Sciences Publication Activity Database

Mutombo, Pingo; Romanyuk, Olexandr

2014-01-01

Roč. 115, č. 20 (2014), "203508-1"-"203508-5" ISSN 0021-8979 Grant - others:AVČR(CZ) M100101201 Institutional support: RVO:68378271 Keywords : non-polar GaN * semipolar GaN * surface reconstructions * DFT Subject RIV: BM - Solid Matter Physics ; Magnetism Impact factor: 2.183, year: 2014

Effect of inorganic inhibitors on the corrosion behavior of 1018 carbon steel in the LiBr + ethylene glycol + H2O mixture

International Nuclear Information System (INIS)

Samiento-Bustos, E.; Rodriguez, J.G. Gonzalez; Uruchurtu, J.; Dominguez-Patino, G.; Salinas-Bravo, V.M.

2008-01-01

The effect of inorganic inhibitors on the corrosion behavior of 1018 carbon steel in the mixture LiBr (55%) + ethylene glycol + H 2 O at room temperature has been evaluated. Used inhibitors included LiNO 3 (Lithium Nitrate), Li 2 MoO 4 (Lithium Molybdate) and Li 2 CrO 4 (Lithium Chromate) at concentrations of 5, 20 and 50 ppm. Electrochemical techniques included potentiodynamic polarization curves, electrochemical noise resistance (EN) and electrochemical impedance spectroscopy (EIS) measurements. Additionally, adsorption isotherms were calculated. The results obtained showed that both, the corrosion rate and the passive current density decreased with inhibitors, and, in general terms, inhibitors efficiency increased with inhibitor concentration, except in the case of Li 2 CrO 4, where the highest efficiency was obtained with 20 ppm of inhibitor. Pitting potential with 5 ppm of inhibitor, regardless its chemical composition, was more active than in absence of inhibitor, increased at 20 ppm, especially with Li 2 CrO 4 , and remained unaltered with 50 ppm. EN measurements showed that at 5 ppm of inhibitor, the number of film rupture/repassivation events was higher than that obtained at 20 or 50 ppm. Adsorption isotherms suggested a different adsorption mechanism for each inhibitor, whereas EIS results suggested that the corrosion process when nitrates were added was under charge transfer control, but in the case of molybdates or chromates was under diffusion control

Cost analysis of the Hemodialysis Reliable Outflow (HeRO) Graft compared to the tunneled dialysis catheter.

Science.gov (United States)

Al Shakarchi, Julien; Inston, Nicholas; Jones, Robert G; Maclaine, Grant; Hollinworth, David

2016-04-01

In end-stage renal disease patients with central venous obstruction, who have limited vascular access options, the Hemodialysis Reliable Outflow (HeRO) Graft is a new alternative with a lower incidence of complications and longer effective device life compared to tunneled dialysis catheters (TDCs). We undertook an economic analysis of introducing the HeRO Graft in the UK. A 1-year cost-consequence decision analytic model was developed comparing management with the HeRO Graft to TDCs from the perspective of the National Health Service in England. The model comprises four 3-month cycles during which the vascular access option either remains functional for hemodialysis or fails, patients can experience access-related infection and device thrombosis, and they can also accrue associated costs. Clinical input data were sourced from published studies and unit cost data from National Health Service 2014-15 Reference Costs. In the base case, a 100-patient cohort managed with the HeRO Graft experienced 6 fewer failed devices, 53 fewer access-related infections, and 67 fewer device thromboses compared to patients managed with TDCs. Although the initial device and placement costs for the HeRO Graft are greater than those for TDCs, savings from the lower incidence of device complications and longer effective device patency reduces these costs. Overall net annual costs are £2600 for each HeRO Graft-managed patient compared to TDC-managed patients. If the National Health Service were to reimburse hemodialysis at a uniform rate regardless of the type of vascular access, net 1-year savings of £1200 per patient are estimated for individuals managed with the HeRO Graft. The base case results showed a marginal net positive cost associated with vascular access with the HeRO Graft compared with TDCs for the incremental clinical benefit of reductions in patency failures, device-related thrombosis, and access-related infection events in a patient population with limited options for

CCR 20th anniversary commentary: In the beginning, there was PS-341.

Science.gov (United States)

Teicher, Beverly A; Anderson, Kenneth C

2015-03-01

Proteasome inhibitors have a 20-year history in cancer therapy. The first proteasome inhibitor, bortezomib, a breakthrough treatment for multiple myeloma, moved rapidly through development from the bench in 1994 to first FDA approval in 2003. Clinical Cancer Research has chronicled the development of proteasome inhibitors with publication of reports on bortezomib, carfilzomib, and the oral proteasome inhibitor ixazomib (MLN9708). ©2015 American Association for Cancer Research.

Synthesis and Application of Pyrrolidone-containing Shale Inhibitors

Science.gov (United States)

Liu, Yonggui; Hou, Jie; Zhang, Yang; Yan, Jing; Song, Tao; Xu, Yongjun

2018-03-01

New generation polyamine inhibitors are amino-terminated polyethers with excellent inhibiting capabilities; they play a key role in borehole stabilization and reservoir protection. However, polyamine inhibitors are limited by their poor thermal stability, which can be attributed to the presence of ether bonds in their molecular structures. We propose a three-step synthesis approach fora novel pyrrolidone-containing polyamine inhibitor (DYNP) by introducing N-vinyl-2-pyrrolidone (NVP) on divinyloxyethane. This polyamine inhibitor exhibits an optimized molecular structure and has enhanced heat resistance. Characterizations by infrared (IR) spectroscopy and evaluation tests demonstrate several advantages of DYNP inhibitors, including excellent inhibiting capability (superior to similar materials such as polyamines), improved heat resistance (reasonable stability at temperatures up to 240°C), and good compatibility with both fresh water and salt water drilling fluids. These can be attributed to the presence of considerable amounts of amino groups in the repeating unit of DYNP molecules. The DYNP inhibitor was applied in over 20 boreholes in tight oil blocks in Daqing Oilfield to relieve hydration of formations with high shale contents. For instance, drilling in the 2033.5m horizontal section of Dragon 2 borehole was smooth, with a borehole diameter expansion ratio below 10%.

Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring

Czech Academy of Sciences Publication Activity Database

Andrs, M.; Kobarecny, J.; Jun, D.; Hodný, Zdeněk; Bartek, Jiří; Kuca, K.

2015-01-01

Roč. 58, č. 1 (2015), s. 41-71 ISSN 0022-2623 R&D Projects: GA MŠk(CZ) CZ.1.07/2.3.00/30.0044 Grant - others:University Hospital Hradec Kralove(CZ) 00179906; Faculty of Military Health Sciences, University of Defence(CZ) SV/FVZ201402 Institutional support: RVO:68378050 Keywords : DEPENDENT PROTEIN-KINASE * STRAND BREAK REPAIR * SELECTIVE PI3K-BETA INHIBITORS * TELANGIECTASIA MUTATED KINASE Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 5.589, year: 2015

Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

Science.gov (United States)

Hu, Essa; Kunz, Roxanne K; Chen, Ning; Rumfelt, Shannon; Siegmund, Aaron; Andrews, Kristin; Chmait, Samer; Zhao, Sharon; Davis, Carl; Chen, Hang; Lester-Zeiner, Dianna; Ma, Ji; Biorn, Christopher; Shi, Jianxia; Porter, Amy; Treanor, James; Allen, Jennifer R

2013-11-14

Our development of PDE10A inhibitors began with an HTS screening hit (1) that exhibited both high p-glycoprotein (P-gp) efflux ratios in rat and human and poor metabolic stability. On the basis of cocrystal structure of 1 in human PDE10A enzyme, we designed a novel keto-benzimidazole 26 with comparable PDE10A potency devoid of efflux liabilities. On target in vivo coverage of PDE10A in rat brain was assessed using our previously reported LC-MS/MS receptor occupancy (RO) technology. Compound 26 achieved 55% RO of PDE10A at 30 mg/kg po and covered PDE10A receptors in rat brain in a dose-dependent manner. Cocrystal structure of 26 in PDE10A confirmed the binding mode of the novel scaffold. Further optimization resulted in the identification of keto-benzimidazole 34, which showed an increased in vivo efficacy of 57% RO in rats at 10 mg/kg po and an improved in vivo rat clearance and oral bioavailability.

Magna Carta Libertatum – osmisté výročí

Czech Academy of Sciences Publication Activity Database

Blahož, Josef

2015-01-01

Roč. 154, č. 6 (2015), s. 449-464 ISSN 0231-6625 Institutional support: RVO:68378122 Keywords : Magna Carta Libertatum * development of constitutionalism * rule of law Subject RIV: AG - Legal Sciences

An information preserving method for producing full coverage CoRoT light curves

Directory of Open Access Journals (Sweden)

Pascual-Granado J.

2015-01-01

Full Text Available Invalid flux measurements, caused mainly by the South Atlantic Anomaly crossing of the CoRoT satellite, introduce aliases in the periodogram and wrong amplitudes. It has been demonstrated that replacing such invalid data with a linear interpolation is not harmless. On the other side, using power spectrum estimators for unevenly sampled time series is not only less computationally efficient but it leads to difficulties in the interpretation of the results. Therefore, even when the gaps are rather small and the duty cycle is high enough the use of gap-filling methods is a gain in frequency analysis. However, the method must preserve the information contained in the time series. In this work we give a short description of an information preserving method (MIARMA and show some results when applying it to CoRoT seismo light curves. The method is implemented as the second step of a pipeline for CoRoT data analysis.

Hydrogen management in the MiRO refinery

Energy Technology Data Exchange (ETDEWEB)

Neumann, G. [Mineraloelraffinerie Oberrhein GmbH und Co. KG, Karlsruhe (Germany)

2010-12-30

The importance of hydrogen in refineries has increased over the last 20 years as new regulations affecting gasoline and diesel composition have been implemented throughout Europe and in an environment of increasingly stringent clean fuel regulations, decreasing heavy fuel oil demand and increasing heavy more sour crude supply. In Germany, the introduction of sulphur free gasoline and diesel with less than 10ppm sulphur(Auto Oil Program) and light home fuel oil with less than 50ppm this year were the last link in a long chain of environmental regulations, which had a considerable effect on the hydrogen demand in refineries. In the complex MiRO-refinery with a large FCC- and Coker-Unit for atmospheric residue conversion and a total throughput of more than 15 Mio.T/ a and more than 14 Mio.T/a crude oils of different origin from high sulphur, bituminous crudes to medium, low sulphur crudes for calcinate-production from green coke the only source of hydrogen for a long time was catalytic reforming. The only chance of balancing the hydrogen production and consumption was to improve the existing catalytic reforming and the optimisation of hydrogen recovery from waste or purge streams and the hydrogen network of the refinery. In 2007 a new hydrogen plant via steam reforming of natural gas went on stream. The main reason for this step was the shrinking market for gasoline in the last ten years and the blending of bio-ethanol into the gasoline pool, which released reforming capacities and the demand for octane. Another important issue is the production planning taking into account the potentials of hydrogen production via catalytic and steam reforming and the hydrogen consumption via desulphurisation and the saturation of olefins and (poly-)aromatics of the main product streams, gasoline, diesel and light home fuel oil. (orig.)

Chronic ethanol administration increases the binding of 3H Ro-15-4513 in primary cultured spinal cord neurons

International Nuclear Information System (INIS)

Mlatre, M.; Ticku, M.K.

1989-01-01

Ro 15-4513 (ethyl-8-azido-5, 6-dihydro-5-methyl-6-oxo-4H-imidazo [1,5α], [1,4] benzodiazepine-3-carboxylate) is reported to be a selective ethanol antagonist in biochemical and behavioral studies. The effect of chronic ethanol treatment on the binding of [ 3 H]Ro 15-4513 was investigated in cultured spinal cord neurons, which are shown to possess all the elements of GABA benzodiazepine receptor complex. Chronic ethanol treatment (50 mM for 6 hr, 12 hr, 18 hr, 3 days, and 5 3 days) produced an increase in the specific binding of [ 3 H]Ro 15-4513. The increase in binding in these neurons was due to an increase in the number (B max ) of receptor sites. This effect was specific for Ro 15-4513, since identical ethanol treatment did not alter the binding of benzodiazepine antagonist [ 3 H]Ro 15-1788 or agonist [ 3 H]flunitrazepam or inverse agonist [ 3 H]methyl-β-carboline-3-carboxylate. Similar results have been reported following chronic ethanol treatment to rats. These results suggest that the Ro 15-4513 binding sites on the oligomeric GABA receptor complex are altered following chronic ethanol administration, and support the notion of a unique role of Ro 15-4513 as an ethanol antagonist

Reconstruction-of-difference (RoD) imaging for cone-beam CT neuro-angiography

Science.gov (United States)

Wu, P.; Stayman, J. W.; Mow, M.; Zbijewski, W.; Sisniega, A.; Aygun, N.; Stevens, R.; Foos, D.; Wang, X.; Siewerdsen, J. H.

2018-06-01

Timely evaluation of neurovasculature via CT angiography (CTA) is critical to the detection of pathology such as ischemic stroke. Cone-beam CTA (CBCT-A) systems provide potential advantages in the timely use at the point-of-care, although challenges of a relatively slow gantry rotation speed introduce tradeoffs among image quality, data consistency and data sparsity. This work describes and evaluates a new reconstruction-of-difference (RoD) approach that is robust to such challenges. A fast digital simulation framework was developed to test the performance of the RoD over standard reference reconstruction methods such as filtered back-projection (FBP) and penalized likelihood (PL) over a broad range of imaging conditions, grouped into three scenarios to test the trade-off between data consistency, data sparsity and peak contrast. Two experiments were also conducted using a CBCT prototype and an anthropomorphic neurovascular phantom to test the simulation findings in real data. Performance was evaluated primarily in terms of normalized root mean square error (NRMSE) in comparison to truth, with reconstruction parameters chosen to optimize performance in each case to ensure fair comparison. The RoD approach reduced NRMSE in reconstructed images by up to 50%–53% compared to FBP and up to 29%–31% compared to PL for each scenario. Scan protocols well suited to the RoD approach were identified that balance tradeoffs among data consistency, sparsity and peak contrast—for example, a CBCT-A scan with 128 projections acquired in 8.5 s over a 180°  +  fan angle half-scan for a time attenuation curve with ~8.5 s time-to-peak and 600 HU peak contrast. With imaging conditions such as the simulation scenarios of fixed data sparsity (i.e. varying levels of data consistency and peak contrast), the experiments confirmed the reduction of NRMSE by 34% and 17% compared to FBP and PL, respectively. The RoD approach demonstrated superior performance in 3D angiography

Cloning and expression of chicken 20-hydroxysteroid dehydrogenase

Czech Academy of Sciences Publication Activity Database

Bryndová, Jana; Klusoňová, Petra; Kučka, Marek; Vagnerová, Karla; Mikšík, Ivan; Pácha, Jiří

2006-01-01

Roč. 37, č. 3 (2006), s. 453-462 ISSN 0952-5041 R&D Projects: GA AV ČR(CZ) IAA6011201 Grant - others:GA UK(CZ) 216/2004 Institutional research plan: CEZ:AV0Z50110509 Keywords : 20-hydroxysteroid dehydrogenase * SDR family Subject RIV: CE - Biochemistry Impact factor: 2.988, year: 2006

A novel chemo-multienzymatic synthesis of bioactive cyclophellitol and epi-cyclophellitol in both enantiopure forms

Czech Academy of Sciences Publication Activity Database

D'Antona, N.; Morrone, R.; Bovicelli, P.; Gambera, G.; Kubáč, David; Martínková, Ludmila

2010-01-01

Roč. 21, č. 20 (2010), s. 2448-2454 ISSN 0957-4166 R&D Projects: GA MŠk OC09046 Institutional research plan: CEZ:AV0Z50200510 Keywords : BETA-GLUCOSIDASE INHIBITOR * FACILE SYNTHESES * CYCLOPHELLITOL Subject RIV: CC - Organic Chemistry Impact factor: 2.484, year: 2010

The changing phases of extrasolar planet CoRoT-1b.

Science.gov (United States)

Snellen, Ignas A G; de Mooij, Ernst J W; Albrecht, Simon

2009-05-28

Hot Jupiters are a class of extrasolar planet that orbit their parent stars at very short distances. They are expected to be tidally locked, which can lead to a large temperature difference between their daysides and nightsides. Infrared observations of eclipsing systems have yielded dayside temperatures for a number of transiting planets. The day-night contrast of the transiting extrasolar planet HD 189733b was 'mapped' using infrared observations. It is expected that the contrast between the daysides and nightsides of hot Jupiters is much higher at visual wavelengths, shorter than that of the peak emission, and could be further enhanced by reflected stellar light. Here we report the analysis of optical photometric data obtained over 36 planetary orbits of the transiting hot Jupiter CoRoT-1b. The data are consistent with the nightside hemisphere of the planet being entirely black, with the dayside flux dominating the optical phase curve. This means that at optical wavelengths the planet's phase variation is just as we see it for the interior planets in the Solar System. The data allow for only a small fraction of reflected light, corresponding to a geometric albedo of <0.20.

Study of microRNAs (miRNAs) that are predicted to target the autoantigens Ro/SSA and La/SSB in primary Sjögren’s Syndrome

Science.gov (United States)

Gourzi, V C; Kapsogeorgou, E K; Kyriakidis, N C; Tzioufas, A G

2015-01-01

The elevated tissue expression of Ro/SSA and La/SSB autoantigens appears to be crucial for the generation and perpetuation of autoimmune humoral responses against these autoantigens in Sjögren’s syndrome (SS). The mechanisms that govern their expression are not known. miRNAs, the post-transcriptional regulators of gene expression, might be implicated. We have identified previously the miRNAs let7b, miR16, miR181a, miR200b-3p, miR200b-5p, miR223 and miR483-5p that are predicted to target Ro/SSA [Ro52/tripartite motif-containing protein 21 (TRIM21), Ro60/TROVE domain family, member 2 (TROVE2)] and La/SSB mRNAs. To study possible associations with autoantigen mRNA expression and disease features, their expression was investigated in minor salivary gland (MSG) tissues, peripheral blood mononuclear cells (PBMC) and long-term cultured non-neoplastic salivary gland epithelial cells (SGEC) from 29 SS patients (20 of 29 positive for autoantibodies to Ro/SSA and La/SSB) and 24 sicca-complaining controls. The levels of miR16 were up-regulated in MSGs, miR200b-3p in SGECs and miR223 and miR483-5p in PBMCs of SS patients compared to sicca-complaining controls. The MSG levels of let7b, miR16, miR181a, miR223 and miR483-5p were correlated positively with Ro52/TRIM21-mRNA. miR181a and miR200b-3p were correlated negatively with Ro52/TRIM21 and Ro60/TROVE2 mRNAs in SGECs, respectively, whereas let7b, miR200b-5p and miR223 associated with La/SSB-mRNA. In PBMCs, let7b, miR16, miR181a and miR483-5p were correlated with Ro52/TRIM21, whereas let7b, miR16 and miR181a were also associated with La/SSB-mRNA expression. Significantly lower miR200b-5p levels were expressed in SS patients with mucosa-associated lymphoid tissue (MALT) lymphoma compared to those without. Our findings indicate that miR16, miR200b-3p, miR223 and miR483-5p are deregulated in SS, but the exact role of this deregulation in disease pathogenesis and autoantigen expression needs to be elucidated. PMID:26201309

A comparison of effects of DPP-4 inhibitor and SGLT2 inhibitor on lipid profile in patients with type 2 diabetes.

Science.gov (United States)

Cha, Seon-Ah; Park, Yong-Moon; Yun, Jae-Seung; Lim, Tae-Seok; Song, Ki-Ho; Yoo, Ki-Dong; Ahn, Yu-Bae; Ko, Seung-Hyun

2017-04-13

Previous studies suggest that dipeptidyl peptidase-4 (DPP-4) inhibitors and sodium glucose cotransporter 2 (SGLT2) inhibitors have different effects on the lipid profile in patients with type 2 diabetes. We investigated the effects of DPP-4 inhibitors and SGLT2 inhibitors on the lipid profile in patients with type 2 diabetes. From January 2013 to December 2015, a total of 228 patients with type 2 diabetes who were receiving a DPP-4 inhibitor or SGLT2 inhibitor as add-on therapy to metformin and/or a sulfonylurea were consecutively enrolled. We compared the effects of DPP-4 inhibitors and SGLT2 inhibitors on the lipid profile at baseline and after 24 weeks of treatment. To compare lipid parameters between the two groups, we used the analysis of covariance (ANCOVA). A total of 184 patients completed follow-up (mean age: 53.1 ± 6.9 years, mean duration of diabetes: 7.1 ± 5.7 years). From baseline to 24 weeks, HDL-cholesterol (HDL-C) levels were increased by 0.5 (95% CI, -0.9 to 2.0) mg/dl with a DPP-4 inhibitor and by 5.1 (95% CI, 3.0 to 7.1) mg/dl with an SGLT2 inhibitor (p = 0.001). LDL-cholesterol (LDL-C) levels were reduced by 8.4 (95% CI, -14.0 to -2.8) mg/dl with a DPP-4 inhibitor, but increased by 1.3 (95% CI, -5.1 to 7.6) mg/dl with an SGLT2 inhibitor (p = 0.046). There was no significant difference in the mean hemoglobin A1c (8.3 ± 1.1 vs. 8.0 ± 0.9%, p = 0.110) and in the change of total cholesterol (TC) (p = 0.836), triglyceride (TG) (p = 0.867), apolipoprotein A (p = 0.726), apolipoprotein B (p = 0.660), and lipoprotein (a) (p = 0.991) between the DPP-4 inhibitor and the SGLT2 inhibitor. The SGLT2 inhibitor was associated with a significant increase in HDL-C and LDL-C after 24 weeks of SGLT2 inhibitor treatment in patients with type 2 diabetes compared with those with DPP-4 inhibitor treatment in this study. This study was conducted by retrospective medical record review.

Inhibitor-decorated Polymer Conjugates Targeting Fibroblast Activation Protein

Czech Academy of Sciences Publication Activity Database

Dvořáková, Petra; Bušek, P.; Knedlík, Tomáš; Schimer, Jiří; Etrych, Tomáš; Kostka, Libor; Stollinová Šromová, L.; Šubr, Vladimír; Šácha, Pavel; Šedo, A.; Konvalinka, Jan

2017-01-01

Roč. 60, č. 20 (2017), s. 8385-8393 ISSN 0022-2623 R&D Projects: GA MZd(CZ) NV15-31379A; GA MŠk(CZ) LM2015064; GA MŠk LO1302 Institutional support: RVO:61388963 ; RVO:61389013 Keywords : dipeptidyl peptidase IV * metastatic colorectal cancer * integral membrane protease Subject RIV: CE - Biochemistry; CD - Macromolecular Chemistry (UMCH-V) OBOR OECD: Biochemistry and molecular biology; Polymer science (UMCH-V) Impact factor: 6.259, year: 2016

Plantio direto de alface americana sobre plantas de cobertura dessecadas ou roçadas

Directory of Open Access Journals (Sweden)

Andréia Cristina Silva Hirata

2014-06-01

Full Text Available O objetivo deste trabalho foi avaliar o plantio direto de alface americana no verão sobre plantas de cobertura dessecadas ou roçadas em cultivos sucessivos. O trabalho foi desenvolvido no município de Álvares Machado, São Paulo, Brasil. O delineamento experimental foi em blocos ao acaso, dispostos em parcelas subdivididas, com quatro repetições. O fator da parcela principal foram dois manejos das plantas de cobertura (dessecadas com herbicida ou roçadas e as subparcelas, seis espécies de plantas de cobertura (Cajanus cajan cv. IAPAR 43, Crotalaria spectabilis, Crotalaria juncea, Mucuna pruriens, Pennisetum glaucum e vegetação natural, além da testemunha sem plantas de cobertura. O manejo roçado apresentou desempenho inferior no primeiro cultivo da alface, todavia não diferiu do manejo químico no segundo cultivo. A cobertura do solo com mucuna apresentou maior produtividade da alface no primeiro cultivo devido ao excesso de palha das demais coberturas, o qual prejudicou o estabelecimento da alface. No segundo cultivo não houve diferenças entre as coberturas. A roçagem de plantas de cobertura é uma opção viável para plantio direto de alface sem herbicidas.

5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases

Czech Academy of Sciences Publication Activity Database

Vymětalová, Ladislava; Havlíček, Libor; Šturc, Antonín; Skrášková, Zuzana; Jorda, Radek; Pospíšil, Tomáš; Strnad, Miroslav; Kryštof, Vladimír

2016-01-01

Roč. 110, MAR 3 (2016), s. 291-301 ISSN 0223-5234 R&D Projects: GA MŠk(CZ) LO1204; GA ČR(CZ) GA15-15264S Institutional support: RVO:61389030 Keywords : Cyclin-dependent kinase * Inhibitor * Selectivity Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 4.519, year: 2016

Hemodialysis Reliable Outflow (HeRO) device in end-stage dialysis access: a decision analysis model.

Science.gov (United States)

Dageforde, Leigh Anne; Bream, Peter R; Moore, Derek E

2012-09-01

The Hemodialysis Reliable Outflow (HeRO) dialysis access device is a permanent tunneled dialysis graft connected to a central venous catheter and is used in patients with end-stage dialysis access (ESDA) issues secondary to central venous stenosis. The safety and effectiveness of the HeRO device has previously been proven, but no study thus far has compared the cost of its use with tunneled dialysis catheters (TDCs) and thigh grafts in patients with ESDA. A decision analytic model was developed to simulate outcomes for patients with ESDA undergoing placement of a HeRO dialysis access device, TDC, or thigh graft. Outcomes of interest were infection, thrombosis, and ischemic events. Baseline values, ranges, and costs were determined from a systematic review of the literature. Total costs were based on 1 year of post-procedure outcomes. Sensitivity analyses were conducted to test model strength. The HeRO dialysis access device is the least costly dialysis access with an average 1-year cost of $6521. The 1-year cost for a TDC was $8477. A thigh graft accounted for $9567 in a 1-year time period. The HeRO dialysis access device is the least costly method of ESDA. The primary determinants of cost in this model are infection in TDCs and leg ischemia necessitating amputation in thigh grafts. Further study is necessary to incorporate patient preference and quality of life into the model. Copyright © 2012 Elsevier Inc. All rights reserved.

The Roles of Tidal Evolution and Evaporative Mass Loss in the Origin of CoRoT-7 b

Science.gov (United States)

Jackson, Brian; Miller, Neil; Barnes, Rory; Raymond, Sean N.; Fortney, Jonathan J.; Greenberg, Richard

2010-01-01

CoRoT-7 b is the first confirmed rocky exoplanet, but, with an orbital semimajor axis of 0.0172 au, its origins may be unlike any rocky planet in our Solar System. In this study, we consider the roles of tidal evolution and evaporative mass loss in CoRoT-7 b's history, which together have modified the planet's mass and orbit. If CoRoT-7 b has always been a rocky body, evaporation may have driven off almost half its original mass, but the mass loss may depend sensitively on the extent of tidal decay of its orbit. As tides caused CoRoT-7 b's orbit to decay, they brought the planet closer to its host star, thereby enhancing the mass loss rate. Such a large mass loss also suggests the possibility that CoRoT-7 b began as a gas giant planet and had its original atmosphere completely evaporated. In this case, we find that CoRoT-7 b's original mass probably did not exceed 200 Earth masses (about two-third of a Jupiter mass). Tides raised on the host star by the planet may have significantly reduced the orbital semimajor axis, perhaps causing the planet to migrate through mean-motion resonances with the other planet in the system, CoRoT-7 c. The coupling between tidal evolution and mass loss may be important not only for CoRoT-7 b but also for other close-in exoplanets, and future studies of mass loss and orbital evolution may provide insight into the origin and fate of close-in planets, both rocky and gaseous.

Immune response against the coiled coil domain of Sjögren's syndrome associated autoantigen Ro52 induces salivary gland dysfunction.

Science.gov (United States)

Sroka, Magdalena; Bagavant, Harini; Biswas, Indranil; Ballard, Abigail; Deshmukh, Umesh S

2018-01-31

The structural domains of Ro52, termed the RING, B-box, coiled coil (CC) and B30.2/SPRY are targets of anti-Ro52 in multiple autoimmune disorders. In Sjögren's syndrome patients, the presence of anti-Ro52 is associated with higher disease severity, and in mice, they induce salivary gland hypofunction. This study was undertaken to investigate whether immune responses against different domains of Ro52, influences salivary gland disease in mice. Female NZM2758 mice were immunised with Ro52 domains expressed as recombinant fusion proteins with maltose binding protein (MBP) [MBP-RING-B-box, MBP-CC, MBP-CC(ΔC19), MBP-B30.2/SPRY]. Sera from immunised mice were studied for IgG antibodies to Ro52 by immunoprecipitation, and to salivary gland cells by immunofluorescence. Pilocarpine-induced saliva production was measured to evaluate salivary gland function. Submandibular glands were investigated by histopathology for inflammation and by immune-histochemistry for IgG deposition. Mice immunised with different Ro52-domains had comparable reactivity to Ro52 and to salivary gland cells. However, only mice immunised with the CC domain and its C-terminal truncated version CC(ΔC19) showed a significant drop in saliva production. None of the mice developed severe salivary gland inflammation. The salivary gland hypofunction significantly correlated with increased intra-lobar IgG deposits in the submandibular salivary glands. Our data demonstrate that epitope specificity of anti-Ro52 antibodies plays a critical role in the induction of glandular dysfunction. Clearly, screening Sjögren's syndrome patients for relative levels of Ro52 domain specific antibodies will be more informative for associating anti-Ro52 with clinical measures of the disorder.

Recent Advances in the Development of Mammalian Geranylgeranyl Diphosphate Synthase Inhibitors

Directory of Open Access Journals (Sweden)

Staci L. Haney

2017-05-01

Full Text Available The enzyme geranylgeranyl diphosphate synthase (GGDPS catalyzes the synthesis of the 20-carbon isoprenoid geranylgeranyl diphosphate (GGPP. GGPP is the isoprenoid donor for protein geranylgeranylation reactions catalyzed by the enzymes geranylgeranyl transferase (GGTase I and II. Inhibitors of GGDPS result in diminution of protein geranylgeranylation through depletion of cellular GGPP levels, and there has been interest in GGDPS inhibitors as potential anti-cancer agents. Here we discuss recent advances in the development of GGDPS inhibitors, including insights gained by structure-function relationships, and review the preclinical data that support the continued development of this novel class of drugs.

E. S. R. study of free radicals formed in the irradiated DNA-Ro 7-0582 complex

Energy Technology Data Exchange (ETDEWEB)

Washino, K; Kuwabara, M; Yoshii, G [Hokkaido Univ., Sapporo (Japan)

1979-01-01

The effect of Ro 7-0582 (1-(2-hydroxy-3-methoxypropyl)-2-nitro-imidazole) on the formation of free radicals in ..gamma..-irradiated dry DNA has been investigated. Dry samples of DNA-Ro 7-0582 and DNA nucleotide-Ro 7-0582 were prepared, and e.s.r. spectra observed at 77 K immediately after gamma-irradiation. The samples were then warmed to 297 K for 30 min, and the spectra again observed at 77 K. The sensitizer brought about an increase of 30 to 40% in radical formation in DNA. The results indicated that Ro 7-0582 acts as an efficient electron scavenger on the TMP and dAMP moieties, increasing the incidence of sugar damage. Since TMP and dAMP form a complementary pair in the DNA double helix, the increase in double strand breaks induced by electron-affinic compounds seems to be responsible for the molecular mechanism of radiosensitization in living cells.

Effect of inorganic inhibitors on the corrosion behavior of 1018 carbon steel in the LiBr + ethylene glycol + H{sub 2}O mixture

Energy Technology Data Exchange (ETDEWEB)

Samiento-Bustos, E. [Centro de Investigacion en Ingenieria y Ciencias Aplicadas, Universidad Autonoma del Estado de Morelos. Av. Universidad 1001, Col. Chamilpa, CP 62210, Cuernavaca, Morelos (Mexico); Rodriguez, J.G. Gonzalez [Centro de Investigacion en Ingenieria y Ciencias Aplicadas, Universidad Autonoma del Estado de Morelos. Av. Universidad 1001, Col. Chamilpa, CP 62210, Cuernavaca, Morelos (Mexico)], E-mail: ggonzalez@uaem.mx; Uruchurtu, J. [Centro de Investigacion en Ingenieria y Ciencias Aplicadas, Universidad Autonoma del Estado de Morelos. Av. Universidad 1001, Col. Chamilpa, CP 62210, Cuernavaca, Morelos (Mexico); Dominguez-Patino, G. [Centro de Investigacion en Ingenieria y Ciencias Aplicadas, Universidad Autonoma del Estado de Morelos. Av. Universidad 1001, Col. Chamilpa, CP 62210, Cuernavaca, Morelos (Mexico); U.A.E.M. Facultad de Ciencias Quimicas e Ingenieria, Av. Universidad 1001, 62209, Cuernavaca, Morelos (Mexico); Salinas-Bravo, V.M. [Instituto de Investigaciones Electricas, Gerencia de Materiales y Proceso Quimicos, Av. Reforma 113, Col. Palmira, CP 62490, Cuernavaca, Morelos (Mexico)

2008-08-15

The effect of inorganic inhibitors on the corrosion behavior of 1018 carbon steel in the mixture LiBr (55%) + ethylene glycol + H{sub 2}O at room temperature has been evaluated. Used inhibitors included LiNO{sub 3} (Lithium Nitrate), Li{sub 2}MoO{sub 4} (Lithium Molybdate) and Li{sub 2}CrO{sub 4} (Lithium Chromate) at concentrations of 5, 20 and 50 ppm. Electrochemical techniques included potentiodynamic polarization curves, electrochemical noise resistance (EN) and electrochemical impedance spectroscopy (EIS) measurements. Additionally, adsorption isotherms were calculated. The results obtained showed that both, the corrosion rate and the passive current density decreased with inhibitors, and, in general terms, inhibitors efficiency increased with inhibitor concentration, except in the case of Li{sub 2}CrO{sub 4,} where the highest efficiency was obtained with 20 ppm of inhibitor. Pitting potential with 5 ppm of inhibitor, regardless its chemical composition, was more active than in absence of inhibitor, increased at 20 ppm, especially with Li{sub 2}CrO{sub 4}, and remained unaltered with 50 ppm. EN measurements showed that at 5 ppm of inhibitor, the number of film rupture/repassivation events was higher than that obtained at 20 or 50 ppm. Adsorption isotherms suggested a different adsorption mechanism for each inhibitor, whereas EIS results suggested that the corrosion process when nitrates were added was under charge transfer control, but in the case of molybdates or chromates was under diffusion control.

MicroRNA let-7 modulates the immune response to Mycobacterium tuberculosis infection via control of A20, an inhibitor of the NF-κB pathway.

Science.gov (United States)

Kumar, Manish; Sahu, Sanjaya Kumar; Kumar, Ranjeet; Subuddhi, Arijita; Maji, Ranjan Kumar; Jana, Kuladip; Gupta, Pushpa; Raffetseder, Johanna; Lerm, Maria; Ghosh, Zhumur; van Loo, Geert; Beyaert, Rudi; Gupta, Umesh D; Kundu, Manikuntala; Basu, Joyoti

2015-03-11

The outcome of the interaction between Mycobacterium tuberculosis (Mtb) and a macrophage depends on the interplay between host defense and bacterial immune subversion mechanisms. MicroRNAs critically regulate several host defense mechanisms, but their role in the Mtb-macrophage interplay remains unclear. MicroRNA profiling of Mtb-infected macrophages revealed the downregulation of miR-let-7f in a manner dependent on the Mtb secreted effector ESAT-6. We establish that let-7f targets A20, a feedback inhibitor of the NF-κB pathway. Expression of let-7f decreases and A20 increases with progression of Mtb infection in mice. Mtb survival is attenuated in A20-deficient macrophages, and the production of TNF, IL-1β, and nitrite, which are mediators of immunity to Mtb, is correspondingly increased. Further, let-7f overexpression diminishes Mtb survival and augments the production of cytokines including TNF and IL-1β. These results uncover a role for let-7f and its target A20 in regulating immune responses to Mtb and controlling bacterial burden. Copyright © 2015 Elsevier Inc. All rights reserved.

Ro og klasseledelse i folkeskolen

DEFF Research Database (Denmark)

Søndergaard, Dorte Marie; Plauborg, Helle; Szulevicz, Thomas

Rapporten giver på baggrund af eksisterende forskning og viden om klasseledelse anbefalinger til, hvordan klasseledelse kan udvikles og undervisningsforstyrrende uro mindskes. https://www.uvm.dk/~/media/UVM/Filer/Udd/Folke/PDF14/Aug/140813%20UVM%20Klasseledelse%20rapport.pdf......Rapporten giver på baggrund af eksisterende forskning og viden om klasseledelse anbefalinger til, hvordan klasseledelse kan udvikles og undervisningsforstyrrende uro mindskes. https://www.uvm.dk/~/media/UVM/Filer/Udd/Folke/PDF14/Aug/140813%20UVM%20Klasseledelse%20rapport.pdf...

The effects of GLP-1 analogues, DPP-4 inhibitors and SGLT2 inhibitors on the renal system.

Science.gov (United States)

Schernthaner, Guntram; Mogensen, Carl Erik; Schernthaner, Gerit-Holger

2014-09-01

Diabetic nephropathy (DN) affects an estimated 20%-40% of patients with type 2 diabetes mellitus (T2DM). Key modifiable risk factors for DN are albuminuria, anaemia, dyslipidaemia, hyperglycaemia and hypertension, together with lifestyle factors, such as smoking and obesity. Early detection and treatment of these risk factors can prevent DN or slow its progression, and may even induce remission in some patients. DN is generally preceded by albuminuria, which frequently remains elevated despite treatment in patients with T2DM. Optimal treatment and prevention of DN may require an early, intensive, multifactorial approach, tailored to simultaneously target all modifiable risk factors. Regular monitoring of renal function, including urinary albumin excretion, creatinine clearance and glomerular filtration rate, is critical for following any disease progression and making treatment adjustments. Dipeptidyl peptidase (DPP)-4 inhibitors and sodium-glucose cotransporter 2 (SGLT2) inhibitors lower blood glucose levels without additional risk of hypoglycaemia, and may also reduce albuminuria. Further investigation of the potential renal benefits of DPP-4 and SGLT2 inhibitors is underway. © The Author(s) 2014.

Vasodilatory effect of the stable vasoactive intestinal peptide analog RO 25-1553 in murine and rat lungs.

Directory of Open Access Journals (Sweden)

Jun Yin

Full Text Available Stable analogs of vasoactive intestinal peptide (VIP have been proposed as novel line of therapy in chronic obstructive pulmonary disease (COPD based on their bronchodilatory and anti-inflammatory effects. We speculated that VIP analogs may provide additional benefits in that they exert vasodilatory properties in the lung, and tested this hypothesis in both ex vivo and in vivo models.In isolated perfused mouse lungs and in an in vivo rat model, pulmonary blood vessels were preconstricted by hypoxia and hemodynamic changes in response to systemic (ex vivo or inhaled (in vivo administration of the cyclic VIP analog RO 25-1553 were determined.In mouse lungs, RO 25-1553 reduced intrinsic vascular resistance at normoxia, and attenuated the increase in pulmonary artery pressure in response to acute hypoxia. Consistently, inhalation of RO 25-1553 (1 mg · mL(-1 for 3 min caused an extensive and sustained (> 60 min inhibition of the pulmonary arterial pressure increase in response to hypoxia in vivo that was comparable to the effects of inhaled sildenafil. This effect was not attributable to systemic cardiovascular effects of RO 25-1553, but to a lung specific reduction in pulmonary vascular resistance, while cardiac output and systemic arterial hemodynamics remained unaffected. No adverse effects of RO 25-1553 inhalation on pulmonary gas exchange, ventilation-perfusion matching, or lung fluid content were detected.Our findings demonstrate that inhaled delivery of the stable VIP analog RO 25-1553 induces a potent and sustained vasodilatory effect in the pulmonary circulation with no detectable adverse effects. Therapeutic inhalation of RO 25-1553 may provide vascular benefits in addition to its reported anti-inflammatory and bronchodilatory effects in COPD, yet caution is warranted given the overall poor results of vasodilator therapies for pulmonary hypertension secondary to COPD in a series of recent clinical trials.

What CoRoT tells us about δ Scuti stars

Directory of Open Access Journals (Sweden)

Michel Eric

2017-01-01

Full Text Available Inspired by the so appealing example of red giants, where going from a handful of stars to thousands revealed the structure of the eigenspectrum, we inspected a large homogeneous set of around 1860 δ Scuti stars observed with CoRoT. This unique data set reveals a common regular pattern which appears to be in agreement with island modes featured by theoretical non-perturbative treatments of fast rotation. The comparison of these data with models and linear stability calculations suggests that spectra can be fruitfully characterized to first order by a few parameters which might play the role of seismic indices for δ Scuti stars, as Δv and vmax do for red giants. The existence of this pattern offers an observational support for guiding further theoretical works on fast rotation. It also provides a framework for further investigation of the observational material collected by CoRoT ([1] and Kepler ([2]. Finally, it sketches out the perspective of using δ Scuti stars pulsations for ensemble asteroseismology

Stimulation of topoisomerase II mediated DNA cleavage at specific sequence elements by the 2-nitroimidazole Ro 15-0216

International Nuclear Information System (INIS)

Sorensen, B.S.; Jensen, P.S.; Andersen, A.H.; Christiansen, K.; Alsner, J.; Thomsen, B.; Westergaard, O.

1990-01-01

The effect of the 2-nitroimidazole Ro 15-0216 upon the interaction between purified topoisomerase II and its DNA substrate was investigated. The cleavage reaction in the presence of this DNA-nonintercalative drug took place with the hallmarks of a regular topoisomerase II mediated cleavage reaction, including covalent linkage of the enzyme to the cleaved DNA. In the presence of Ro 15-0216, topoisomerase II mediated cleavage was extensively stimulated at major cleavage sites of which only one existed in the 4363 base pair pBR322 molecule. The sites stimulated by Ro 15-0216 shared a pronounced sequence homology, indicating that a specific nucleotide sequence is crucial for the action of this drug. The effect of Ro 15-0216 thus differs from that of the clinically important topoisomerase II targeted agents such as mAMSA, VM26, and VP16, which enhance enzyme-mediated cleavage at a multiple number of sites. In contrast to the previous described drugs, Ro 15-0216 did not exert any inhibitory effect on the enzyme's catalytic activity. This observation might be ascribed to the low stability of the cleavage complexes formed in the presence of Ro 15-0216 as compared to the stability of the ones formed in the presence of traditional topoisomerase II targeted drugs

Use of p38 MAPK Inhibitors for the Treatment of Werner Syndrome

Directory of Open Access Journals (Sweden)

Mark C. Bagley

2010-06-01

Full Text Available Werner syndrome provides a convincing model for aspects of the normal ageing phenotype and may provide a suitable model for therapeutic interventions designed to combat the ageing process. Cultured primary fibroblast cells from Werner syndrome patients provide a powerful model system to study the link between replicative senescence in vitro and in vivo pathophysiology. Genome instability, together with an increased pro-oxidant state, and frequent replication fork stalling, all provide plausible triggers for intracellular stress in Werner syndrome cells, and implicates p38 MAPK signaling in their shortened replicative lifespan. A number of different p38 MAPK inhibitor chemotypes have been prepared rapidly and efficiently using microwave heating techniques for biological study in Werner syndrome cells, including SB203580, VX-745, RO3201195, UR-13756 and BIRB 796, and their selectivity and potency evaluated in this cellular context. Werner syndrome fibroblasts treated with a p38 MAPK inhibitor reveal an unexpected reversal of the accelerated ageing phenotype. Thus the study of p38 inhibition and its effect upon Werner pathophysiology is likely to provide new revelations into the biological mechanisms operating in cellular senescence and human ageing in the future.

Development of silica RO membranes

International Nuclear Information System (INIS)

Ikeda, Ayumi; Kawamoto, Takashi; Matsuyama, Emi; Utsumi, Keisuke; Nomura, Mikihiro; Sugimoto, Masaki; Yoshikawa, Masato

2012-01-01

Silica based membranes have been developed by using a counter diffusion CVD method. Effects of alkyl groups in the silica precursors and deposition temperatures had investigated in order to control pore sizes of the silica membranes. In this study, this type of a silica membrane was applied for RO separation. Effects of silica sources, deposition temperatures and post treatments had been investigated. Tetramethoxysilane (TMOS), Ethyltrimethoxysilane (ETMOS) and Phenyltrimethoxysilane (PhTMOS) were used as silica precursors. A counter diffusion CVD method was carried out for 90 min at 270 - 600degC on γ-alumina capillary substrates (effective length: 50 mm, φ: 4 nm: NOK Co.). O 3 or O 2 was introduced into the inside of the substrate at the O 2 rate of 0.2 L min -1 . Ion beam irradiation was carried out for a post treatment using Os at 490 MeV for 1.0 x 10 10 ions cm -2 or 3.0 x 10 10 ions cm -2 . Single gas permeance was measured by using H 2 , N 2 and SF 6 . RO tests were employed at 3.0 or 5.4 MPa for 100 mg L -1 of feed NaCl solution. First, effects of the silica sources were investigated. The total fluxes increased by increasing N 2 permeance through the silica membrane deposited by ETMOS. The maximum NaCl rejection was 28.2% at 12.2 kg m -2 h -1 of the total flux through the membrane deposited at 270degC. N 2 permeance was 9.6 x 10 -9 mol m -2 s -1 Pa -1 . While, total fluxes through the membrane deposited by using PhTMOS were smaller than those through the ETMOS membranes. The phenyl groups for the PhTMOS membrane must be important for the hydrophobic properties through the membrane. Next, effects of ion beam irradiation were tested for the TMOS membranes. Water is difficult to permeate through the TMOS membranes due to the low N 2 permeance through the membrane (3.1 x 10 -11 mol m -2 s -1 Pa -1 ). N 2 permeance increased to 7.3 x 10 -9 mol m -2 s -1 Pa -1 by the irradiation. Irradiation amounts had little effects on N 2 permeance. However, NaCl rejections

Synthesis of poly[N-(2-hydroxypropyl)methacrylamide] conjugates of inhibitors of the ABC transporter that overcome multidrug resistance in doxorubicin-resistant P388 cells in vitro

Czech Academy of Sciences Publication Activity Database

Šubr, Vladimír; Sivák, Ladislav; Koziolová, Eva; Braunová, Alena; Pechar, Michal; Strohalm, Jiří; Kabešová, Martina; Říhová, Blanka; Ulbrich, Karel; Kovář, Marek

2014-01-01

Roč. 15, č. 8 (2014), s. 3030-3043 ISSN 1525-7797 R&D Projects: GA ČR GAP301/12/1254; GA MŠk(CZ) ED1.1.00/02.0109 Institutional support: RVO:61389013 ; RVO:61388971 Keywords : N-(2-hydroxypropyl)methacrylamide copolymers * multidrug resistance * P-glycoprotein inhibitors Subject RIV: CD - Macromolecular Chemistry; FD - Oncology ; Hematology (MBU-M) Impact factor: 5.750, year: 2014

NOVÉ NA STARÉ – Brno, nároží Bratislavská - Stará

OpenAIRE

Červinková, Kateřina

2014-01-01

Řešené území se nachází v městské části Brno-střed, na nárožní poloze ulic Bratislavská a Stará. Je tvořeno několika parcelami, které jsou v současné době nezastaveny, nebo se na nich nachází stavby dočasného charakteru. Část vymezeného území dnes slouží jako parkoviště Policie České republiky. Od historického centra ji dělí dopravní - malý městský okruh vedoucí ulicí Koliště. V blízkosti řešeného území jsou městské domy většinou s obchodním parterem, postavené v rozmezí konce 19. - 1.pol. 20...

Inhibitors

Science.gov (United States)

... JM, and the Hemophilia Inhibitor Research Study Investigators. Validation of Nijmegen-Bethesda assay modifications to allow inhibitor ... webinars on blood disorders Language: English (US) Español (Spanish) File Formats Help: How do I view different ...

Efficiently Combining Water Reuse and Desalination through Forward Osmosis-Reverse Osmosis (FO-RO) Hybrids: A Critical Review.

Science.gov (United States)

Blandin, Gaetan; Verliefde, Arne R D; Comas, Joaquim; Rodriguez-Roda, Ignasi; Le-Clech, Pierre

2016-07-01

Forward osmosis (FO) is a promising membrane technology to combine seawater desalination and water reuse. More specifically, in a FO-reverse osmosis (RO) hybrid process, high quality water recovered from the wastewater stream is used to dilute seawater before RO treatment. As such, lower desalination energy needs and/or water augmentation can be obtained while delivering safe water for direct potable reuse thanks to the double dense membrane barrier protection. Typically, FO-RO hybrid can be a credible alternative to new desalination facilities or to implementation of stand-alone water reuse schemes. However, apart from the societal (public perception of water reuse for potable application) and water management challenges (proximity of wastewater and desalination plants), FO-RO hybrid has to overcome technical limitation such as low FO permeation flux to become economically attractive. Recent developments (i.e., improved FO membranes, use of pressure assisted osmosis, PAO) demonstrated significant improvement in water flux. However, flux improvement is associated with drawbacks, such as increased fouling behaviour, lower rejection of trace organic compounds (TrOCs) in PAO operation, and limitation in FO membrane mechanical resistance, which need to be better considered. To support successful implementation of FO-RO hybrid in the industry, further work is required regarding up-scaling to apprehend full-scale challenges in term of mass transfer limitation, pressure drop, fouling and cleaning strategies on a module scale. In addition, refined economics assessment is expected to integrate fouling and other maintenance costs/savings of the FO/PAO-RO hybrid systems, as well as cost savings from any treatment step avoided in the water recycling.

Immune checkpoint inhibitors for metastatic bladder cancer.

Science.gov (United States)

Massari, Francesco; Di Nunno, Vincenzo; Cubelli, Marta; Santoni, Matteo; Fiorentino, Michelangelo; Montironi, Rodolfo; Cheng, Liang; Lopez-Beltran, Anto; Battelli, Nicola; Ardizzoni, Andrea

2018-03-01

Chemotherapy has represented the standard therapy for unresectable or metastatic urothelial carcinoma for more than 20 years. The growing knowledge of the interaction between tumour and immune system has led to the advent of new classes of drugs, the immune-checkpoints inhibitors, which are intended to change the current scenario. To date, immunotherapy is able to improve the overall responses and survival. Moreover, thanks to its safety profile immune-checkpoint inhibitors could be proposed also to patients unfit for standard chemotherapy. No doubts that these agents have started a revolution expected for years, but despite this encouraging results it appears clear that not all subjects respond to these agents and requiring the development of reliable predictive response factors able to isolate patients who can more benefit from these treatments as well as new strategies aimed to improve immunotherapy clinical outcome. In this review we describe the active or ongoing clinical trials involving Programmed Death Ligand 1 (PD-L1), Programmed Death receptor 1 (PD-1) and Cytotoxic-T Lymphocyte Antigen 4 (CTLA 4) inhibitors in urothelial carcinoma focusing our attention on the developing new immune-agents and combination strategies with immune-checkpoint inhibitors. Copyright © 2017 Elsevier Ltd. All rights reserved.

The effect of MEP pathway and other inhibitors on the intracellular localization of a plasma membrane-targeted, isoprenylable GFP reporter protein in tobacco BY-2 cells

Science.gov (United States)

Bach, Thomas J

2013-01-01

We have established an in vivo visualization system for the geranylgeranylation of proteins in a stably transformed tobacco BY-2 cell line, based on the expression of a dexamethasone-inducible GFP fused to the carboxy-terminal basic domain of the rice calmodulin CaM61, which naturally bears a CaaL geranylgeranylation motif (GFP-BD-CVIL). By using pathway-specific inhibitors it was demonstrated that inhibition of the methylerythritol phosphate (MEP) pathway with known inhibitors like oxoclomazone and fosmidomycin, as well as inhibition of the protein geranylgeranyltransferase type 1 (PGGT-1), shifted the localization of the GFP-BD-CVIL protein from the membrane to the nucleus. In contrast, the inhibition of the mevalonate (MVA) pathway with mevinolin did not affect the localization. During the present work, this test system has been used to examine the effect of newly designed inhibitors of the MEP pathway and inhibitors of sterol biosynthesis such as squalestatin, terbinafine and Ro48-8071. In addition, we also studied the impact of different post-prenylation inhibitors or those suspected to affect the transport of proteins to the plasma membrane on the localization of the geranylgeranylable fusion protein GFP-BD-CVIL. PMID:24555083

Pengaruh Kepuasan Dan Kepercayaan Terhadap Keputusan Pembelian Ulang Pada Depot Air Minum Tris Water Reverse Osmosis System (Ro)

OpenAIRE

Fitria, Ika

2011-01-01

Kind of this survey is asociative survey which watch influence of customer satisfaction and trust to re-purchase decision on Depot Air Minum Tris Water Reverse Osmosis System (RO) and test of hypothesis use Multiple Linear Regression Analysist on α=5%. This survey used SPSS 16.00 version for windows. Research population is consumers of Depot Air Minum Tris Water Reverse Osmosis System (RO). Sample was used in this survey from customers of Depot Air Minum Tris Water Reverse Osmosis System (RO)...

The autoantigen Ro52 is an E3 ligase resident in the cytoplasm but enters the nucleus upon cellular exposure to nitric oxide

International Nuclear Information System (INIS)

Espinosa, Alexander; Oke, Vilija; Elfving, Ase; Nyberg, Filippa; Covacu, Ruxandra; Wahren-Herlenius, Marie

2008-01-01

Patients with the systemic autoimmune diseases Sjoegrens's syndrome and systemic lupus erythematosus often have autoantibodies against the intracellular protein Ro52. Ro52 is an E3 ligase dependent on the ubiquitin conjugation enzymes UBE2D1 and UBE2E1. While Ro52 and UBE2D1 are cytoplasmic proteins, UBE2E1 is localized to the nucleus. Here, we investigate how domains of human Ro52 regulate its intracellular localization. By expressing fluorescently labeled Ro52 and Ro52 mutants in HeLa cells, an intact coiled-coil domain was found to be necessary for the cytoplasmic localization of Ro52. The amino acids 381-470 of the B30.2 region were essential for translocation into the nucleus. Furthermore, after exposure of HeLa cells to the inflammatory mediator nitric oxide (NO), Ro52 translocated to the nucleus. A nuclear localization of Ro52 in inflamed tissue expressing inducible NO synthetase (iNOS) from cutaneous lupus patients was observed by immunohistochemistry and verified in NO-treated cultures of patient-derived primary keratinocytes. Our results show that the localization of Ro52 is regulated by endogenous sequences, and that nuclear translocation is induced by an inflammatory mediator. This suggests that Ro52 has both cytoplasmic and nuclear substrates, and that Ro52 mediates ubiquitination through UBE2D1 in the cytoplasm and through UBE2E1 in the nucleus

Identification by shape-based virtual screening and evaluation of new tyrosinase inhibitors

Directory of Open Access Journals (Sweden)

Qi Li

2018-01-01

Full Text Available Targeting tyrosinase is considered to be an effective way to control the production of melanin. Tyrosinase inhibitor is anticipated to provide new therapy to prevent skin pigmentation, melanoma and neurodegenerative diseases. Herein, we report our results in identifying new tyrosinase inhibitors. The shape-based virtual screening was performed to discover new tyrosinase inhibitors. Thirteen potential hits derived from virtual screening were tested by biological determinations. Compound 5186-0429 exhibited the most potent inhibitory activity. It dose-dependently inhibited the activity of tyrosinase, with the IC50 values 6.2 ± 2.0 µM and 10.3 ± 5.4 µM on tyrosine and L-Dopa formation, respectively. The kinetic study of 5186-0429 demonstrated that this compound acted as a competitive inhibitor. We believe the discoveries here could serve as a good starting point for further design of potent tyrosinase inhibitor.

Cocteau au cirque: The Poetics of Parade and "Le Numéro Barbette"

Directory of Open Access Journals (Sweden)

Jennifer Forrest

2003-01-01

Full Text Available Parade (1917 was a joint effort production with libretto by Jean Cocteau music by Erik Satie, decor, costumes, and curtain by Pablo Picasso, and choreography by Léonide Massine. It was not only Cocteau's first truly original work, but, as Pierre Gobin contends, Parade is central to an understanding of the structures that would inform all of his subsequent work. Equally central, proposes Lydia Crowson, is Cocteau's July 1926 Nouvelle Revue Française article on "Le Numéro Barbette." The essay on the transvestite striptease trapezist Barbette offers a poetics of the theater that will have changed little by the time of his last play, L'Impromptu du Palais Royal . The underlying system structuring the Coctelian poetics perceived by Gobin and Crowson is perhaps neither in Parade nor in "Le Numéro Barbette" alone, but in both as they propose a poetics of Coctelian art as illusion, and reference and actualize the semantic register of a particular signifying system: not the fairground parade , as contends Gobin and other critics, but the circus and circus culture. But while Parade and "Le Numéro Barbette" share a circus-related theme, the circus does not function merely as a metaphor. Each work in a different way appropriates and promotes rather the circus's revolutionary orientation toward space, its creation of "real" time, and its undermining of social signifying systems, in particular those pertaining to race and gender. The circus space is like that of dreams in that it permits the irresolution and co-existence of the sort of contradictions cited by Guillaume Apollinaire in the celebrated program notes for Parade , and produced by Barbette in his aerial number. This he learned from the circus. Parade and "Le Numéro Barbette" are indeed pivotal texts in the formulation of Cocteau's very twentieth-century poétique .

Efficiently Combining Water Reuse and Desalination through Forward Osmosis—Reverse Osmosis (FO-RO Hybrids: A Critical Review

Directory of Open Access Journals (Sweden)

Gaetan Blandin

2016-07-01

Full Text Available Forward osmosis (FO is a promising membrane technology to combine seawater desalination and water reuse. More specifically, in a FO-reverse osmosis (RO hybrid process, high quality water recovered from the wastewater stream is used to dilute seawater before RO treatment. As such, lower desalination energy needs and/or water augmentation can be obtained while delivering safe water for direct potable reuse thanks to the double dense membrane barrier protection. Typically, FO-RO hybrid can be a credible alternative to new desalination facilities or to implementation of stand-alone water reuse schemes. However, apart from the societal (public perception of water reuse for potable application and water management challenges (proximity of wastewater and desalination plants, FO-RO hybrid has to overcome technical limitation such as low FO permeation flux to become economically attractive. Recent developments (i.e., improved FO membranes, use of pressure assisted osmosis, PAO demonstrated significant improvement in water flux. However, flux improvement is associated with drawbacks, such as increased fouling behaviour, lower rejection of trace organic compounds (TrOCs in PAO operation, and limitation in FO membrane mechanical resistance, which need to be better considered. To support successful implementation of FO-RO hybrid in the industry, further work is required regarding up-scaling to apprehend full-scale challenges in term of mass transfer limitation, pressure drop, fouling and cleaning strategies on a module scale. In addition, refined economics assessment is expected to integrate fouling and other maintenance costs/savings of the FO/PAO-RO hybrid systems, as well as cost savings from any treatment step avoided in the water recycling.

Efficiently Combining Water Reuse and Desalination through Forward Osmosis—Reverse Osmosis (FO-RO) Hybrids: A Critical Review

Science.gov (United States)

Blandin, Gaetan; Verliefde, Arne R.D.; Comas, Joaquim; Rodriguez-Roda, Ignasi; Le-Clech, Pierre

2016-01-01

Forward osmosis (FO) is a promising membrane technology to combine seawater desalination and water reuse. More specifically, in a FO-reverse osmosis (RO) hybrid process, high quality water recovered from the wastewater stream is used to dilute seawater before RO treatment. As such, lower desalination energy needs and/or water augmentation can be obtained while delivering safe water for direct potable reuse thanks to the double dense membrane barrier protection. Typically, FO-RO hybrid can be a credible alternative to new desalination facilities or to implementation of stand-alone water reuse schemes. However, apart from the societal (public perception of water reuse for potable application) and water management challenges (proximity of wastewater and desalination plants), FO-RO hybrid has to overcome technical limitation such as low FO permeation flux to become economically attractive. Recent developments (i.e., improved FO membranes, use of pressure assisted osmosis, PAO) demonstrated significant improvement in water flux. However, flux improvement is associated with drawbacks, such as increased fouling behaviour, lower rejection of trace organic compounds (TrOCs) in PAO operation, and limitation in FO membrane mechanical resistance, which need to be better considered. To support successful implementation of FO-RO hybrid in the industry, further work is required regarding up-scaling to apprehend full-scale challenges in term of mass transfer limitation, pressure drop, fouling and cleaning strategies on a module scale. In addition, refined economics assessment is expected to integrate fouling and other maintenance costs/savings of the FO/PAO-RO hybrid systems, as well as cost savings from any treatment step avoided in the water recycling. PMID:27376337

Removing Fe, Zn and Mn from steel making plant wastewater using RO and NF membranes

Directory of Open Access Journals (Sweden)

Seyed Ahmad Mirbagheri

2016-12-01

Full Text Available Background and purpose: Excessive amount of heavy metals in industrial wastewater is a seriously crucial issue and requires efficient methods to be introduced and dealt with. Meanwhile, steel making plants as productive units in every country release large amounts of fluid into surface and underground sources. Typically, this wastewater contains heavy metals in minor amounts, while this amount could cause severe damages to the living organisms. Materials and methods: In this study, removing iron, manganese, zinc and total dissolved solid in a typical wastewater resulted from steel making plant was considered using reverse osmosis (RO and nanofiltration (NF membranes. At first, different pH values and operating pressures were applied to the wastewater. Then, these parameters were evaluated for a wastewater only containing iron to compare the interaction of other elements in iron removal. Results: The results indicated that RO and NF membranes could successfully treat industrial wastewater containing several heavy metals with high concentrations of Fe, Zn and Mn, especially at optimum pH and pressure. Moreover, the interaction of other heavy metals and components in the influent decreased the efficiency of RO but improved the NF efficiency to remove iron. To have a better image, a formula was proposed for each method to represent the influence of the parameters on removal rates. Finally, cost estimation for both procedures showed that RO was not economically-technically efficient in comparison with NF. Conclusion: NF showed an acceptable performance with high water flow which made it more suitable for industries. At the end, the relative cost analysis showed that even if the initial price of NF is high, the energy consumption and total cost of RO will be higher.

26 CFR 1.72-4 - Exclusion ratio.

Science.gov (United States)

2010-04-01

... balance of $250.80 ($1,200 less $949.20) is the amount to be included in gross income. If A instead..., whichever is the later; and (iv) In the case of an employee who has retired from work because of personal... applicable multiple (whether for a term certain, life, or lives) which would otherwise be used in determining...

Alterations in in-vivo benzodiazepine-receptor binding of C-11-Ro15-1788 (flumazepil)

International Nuclear Information System (INIS)

Yamasaki, T.; Inoue, O.; Shinoto, H.; Ito, T.; Hashimoto, K.; Suzuki, K.; Tateno, Y.

1985-01-01

Alterations of the central benzodiazepine - receptor function caused by the change of physiological or psychological conditions, were recognized in both animal and human studies. Before the human study, animal experiments using tritiated Ro15-1788 were carried out. The stress was produced by forcing the mice to swim in a water-basin at 16 0 C for 5 min. Within 3 min after the forced swimming, the tracer was injected. Brain radioactivities in stress-loaded mice increased over a period of 15 min after the intra-venous injection of tracers, while brain activities of carrier-added tracer decreased. In human study, approximately 5 mCi of C-11-Ro15-1788, which specific activity is 0.3-1.0 Ci/μmol, were intravenously injected to each case. Measurements of the brain activity were performed using positron-CT, with blood sample collection. 31 human studies were performed on. Cerebral cortex time activity curves in several volunteers in nervous and stressful state, showed the same pattern to that in the stress-loaded animal experiment. It is important that the significant different time course of cerebral activity after the injection of labelled Ro15-1788, was observed in stressful state, compared with control, in both human and animal study. From these results, it will be concluded the positron CT study using /sup 11/C-Ro15-1788 will become a new technic to detect the change of psychological conditions in human brain and to diagnose some kind of neuropsychiatric disease

Solvents in membrane synthesis and their effect on NF/RO performance: from conventional organic solvents to ionic liquids:Solventen in membraansynthese en hun effect op NF/RO performantie: van conventionele organische solventen naar ionische vloeistoffen

OpenAIRE

Mariën, Hanne

2017-01-01

Membrane technology has grown significantly over the last decades and is used in a broad range of applications nowadays. Nanofiltration (NF) and reverse osmosis (RO) are applied for the separation of low molecular weight components (< 1000 Da) and salts from the feed stream. The main part of the commercial NF and RO membranes are either integrally skinned asymmetric (ISA) or interfacially polymerized thin film composite (TFC) membranes. Polyamide (PA) TFC membranes are the standard in aqueous...

A MCDM Analysis of the Roşia Montană Gold Mining Project

Directory of Open Access Journals (Sweden)

Adriana Mihai

2015-06-01

Full Text Available The need and estimated utility for a structured analysis of the Roşia Montană gold exploitation project have been palpable in the Romanian public sphere during the last 15 years and there is a vast amount of conflicting information and opinions on the benefits and risks involved. This article provides a comprehensive decision analysis of the Roşia Montană project. Over 100 documents from the past years have been gathered regarding the Roşia Montană mining project, which cover the main official, formal and less formal documents covering the case and produced by a wide range of stakeholders. These were then analyzed while designing a multi-criteria tree including the relevant perspectives under which the most commonly discussed four alternatives were analyzed. The result of this can be translated into a valuable recommendation for the mining company and for the political decision-makers. If these stakeholders want the continuation of the project and its acceptance by civil society, the key challenge is to increase the transparency of the process and improve the credibility and legal aspects; if these aspects cannot be met, the decision-makers need to pay attention to the alternatives available for a sustainable development in the area.

60 kD Ro and nRNP A frequently initiate human lupus autoimmunity.

Directory of Open Access Journals (Sweden)

Latisha D Heinlen

2010-03-01

Full Text Available Systemic lupus erythematosus (SLE is a clinically heterogeneous, humoral autoimmune disorder. The unifying feature among SLE patients is the production of large quantities of autoantibodies. Serum samples from 129 patients collected before the onset of SLE and while in the United States military were evaluated for early pre-clinical serologic events. The first available positive serum sample frequently already contained multiple autoantibody specificities (65%. However, in 34 SLE patients the earliest pre-clinical serum sample positive for any detectable common autoantibody bound only a single autoantigen, most commonly 60 kD Ro (29%, nRNP A (24%, anti-phospholipids (18% or rheumatoid factor (15%. We identified several recurrent patterns of autoantibody onset using these pre-diagnostic samples. In the serum samples available, anti-nRNP A appeared before or simultaneously with anti-nRNP 70 K in 96% of the patients who had both autoantibodies at diagnosis. Anti-60 kD Ro antibodies appeared before or simultaneously with anti-La (98% or anti-52 kD Ro (95%. The autoantibody response in SLE patients begins simply, often binding a single specific autoantigen years before disease onset, followed by epitope spreading to additional autoantigenic specificities that are accrued in recurring patterns.

MO-AB-204-00: Interoperability in Radiation Oncology: IHE-RO Committee Update

Energy Technology Data Exchange (ETDEWEB)

NONE

2016-06-15

You’ve experienced the frustration: vendor A’s device claims to work with vendor B’s device, but the practice doesn’t match the promise. Getting devices working together is the hidden art that Radiology and Radiation Oncology staff have to master. To assist with that difficult process, the Integrating the Healthcare Enterprise (IHE) effort was established in 1998, with the coordination of the Radiological Society of North America. Integrating the Healthcare Enterprise (IHE) is a consortium of healthcare professionals and industry partners focused on improving the way computer systems interconnect and exchange information. This is done by coordinating the use of published standards like DICOM and HL7. Several clinical and operational IHE domains exist in the healthcare arena, including Radiology and Radiation Oncology. The ASTRO-sponsored IHE Radiation Oncology (IHE-RO) domain focuses on radiation oncology specific information exchange. This session will explore the IHE Radiology and IHE RO process for; IHE solicitation process for new profiles. Improving the way computer systems interconnect and exchange information in the healthcare enterprise Supporting interconnectivity descriptions and proof of adherence by vendors Testing and assuring the vendor solutions to connectivity problems. Including IHE profiles in RFPs for future software and hardware purchases. Learning Objectives: Understand IHE role in improving interoperability in health care. Understand process of profile development and implantation. Understand how vendors prove adherence to IHE RO profiles. S. Hadley, ASTRO Supported Activity.

MO-AB-204-00: Interoperability in Radiation Oncology: IHE-RO Committee Update

International Nuclear Information System (INIS)

2016-01-01

You’ve experienced the frustration: vendor A’s device claims to work with vendor B’s device, but the practice doesn’t match the promise. Getting devices working together is the hidden art that Radiology and Radiation Oncology staff have to master. To assist with that difficult process, the Integrating the Healthcare Enterprise (IHE) effort was established in 1998, with the coordination of the Radiological Society of North America. Integrating the Healthcare Enterprise (IHE) is a consortium of healthcare professionals and industry partners focused on improving the way computer systems interconnect and exchange information. This is done by coordinating the use of published standards like DICOM and HL7. Several clinical and operational IHE domains exist in the healthcare arena, including Radiology and Radiation Oncology. The ASTRO-sponsored IHE Radiation Oncology (IHE-RO) domain focuses on radiation oncology specific information exchange. This session will explore the IHE Radiology and IHE RO process for; IHE solicitation process for new profiles. Improving the way computer systems interconnect and exchange information in the healthcare enterprise Supporting interconnectivity descriptions and proof of adherence by vendors Testing and assuring the vendor solutions to connectivity problems. Including IHE profiles in RFPs for future software and hardware purchases. Learning Objectives: Understand IHE role in improving interoperability in health care. Understand process of profile development and implantation. Understand how vendors prove adherence to IHE RO profiles. S. Hadley, ASTRO Supported Activity

Self protection from anti-viral responses--Ro52 promotes degradation of the transcription factor IRF7 downstream of the viral Toll-Like receptors.

LENUS (Irish Health Repository)

Higgs, Rowan

2010-01-01

Ro52 is a member of the TRIM family of single-protein E3 ligases and is also a target for autoantibody production in systemic lupus erythematosus and Sjögren\\'s syndrome. We previously demonstrated a novel function of Ro52 in the ubiquitination and proteasomal degradation of IRF3 following TLR3\\/4 stimulation. We now present evidence that Ro52 has a similar role in regulating the stability and activity of IRF7. Endogenous immunoprecipitation of Ro52-bound proteins revealed that IRF7 associates with Ro52, an effect which increases following TLR7 and TLR9 stimulation, suggesting that Ro52 interacts with IRF7 post-pathogen recognition. Furthermore, we show that Ro52 ubiquitinates IRF7 in a dose-dependent manner, resulting in a decrease in total IRF7 expression and a subsequent decrease in IFN-alpha production. IRF7 stability was increased in bone marrow-derived macrophages from Ro52-deficient mice stimulated with imiquimod or CpG-B, consistent with a role for Ro52 in the negative regulation of IRF7 signalling. Taken together, these results suggest that Ro52-mediated ubiquitination promotes the degradation of IRF7 following TLR7 and TLR9 stimulation. As Ro52 is known to be IFN-inducible, this system constitutes a negative-feedback loop that acts to protect the host from the prolonged activation of the immune response.

Effect of protease inhibitors on thermal gelation of squid (Illex argentinus. mantle paste

Directory of Open Access Journals (Sweden)

Maria Elida Paredi

2014-04-01

Full Text Available The characteristics of the thermal gelation of squid mantle paste and the effect of protease inhibitors on them were investigated. Pastes in the absence and presence the protease inhibitors, ethylendiaminetetracetic acid (EDTA and phenylmethylsulfonyl fluoride (PMSF, were formulated. Pastes were made by the respective one or two step thermal treatments: direct heating at 85°C for 20 min and preincubation at 27 or 40 °C for 3 or 2 hours, followed by heating at 85 °C for 20 min. The gel strength, water holding capacity (WHC and whiteness of gelled pastes were analyzed. The tricloroacetic acid (TCA soluble peptides in homogenate of the muscle were determined. Gel strength decreased when heating was made in two steps. EDTA and PMSF were effective in avoiding that decrease when pre-incubation was made at 40 °C. Maximum gel strength was observed for the gels in presence of EDTA, giving values of 255 and 219 g x cm for the samples made by direct heating and pre-incubated at 40 °C  respectively. TCA soluble peptides increased between 20 and 60 °C, with maximum values reached at 30 and 60 °C. No significant differences (p>0.05 were observed in gel whiteness, neither with the thermal treatment nor with the inhibitors. The WHC was higher (p<0.05 in the gelated paste formulated with EDTA. These results show a good gelation capacity of I argentinus pastes and improvements with protease inhibitors. 

[The life of Dr. RO Kishun, a reflection of modern Korean medical history of the borders].

Science.gov (United States)

Shin, Young-Jeon; Park, Se-Hong

2009-06-01

RO Kishun was born on February 2, 1893 in Ongjin County, Hwanghae Province of Joseon Korea. He graduated from the Medical Training Center, a campus associated with the Joseon Government-General Hospital, in 1915, and from Kyushu Imperial University School of Medicine in 1917. He continued his medical study at the university in 1929, majoring in biochemistry, and earned a doctorate in medicine in 1932. Dr. RO, one of the earliest pioneers in Korean biochemistry, was active in his research, publishing four studies in the Japanese Journal of Biochemistry between 1931 and 1932. After returning from Japan in 1932, Dr. RO opened a medical practice in Mokpo and Busan, port cities situated on the southern tip of Korea. Later in 1936, he moved north to Manchuria (northeast China) to practice medicine at the International Hospital in Mukden (present-day Shenyang). He also served as president of Tumen Public Hospital between 1942 and 1946. When Japan signed unconditional surrender bringing World War II to an end, Dr. RO relocated to Yanbian and began providing medical training to ethnic Koreans. In October 1946, he was appointed dean of the First Branch School of China Medical University in Longjing, and in October 1948 the first dean of Yanbian Medical School, the predecessor of Yanbian University College of Medicine. Dr. RO dedicated his life to medical practice, teaching and training students, and mentoring younger faculty. A brilliant clinician, he also inspired and helped his colleagues with his outstanding ability to diagnose and treat patients. He was one of the founding members of Yanbian University College of Medicine. RO Kishun died on June 7, 1957 at age 64. Ethnic Koreans hailed him as Sinui (literally, the physician of God), and a bronze statue of himself was erected in front of the medical college in 1988. Dr. RO's life brings modern historians' attention to the issue of determining geographical territories and nationality, in that his life unfolded at the

A floating desalination/co-generation system using the KLT-40 reactor and Canadian RO desalination technology

International Nuclear Information System (INIS)

Humphries, J.R.; Davies, K.

2000-01-01

As the global consumption of water increases with growing populations and rising levels of industrialization, major new sources of potable water production must be developed. To address this issue efficiently and economically, a new approach has been developed in Canada for the integration of reverse osmosis (RO) desalination systems with nuclear reactors as an energy source. The resulting nuclear desalination/cogeneration plant makes use of waste heat from the electrical generation process to preheat the RO feedwater, advanced feedwater pre-treatment and sophisticated system design integration and optimization techniques. These innovations have led to improved water production efficiency, lower water production costs and reduced environmental impact. The Russian Federation is developing the KLT-40 reactor for application as a Floating Power Unit (FPU). The reactor is ideally suited for such purposes, having bad many years of successful operation as a marine propulsion reactor aboard floating nuclear powered icebreakers and other nuclear propelled vessels. Under the terms of a cooperation agreement with the Russian Federation Ministry of Atomic Energy, CANDESAL Enterprises Ltd has evaluated the FPU, containing two KLT-40 reactors, as a source of electrical energy and waste heat for RO desalination. A design concept for a floating nuclear desalination complex consisting of the FPU and a barge mounted RO desalination unit has been analyzed to establish preliminary performance characteristics for the complex. The FPU, operating as a barge mounted electrical generating station, provides electricity to the desalination barge. In addition, the condenser cooling water from the FPU is used as a source of preheated feedwater for the RO system on the desalination barge. The waste heat produced by the electrical generating process is sufficient to provide RO feedwater at a temperature of about 10 deg. C above ambient seawater temperature. Preliminary design studies have

The effect of nonsteroidal anti-inflammatory drugs ibuprofen, flurbiprofen, and diclofenac on in vitro and in vivo growth of mouse fibrosarcoma

Czech Academy of Sciences Publication Activity Database

Hoferová, Zuzana; Fedoročko, P.; Hofmanová, Jiřina; Hofer, Michal; Znojil, V.; Minksová, Kateřina; Souček, Karel; Egyed, A.; Kozubík, Alois

2002-01-01

Roč. 20, č. 4 (2002), s. 490-498 ISSN 0735-7907 R&D Projects: GA AV ČR IBS5004009 Grant - others:VEGA MŠ SR(SK) 1/6026/99 Institutional research plan: CEZ:AV0Z5004920 Keywords : cyclooxygenase (COX) inhibitors * fibrosarcoma cells Subject RIV: BO - Biophysics Impact factor: 1.850, year: 2002

Purification, partial characterization, and immunological relationships of multiple low molecular weight protease inhibitors of soybean

Energy Technology Data Exchange (ETDEWEB)

Hwang, D L.R.; Lin, K T.D.; Yang, W K; Foard, D E

1977-01-01

Five protease inhibitors, I-V, in the molecular weight range 7000-8000 were purified from Tracy soybeans by ammonium sulfate precipitation, gel filtration on Sephadex G-100 and G-75, and column chromatography on DEAE-cellulose. In common with previously described trypsin inhibitors from legumes, I-V have a high content of half-cystine and lack tryptophan. By contrast with other legume inhibitors, inhibitor II contains 3 methionine residues. Isoelectric points range from 6.2 to 4.2 in order from inhibitor I to V. Molar ratios (inhibitor/enzyme) for 50% trypsin inhibition are I = 4.76, II = 1.32, III = 3.22, IV = 2.17, V = 0.97. Only V inhibits chymotrypsin significantly (molar ratio = 1.33 for 50% inhibition). The sequence of the first 16 N-terminal amino acid residues of inhibitor V is identical to that of the Bowman-Birk inhibitor; all other observations also indicate that inhibitor V and Bowman-Birk are identical. The first 20 N-terminal amino acid residues of inhibitor II show high homology to those of Bowman-Birk inhibitor, differing by 1 deletion and 5 substitutions. Immunological tests show that inhibitors I through IV are fully cross-reactive with each other but are distinct from inhibitor V.

Numerical simulation of turbulent flows past the RoBin helicopter with a four-bladed rotor

Energy Technology Data Exchange (ETDEWEB)

Xu, H.; Mamou, M.; Khalid, M. [National Research Council, Inst. for Aerospace Research, Ottawa, Ontario (Canada)]. E-mail: Hongyi.Xu@nrc.ca

2003-07-01

The current paper presents a turbulent flow simulation study past a generic helicopter RoBin with a four-bladed rotor using the Chimera moving grid approach. The aerodynamic performance of the rotor blades and their interactions with the RoBin fuselage are investigated using the k - {omega} SST turbulence model contained in the WIND code. The rotor is configured as a Chimera moving grid in a quasisteady flow field. The rotor blades are rectangular, untapered, linearly twisted and are made from NACA 0012 airfoil profile. The blade motion (rotation and cyclic pitching) schedule is specified in the NASA wind tunnel testing of a generic helicopter RoBin. The aerodynamic radial load distributions in the rotor plane are generated by integrating the pressure on each blade surfaces along the blade chordwise direction. The rotor flow interacts strongly with the flow coming off from the fuselage and thus has a significant impact on helicopter aerodynamic performance. (author)

Study on treating of low-level radioactive reactor wastewater by combined membrane process (UF-RO)

International Nuclear Information System (INIS)

Lu Yunyun; Cao Qiru; Chen Yunming; Huang Lijuan; Bai Xiaofeng; Li Bing; Feng Liang

2013-01-01

According to the characteristics of radionuclide exists in the low-level radioactive reactor waste water from HFETR, we use a new combined membrane process separation technology to study the efficient treating of low-lever radioactive reactor wastewater. First, the prepared the simulated wastewater contained Cs + , Sr 2+ , CO 2+ , Ni 2+ , and Fe 3+ . Then, we sequentially investigated the pressure, ion concentration, pH value and EDTA, which have effects on the desalination rate of membrane processing metal ions in wastewater. The results show that: in the condition of pH = 7, and added 0.15 mol/L EDTA, the simulated wastewater separated by UF-RO, desalination rates of Cs + , Sr 2+ , CO 2+ , Ni 2+ and Fe 3+ are all above 95%; In the subsequent trials, adding 0.15 mol/L EDTA into the radioactive residuary solution, and then treating by UF-RO-RO, the decontamination efficiency can reach 95.7%. (authors)

Binding of antibodies to the extractable nuclear antigens SS-A/Ro and SS-B/La is induced on the surface of human keratinocytes by ultraviolet light (UVL): Implications for the pathogenesis of photosensitive cutaneous lupus

International Nuclear Information System (INIS)

Furukawa, F.; Kashihara-Sawami, M.; Lyons, M.B.; Norris, D.A.

1990-01-01

Autoantibodies to the non-histone nucleoprotein antigens SS-A/Ro, SS-B/La, and RNP are highly associated with photosensitive cutaneous lupus erythematosus (LE). In order to better understand the potential mechanisms of ultraviolet (UV) light on photosensitivity in patients with cutaneous LE, we designed immunopathologic in vitro and in vivo experiments to evaluate the effects of UV on the binding of such autoantibodies to the surface of human keratinocytes, one major target of immunologic damage in photosensitive LE. Short-term 2% paraformaldehyde fixation of suspensions of cultured human keratinocytes previously incubated with monospecific antiserum probes enabled the detection of ENA expression on the cell surface by flow-cytometry analysis. UVB light (280-320 nm) induced the binding of monospecific antibody probes for SS-A/Ro and SS-B/La on keratinocytes in a dose-dependent pattern with maximal induction observed at the dose of 200 mJ/cm2 UVB. Binding of SS-A/Ro, SS-B/La, and RNP antibody was augmented strongly, but binding of anti-Sm was very weak. In contrast, UVA (320-400 nm) light had no effect on the induction of binding of these antibody probes. Identical results were seen by standard immunofluorescence techniques. Hydroxyurea-treated keratinocytes showed similar induction of those antigens by UVB irradiation, which suggested that ENA expression on cultured keratinocytes by UVB were cell-cycle independent. Tunicamycin, an inhibitor of glycosylation of proteins, reduced UVB light effect on the SS-A/Ro and SS-B/La antigen's expression. These in vitro FACS analyses revealed that ENA augmentation on the keratinocyte cell surface was dose dependent, UVB dependent, glycosylation dependent, and cell-cycle independent. In vivo ENA augmentation on the keratinocyte surface was examined in suction blister epidermal roofs

A new approach for determination of fouling potential by colloidal nanoparticles during reverse osmosis (RO) membrane filtration of seawater

International Nuclear Information System (INIS)

Park, Ji Yeon; Lim, Sungil; Park, Kihong

2013-01-01

A direct measurement of number concentration of colloidal nanoparticles (15–450 nm) in water was made with the membrane filtration-differential mobility analyzer technique, and its corresponding flux decline rate (FDR) was determined by laboratory-scale RO fouling test unit using varying number concentrations of silica nanoparticles in artificial seawaters. This relationship was used to predict fouling potential of colloidal nanoparticles in reverse osmosis (RO) membrane process of seawaters in RO plant. It was found that the FDR linearly increased with the increasing number of colloidal nanoparticles for the given concentration range and that the relationship between the number concentration and the FDR also depended on RO membrane surface properties. Data for estimated FDR values for natural seawaters after pretreatment showed a clear difference among samples, which is contrary to the pre-existing index such as silt density index and modified fouling index. Our data suggest that measurement of colloidal nanoparticles is useful for selection of proper pretreatment and successful operation of RO membrane process along with other particle fouling predictors accounting for large particles (>450 nm).

A new approach for determination of fouling potential by colloidal nanoparticles during reverse osmosis (RO) membrane filtration of seawater

Energy Technology Data Exchange (ETDEWEB)

Park, Ji Yeon; Lim, Sungil; Park, Kihong, E-mail: kpark@gist.ac.kr [Gwangju Institute of Science and Technology (GIST), School of Environmental Science and Engineering (Korea, Republic of)

2013-04-15

A direct measurement of number concentration of colloidal nanoparticles (15-450 nm) in water was made with the membrane filtration-differential mobility analyzer technique, and its corresponding flux decline rate (FDR) was determined by laboratory-scale RO fouling test unit using varying number concentrations of silica nanoparticles in artificial seawaters. This relationship was used to predict fouling potential of colloidal nanoparticles in reverse osmosis (RO) membrane process of seawaters in RO plant. It was found that the FDR linearly increased with the increasing number of colloidal nanoparticles for the given concentration range and that the relationship between the number concentration and the FDR also depended on RO membrane surface properties. Data for estimated FDR values for natural seawaters after pretreatment showed a clear difference among samples, which is contrary to the pre-existing index such as silt density index and modified fouling index. Our data suggest that measurement of colloidal nanoparticles is useful for selection of proper pretreatment and successful operation of RO membrane process along with other particle fouling predictors accounting for large particles (>450 nm).

Electrophysiological effects of Ro 22-9194, a new antiarrhythmic agent, on guinea-pig ventricular cells.

OpenAIRE

Maruyama, K; Kodama, I; Anno, T; Suzuki, R; Toyama, J

1995-01-01

1. Cardiac effects of Ro 22-9194 were examined in papillary muscles and single ventricular myocytes isolated from guinea-pigs and compared with those of moricizine. 2. In papillary muscles, both Ro 22-9194 (> or = 10 microM) and moricizine (> or = 1 microM) caused a significant dose-dependent decrease in the maximum upstroke velocity (Vmax) and a shortening of the action potential duration. 3. In the presence of either drug, trains of stimuli at rates > or = 0.2 Hz led to an exponential decli...

RoMPS concept review automatic control of space robot, volume 2

Science.gov (United States)

Dobbs, M. E.

1991-01-01

Topics related to robot operated materials processing in space (RoMPS) are presented in view graph form and include: (1) system concept; (2) Hitchhiker Interface Requirements; (3) robot axis control concepts; (4) Autonomous Experiment Management System; (5) Zymate Robot Controller; (6) Southwest SC-4 Computer; (7) oven control housekeeping data; and (8) power distribution.

Characterization and biotoxicity assessment of dissolved organic matter in RO concentrate from a municipal wastewater reclamation reverse osmosis system.

Science.gov (United States)

Sun, Ying-Xue; Gao, Yue; Hu, Hong-Ying; Tang, Fang; Yang, Zhe

2014-12-01

Reverse osmosis (RO) concentrate from municipal wastewater reclamation reverse osmosis (mWRRO) system containing organic compounds may associate with toxic risk, and its discharge might pose an environmental risk. To identify a basis for the selection of feasible technology in treating RO concentrates, the characteristics and biotoxicity of different fractions of dissolved organic matter (DOM) in RO concentrates from an mWRRO system were investigated. The results indicated that the hydrophilic neutrals (HIN), hydrophobic acids (HOA) and hydrophobic bases (HOB) accounted for 96% of the dissolved organic carbon (DOC) of the total DOM in the RO concentrate. According to the SEC chromatograph detected at 254 nm wavelength of UV, the DOM with molecular weight (MW) 1-3 kDa accounted for the majority of the basic and neutral fractions. The fluorescence spectra of the excitation emission matrix (EEM) indicated that most aromatic proteins, humic/fulvic acid-like and soluble microbial by-product-like substances existed in the fractions HOA and hydrophobic neutrals (HON). The genotoxicity and anti-estrogenic activity of the RO concentrate were 1795.6 ± 57.2 μg 4-NQOL(-1) and 2.19 ± 0.05 mg TAM L(-1), respectively. The HIN, HOA, and HOB contributed to the genotoxicity of the RO concentrate, and the HIN was with the highest genotoxic level of 1007.9 ± 94.8 μg 4-NQOL(-1). The HOA, HON, and HIN lead to the total anti-estrogenic activity of the RO concentrate, and HOA occupied approximately 60% of the total, which was 1.3 ± 0.17 mg TAM L(-1). Copyright © 2014 Elsevier Ltd. All rights reserved.

Computational molecular spectroscopy of X ˜ 2 Π NCS: Electronic properties and ro-vibrationally averaged structure

Science.gov (United States)

Hirano, Tsuneo; Nagashima, Umpei; Jensen, Per

2018-04-01

For NCS in the X ˜ 2 Π electronic ground state, three-dimensional potential energy surfaces (3D PESs) have been calculated ab initio at the core-valence, full-valence MR-SDCI+Q/[aug-cc-pCVQZ (N, C, S)] level of theory. The ab initio 3D PESs are employed in second-order-perturbation-theory and DVR3D calculations to obtain various molecular constants and ro-vibrationally averaged structures. The 3D PESs show that the X ˜ 2 Π NCS has its potential minimum at a linear configuration, and hence it is a "linear molecule." The equilibrium structure has re (N-C) = 1.1778 Å, re (C-S) = 1.6335 Å, and ∠e (N-C-S) = 180°. The ro-vibrationally averaged structure, determined as expectation values over DVR3D wavefunctions, has 〈 r (N-C)〉0 = 1.1836 Å, 〈 r (C-S)〉0 = 1.6356 Å, and 〈 ∠ (N-C-S)〉0 = 172.5°. Using these expectation values as the initial guess, a bent r0 structure having an 〈 ∠ (N-C-S)〉0 of 172.2° is deduced from the experimentally reported B0 values for NC32S and NC34S. Our previous prediction that a linear molecule, in any ro-vibrational state including the ro-vibrational ground state, is to be "observed" as being bent on ro-vibrational average, has been confirmed here theoretically through the expectation value for the bond-angle deviation from linearity, 〈 ρ bar 〉 , and experimentally through the interpretation of the experimentally derived rotational-constant values.

THE CoRoT DISCOVERY OF A UNIQUE TRIPLE-MODE CEPHEID IN THE GALAXY

Energy Technology Data Exchange (ETDEWEB)

Poretti, E. [INAF-Osservatorio Astronomico di Brera, Via E. Bianchi 46, I-23807 Merate (Italy); Baglin, A. [LESIA, Université Pierre et Marie Curie, Université Denis Diderot, Observatoire de Paris, F-92195 Meudon Cedex (France); Weiss, W. W., E-mail: ennio.poretti@brera.inaf.it [Institute of Astronomy, University of Vienna, Türkenschanzstrasse 17, A-1180 Vienna (Austria)

2014-11-10

The exploitation of the CoRoT treasure of stars observed in the exoplanetary field allowed the detection of a unusual triple-mode Cepheid in the Milky Way, CoRoT 0223989566. The two modes with the largest amplitudes and a period ratio of 0.80 are identified with the first (P {sub 1} = 1.29 days) and second (P {sub 2} = 1.03 days) radial overtones. The third period, which has the smallest amplitude but is able to produce combination terms with the other two, is the longest one (P {sub 3} = 1.89 days). The ratio of 0.68 between the first-overtone period and the third period is the unusual feature. Its identification with the fundamental radial or a nonradial mode is discussed with respect to similar cases in the Magellanic Clouds. In both cases, the period triplet and the respective ratios make the star unique in our Galaxy. The distance derived from the period-luminosity relation and the galactic coordinates put CoRoT 0223989566 in the metal-rich environment of the ''outer arm'' of the Milky Way.

In vitro culture and characterization of putative porcine embryonic germ cells derived from domestic breeds and yucatan mini pig embryos at days 20-24 of gestation

DEFF Research Database (Denmark)

Petkov, Stoyan Gueorguiev; Marks, Hendrik; Klein, Tino

2011-01-01

Embryonic germ cells (EGC) are cultured pluripotent cells derived from primordial germ cells (PGC). This study explored the possibility of establishing porcine EGC from domestic breeds and Yucatan mini pigs using embryos at Days 17-24 of gestation. In vitro culture of PGC from both pooled...

Implementation of a GPS-RO data processing system for the KIAPS-LETKF data assimilation system

Science.gov (United States)

Kwon, H.; Kang, J.-S.; Jo, Y.; Kang, J. H.

2015-03-01

The Korea Institute of Atmospheric Prediction Systems (KIAPS) has been developing a new global numerical weather prediction model and an advanced data assimilation system. As part of the KIAPS package for observation processing (KPOP) system for data assimilation, preprocessing, and quality control modules for bending-angle measurements of global positioning system radio occultation (GPS-RO) data have been implemented and examined. The GPS-RO data processing system is composed of several steps for checking observation locations, missing values, physical values for Earth radius of curvature, and geoid undulation. An observation-minus-background check is implemented by use of a one-dimensional observational bending-angle operator, and tangent point drift is also considered in the quality control process. We have tested GPS-RO observations utilized by the Korean Meteorological Administration (KMA) within KPOP, based on both the KMA global model and the National Center for Atmospheric Research Community Atmosphere Model with Spectral Element dynamical core (CAM-SE) as a model background. Background fields from the CAM-SE model are incorporated for the preparation of assimilation experiments with the KIAPS local ensemble transform Kalman filter (LETKF) data assimilation system, which has been successfully implemented to a cubed-sphere model with unstructured quadrilateral meshes. As a result of data processing, the bending-angle departure statistics between observation and background show significant improvement. Also, the first experiment in assimilating GPS-RO bending angle from KPOP within KIAPS-LETKF shows encouraging results.

The efficiency of a corrosion inhibitor on steel in a simulated concrete environment

Energy Technology Data Exchange (ETDEWEB)

Gartner, Nina; Kosec, Tadeja, E-mail: tadeja.kosec@zag.si; Legat, Andraž

2016-12-01

The aim of the present work was to characterize the efficiency of a corrosion inhibitor on steel in a simulated concrete pore solution. Laboratory measurements were performed at various chloride and inhibitor concentrations in order to simulate different applications of the inhibitor when used for the protection or rehabilitation of steel reinforcement in concrete. Two electrochemical techniques, i.e. potentiodynamic polarization scans and electrochemical impedance spectroscopy, were used for this study. The exposed surfaces of the steel specimens were subsequently investigated by Raman spectroscopy and scanning electron microscopy. It was found that the inhibitor can efficiently retard the corrosion of steel in a simulated concrete pore solution at concentrations of the inhibitor >2.0% and of chlorides <0.3% at a pH 10.5. On the other hand, when these conditions are not fulfilled, localized corrosion was observed. The results of the Raman and SEM/EDS analysis showed various morphologies of corrosion products and different types of corrosion attack depending on the pH of the pore solution, and the applied concentrations of the chlorides and the inhibitor. - Highlights: • Electrochemical studies performed at various Cl{sup −} and inhibitor concentrations. • Exposed steel surfaces investigated by Raman spectroscopy and SEM. • Cl{sup −}/inhibitor ratio is important parameter for the inhibitor's efficiency. • The corrosion can re-occur if the concentration of the inhibitor is reduced. • Different corrosion behaviour and oxides in the presence of inhibitor and/or Cl{sup −}.

In-Building Wireless Distribution in legacy Multimode Fiber with an improved RoMMF system

DEFF Research Database (Denmark)

Visani, Davide; Petersen, Martin Nordal; Sorci, Francesca

2012-01-01

A radio over multimode fiber (RoMMF) system for in-building wireless distribution employing a directly modulated Fabry-Perot (FP) transmitter and the central launch technique is presented. The worst-case spurious free dynamic range (SFDR) exceeds 105 dB×Hz2/3 up to 525 m of OM2 multimode fiber (MMF......). Experimental and theoretical results are reported showing that this scheme outperforms a RoMMF system employing a distributed feed-back (DFB) laser diode (LD) and/or a mode scrambler to achieve overfilled launch (OFL). Long Term Evolution (LTE) signal transmission is achieved with high quality in terms...... of Adjacent Channel Leakage Ratio (ACLR) and Error Vector Magnitude (EVM)....

Photonic microwave carrier recovery using period-one nonlinear dynamics of semiconductor lasers for OFDM-RoF coherent detection.

Science.gov (United States)

Hung, Yu-Han; Yan, Jhih-Heng; Feng, Kai-Ming; Hwang, Sheng-Kwang

2017-06-15

This study investigates an all-optical scheme based on period-one (P1) nonlinear dynamics of semiconductor lasers, which regenerates the microwave carrier of an orthogonal frequency division multiplexing radio-over-fiber (OFDM-RoF) signal and uses it as a microwave local oscillator for coherent detection. Through the injection locking established between the OFDM-RoF signal and the P1 dynamics, frequency synchronization with highly preserved phase quality is inherently achieved between the recovered microwave carrier and the microwave carrier of the OFDM-RoF signal. A bit-error ratio down to 1.9×10-9 is achieved accordingly using the proposed scheme for coherent detection of a 32-GHz OFDM-RoF signal carrying 4  Gb/s 16-quadrature amplitude modulation data. No electronic microwave generators or electronic phase-locked loops are thus required. The proposed system can be operated up to at least 100 GHz and can be self-adapted to certain changes in the operating microwave frequency.

Optimization of AMI-MDM-RoFSO under atmospheric turbulence

Directory of Open Access Journals (Sweden)

Chaudhary Sushank

2017-01-01

Full Text Available Radio over Free Space (Ro-FSO is promising candidate for providing ubiquitous digital services especially in rural areas. This work investigates the performance of MDM of two 5Gbps-10GHz data channels over FSO link using LP 01 and LP 02 modes under the effect of atmospheric turbulences. The signal to noise ratio (SNR, total received power, modal decomposition at receiver at the receiver is also reported. The reported result shows the successful transmission of two channels with acceptable SNR over FSO link under atmospheric turbulences.

Cellular reactions of CD3+ CD4+ CD45RO+ T-lymphocytes on dexamethason in in normal patients and in patients with with rheumatoid arthritis in vitro

Directory of Open Access Journals (Sweden)

L. S. Litvinova

2017-01-01

Full Text Available The aim of the study was to analyze the influence of glucocorticoid (GC dexamethasone (Dex on changes in CD4+ T-cells expressing the surface molecule of activation (CD25, CD71, HLA-DR and CD95 and their ability to produce proinflammatory mediators in cultures of TCR-stimulated CD3+CD45RO+ T-lymphocytes obtained from healthy donors and patients with rheumatoid arthritis in vitro.Materials and methods. The study included 50 patients and 20 healthy donors. T-cell cultures (CD3+ CD45RO+ were obtained from mononuclear leukocytes of immunomagnetic separation (MACS® technology. As an activator of T-lymphocytes, antibiotic particles with biotinylated antibodies against CD2+, CD3+, CD28+, which simulate the process of costimulation of T cells by antigen-presenting cells, were used. The following concentrations of dexamethasone (2, 8, 16, 32, 64 mg were used in the experiment. The change in the immunophenotype of T-lymphocytes was analyzed by flow cytofluoometry. The secretion of CD3+CD45RO+ T-cells of proinflammatory cytokines IL-2, IFNγ, TNFα, IL-17 and IL-21 was evaluated by enzyme-linked immunosorbent assay.Results. The general suppressor effect of Dex on CD3+CD45RO+ T-cell cultures mediated by a decrease in the number of CD4 + T cells expressing activation molecules (CD25 and proliferation (CD71, as well as inhibition of the production of inflammatory mediators: IFNγ, IL-2 and TNFα. It is shown that against the background of TCR activation Dex increases the number of CD4+CD95+HLA-DR+ cells in CD3+CD45RO+ cultures obtained from RA patients and does not change their content in the control. The correlations between the number of proinflammatory factors (IL-17, IL-21 and TNFα in CD4+CD45RO+CD95+HLA-DR+ T cells in supernatants of cell cultures in RA patients indicate the presence of a pro-inflammatory potential of this population of T cells. We assume that the resistance of CD4+CD45RO+CD95+HLA-DR+ T cells in RA patients to the suppressor effect of

Piinatud birmalased ootavad ÜRO seni jõuetut abikätt / Karin Dean

Index Scriptorium Estoniae

Dean, Karin

2007-01-01

Buda munkade eestvedmisel toimunud massimeeleavalduste mahasurumisest Birmas. ÜRO erisaadiku Ibrahim Gambari kohtumisest nii Birma kindralite kui ka opositsiooniliidri Aung San Suu Kyiga oodatakse tulemusi ja sanktsioone Lisa: Sõjaväe haardes riik

Sexuality: zpráva z 2. ročníku vědecké konference s mezinárodní účastí konané v Nitře

Czech Academy of Sciences Publication Activity Database

Sloboda, Zdeněk

2008-01-01

Roč. 9, č. 2 (2008), s. 85-87 ISSN 1213-0028. [ Sexuality 2008. Nitra, 20.09.2007-21.09.2007] R&D Projects: GA AV ČR 1QS700280503; GA AV ČR IAA700280804 Institutional research plan: CEZ:AV0Z70280505 Keywords : sexualities * sexuality * conference Subject RIV: AO - Sociology, Demography

Effect of kinase inhibitors on the therapeutic properties of monoclonal antibodies.

Science.gov (United States)

Duong, Minh Ngoc; Matera, Eva-Laure; Mathé, Doriane; Evesque, Anne; Valsesia-Wittmann, Sandrine; Clémenceau, Béatrice; Dumontet, Charles

2015-01-01

Targeted therapies of malignancies currently consist of therapeutic monoclonal antibodies and small molecule kinase inhibitors. The combination of these novel agents raises the issue of potential antagonisms. We evaluated the potential effect of 4 kinase inhibitors, including the Bruton tyrosine kinase inhibitor ibrutinib, and 3 PI3K inhibitors idelalisib, NVP-BEZ235 and LY294002, on the effects of the 3 monoclonal antibodies, rituximab and obinutuzumab (directed against CD20) and trastuzumab (directed against HER2). We found that ibrutinib potently inhibits antibody-dependent cell-mediated cytotoxicity exerted by all antibodies, with a 50% inhibitory concentration of 0.2 microM for trastuzumab, 0.5 microM for rituximab and 2 microM for obinutuzumab, suggesting a lesser effect in combination with obinutuzumab than with rituximab. The 4 kinase inhibitors were found to inhibit phagocytosis by fresh human neutrophils, as well as antibody-dependent cellular phagocytosis induced by the 3 antibodies. Conversely co-administration of ibrutinib with rituximab, obinutuzumab or trastuzumab did not demonstrate any inhibitory effect of ibrutinib in vivo in murine xenograft models. In conclusion, some kinase inhibitors, in particular, ibrutinib, are likely to exert inhibitory effects on innate immune cells. However, these effects do not compromise the antitumor activity of monoclonal antibodies in vivo in the models that were evaluated.

Evaluation of TEG(®) and RoTEM(®) inter-changeability in trauma patients.

Science.gov (United States)

Hagemo, Jostein S; Næss, Paal A; Johansson, Pär; Windeløv, Nis A; Cohen, Mitchell Jay; Røislien, Jo; Brohi, Karim; Heier, Hans Erik; Hestnes, Morten; Gaarder, Christine

2013-05-01

Massive haemorrhage is a leading cause of preventable deaths in trauma. Traumatic coagulopathy is frequently present early after trauma, and is associated with increased mortality. A number of recent trials suggest that viscoelastic haemostatic assays (VHA), such as thromboelastography and thromboelastometry, are useful tools in guiding transfusion. Treatment algorithms exist for the use of VHAs but are not validated in traumatic haemorrhage. In this study we examined the inter-changeability of two commonly used VHAs, TEG(®) and RoTEM(®). A total of 184 trauma patients over the age of 18, requiring full trauma team activation, were included at three different hospitals in three different countries (Copenhagen, Denmark, San Francisco, CA, USA and Oslo, Norway). Blood samples were drawn immediately upon arrival, and TEG(®) and RoTEM(®) analyzed simultaneously. Correlations were calculated using. Spearman's rank correlation coefficient. Agreement was evaluated by Bland-Altman plots and calculation of limits of agreement. The mean ISS in the total population was 17, and the mortality was 16.5%. Mean base excess was -2.8 (SD: 4.2). The correlation coefficient for corresponding values for the two devices was 0.24 for the R-time vs CT in all centres combined. For the K-time vs CFT the correlation was 0.48, for the α-angleTEG vs α-angleRoTEM 0.44, and for MA vs MCF 0.76. Limits of agreement exceeded the preset clinically acceptable deviation of 10% for all variables in all centres except for MA/MCF in one centre (Copenhagen). Generally, correlation coefficients were lower and agreement poorer in the one centre (Oslo) where measurements were performed bedside by clinicians. Inter-changeability between TEG(®) and RoTEM(®) is limited in the trauma setting. Agreement seems poorer when clinicians operate the devices. Development and validation of separate treatment algorithms for the two devices is required. Copyright © 2012 Elsevier Ltd. All rights reserved.

Oxindole based oxadiazole hybrid analogs: Novel α-glucosidase inhibitors.

Science.gov (United States)

Taha, Muhammad; Imran, Syahrul; Rahim, Fazal; Wadood, Abdul; Khan, Khalid Mohammed

2018-02-01

Inhibition of α-glucosidase is an effective strategy for controlling post-prandial hyperglycemia in diabetic patients. Beside these α-glucosidase inhibitors has been also used as anti-obesity and anti-viral drugs. Keeping in view the greater importance of α-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1-20) synthesis, characterized by different spectroscopic techniques including 1 H NMR and EI-MS and their α-glucosidase inhibitory activity. All compounds were found potent inhibitors for the enzyme with IC 50 values ranging between 1.25 ± 0.05 and 268.36 ± 4.22 µM when compared with the standard drug acarbose having IC 50 value 895.09 ± 2.04 µM. Our study identifies novel series of potent α-glucosidase inhibitors and further investigation on this may led to the lead compounds. A structure activity relationship has been established for all compounds. The interactions of the active compounds and enzyme active site were established with the help of molecular docking studies. Copyright © 2017 Elsevier Inc. All rights reserved.

A Comprehensive Study on the Application of Reverse Osmosis (RO Technology for the Petroleum Industry Wastewater Treatment

Directory of Open Access Journals (Sweden)

Shahryar Jafarinejad

2017-10-01

Full Text Available Large quantities of oily wastewaters can be generated from the activities and processes in the petroleum industry which draining of these effluents not only pollutes the environment but also reduces the yield of oil and water. Therefore, development of treatment processes for petroleum industry wastewaters is vital in order to prevent serious environmental damage and provide a source of water for beneficial use. Reverse osmosis (RO can be the most common membrane process used for desalination from oily wastewater and can produce water suitable for reuse at the petroleum industry. In this study, the application of RO technology for the petroleum industry wastewater treatment in different laboratory, pilot, field, and industrial scales have been reviewed. In addition, membrane fouling control, performance efficiency, treatment system configurations, pretreatment methods, quality of treated water, and economic issues have been investigated. With mixtures as complex as petroleum industry wastewaters, membrane fouling becomes a significant hurdle to implement the RO-based purification system. Operating the system within the critical flux range or adding chemicals, and/or pretreatment can usually control membrane fouling. Salt rejection of RO membranes can be 99% or higher.

Sté výročí narození Simone de Beauvoir

Czech Academy of Sciences Publication Activity Database

Uhde, Zuzana

2008-01-01

Roč. 44, č. 4 (2008), s. 797-799 ISSN 0038-0288 R&D Projects: GA AV ČR 1QS700280503 Institutional research plan: CEZ:AV0Z70280505 Keywords : Simone de Beauvoir * Feminism Subject RIV: AO - Sociology, Demography Impact factor: 0.427, year: 2008

Multiple dose study of the combined radiosensitizers Ro 03-8799 (pimonidazole) and SR 2508 (etanidazole)

International Nuclear Information System (INIS)

Bleehen, N.M.; Newman, H.F.; Maughan, T.S.; Workman, P.

1989-01-01

The hypoxic cell radiosensitizers Ro 03-8799 and SR 2508 have different clinical toxicities. The former produces an acute but transient central nervous system syndrome, whereas the latter produces cumulative peripheral neuropathy. Following single dose studies, an escalating multiple dose schedule using both drugs in combination showed no unexpected adverse reactions at lower doses. This study identifies the clinical tolerance and pharmacokinetics when doses in the region of the maximal tolerated dose are given to 26 patients receiving infusions of 0.75 g/m2 Ro 03-8799 and 2 g/m2 SR 2508 three times per week. At 15 doses, 3/4 patients experienced WHO grade 2 peripheral neuropathy, whereas at 12 doses 1/9 developed grade 2 and 6/9 developed grade 1 neuropathies. This represents a lower dose of SR 2508 than can be given alone suggesting that some interaction between the two drugs does exist in terms of chronic peripheral neurotoxicity. Pharmacokinetic studies show no adverse interactions between the two drugs and minimal inter-patient variation. From bivariate analysis, cumulative AUC for Ro 03-8799 has the most significant correlation with the development of peripheral neuropathy. Tumor drug concentrations normalized to the administered dose show mean values of 34 micrograms/g Ro 03-8799 and 76 micrograms/g SR 2508 30 minutes after infusion. These could be expected to produce a single dose sensitizer enhancement ratio of 1.5. The combination of the two sensitizers at the maximum tolerable dose may be expected to give an increased therapeutic efficacy over either drug alone

Usos da história na formação de pessoas: as experiências do Marquês de Condorcet (1743-1794 e de Immanuel Kant (1724-1804

Directory of Open Access Journals (Sweden)

Itamar Freitas

2017-12-01

Full Text Available Este artigo examina a posição de dois pensadores da ilustração – Immnuel Kant (1724/1804 e Marie Jean Antoine Nicolas de Caritat (1743/1794 – e se propõe a responder à seguinte questão: se não se nasce pessoa, torna-se pessoa, qual o lugar da história na formação dos humanos no período anterior à referida autonomização da disciplina escolar? Aqui, são examinados os textos, produzidos entre 1791 e 1803, que anunciam as visões de homem, vida, filosofia da história, história empírica e educação humana com o objetivo de discutir a presença da história como saber ensinável no século XVIII, contribuindo, assim, para o conhecimento dos usos da história na formação de pessoas numa perspectiva de longa duração.   Palavras-chave: , ensino de história, Condorcet, Kant, século XVIII.

VizieR Online Data Catalog: Spectral types of stars in CoRoT fields (Sebastian+, 2012)

Science.gov (United States)

Sebastian, D.; Guenther, E. W.; Schaffenroth, V.; Gandolfi, D.; Geier, S.; Heber, U.; Deleuil, M.; Moutou, C.

2012-03-01

Spectroscopic classification for 2950 O-, B-, and A-type stars in the CoRoT-fields IRa01, LRa01, and LRa02. Stars are named by their CoRoT-identifier and Coordinates are given. The visual magnitudes were obtained with the Wide Field Camera filter-system of the Isaac Newton Telescope at Roque de los Muchachos Observatory on La Palma and can be converted into Landolt standards, as shown in Deleuil et al. (2009AJ....138..649D). (1 data file).

Models of red giants in the CoRoT asteroseismology fields combining asteroseismic and spectroscopic constraints

Science.gov (United States)

Nadège, Lagarde

The availability of asteroseismic constraints for a large sample of red-giant stars from the CoRoT and Kepler missions paves the way for various statistical studies of the seismic properties of stellar populations. We use a detailed spectroscopic study of 19 CoRoT red-giant stars (Morel et al. 2014) to compare theoretical stellar evolution models to observations of the open cluster NGC 6633 and field stars. This study is already published in Lagarde et al. (2015)

Formestane, a steroidal aromatase inhibitor after failure of non-steroidal aromatase inhibitors (anastrozole and letrozole): is a clinical benefit still achievable?

Science.gov (United States)

Carlini, P; Frassoldati, A; De Marco, S; Casali, A; Ruggeri, E M; Nardi, M; Papaldo, P; Fabi, A; Paoloni, F; Cognetti, F

2001-11-01

There are few clinical data on the sequential use of aromatase inhibitors (AI). This paper focuses on the relevance of clinical benefit CB (CR + PR + SD > or = 6 months) in postmenopausal metastatic breast cancer (MBC) patients treated with the steroidal aromatase inhibitor (SAI) formestane (FOR). who had already received non-steroidal aromatase inhibitor (nSAI): letrozole (LTZ) or anastrozole (ANZ). Twenty postmenopausal women with MBC were analysed in this retrospective two-centre study with the sequence nSAI-FOR. When receiving ANZ, 1 of 11 achieved a complete response and 9 of 11 a stable disease > or = 6 months, and receiving LTZ 1 of 9 achieved a partial response and 4 of 9 a stable disease > or = 6 months. The analysis of the entire population treated with FOR showed an overall CB of 55% (11 of 20) with a median duration of 15 months and median time to progression (TTP) of 6 months. Formestane 250 mg once bi-weekly seems to be an attractive alternative third-line hormonal therapy for the treatment of patients with MBC, previously treated with nSAI.

Characteristics of solar-like oscillations in red giants observed in the CoRoT exoplanet field

Science.gov (United States)

Hekker, S.; Kallinger, T.; Baudin, F.; De Ridder, J.; Barban, C.; Carrier, F.; Hatzes, A. P.; Weiss, W. W.; Baglin, A.

2009-10-01

Context: Observations during the first long run (~150 days) in the exo-planet field of CoRoT increase the number of G-K giant stars for which solar-like oscillations are observed by a factor of 100. This opens the possibility to study the characteristics of their oscillations in a statistical sense. Aims: We aim to understand the statistical distribution of the frequencies of maximum oscillation power (ν_max) in red giants and to search for a possible correlation between ν_max and the large separation (Δ ν). Methods: Red giants with detectable solar-like oscillations are identified using both semi-automatic and manual procedures. For these stars, we determine ν_max as the centre of a Gaussian fit to the oscillation power excess. For the determination of Δ ν, we use the autocorrelation of the Fourier spectra, the comb response function and the power spectrum of the power spectrum. Results: The resulting ν_max distribution shows a pronounced peak between 20-40 μHz. For about half of the stars we obtain Δ ν with at least two methods. The correlation between ν_max and Δ ν follows the same scaling relation as inferred for solar-like stars. Conclusions: The shape of the ν_max distribution can partly be explained by granulation at low frequencies and by white noise at high frequencies, but the population density of the observed stars turns out to be also an important factor. From the fact that the correlation between Δ ν and ν_max for red giants follows the same scaling relation as obtained for sun-like stars, we conclude that the sound travel time over the pressure scale height of the atmosphere scales with the sound travel time through the whole star irrespective of evolution. The fraction of stars for which we determine Δ ν does not correlate with ν_max in the investigated frequency range, which confirms theoretical predictions. The CoRoT space mission which was developed and is operated by the French space agency CNES, with participation of ESA

Modulation of cholinephosphotransferase activity in breast cancer cell lines by Ro5-4864, a peripheral benzodiazepine receptor agonist

International Nuclear Information System (INIS)

Akech, Jacqueline; Roy, Somdutta Sinha; Das, Salil K.

2005-01-01

Changes in phospholipid and fatty acid profile are hallmarks of cancer progression. Increase in peripheral benzodiazepine receptor expression has been implicated in breast cancer. The benzodiazepine, Ro5-4864, increases cell proliferation in some breast cancer cell lines. Biosynthesis of phosphatidylcholine (PC) has been identified as a marker for cells proliferating at high rates. Cholinephosphotransferase (CPT) is the terminal enzyme for the de novo biosynthesis of PC. We have addressed here whether Ro5-4864 facilitates some cancer causing mechanisms in breast cancer. We report that cell proliferation increases exponentially in aggressive breast cancer cell lines 11-9-1-4 and BT-549 when treated with nanomolar concentrations of Ro5-4864. This increase is seen within 24 h of treatment, consistent with the cell doubling time in these cells. Ro5-4864 also upregulates c-fos expression in breast cancer cell lines 11-9-1-4 and BT-549, while expression in non-tumorigenic cell line MCF-12A was either basal or slightly downregulated. We further examined the expression of the CPT gene in breast cancer (11-9-1-4, BT-549) and non-tumorigenic cell lines (MCF-12A, MCF-12F). We found that the CPT gene is overexpressed in breast cancer cell lines compared to the non-tumorigenic cell lines. Furthermore, the activity of CPT in forming PC is increased in the breast cancer cell lines cultured for 24 h. Additionally, we examined the CPT activity in the presence of nanomolar concentrations of Ro5-4864. Biosynthesis of PC was increased in breast cancer cell lines upon treatment. We therefore propose that Ro5-4864 facilitates PC formation, a process important in membrane biogenesis for proliferating cells

Beneficial phosphate recovery from reverse osmosis (RO) concentrate of an integrated membrane system using polymeric ligand exchanger (PLE).

Science.gov (United States)

Kumar, Manish; Badruzzaman, Mohammad; Adham, Samer; Oppenheimer, Joan

2007-05-01

Phosphorus (P) discharge to surface water is a major environmental problem. Wastewater treatment is targeted towards removal of this nutrient to prevent degradation of surface water. Integrated membrane systems (IMS) are increasingly being considered for wastewater reclamation, and provide excellent removal of P compounds. However, reverse osmosis (RO), which forms an integral part of these IMSs, concentrates most dissolved substances including P-species such as phosphates in the RO waste stream. In this study, removal of phosphate from this stream using polymeric ligand exchange (PLE) resins was investigated. Further, the possibility of phosphate recovery through struvite (MgNH(4)PO(4).6H(2)O) precipitation was tested. Struvite has been promoted as a slow release fertilizer in recent years. This study demonstrates that PLEs can be successfully used to remove phosphate from RO-concentrate, and to recover more than 85% of the adsorbed phosphorus from the exhausted media and precipitated as a beneficial product (struvite). The approach, presented in this study, suggests advantages of providing economic benefit from a waste product (RO) while avoiding phosphorus discharge to the environment.

Efficacy of an integrated continuing medical education (CME) and quality improvement (QI) program on radiation oncologist (RO) clinical practice

International Nuclear Information System (INIS)

Leong, Cheng Nang; Shakespeare, Thomas Philip; Mukherjee, Rahul K.; Back, Michael F.; Lee, Khai Mun; Lu, Jiade Jay; Wynne, Christopher J.; Lim, Keith; Tang, Johann; Zhang Xiaojian

2006-01-01

Purpose: There has been little radiation oncologist (RO)-specific research in continuing medical education (CME) or quality improvement (QI) program efficacy. Our aim was to evaluate a CME/QI program for changes in RO behavior, performance, and adherence to department protocols/studies over the first 12 months of the program. Methods and Materials: The CME/QI program combined chart audit with feedback (C-AWF), simulation review AWF (SR-AWF), reminder checklists, and targeted CME tutorials. Between April 2003 and March 2004, management of 75 patients was evaluated by chart audit with feedback (C-AWF) and 178 patients via simulation review audit (SR-AWF) using a validated instrument. Scores were presented, and case management was discussed with individualized educational feedback. RO behavior and performance was compared over the first year of the program. Results: Comparing the first and second 6 months, there was a significant improvement in mean behavior (12.7-13.6 of 14, p = 0.0005) and RO performance (7.6-7.9 of 8, p = 0.018) scores. Protocol/study adherence significantly improved from 90.3% to 96.6% (p = 0.005). A total of 50 actions were generated, including the identification of learning needs to direct CME tutorials, the systematic change of suboptimal RO practice, and the alteration of deficient management of 3% of patients audited during the program. Conclusion: An integrated CME/QI program combining C-AWF, SR-AWF, QI reminders, and targeted CME tutorials effectively improved targeted RO behavior and performance over a 12-month period. There was a corresponding increase in departmental protocol and study adherence

Y a-t-il eu un instant zéro ?

CERN Document Server

Klein, Etienne

2015-01-01

D'où vient l'univers ? Et d'où vient même qu'il y ait un univers ? Aura-t-il une fin ? Pourquoi les humains y sont-ils apparus ? Si ces questions nous obsèdent depuis toujours, celle de l'origine demeure la plus mystérieuse, la plus vertigineuse, d'où la profusion de discours — mythologiques, religieux ou philosophiques — qui tentent d'y répondre. C'est grâce à la science, aux découvertes de Newton, Galilée, Edwin Hubble, Alexandre Friedmann et Georges Lemaître, qu'on peut retracer le grand récit de l'univers, remonter son histoire à 13,7 milliards d'années, jusqu'à cette phase très dense et très chaude qu'on a appelée le big bang. Mais celui-ci n'est pas pour autant, comme on l'a imaginé, cette explosion originelle qui aurait créé tout ce qui existe. Cet instant zéro, peut-on le décrire, le penser, raconter d'où il peut bien provenir ? Et d'où serait venu l'univers d'avant le big bang ? Mystère ! Qu'il y ait eu origine ou pas, on ne part donc jamais de zéro. En parler, c'est p...

Analysis of different sub-carrier allocation of M-ary QAM-OFDM downlink in RoF system

Science.gov (United States)

Shao, Yu-feng; Chen, Luo; Wang, An-rong; Zhao, Yun-jie; Long, Ying; Ji, Xing-ping

2018-01-01

In this paper, the performance of a 60 GHz radio over fiber (RoF) system with 4/16/64 quadrature amplitude modulation (QAM) orthogonal frequency division multiplexing (OFDM) downstream signals is studied. Delivery of 10 Gbit/s M-ary QAM (MQAM) OFDM signals through the 20-km-long single-mode fiber (SMF) is complicated in terms of intensity modulation and direct detection (IM/DD). Using self-homodyne method, the beating of two independent light waves generating the millimeter-wave at the photodetector can be down-converted to baseband in the electrical domain. Meanwhile, three kinds of sub-carrier arrangement schemes are compared and discussed, and the simulation results show that lower peak-to-average power ratio ( PAPR) can be obtained adopting the adjacent scheme. At bit error rate ( BER) of 10-3, the receiver sensitivity using 4QAM-OFDM sub-carrier signal is almost enhanced by 4 dB and 9 dB compared with those of 16QAM-OFDM signal and 64QAM-OFDM signal.

Locus pietatis et vitae II, Vranov u Brna 20.–22. 9. 2010

Czech Academy of Sciences Publication Activity Database

Freemanová, Michaela

2010-01-01

Roč. 47, č. 4 (2010), s. 407-409 ISSN 0018-7003. [Locus pietatis et vitae II. Vranov u Brna, 20.09.2010–22.09.2010] Institutional research plan: CEZ:AV0Z90580513 Keywords : history * monastic orders * conference Subject RIV: AL - Art, Architecture, Cultural Heritage

Combination of cupric ion with hydroxylamine and hydrogen peroxide for the control of bacterial biofilms on RO membranes.

Science.gov (United States)

Lee, Hye-Jin; Kim, Hyung-Eun; Lee, Changha

2017-03-01

Combinations of Cu(II) with hydroxylamine (HA) and hydrogen peroxide (H 2 O 2 ) (i.e., Cu(II)/HA, Cu(II)/H 2 O 2 , and Cu(II)/HA/H 2 O 2 systems) were investigated for the control of P. aeruginosa biofilms on reverse osmosis (RO) membranes. These Cu(II)-based disinfection systems effectively inactivated P. aeruginosa cells, exhibiting different behaviors depending on the state of bacterial cells (planktonic or biofilm) and the condition of biofilm growth and treatment (normal or pressurized condition). The Cu(II)/HA and Cu(II)/HA/H 2 O 2 systems were the most effective reagents for the inactivation of planktonic cells. However, these systems were not effective in inactivating cells in biofilms on the RO membranes possibly due to the interactions of Cu(I) with extracellular polymeric substances (EPS), where biofilms were grown and treated in center for disease control (CDC) reactors. Different from the results using CDC reactors, in a pressurized cross-flow RO filtration unit, the Cu(II)/HA/H 2 O 2 treatment significantly inactivated biofilm cells formed on the RO membranes, successfully recovering the permeate flux reduced by the biofouling. The pretreatment of feed solutions by Cu(II)/HA and Cu(II)/HA/H 2 O 2 systems (applied before the biofilm formation) effectively mitigated the permeate flux decline by preventing the biofilm growth on the RO membranes. Copyright © 2016 Elsevier Ltd. All rights reserved.

Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease.

Science.gov (United States)

Chong, Jimmy; Leung, Bonnie; Poole, Phillippa

2017-09-19

Chronic obstructive pulmonary disease (COPD) is associated with cough, sputum production or dyspnoea and a reduction in lung function, quality of life and life expectancy. Apart from smoking cessation, there are no other treatments that slow lung function decline. Roflumilast and cilomilast are oral phosphodiesterase 4 (PDE 4 ) inhibitors proposed to reduce the airway inflammation and bronchoconstriction seen in COPD. This is an update of a Cochrane review first published in 2011 and updated in 2013. To evaluate the efficacy and safety of oral PDE 4 inhibitors in the management of stable COPD. We identified randomised controlled trials (RCTs) from the Cochrane Airways Trials Register (date of last search October 2016). We found other trials from web-based clinical trials registers. We included RCTs if they compared oral PDE 4 inhibitors with placebo in people with COPD. We allowed co-administration of standard COPD therapy. One review author extracted data and a second review author checked the data. We reported pooled data in Review Manager as mean differences (MD), standardised mean differences (SMD) or odds ratios (OR). We converted the odds ratios into absolute treatment effects in a 'Summary of findings' table. Thirty-four separate RCTs studying roflumilast (20 trials with 17,627 participants) or cilomilast (14 trials with 6457 participants) met the inclusion criteria, with a duration of between six weeks and one year. These included people across international study centres with moderate to very severe COPD (Global Initiative for Chronic Obstructive Lung Disease (GOLD) grades II-IV), with a mean age of 64 years.We considered that the methodological quality of the 34 published and unpublished trials was acceptable overall. Treatment with a PDE 4 inhibitor was associated with a significant improvement in forced expiratory volume in one second (FEV 1 ) over the trial period compared with placebo (MD 51.53 mL, 95% confidence interval (CI) 43.17 to 59.90, 27

Dry eye syndrome in aromatase inhibitor users.

Science.gov (United States)

Turaka, Kiran; Nottage, Jennifer M; Hammersmith, Kristin M; Nagra, Parveen K; Rapuano, Christopher J

2013-04-01

Aromatase inhibitors are frequently used as an adjuvant therapy in the treatment of breast cancer. We observed that several patients taking aromatase inhibitors presented with severe dry eye symptoms, and we investigated whether there is a relationship between aromatase inhibitors and dry eyes in these patients. Retrospective chart review. Forty-one women. A computerized search of health records was performed to identify patients using anastrazole, letrozole and exemestane seen by the Cornea Service from August 2008 to March 2011. The results were compared with age-matched controls. Ocular surface changes among aromatase inhibitors users. Of the 41 women, 39 were Caucasians. Thirty-nine patients had breast cancer (95%), one patient had ovarian cancer (2.5%) and one had an unknown primary cancer. Mean age was 68 ± 11.3 years (range 47-95). Most common presenting symptoms were blurred vision in 28 (68%) patients, irritation/foreign body sensation in 12 (29%) patients, redness in 9 (22%) patients, tearing in 6 (22%) patients and photosensitivity in 2 (5%) patients. Mean Schirmer's test measurement was 11 ± 5.8 mm (range 0.5-20 mm). Blepharitis was noted in 68 of 82 eyes (73%), decreased or poor tear function in 24 eyes (29%), conjunctival injection in 18 eyes (22%) and superficial punctate keratitis in 12 eyes (29%). Among an age-matched population (45-95 years), dry eye syndrome was found in only 9.5% of patients. Because the prevalence of ocular surface disease signs and symptoms appears to be higher in study group than control patients, aromatase inhibitors might be a contributing factor to the dry eye symptoms. © 2012 The Authors. Clinical and Experimental Ophthalmology © 2012 Royal Australian and New Zealand College of Ophthalmologists.

Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging

Directory of Open Access Journals (Sweden)

Vadim Bernard-Gauthier

2015-12-01

Full Text Available Over the last 20 years, intensive investigation and multiple clinical successes targeting protein kinases, mostly for cancer treatment, have identified small molecule kinase inhibitors as a prominent therapeutic class. In the course of those investigations, radiolabeled kinase inhibitors for positron emission tomography (PET imaging have been synthesized and evaluated as diagnostic imaging probes for cancer characterization. Given that inhibitor coverage of the kinome is continuously expanding, in vivo PET imaging will likely find increasing applications for therapy monitoring and receptor density studies both in- and outside of oncological conditions. Early investigated radiolabeled inhibitors, which are mostly based on clinically approved tyrosine kinase inhibitor (TKI isotopologues, have now entered clinical trials. Novel radioligands for cancer and PET neuroimaging originating from novel but relevant target kinases are currently being explored in preclinical studies. This article reviews the literature involving radiotracer design, radiochemistry approaches, biological tracer evaluation and nuclear imaging results of radiolabeled kinase inhibitors for PET reported between 2010 and mid-2015. Aspects regarding the usefulness of pursuing selective vs. promiscuous inhibitor scaffolds and the inherent challenges associated with intracellular enzyme imaging will be discussed.

Inhibition of Cytokinin-Glucose Conjugation in Derooted Radish, Tobacco and Bean Seedlings

Czech Academy of Sciences Publication Activity Database

Blagoeva, Elitsa; Dobrev, Petre; Vaňková, Radomíra

2003-01-01

Roč. 29, 1/2 (2003), s. 13-20 ISSN 1310-4586 R&D Projects: GA ČR GA522/99/1130; GA ČR GP522/02/D058; GA MŠk LN00A081 Institutional research plan: CEZ:AV0Z5038910 Keywords : dihydrozeatin * cyclin-dependent kinase inhibitors * radish (Raphanus sativus L.) Subject RIV: EB - Genetics ; Molecular Biology

Expression and regulation of murine SPINK12, a potential orthologue of human LEKTI2

Czech Academy of Sciences Publication Activity Database

Reiss, K.; Meyer-Hoffert, U.; Fischer, J.; Sperrhacke, M.; Wu, Z.; Dimitrieva, O.; Křenek, Pavel; Suchanová, Šárka; Buryová, Halka; Brauer, Rena; Sedláček, Radislav

2011-01-01

Roč. 20, č. 11 (2011), s. 905-910 ISSN 0906-6705 R&D Projects: GA ČR GC301/08/J053 Grant - others:Deutsche Forschungsgemeinschaft (DFG)(DE) Me2037/3-1 Institutional research plan: CEZ:AV0Z50520514 Keywords : epidermis * inhibitor * kallikrein * serine protease * spink Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 3.543, year: 2011

RoCoMAR: Robots' Controllable Mobility Aided Routing and Relay Architecture for Mobile Sensor Networks

Science.gov (United States)

Van Le, Duc; Oh, Hoon; Yoon, Seokhoon

2013-01-01

In a practical deployment, mobile sensor network (MSN) suffers from a low performance due to high node mobility, time-varying wireless channel properties, and obstacles between communicating nodes. In order to tackle the problem of low network performance and provide a desired end-to-end data transfer quality, in this paper we propose a novel ad hoc routing and relaying architecture, namely RoCoMAR (Robots' Controllable Mobility Aided Routing) that uses robotic nodes' controllable mobility. RoCoMAR repeatedly performs link reinforcement process with the objective of maximizing the network throughput, in which the link with the lowest quality on the path is identified and replaced with high quality links by placing a robotic node as a relay at an optimal position. The robotic node resigns as a relay if the objective is achieved or no more gain can be obtained with a new relay. Once placed as a relay, the robotic node performs adaptive link maintenance by adjusting its position according to the movements of regular nodes. The simulation results show that RoCoMAR outperforms existing ad hoc routing protocols for MSN in terms of network throughput and end-to-end delay. PMID:23881134

RoCoMAR: Robots’ Controllable Mobility Aided Routing and Relay Architecture for Mobile Sensor Networks

Directory of Open Access Journals (Sweden)

Seokhoon Yoon

2013-07-01

Full Text Available In a practical deployment, mobile sensor network (MSN suffers from a low performance due to high node mobility, time-varying wireless channel properties, and obstacles between communicating nodes. In order to tackle the problem of low network performance and provide a desired end-to-end data transfer quality, in this paper we propose a novel ad hoc routing and relaying architecture, namely RoCoMAR (Robots’ Controllable Mobility Aided Routing that uses robotic nodes’ controllable mobility. RoCoMAR repeatedly performs link reinforcement process with the objective of maximizing the network throughput, in which the link with the lowest quality on the path is identified and replaced with high quality links by placing a robotic node as a relay at an optimal position. The robotic node resigns as a relay if the objective is achieved or no more gain can be obtained with a new relay. Once placed as a relay, the robotic node performs adaptive link maintenance by adjusting its position according to the movements of regular nodes. The simulation results show that RoCoMAR outperforms existing ad hoc routing protocols for MSN in terms of network throughput and end-to-end delay.

Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao Flowers

Directory of Open Access Journals (Sweden)

Zhanwu Sheng

2014-07-01

Full Text Available The use of α-glucosidase inhibitors is considered to be an effective strategy in the treatment of diabetes. Using a bioassay-guided fractionation technique, five Bacillus stearothermophilus α-glucosidase inhibitors were isolated from the flowers of Musa spp. (Baxijiao. Using NMR spectroscopy analysis they were identified as vanillic acid (1, ferulic acid (2, β-sitosterol (3, daucosterol (4 and 9-(4′-hydroxyphenyl-2-methoxyphenalen-1-one (5. The half maximal inhibitory concentration (IC50 values of compounds 1–5 were 2004.58, 1258.35, 283.67, 247.35 and 3.86 mg/L, respectively. Compared to a known α-glucosidase inhibitor (acarbose, IC50 = 999.31 mg/L, compounds 3, 4 and 5 showed a strong α-glucosidase inhibitory effect. A Lineweaver-Burk plot indicated that compound 5 is a mixed-competitive inhibitor, while compounds 3 and 4 are competitive inhibitors. The inhibition constants (Ki of compounds 3, 4 and 5 were 20.09, 2.34 and 4.40 mg/L, respectively. Taken together, these data show that the compounds 3, 4 and 5 are potent α-glucosidase inhibitors.

Tourismusbüro von Dubai in der Schweiz & Österreich: Analyse des Business Plan & Budget 2013

OpenAIRE

Wyss, Anja; Stampfli, Michèle

2014-01-01

Das Department of Tourism and Commerce Marketing of Dubai (DTCM) hat in der Schweiz ein Auslandbüro, das für die Märkte Schweiz und Österreich zuständig ist. Dieses Tourismusbüro ist in den beiden Ländern mehrheitlich für die touristische sowohl als auch für die ökonomische Vermarktung der Destination Dubai zuständig. Um die Marketingaktivitäten im Groben zu planen, wird jährlich ein Marketingkonzept erstellt, das jedoch nicht auf statistischen Werten oder einer detaillierten Marktanalyse bas...

Investigation of interaction studies of cefpirome with ACE-inhibitors in various buffers

Science.gov (United States)

Nawaz, Muhammad; Arayne, Muhammad Saeed; Sultana, Najma; Abbas, Hira Fatima

2015-02-01

This work describes a RP-HPLC method for the determination and interaction studies of cefpirome with ACE-inhibitors (captopril, enalapril and lisinopril) in various buffers. The separation and interaction of cefpirome with ACE-inhibitors was achieved on a Purospher Star, C18 (5 μm, 250 × 4.6 mm) column. Mobile phase consisted of methanol: water (80:20, v/v, pH 3.3); however, for the separation of lisinopril, it was modified to methanol-water (40:60, v/v, pH 3.3) and pumped at a flow rate of 1 mL min-1. In all cases, UV detection was performed at 225 nm. Interactions were carried out in physiological pH i.e., pH 1 (simulated gastric juice), 4 (simulated full stomach), 7.4 (blood pH) and 9 (simulated GI), drug contents were analyzed by reverse phase high performance liquid chromatography. Method was found linear in the concentration range of 1.0-50.0 μg mL-1 with correlation coefficient (r2) of 0.999. Precision (RSD%) was less than 2.0%, indicating good precision of the method and accuracy was 98.0-100.0%. Furthermore, cefpirome-ACE-inhibitors' complexes were also synthesized and results were elucidated on the basis of FT-IR, and 1H NMR. The interaction results show that these interactions are pH dependent and for the co-administration of cefpirome and ACE-inhibitors, a proper interval should be given.

19-nor vitamin-D analogs: a new class of potent inhibitors of proliferation and inducers of differentiation of human myeloid leukemia cell lines.

Science.gov (United States)

Asou, H; Koike, M; Elstner, E; Cambell, M; Le, J; Uskokovic, M R; Kamada, N; Koeffler, H P

1998-10-01

We have studied the in vitro biological activities and mechanisms of action of 1,25-dihydroxyvitamin D3 (1,25D3) and nine potent 1,25D3 analogs on proliferation and differentiation of myeloid leukemia cell lines (HL-60, retinoic acid-resistant HL-60 [RA-res HL-60], NB4 and Kasumi-1). The common novel structural motiff for almost all the analogs included removal of C-19 (19-nor); each also had unsaturation of the side chain. All the compounds were potent; for example, the concentration of analogs producing a 50% clonal inhibition (ED50) ranged between 1 x 10(-9) to 4 x 10(-11) mol/L when using the HL-60 cell line. The most active compound [1, 25(OH)2-16,23E-diene-26-trifluoro-19-nor-cholecalciferol (Ro 25-9716)] had an ED50 of 4 x 10(-11) mol/L; in contrast, the 1,25D3 produced an ED50 of 10(-9) mol/L with the HL-60 target cells. Ro 25-9716 (10(-9) mol/L, 3 days) was a strong inducer of myeloid differentiation because it caused 92% of the HL-60 cells to express CD11b and 75% of these cells to reduce nitroblue tetrazolium (NBT). This compound (10(-8) mol/L, 4 days) also caused HL-60 cells to arrest in the G1 phase of the cell cycle (88% cells in G1 v 48% of the untreated control cells). The p27(kip-1), a cyclin-dependent kinase inhibitor which is important in blocking the cell cycle, was induced more quickly and potently by Ro 25-9716 (10(-7) mol/L, 0 to 5 days) than by 1,25D3, suggesting a possible mechanism by which these analogs inhibit proliferation of leukemic growth. The NB4 promyelocytic leukemia cells cultured with the Ro 25-9716 were also inhibited in their clonal proliferation (ED50, 5 x 10(-11) mol/L) and their expression of CD11b was enhanced (80% positive [10(-9) mol/L, 4 days] v 27% untreated NB4 cells). Moreover, the combination of Ro 25-9716 (10(-9) mol/L) and all-trans retinoic acid (ATRA, 10(-7) mol/L) induced 92% of the NB4 cells to reduce NBT, whereas only 26% of the cells became NBT positive after a similar exposure to the combination of 1,25D3

Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8

Energy Technology Data Exchange (ETDEWEB)

Judge, Russell A.; Zhu, Haizhong; Upadhyay, Anup K.; Bodelle, Pierre M.; Hutchins, Charles W.; Torrent, Maricel; Marin, Violeta L.; Yu, Wenyu; Vedadi, Masoud; Li, Fengling; Brown, Peter J.; Pappano, William N.; Sun, Chaohong; Petros, Andrew M.

2016-12-08

SETD8 is a histone H4–K20 methyltransferase that plays an essential role in the maintenance of genomic integrity during mitosis and in DNA damage repair, making it an intriguing target for cancer research. While some small molecule inhibitors for SETD8 have been reported, the structural binding modes for these inhibitors have not been revealed. Using the complex structure of the substrate peptide bound to SETD8 as a starting point, different natural and unnatural amino acid substitutions were tested, and a potent (Ki 50 nM, IC50 0.33 μM) and selective norleucine containing peptide inhibitor has been obtained.

The TROVE module: a common element in Telomerase, Ro and Vault ribonucleoproteins.

Science.gov (United States)

Bateman, Alex; Kickhoefer, Valerie

2003-10-16

Ribonucleoproteins carry out a variety of important tasks in the cell. In this study we show that a number of these contain a novel module, that we speculate mediates RNA-binding. The TROVE module--Telomerase, Ro and Vault module--is found in TEP1 and Ro60 the protein components of three ribonucleoprotein particles. This novel module, consisting of one or more domains, may be involved in binding the RNA components of the three RNPs, which are telomerase RNA, Y RNA and vault RNA. A second conserved region in these proteins is shown to be a member of the vWA domain family. The vWA domain in TEP1 is closely related to the previously recognised vWA domain in VPARP a second component of the vault particle. This vWA domain may mediate interactions between these vault components or bind as yet unidentified components of the RNPs. This work suggests that a number of ribonucleoprotein components use a common RNA-binding module. The TROVE module is also found in bacterial ribonucleoproteins suggesting an ancient origin for these ribonucleoproteins.

Discovery of natural mouse serum derived HIV-1 entry inhibitor(s).

Science.gov (United States)

Wei, M; Chen, Y; Xi, J; Ru, S; Ji, M; Zhang, D; Fang, Q; Tang, B

Among rationally designed human immunodeficiency virus 1 (HIV-1) inhibitors, diverse natural factors have showed as potent anti-HIV activity in human blood. We have discovered that the boiled supernatant of healthy mouse serum could suppress HIV-1 entry, and exhibited reduced inhibitory activity after trypsin digestion. Further analysis demonstrated that only the fraction containing 10-25 K proteins could inhibit HIV-1 mediated cell-cell fusion. These results suggest that the 10-25 K protein(s) is novel natural HIV-1 entry inhibitor(s). Our findings provide important information about novel natural HIV entry inhibitors in mouse serum.

Paleogeothermal record of the Emeishan mantle plume: evidences from borehole Ro data in the Sichuan basin, SW China

Science.gov (United States)

Hu, S.

2013-12-01

The Emeishan basalt province located in the southwest of China is widely accepted to be a result of the eruption of a mantle plume at the time of middle-late Permian. If it was a mantle plume, the ambient sedimentary rocks must be heated up during the development of the mantle plume and this thermal effect must be recorded by some geothermometers in the country rocks. The vitrinite reflectance (Ro) data as a maximum paleotemperature recorder from boreholes in Sichuan basin was employed to expose the thermal regime related to the proposed Emeishan mantle plume. The Ro profiles from boreholes which drilled close to the Emeishan basalts shows a ';dog-leg' (break) style at the unconformity between the middle and the upper Permian, and the Ro profiles in the lower subsection (pre-middle Permian) shows a significantly higher slopes (gradients) than those in the upper subsection. In contrast, those Ro profiles from boreholes far away from the center of the basalt province have no break at the uncomformity. Based on the chemical kinetic model of Ro, the paleo-temperature gradients for the upper and the lower subsections in different boreholes, as well as the erosion at the unconformity between the middle and the upper Permian, were reconstructed to reveal the variations of the temperature gradients and erosion thickness with geological time and space. Both the thermal regime and the erosion thickness together with their spatial variation (structure) provide strong geothermal evidence for the existence of the Emeishan mantle plume in the middle-late Permian.

Phosphodiesterase 4 inhibitor and phosphodiesterase 5 inhibitor combination therapy has antifibrotic and anti-inflammatory effects in mdx mice with Duchenne muscular dystrophy.

Science.gov (United States)

Nio, Yasunori; Tanaka, Masayuki; Hirozane, Yoshihiko; Muraki, Yo; Okawara, Mitsugi; Hazama, Masatoshi; Matsuo, Takanori

2017-12-01

Duchenne muscular dystrophy (DMD) is the most common inherited muscular dystrophy. Patients experience DMD in their 20s from cardiac or respiratory failure related to progressive muscle wasting. Currently, the only treatments for the symptoms of DMD are available. Muscle fibrosis, a DMD feature, leads to reduced muscle function and muscle mass, and hampers pharmaceutical therapeutic efficacy. Although antifibrotic agents may be useful, none is currently approved. Phosphodiesterase 4 (PDE4) inhibitors have exhibited antifibrotic effects in human and animal models. In this study, we showed beneficial effects of the PDE4 inhibitor piclamilast in the DMD mdx mouse. Piclamilast reduced the mRNA level of profibrotic genes, including collagen 1A1, in the gastrocnemius and diaphragm, in the mdx mouse, and significantly reduced the Sirius red staining area. The PDE5 inhibitors sildenafil and tadalafil ameliorated functional muscle ischemia in boys with DMD, and sildenafil reversed cardiac dysfunction in the mdx mouse. Single-treatment piclamilast or sildenafil showed similar antifibrotic effects on the gastrocnemius; combination therapy showed a potent antifibrotic effect, and piclamilast and combination therapy increased peroxisome proliferator-activated receptor γ coactivator-1α mRNA in mouse gastrocnemius. In summary, we confirmed that piclamilast has significant antifibrotic effects in mdx mouse muscle and is a potential treatment for muscle fibrosis in DMD.-Nio, Y., Tanaka, M., Hirozane, Y., Muraki, Y., Okawara, M., Hazama, M., Matsuo, T. Phosphodiesterase 4 inhibitor and phosphodiesterase 5 inhibitor combination therapy has antifibrotic and anti-inflammatory effects in mdx mice with Duchenne muscular dystrophy. © FASEB.

Metabolite analysis of [11C]Ro15-4513 in mice, rats, monkeys and humans

International Nuclear Information System (INIS)

Kida, T.; Noguchi, J.; Zhang, M.-R.; Suhara, T.; Suzuki, K.

2003-01-01

We performed in vitro and in vivo assays of the metabolism of [ 11 C]Ro15-4513 over time in the plasma of mice, rats, monkeys and humans, using a radio-HPLC equipped with a sensitive positron detector, in order to compare the metabolic rates of the radiopharmaceutical agent among the different animal species and to establish a highly sensitive analytical method for the radiotracer agent. We also examined the metabolism of [ 11 C]Ro15-4513 in the brain tissue of mice and rats. The analytical method used in this study permitted detection of even extremely low levels of radioactivity (approximately 5,000 dpm). In vitro experiments revealed that [ 11 C]Ro15-4513 in the blood was metabolized to hydrolysate [ 11 C]A. The species were classified in descending order of the metabolic rate of the radiotracer in vitro as follows; mice, rats, and monkeys/humans. In the in vitro experiment, the percentage of the unchanged drug in the plasma at 60 minutes postdose was 9% in mice, 70% in rats, 97% in monkeys, and 98% in humans. In vivo metabolite analysis in the blood showed the presence of two radioactive metabolites, consisting of one hydrolysate [ 11 C]A and another unidentified substance. The species were classified in descending order of the metabolic rate of the radiotracer in vivo as follows; mice, rats/humans, and monkeys. The percentage of the unchanged drug in the plasma was 6% in mice, 21% in rats, 26% in humans, and 40% in monkeys. Furthermore, the in vitro and in vivo experiments conducted to analyze the metabolism of [ 11 C]Ro15-4513 in the brain tissue of mice and rats revealed that the radiotracer was metabolized to some extent in the brain tissue of these animals. In the in vivo experiment, the percentage of the unchanged drug at 60 min postdose was 86% in the brain tissue of mice and 88% in the brain tissue of rats, while in the in vitro experiment, the corresponding percentage was 93% in mice, and 91% in rats

Partial agonist of benzodiazepine receptors Ro 19-2088 elicits withdrawal symptoms after short-term administration in immature rats

Czech Academy of Sciences Publication Activity Database

Kubová, Hana; Mareš, Pavel

2012-01-01

Roč. 61, č. 3 (2012), s. 319-323 ISSN 0862-8408 R&D Projects: GA ČR(CZ) GA305/09/0846; GA ČR(CZ) GBP304/12/G069 Institutional research plan: CEZ:AV0Z50110509 Institutional support: RVO:67985823 Keywords : Ro 19-2088 * iatrogenic withdrawal * pentylentetrazol-induced seizures * immature rats Subject RIV: FH - Neurology Impact factor: 1.531, year: 2012

Supercritical Fluid Extraction of Cynaropicrin and 20-Hydroxyecdysone from Leuzea carthamoides DC

Czech Academy of Sciences Publication Activity Database

Sovová, Helena; Opletal, L.; Sajfrtová, Marie; Bártlová, Milena

2008-01-01

Roč. 31, č. 8 (2008), s. 1387-1392 ISSN 1615-9306 R&D Projects: GA ČR GA104/06/1174; GA MŠk 2B06024 Institutional research plan: CEZ:AV0Z40720504 Keywords : 20-hydroxyecdysone * cynaropicrin * leuzea carthamoides Subject RIV: CI - Industrial Chemistry, Chemical Engineering Impact factor: 2.746, year: 2008

Inventory of Onshore Hydrocarbon Seeps in Romania (HYSED-RO Database

Directory of Open Access Journals (Sweden)

Artur Ionescu

2017-06-01

Full Text Available Seeps are the expression of the migration of hydrocarbons from subsurface accumulations to the surface in sedimentary basins. They may represent an important indication of the presence of petroleum (gas and oil reservoirs and faults, and are a natural source of greenhouse gas (methane and atmospheric pollutants (ethane, propane to the atmosphere. Romania is one of the countries with the largest number of seeps in the world, due to the high petroleum potential and active tectonics. Based on a review of the available literature, and on the field surveys performed by the authors during the last 17 years, we report the first comprehensive GIS-based inventory of 470 seeps in Romania (HYSED-RO, including gas seeps (10.4% of the total, oil seeps (11.7%, mud volcanoes (50.4%, gas-rich springs (12.6%, asphalt (solid seeps (4.3%, unclassified manifestations (4.0%, and uncertain seeps (6.6%. Seeps are typically located in correspondence with major faults and vertical and fractured stratigraphic contacts associated to petroleum reservoirs (anticlines in low heat flow areas, and their gas-geochemistry reflects that of the subsurface reservoirs. The largest and most active seeps occur in the Carpathian Foredeep, where they release thermogenic gas, and subordinately in the Transylvanian Basin, where gas is mainly microbial. HYSED-RO may represent a key reference for baseline characterization prior to subsurface petroleum extraction, for environmental studies, and atmospheric greenhouse gas emission estimates in Romania.

Ke stému ročníku Chemických Listů

Czech Academy of Sciences Publication Activity Database

Holý, Petr

2006-01-01

Roč. 100, č. 4 (2006), s. 227-232 ISSN 0009-2770 Keywords : history and significance of the journal * notable members of editorial board Subject RIV: CC - Organic Chemistry Impact factor: 0.431, year: 2006

Brain perfusion imaging using a Reconstruction-of-Difference (RoD) approach for cone-beam computed tomography

Science.gov (United States)

Mow, M.; Zbijewski, W.; Sisniega, A.; Xu, J.; Dang, H.; Stayman, J. W.; Wang, X.; Foos, D. H.; Koliatsos, V.; Aygun, N.; Siewerdsen, J. H.

2017-03-01

Purpose: To improve the timely detection and treatment of intracranial hemorrhage or ischemic stroke, recent efforts include the development of cone-beam CT (CBCT) systems for perfusion imaging and new approaches to estimate perfusion parameters despite slow rotation speeds compared to multi-detector CT (MDCT) systems. This work describes development of a brain perfusion CBCT method using a reconstruction of difference (RoD) approach to enable perfusion imaging on a newly developed CBCT head scanner prototype. Methods: A new reconstruction approach using RoD with a penalized-likelihood framework was developed to image the temporal dynamics of vascular enhancement. A digital perfusion simulation was developed to give a realistic representation of brain anatomy, artifacts, noise, scanner characteristics, and hemo-dynamic properties. This simulation includes a digital brain phantom, time-attenuation curves and noise parameters, a novel forward projection method for improved computational efficiency, and perfusion parameter calculation. Results: Our results show the feasibility of estimating perfusion parameters from a set of images reconstructed from slow scans, sparse data sets, and arc length scans as short as 60 degrees. The RoD framework significantly reduces noise and time-varying artifacts from inconsistent projections. Proper regularization and the use of overlapping reconstructed arcs can potentially further decrease bias and increase temporal resolution, respectively. Conclusions: A digital brain perfusion simulation with RoD imaging approach has been developed and supports the feasibility of using a CBCT head scanner for perfusion imaging. Future work will include testing with data acquired using a 3D-printed perfusion phantom currently and translation to preclinical and clinical studies.

Oscillations in roAp and & Scuti Stars : Theory and observations

OpenAIRE

Pinheiro, Fernando Jorge Gutiérrez

1999-01-01

As estrelas d Scuti e as estrelas roAp encontram-se na região da Faixa de Instabilidade das Cefeides que é atravessada pela Sequência principal. Cada tipo de estrelas apresenta frequências de oscilação que o outro género de estrelas não apresenta. Estas oscilações dependem da estrutura das estrelas, e podem ser descritas pelos modelos apropriados.De modo inverso, podemos a partir de observações obter as características de uma estrela, usando os modelos adequados.Discutiremos os modos de obter...

Plasminogen activator inhibitor-1 polymers, induced by inactivating amphipathic organochemical ligands

DEFF Research Database (Denmark)

Pedersen, Katrine E; Einholm, Anja P; Christensen, Anni

2003-01-01

Negatively charged organochemical inactivators of the anti-proteolytic activity of plasminogen activator inhibitor-1 (PAI-1) convert it to inactive polymers. As investigated by native gel electrophoresis, the size of the PAI-1 polymers ranged from dimers to multimers of more than 20 units. As com...

PI3Kδ inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kδ and BTK inhibitors.

Directory of Open Access Journals (Sweden)

Anella Yahiaoui

Full Text Available Activated B-cell-like diffuse large B-cell lymphoma relies on B-cell receptor signaling to drive proliferation and survival. Downstream of the B-cell receptor, the key signaling kinases Bruton's tyrosine kinase and phosphoinositide 3-kinase δ offer opportunities for therapeutic intervention by agents such as ibrutinib, ONO/GS-4059, and idelalisib. Combination therapy with such targeted agents could provide enhanced efficacy due to complimentary mechanisms of action. In this study, we describe both the additive interaction of and resistance mechanisms to idelalisib and ONO/GS-4059 in a model of activated B-cell-like diffuse large B-cell lymphoma. Significant tumor regression was observed with a combination of PI3Kδ and Bruton's tyrosine kinase inhibitors in the mouse TMD8 xenograft. Acquired resistance to idelalisib in the TMD8 cell line occurred by loss of phosphatase and tensin homolog and phosphoinositide 3-kinase pathway upregulation, but not by mutation of PIK3CD. Sensitivity to idelalisib could be restored by combining idelalisib and ONO/GS-4059. Further evaluation of targeted inhibitors revealed that the combination of idelalisib and the phosphoinositide-dependent kinase-1 inhibitor GSK2334470 or the AKT inhibitor MK-2206 could partially overcome resistance. Characterization of acquired Bruton's tyrosine kinase inhibitor resistance revealed a novel tumor necrosis factor alpha induced protein 3 mutation (TNFAIP3 Q143*, which led to a loss of A20 protein, and increased p-IκBα. The combination of idelalisib and ONO/GS-4059 partially restored sensitivity in this resistant line. Additionally, a mutation in Bruton's tyrosine kinase at C481F was identified as a mechanism of resistance. The combination activity observed with idelalisib and ONO/GS-4059, taken together with the ability to overcome resistance, could lead to a new therapeutic option in activated B-cell-like diffuse large B-cell lymphoma. A clinical trial is currently underway to

Mathematical Verification for Transmission Performance of Centralized Lightwave WDM-RoF-PON with Quintuple Services Integrated in Each Wavelength Channel

Directory of Open Access Journals (Sweden)

Shuai Chen

2015-01-01

Full Text Available Wavelength-division-multiplexing passive-optical-network (WDM-PON has been recognized as a promising solution of the “last mile” access as well as multibroadband data services access for end users, and WDM-RoF-PON, which employs radio-over-fiber (RoF technique in WDM-PON, is even a more attractive approach for future broadband fiber and wireless access for its strong availability of centralized multiservices transmission operation and its transparency for bandwidth and signal modulation formats. As for multiservices development in WDM-RoF-PON, various system designs have been reported and verified via simulation or experiment till now, and the scheme with multiservices transmitted in each single wavelength channel is believed as the one that has the highest bandwidth efficiency; however, the corresponding mathematical verification is still hard to be found in state-of-the-art literature. In this paper, system design and data transmission performance of a quintuple services integrated WDM-RoF-PON which jointly employs carrier multiplexing and orthogonal modulation techniques, have been theoretically analyzed and verified in detail; moreover, the system design has been duplicated and verified experimentally and the theory system of such WDM-RoF-PON scheme has thus been formed.

A modified CoRoT detrend algorithm and the discovery of a new planetary companion

Science.gov (United States)

Boufleur, Rodrigo C.; Emilio, Marcelo; Janot-Pacheco, Eduardo; Andrade, Laerte; Ferraz-Mello, Sylvio; do Nascimento, José-Dias, Jr.; de La Reza, Ramiro

2018-01-01

We present MCDA, a modification of the COnvection ROtation and planetary Transits (CoRoT) detrend algorithm (CDA) suitable to detrend chromatic light curves. By means of robust statistics and better handling of short-term variability, the implementation decreases the systematic light-curve variations and improves the detection of exoplanets when compared with the original algorithm. All CoRoT chromatic light curves (a total of 65 655) were analysed with our algorithm. Dozens of new transit candidates and all previously known CoRoT exoplanets were rediscovered in those light curves using a box-fitting algorithm. For three of the new cases, spectroscopic measurements of the candidates' host stars were retrieved from the ESO Science Archive Facility and used to calculate stellar parameters and, in the best cases, radial velocities. In addition to our improved detrend technique, we announce the discovery of a planet that orbits a 0.79_{-0.09}^{+0.08} R⊙ star with a period of 6.718 37 ± 0.000 01 d and has 0.57_{-0.05}^{+0.06} RJ and 0.15 ± 0.10 MJ. We also present the analysis of two cases in which parameters found suggest the existence of possible planetary companions.

[Proton pump inhibitors in gastro-oesophageal reflux disease: what is the further step?].

Science.gov (United States)

Simon, Mireille; Zerbib, Frank

2013-01-01

Optimisation of proton pump inhibitors use may improve reflux symptoms in 20-25% of the patients. Pathological gastro-oesophageal reflux should be documented in a patient with refractory reflux symptoms using upper endoscopy and/or pH testing. While on proton pump inhibitors twice daily, persistent symptoms are not related to gastro-oesophageal refluxdisease(GERD) in 50% of the patients. The new anti-reflux compounds have yet a limited efficacy and side effects that currently limit their development. Copyright © 2012. Published by Elsevier Masson SAS.

Adsorção dos corantes RO16, RR2 e RR141 utilizando lodo residual da indústria têxtil Adsorption of dyes RO16, RR2 and RR141 using residual sludge of textile industry

Directory of Open Access Journals (Sweden)

Andressa Regina Vasques

2011-09-01

Full Text Available A adsorção é uma das técnicas empregadas com sucesso para remoção efetiva da cor presente em efluentes têxteis. Com o objetivo de avaliar os diferentes parâmetros adsortivos, bem como determinar a eficiência de um adsorvente alternativo desenvolvido a partir de lodo residual têxtil na remoção de corantes, foram determinadas curvas de cinética de adsorção e isotermas. Por meio dos dados cinéticos e de equilíbrio obtidos, verificou-se que a 25ºC a adsorção foi favorável para todos os corantes, sendo esta a melhor condição para os corantes RO16 e RR2 na ausência de sais. Para o corante RR141, a adição de NaCl aumentou a capacidade de adsorção do adsorvente no equilíbrio e a adição de Na2SO4 favoreceu a adsorção para o corante RO16, ao contrário do que se observou para os outros dois corantes. A quantidade máxima de corante adsorvida por unidade de massa de adsorvente (q max nas melhores condições adsortivas para os corantes RO16, RR2 e RR141 foi de 81,30, 53,48 e 78,74 mg.g-1, respectivamente.The adsorption is one of the techniques that have been successfully used for effective removal of the dyes present in textile effluents. With the objective to evaluate the different adsorptive parameters, as well as determining the efficiency of one alternative adsorbent in the removal of dyes, kinetics and equilibrium data of adsorption were determined. By the kinetic data and of equilibrium, it was verified that the adsorption was favorable for all the dyes in 25ºC, being the best condition for the dye RO16 and RR2 in the total absence of salt. For the dye RR141, the addition of NaCl increased the adsorption capacity of adsorbent in the equilibrium and the addition of Na2SO4 favored the adsorption for the dye RO16, in contrast to what was observed for the two other dyes. The maximum quantity of dye adsorbed per unit mass of adsorbent (q max in the best adsorptive conditions for the dyes RO16, RR2 and RR141 was of 81

Sodium-glucose cotransporter 2 (SGLT2) inhibitors and fracture risk in patients with type 2 diabetes mellitus: A meta-analysis.

Science.gov (United States)

Ruanpeng, Darin; Ungprasert, Patompong; Sangtian, Jutarat; Harindhanavudhi, Tasma

2017-09-01

Sodium-glucose cotransporter 2 (SGLT2) inhibitors could potentially alter calcium and phosphate homeostasis and may increase the risk of bone fracture. The current meta-analysis was conducted to investigate the fracture risk among patients with type 2 diabetes mellitus treated with SGLT2 inhibitors. Randomized controlled trials that compared the efficacy of SGLT2 inhibitors to placebo were identified. The risk ratios of fracture among patients who received SGLT2 inhibitors versus placebo were extracted from each study. Pooled risk ratios and 95% confidence intervals were calculated using a random-effect, Mantel-Haenszel analysis. A total of 20 studies with 8286 patients treated with SGLT2 inhibitors were included. The pooled risk ratio of bone fracture in patients receiving SGLT2 inhibitors versus placebo was 0.67 (95% confidence interval, 0.42-1.07). The pooled risk ratio for canagliflozin, dapagliflozin, and empagliflozin was 0.66 (95% confidence interval, 0.37-1.19), 0.84 (95% confidence interval, 0.22-3.18), and 0.57 (95% confidence interval, 0.20-1.59), respectively. Increased risk of bone fracture among patients with type 2 diabetes mellitus treated with SGLT2 inhibitors compared with placebo was not observed in this meta-analysis. However, the results were limited by short duration of treatment/follow-up and low incidence of the event of interest. Copyright © 2017 John Wiley & Sons, Ltd.

Phase I study of the mTOR inhibitor ridaforolimus and the HDAC inhibitor vorinostat in advanced renal cell carcinoma and other solid tumors.

Science.gov (United States)

Zibelman, Matthew; Wong, Yu-Ning; Devarajan, Karthik; Malizzia, Lois; Corrigan, Alycia; Olszanski, Anthony J; Denlinger, Crystal S; Roethke, Susan K; Tetzlaff, Colleen H; Plimack, Elizabeth R

2015-10-01

Drugs inhibiting the mammalian target of rapamycin (mTOR) are approved in the treatment of renal cell carcinoma (RCC), but resistance inevitably emerges. Proposed escape pathways include increased phosphorylation of Akt, which can be down regulated by histone deacetylase (HDAC) inhibitors. We hypothesized that co-treatment with the mTOR inhibitor ridaforolimus and the HDAC inhibitor vorinostat may abrogate resistance in RCC. This phase 1 study evaluated the co-administration of ridaforolimus and vorinostat in patients with advanced solid tumors. The primary objective was to determine the maximum tolerated dose (MTD) in RCC patients. Although all solid tumors were allowed, prior cytotoxic chemotherapy was limited to 1 regimen. Using a modified 3 + 3 dose escalation design, various dose combinations were tested concurrently in separate cohorts. Efficacy was a secondary endpoint. Fifteen patients were treated at one of three dose levels, thirteen with RCC (10 clear cell, 3 papillary). Dosing was limited by thrombocytopenia. The MTD was determined to be ridaforolimus 20 mg daily days 1-5 with vorinostat 100 mg BID days 1-3 weekly, however late onset thrombocytopenia led to a lower recommended phase II dose: ridaforolimus 20 mg daily days 1-5 with vorinostat 100 mg daily days 1-3 weekly. Two patients, both with papillary RCC, maintained disease control for 54 and 80 weeks, respectively. The combination of ridaforolimus and vorinostat was tolerable at the recommended phase II dose. Two patients with papillary RCC experienced prolonged disease stabilization, thus further study of combined HDAC and mTOR inhibition in this population is warranted.

Benzodiazepine receptor binding in vivo with (/sup 3/)-Ro 15-1788

Energy Technology Data Exchange (ETDEWEB)

Goeders, N.E.; Kuhar, M.J.

1985-07-29

In vivo benzodiazepine receptor binding has generally been studied by ex vivo techniques. In this investigation, the authors identify the conditions where (/sup 3/H)-Ro 15-1788 labels benzodiazepine receptors by true in vivo binding, i.e. where workable specific to nonspecific ratios are obtained in intact tissues without homogenization or washing. (/sup 3/H)-Flunitrazepam and (/sup 3/H)-clonazepam did not exhibit useful in vivo receptor binding. 39 references, 5 figures, 1 table.

Review of serious events in cases of (suspected) child abuse and/or neglect: A RoSE by any other name?

Science.gov (United States)

Raman, Shanti; Maiese, Michelle; Vasquez, Viviana; Gordon, Paola; Jones, Jennifer M

2017-08-01

Child abuse and neglect (CAN) cases presenting to health-services may be complex; when things go seriously wrong such as a child death or near miss, cases are reviewed and health-services and professionals subject to intense scrutiny. While there are a variety of mechanisms to review critical incidents in health-services no formal process for the review of cases where child protection is the primary concern exists in Australia. We aimed to develop a systematic process to review serious events in cases of suspected CAN across two health districts in Sydney, so that shared learnings could fuel system change. Drawing upon mapping, case review, literature findings and using quality improvement methodology, we developed a model named Review of Serious Events (RoSE), in suspected cases of CAN. The RoSE model has the key features of: being child focused; seeking to examine care over a period of time; using child protection staff as lead reviewers; involving health professionals/services in the review who have been involved with the child; and actioning systems change at local levels. The RoSE model was trialled through 2014-2015. Eight cases were reviewed using RoSE; cases were similar to those reviewed prior to having a model. Participant feedback from RoSE group processes was overwhelmingly positive; outputs were transparent and accessible to key stakeholders, there was mixed progress with implementation. The RoSE model is a serious case review process that is strongly child-focused, is both investigative and reflective, led by child protection experts; and can be adapted to other settings and systems. Crown Copyright © 2017. Published by Elsevier Ltd. All rights reserved.

A High-Throughput Oxidative Stress Biosensor Based on Escherichia coli roGFP2 Cells Immobilized in a k-Carrageenan Matrix

Directory of Open Access Journals (Sweden)

Lia Ooi

2015-01-01

Full Text Available Biosensors fabricated with whole-cell bacteria appear to be suitable for detecting bioavailability and toxicity effects of the chemical(s of concern, but they are usually reported to have drawbacks like long response times (ranging from hours to days, narrow dynamic range and instability during long term storage. Our aim is to fabricate a sensitive whole-cell oxidative stress biosensor which has improved properties that address the mentioned weaknesses. In this paper, we report a novel high-throughput whole-cell biosensor fabricated by immobilizing roGFP2 expressing Escherichia coli cells in a k-carrageenan matrix, for the detection of oxidative stress challenged by metalloid compounds. The E. coli roGFP2 oxidative stress biosensor shows high sensitivity towards arsenite and selenite, with wide linear range and low detection limit (arsenite: 1.0 × 10−3–1.0 × 101 mg·L−1, LOD: 2.0 × 10−4 mg·L−1; selenite: 1.0 × 10−5–1.0 × 102 mg·L−1, LOD: 5.8 × 10−6 mg·L−1, short response times (0–9 min, high stability and reproducibility. This research is expected to provide a new direction in performing high-throughput environmental toxicity screening with living bacterial cells which is capable of measuring the bioavailability and toxicity of environmental stressors in a friction of a second.

Lack of immunotoxicity of saquinavir (Ro 31-8959) used alone or in double or triple combination with AZT and ddC.

Science.gov (United States)

Viora, M; Di Genova, G; Quaranta, M G; Boirivant, M; Camponeschi, B

1998-09-01

Saquinavir (Ro 31-8959; SQV) has been demonstrated to be a potent inhibitor of human immunodeficiency virus (HIV) proteinases and acts synergistically with dideoxynucleoside analogues. The aim of this study was to investigate the in vitro immunomodulatory effects of SQV on normal human peripheral blood mononuclear cells (PBMC) and on lamina propria mononuclear cells (LPMC). We used the drug either alone or in double and triple combination with AZT and ddC to assess whether SQV enhances the immunomodulatory effects induced by AZT and ddC that we previously observed. We demonstrated that SQV did not induce any modulation of the proliferative response either in PBMC or in LPMC. Similarly, NK cell-mediated cytotoxic activity and cytokine production were not modified by SQV. More importantly, SQV/AZT, SQV/ddC, and SQV/AZT/ddC combinations did not strengthen neither the inhibition of PBMC and LPMC proliferative response or the modulation of cytokine production induced by AZT, ddC, and AZT/ddC. On the other hand, the increased IL-2 production induced by AZT and ddC was not observed adding SQV to the dideoxynucleoside analogues. In conclusion, we demonstrated that SQV used in combination with AZT and ddC did not add any further immunotoxicity.

The TROVE module: A common element in Telomerase, Ro and Vault ribonucleoproteins

Directory of Open Access Journals (Sweden)

Bateman Alex

2003-10-01

Full Text Available Abstract Background Ribonucleoproteins carry out a variety of important tasks in the cell. In this study we show that a number of these contain a novel module, that we speculate mediates RNA-binding. Results The TROVE module – Telomerase, Ro and Vault module – is found in TEP1 and Ro60 the protein components of three ribonucleoprotein particles. This novel module, consisting of one or more domains, may be involved in binding the RNA components of the three RNPs, which are telomerase RNA, Y RNA and vault RNA. A second conserved region in these proteins is shown to be a member of the vWA domain family. The vWA domain in TEP1 is closely related to the previously recognised vWA domain in VPARP a second component of the vault particle. This vWA domain may mediate interactions between these vault components or bind as yet unidentified components of the RNPs. Conclusions This work suggests that a number of ribonucleoprotein components use a common RNA-binding module. The TROVE module is also found in bacterial ribonucleoproteins suggesting an ancient origin for these ribonucleoproteins.

An Intercomparison of GPS RO Retrievals with Colocated Analysis and In Situ Observations within Tropical Cyclones

Directory of Open Access Journals (Sweden)

Henry R. Winterbottom

2010-01-01

Full Text Available Observations from four Global Position System (GPS Radio Occultation (RO missions: Global Positioning System/Meteorology, CHAallenging Minisatellite Payload, Satellite de Aplicaciones Cientificas-C, and Constellation Observing System for Meteorology, Ionosphere and Climate and Taiwan's FORMOsa SATellite Mission #3 (COSMIC/FORMOSAT-3 are collected within a 600 km radius and ±180 minute temporal window of all observed tropical cyclones (TCs from 1995 to 2006 that were recorded in the global hurricane best-track reanalysis data set (Jarvinen et al. (1984; Davis et al. (1984. A composite analysis of tropical cyclone radial mean temperature and water vapor profiles is carried out using the GPS RO retrievals which are colocated with global analysis profiles and available in situ radiosonde observations. The differences between the respective observations and analysis profiles are quantified and the preliminary results show that the observations collected within TCs correspond favorably with both the analysis and radiosonde profiles which are colocated. It is concluded that GPS RO observations will contribute significantly to the understanding and modeling of TC structures, especially those related to vertical variability of the atmospheric state within TCs.

The effect of chemical anti-inhibitors on fibrinolytic enzymes and inhibitors

DEFF Research Database (Denmark)

Sidelmann, Johannes Jakobsen; Jespersen, J; Kluft, C

1997-01-01

proteases. We studied the influence of chemical anti-inhibitors (chloramine T, flufenamate, sodium lauryl sulfate, and methylamine) on fibrinolytic serine proteases and fibrinolytic enzyme inhibitors using the physiological substrate fibrin as plasmin substrate. Low concentrations of chloramine T (0.01 mmol......%) and plasminogen activators (apparent recovery > 200%). Sodium lauryl sulfate eliminates the major fibrinolytic enzyme inhibitors, but increases the activity of plasmin (apparent recovery > 200%) and plasminogen activator, urokinase type (apparent recovery 130%). Methylamine affects only plasmin inhibition. We...

An Automated Planning Model for RoF Heterogeneous Wireless Networks

DEFF Research Database (Denmark)

Shawky, Ahmed; Bergheim, Hans; Ragnarsson, Ólafur

2010-01-01

The number of users in wireless WANs is increasing like never before, at the same time as the bandwidth demands by users increase.The structure of the third generation Wireless WANs makes it expensive for Wireless ISPs to meet these demands.The FUTON architecture is a RoF heterogeneous wireless...... network architecture under development,that will be cheaper to deploy and operate.This paper shows a method to plan an implementation of this architecture.The planning is done as automatic as possible,covering radio planning, fiber planning and network dimensioning. The out come of the paper is a planning...

A close insight to factor VIII inhibitor in the congenital hemophilia A.

Science.gov (United States)

Tabriznia-Tabrizi, Shamsoreza; Gholampour, Marzie; Mansouritorghabeh, Hassan

2016-09-01

Hemophilia A (HA) has an X-linked pattern of inheritance and is the most common of the hemorrhagic disorders. HA is caused by a decreased or deficiency of the functional clotting factor VIII (FVIII) and effects 1 in 5000-10,000 male births. The common treatment for hemophilia is replacement therapy by plasma-derived or recombinant FVIII. Approximately 20-30% of people with a severe type of HA develop an inhibitor and this phenomenon is the main challenge in the management of these patients. Genetic factors and environmental determinants contribute to inhibitor development. Here, the roles of various genetic and environmental factors such as the type of FVIII concentrate used, the number of exposure days, and peak treatment time will be discussed in detail. It seems this information is helpful for hematologists. A literature review was done in January 2016 on PubMed and Scopus using the following keywords:' h(a)emophilia A & factor VIII inhibitor', 'h(a)emophilia A & factor VIII alloantibody', 'h(a)emophilia A & inhibitor'. There was no time limitation; however, there was an English language limitation placed on the articles selected. Expert commentary: Influential genetic and environmental factors in developing inhibitors have been discussed. Most of the risk factors are related to previously untreated patients with hemophili.

Combined effects of EGFR tyrosine kinase inhibitors and vATPase inhibitors in NSCLC cells

Energy Technology Data Exchange (ETDEWEB)

Jin, Hyeon-Ok [KIRAMS Radiation Biobank, Korea Institute of Radiological and Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul, 139–706 (Korea, Republic of); Hong, Sung-Eun [Division of Radiation Cancer Research, Korea Institute of Radiological and Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul, 139–706 (Korea, Republic of); Kim, Chang Soon [Department of Microbiological Engineering, Kon-Kuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul, 143–701 (Korea, Republic of); Park, Jin-Ah; Kim, Jin-Hee; Kim, Ji-Young; Kim, Bora [KIRAMS Radiation Biobank, Korea Institute of Radiological and Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul, 139–706 (Korea, Republic of); Chang, Yoon Hwan; Hong, Seok-Il; Hong, Young Jun [Department of Laboratory Medicine, Korea Cancer Center Hospital, Korea Institute of Radiological and Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul, 139–706 (Korea, Republic of); Park, In-Chul, E-mail: parkic@kirams.re.kr [Division of Radiation Cancer Research, Korea Institute of Radiological and Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul, 139–706 (Korea, Republic of); Lee, Jin Kyung, E-mail: jklee@kirams.re.kr [KIRAMS Radiation Biobank, Korea Institute of Radiological and Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul, 139–706 (Korea, Republic of); Department of Laboratory Medicine, Korea Cancer Center Hospital, Korea Institute of Radiological and Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul, 139–706 (Korea, Republic of)

2015-08-15

Despite excellent initial clinical responses of non-small cell lung cancer (NSCLC) patients to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs), many patients eventually develop resistance. According to a recent report, vacuolar H + ATPase (vATPase) is overexpressed and is associated with chemotherapy drug resistance in NSCLC. We investigated the combined effects of EGFR TKIs and vATPase inhibitors and their underlying mechanisms in the regulation of NSCLC cell death. We found that combined treatment with EGFR TKIs (erlotinib, gefitinib, or lapatinib) and vATPase inhibitors (bafilomycin A1 or concanamycin A) enhanced synergistic cell death compared to treatments with each drug alone. Treatment with bafilomycin A1 or concanamycin A led to the induction of Bnip3 expression in an Hif-1α dependent manner. Knock-down of Hif-1α or Bnip3 by siRNA further enhanced cell death induced by bafilomycin A1, suggesting that Hif-1α/Bnip3 induction promoted resistance to cell death induced by the vATPase inhibitors. EGFR TKIs suppressed Hif-1α and Bnip3 expression induced by the vATPase inhibitors, suggesting that they enhanced the sensitivity of the cells to these inhibitors by decreasing Hif-1α/Bnip3 expression. Taken together, we conclude that EGFR TKIs enhance the sensitivity of NSCLC cells to vATPase inhibitors by decreasing Hif-1α/Bnip3 expression. We suggest that combined treatment with EGFR TKIs and vATPase inhibitors is potentially effective for the treatment of NSCLC. - Highlights: • Co-treatment with EGFR TKIs and vATPase inhibitors induces synergistic cell death • EGFR TKIs enhance cell sensitivity to vATPase inhibitors via Hif-1α downregulation • Co-treatment of these inhibitors is potentially effective for the treatment of NSCLC.

ROS inhibitor N-acetyl-L-cysteine antagonizes the activity of proteasome inhibitors.

Science.gov (United States)

Halasi, Marianna; Wang, Ming; Chavan, Tanmay S; Gaponenko, Vadim; Hay, Nissim; Gartel, Andrei L

2013-09-01

NAC (N-acetyl-L-cysteine) is commonly used to identify and test ROS (reactive oxygen species) inducers, and to inhibit ROS. In the present study, we identified inhibition of proteasome inhibitors as a novel activity of NAC. Both NAC and catalase, another known scavenger of ROS, similarly inhibited ROS levels and apoptosis associated with H₂O₂. However, only NAC, and not catalase or another ROS scavenger Trolox, was able to prevent effects linked to proteasome inhibition, such as protein stabilization, apoptosis and accumulation of ubiquitin conjugates. These observations suggest that NAC has a dual activity as an inhibitor of ROS and proteasome inhibitors. Recently, NAC was used as a ROS inhibitor to functionally characterize a novel anticancer compound, piperlongumine, leading to its description as a ROS inducer. In contrast, our own experiments showed that this compound depicts features of proteasome inhibitors including suppression of FOXM1 (Forkhead box protein M1), stabilization of cellular proteins, induction of ROS-independent apoptosis and enhanced accumulation of ubiquitin conjugates. In addition, NAC, but not catalase or Trolox, interfered with the activity of piperlongumine, further supporting that piperlongumine is a proteasome inhibitor. Most importantly, we showed that NAC, but not other ROS scavengers, directly binds to proteasome inhibitors. To our knowledge, NAC is the first known compound that directly interacts with and antagonizes the activity of proteasome inhibitors. Taken together, the findings of the present study suggest that, as a result of the dual nature of NAC, data interpretation might not be straightforward when NAC is utilized as an antioxidant to demonstrate ROS involvement in drug-induced apoptosis.

A 0.8-2.4 μm Transmission spectrum of the hot Jupiter CoRoT-1b

Energy Technology Data Exchange (ETDEWEB)

Schlawin, E.; Herter, T. [Astronomy Department, Cornell University, Ithaca, NY 14853 (United States); Zhao, M. [Department of Astronomy, Pennsylvania State University, University Park, PA 16802 (United States); Teske, J. K. [Astronomy Department, The University of Arizona, Tucson, AZ 85721 (United States)

2014-03-01

Hot Jupiters with brightness temperatures ≳2000 K can have TiO and VO molecules as gaseous species in their atmospheres. The TiO and VO molecules can potentially induce temperature inversions in hot Jupiter atmospheres and also have an observable signature of large optical to infrared transit depth ratios. Previous transmission spectra of very hot Jupiters have shown a lack of TiO and VO, but only in planets that also appear to lack temperature inversions. We measure the transmission spectrum of CoRoT-1b, a hot Jupiter that was predicted to have a temperature inversion potentially due to significant TiO and VO in its atmosphere. We employ the multi-object spectroscopy method using the SpeX and MORIS instruments on the Infrared Telescope Facility (IRTF) and the Gaussian process method to model red noise. By using a simultaneous reference star on the slit for calibration and a wide slit to minimize slit losses, we achieve transit depth precision of 0.03%-0.09%, comparable to the atmospheric scale height but detect no statistically significant molecular features. We combine our IRTF data with optical CoRoT transmission measurements to search for differences in the optical and near-infrared absorption that would arise from TiO/VO. Our IRTF spectrum and the CoRoT photometry disfavor a TiO/VO-rich spectrum for CoRoT-1b, suggesting that the atmosphere has another absorber that could create a temperature inversion or that the blackbody-like emission from the planet is due to a spectroscopically flat cloud, dust, or haze layer that smoothes out molecular features in both CoRoT-1b's emission and transmission spectra. This system represents the faintest planet hosting star (K = 12.2) with a measured planetary transmission spectrum.

Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitors.

Directory of Open Access Journals (Sweden)

Hannes C A Drexler

Full Text Available Cells adapt to endoplasmic reticulum (ER-stress by arresting global protein synthesis while simultaneously activating specific transcription factors and their downstream targets. These processes are mediated in part by the phosphorylation-dependent inactivation of the translation initiation factor eIF2alpha. Following restoration of homeostasis protein synthesis is resumed when the serine/threonine-protein phosphatase PP1 dephosphorylates and reactivates eIF2alpha. Proteasome inhibitors, used to treat multiple myeloma patients evoke ER-stress and apoptosis by blocking the ER-associated degradation of misfolded proteins (ERAD, however, the role of eIF2alpha phosphorylation in leukemic cells under conditions of proteasome inhibitor-mediated ER stress is currently unclear.Bcr-Abl-positive and negative leukemic cell lines were used to investigate the functional implications of PP1-related phosphatase activities on eIF2alpha phosphorylation in proteasome inhibitor-mediated ER stress and apoptosis. Rather unexpectedly, salubrinal, a recently identified PP1 inhibitor capable to protect against ER stress in various model systems, strongly synergized with proteasome inhibitors to augment apoptotic death of different leukemic cell lines. Salubrinal treatment did not affect the phosphorlyation status of eIF2alpha. Furthermore, the proapoptotic effect of salubrinal occurred independently from the chemical nature of the proteasome inhibitor, was recapitulated by a second unrelated phosphatase inhibitor and was unaffected by overexpression of a dominant negative eIF2alpha S51A variant that can not be phosphorylated. Salubrinal further aggravated ER-stress and proteotoxicity inflicted by the proteasome inhibitors on the leukemic cells since characteristic ER stress responses, such as ATF4 and CHOP synthesis, XBP1 splicing, activation of MAP kinases and eventually apoptosis were efficiently abrogated by the translational inhibitor cycloheximide.Although PP1

RoMo: An efficient strategy for functional mosaic analysis via stochastic Cre recombination and gene targeting in the ROSA26 locus.

Science.gov (United States)

Movahedi, Kiavash; Wiegmann, Robert; De Vlaminck, Karen; Van Ginderachter, Jo A; Nikolaev, Viacheslav O

2018-07-01

Functional mosaic analysis allows for the direct comparison of mutant cells with differentially marked control cells in the same organism. While this offers a powerful approach for elucidating the role of specific genes or signalling pathways in cell populations of interest, genetic strategies for generating functional mosaicism remain challenging. We describe a novel and streamlined approach for functional mosaic analysis, which combines stochastic Cre/lox recombination with gene targeting in the ROSA26 locus. With the RoMo strategy a cell population of interest is randomly split into a cyan fluorescent and red fluorescent subset, of which the latter overexpresses a chosen transgene. To integrate this approach into high-throughput gene targeting initiatives, we developed a procedure that utilizes Gateway cloning for the generation of new targeting vectors. RoMo can be used for gain-of-function experiments or for altering signaling pathways in a mosaic fashion. To demonstrate this, we developed RoMo-dnGs mice, in which Cre-recombined red fluorescent cells co-express a dominant-negative Gs protein. RoMo-dnGs mice allowed us to inhibit G protein-coupled receptor activation in a fraction of cells, which could then be directly compared to differentially marked control cells in the same animal. We demonstrate how RoMo-dnGs mice can be used to obtain mosaicism in the brain and in peripheral organs for various cell types. RoMo offers an efficient new approach for functional mosaic analysis that extends the current toolbox and may reveal important new insights into in vivo gene function. © 2018 Wiley Periodicals, Inc.

Water Quality of Hills Water, Supply Water and RO Water Machine at Ulu Yam Selangor

Science.gov (United States)

Ngadiman, N.; ‘I Bahari, N.; Kaamin, M.; Hamid, N. B.; Mokhtar, M.; Sahat, S.

2016-07-01

The rapid development resulted in the deterioration of the quality of drinking water in Malaysia. Recognizing the importance of water quality, new alternatives for drinking water such as mineral water processing from reverse osmosis (RO) machine become more popular. Hence, the demand for mineral water, natural spring water or water from the hills or mountains rose lately. More consumers believed the quality of these spring water better than other source of drinking water. However, the quality of all the drinking water sources is to meet the required quality standard. Therefore, this paper aims to measure the quality of the waters from hills, from RO machine and the water supply in Ulu Yam, Selangor Batang Kali, Malaysia. The water quality was determined based on following parameters: ammoniacal nitrogen (NH3), iron (Fe), turbidity (NTU) and pH. The results show that the water from hills has better quality compared to water supply and water from RO machine. The value of NH3 ranged from 0.03 mg/L- 0.67 mg/L; Fe was from 0.03mg/L - 0.12 mg/L, turbidity at 0.42 NTU - 0.88 NTU and pH is at 6.60 - 0.71. Based on the studied parameters, all three types of water are fit for drinking and have met the required national drinking water quality standard.

PD-1/PD-L1 Inhibitors for Immuno-oncology: From Antibodies to Small Molecules.

Science.gov (United States)

Geng, Qiaohong; Jiao, Peifu; Jin, Peng; Su, Gaoxing; Dong, Jinlong; Yan, Bing

2018-02-12

The recent regulatory approvals of immune checkpoint protein inhibitors, such as ipilimumab, pembrolizumab, nivolumab, atezolizumab, durvalumab, and avelumab ushered a new era in cancer therapy. These inhibitors do not attack tumor cells directly but instead mobilize the immune system to re-recognize and eradicate tumors, which endows them with unique advantages including durable clinical responses and substantial clinical benefits. PD-1/PD-L1 inhibitors, a pillar of immune checkpoint protein inhibitors, have demonstrated unprecedented clinical efficacy in more than 20 cancer types. Besides monoclonal antibodies, diverse PD- 1/PD-L1 inhibiting candidates, such as peptides, small molecules have formed a powerful collection of weapons to fight cancer. The goal of this review is to summarize and discuss the current PD-1/PD-L1 inhibitors including candidates under clinical development, their molecular interactions with PD-1 or PD-L1, the disclosed structureactivity relationships of peptides and small molecules as inhibitors. Current PD-1/PD-L1 inhibitors under clinical development are exclusively dominated by antibodies. The molecular interactions of therapeutic antibodies with PD-1 or PD-L1 have been gradually elucidated for the design of novel inhibitors. Various peptides and traditional small molecules have been investigated in preclinical model to discover novel PD-1/PD-L1 inhibitors. Peptides and small molecules may play an important role in immuno-oncology because they may bind to multiple immune checkpoint proteins via rational design, opening opportunity for a new generation of novel PD-1/PD-L1 inhibitors. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Potentiation by cholinesterase inhibitors of cholinergic activity in rat isolated stomach and colon.

Science.gov (United States)

Jarvie, Emma M; Cellek, Selim; Sanger, Gareth J

2008-01-01

Acetylcholinesterase (AChE) inhibitors stimulate gastrointestinal (GI) motility and are potential treatments of conditions associated with inadequate GI motility. The ability of itopride to facilitate neuronally (predominantly cholinergic) mediated contractions of rat isolated stomach, evoked by electrical field stimulation (EFS), has been compared with other cholinesterase inhibitors and with tegaserod, a clinically effective prokinetic and non-selective 5-HT(4) receptor agonist which also facilitates GI cholinergic function. Neostigmine greatly increased EFS-evoked contractions over a narrow concentration range (0.01-1 microM; 754+/-337% facilitation at 1 microM); higher concentrations (1, 3 microM) also increased muscle tension. Donepezil increased EFS-evoked contractions gradually over the full range of concentrations (0.01-10 microM; maximum increase 516+/-20% at 10 microM). Itopride increased the contractions even more gradually, rising to 188+/-84% at 10 microM. The butyrylcholinesterase inhibitor iso-OMPA 0.01-10 microM also increased EFS-evoked contractions, to a maximum of 36+/-5.0% at 10 microM, similar to that caused by tegaserod (35+/-5.2% increase at 1 microM). The effects of tegaserod, but not itopride were inhibited by the 5-HT(4) receptor antagonist SB-204070A 0.3 microM. In rat isolated colon, neostigmine was again the most efficacious, causing a defined maximum increase in EFS-evoked contractions (343+/-82% at 10 microM), without changing muscle tension. Maximum increases caused by donepezil and itopride were, respectively, 57.6+/-20 and 43+/-15% at 10 microM. These data indicate that the abilities of different AChE inhibitors to increase GI cholinergic activity differ markedly. Understanding the reasons is essential if AChE inhibitors are to be optimally developed as GI prokinetics.

Three-gradual pilot unit of JP3RO for cleanings and concentration of radioactive sewage by method of upturned osmosis

International Nuclear Information System (INIS)

Chmielewski, A.G.; Harasimowicz, M.; Tyminski, B.; Zakrzewska-Trznadel, G.

2001-01-01

For many years the Institute of Nuclear Chemistry and Technology has worked on the application of different membrane processes to nuclear technology. The experiments with ultrafiltration, ultrafiltration combined with chemical complexation, membrane distillation and reverse osmosis were conducted. Reverse osmosis (RO) as a method for liquid radioactive waste treatment has been examined at laboratory and pilot plant installations. Thr purification of radioactive model solutions as well as liquid low and medium level radioactive waste samples has been examined with various reverse osmotic modules equipped with thin composite polymeric membranes. The experience with the process led to design and construction of the JP3RO industrial plant, 1 m 3 capacity, composed of three RO stages. On the basis of earlier investigations, membrane modules were selected for the plant. The installation is described in this paper, and the results of experiments are presented. The JP3RO installation was included into the system of liquid low and medium-level radioactive wastes treatment at Institute of Nuclear Energy in Swierk. (author)

Symmetry-Adapted Ro-vibrational Basis Functions for Variational Nuclear Motion Calculations: TROVE Approach.

Science.gov (United States)

Yurchenko, Sergei N; Yachmenev, Andrey; Ovsyannikov, Roman I

2017-09-12

We present a general, numerically motivated approach to the construction of symmetry-adapted basis functions for solving ro-vibrational Schrödinger equations. The approach is based on the property of the Hamiltonian operator to commute with the complete set of symmetry operators and, hence, to reflect the symmetry of the system. The symmetry-adapted ro-vibrational basis set is constructed numerically by solving a set of reduced vibrational eigenvalue problems. In order to assign the irreducible representations associated with these eigenfunctions, their symmetry properties are probed on a grid of molecular geometries with the corresponding symmetry operations. The transformation matrices are reconstructed by solving overdetermined systems of linear equations related to the transformation properties of the corresponding wave functions on the grid. Our method is implemented in the variational approach TROVE and has been successfully applied to many problems covering the most important molecular symmetry groups. Several examples are used to illustrate the procedure, which can be easily applied to different types of coordinates, basis sets, and molecular systems.

In vivo and in vitro effect of Acacia nilotica seed proteinase inhibitors ...

Indian Academy of Sciences (India)

2012-05-04

May 4, 2012 ... high stability at different pH values (2.0 to 10.0) except at pH 5.0 and are thermolabile beyond 80°C for ... plant proteins like lectins, PIs and amylase inhibitors in the ..... competitive inhibition was characterized by no changes.

Active inhibitor-1 maintains protein hyper-phosphorylation in aging hearts and halts remodeling in failing hearts.

Science.gov (United States)

Pritchard, Tracy J; Kawase, Yoshiaki; Haghighi, Kobra; Anjak, Ahmad; Cai, Wenfeng; Jiang, Min; Nicolaou, Persoulla; Pylar, George; Karakikes, Ioannis; Rapti, Kleopatra; Rubinstein, Jack; Hajjar, Roger J; Kranias, Evangelia G

2013-01-01

Impaired sarcoplasmic reticulum calcium cycling and depressed contractility are key characteristics in heart failure. Defects in sarcoplasmic reticulum function are characterized by decreased SERCA2a Ca-transport that is partially attributable to dephosphorylation of its regulator phospholamban by increased protein phosphatase 1 activity. Inhibition of protein phosphatase 1 through activation of its endogenous inhibitor-1 has been shown to enhance cardiac Ca-handling and contractility as well as protect from pathological stress remodeling in young mice. In this study, we assessed the long-term effects of inducible expression of constitutively active inhibitor-1 in the adult heart and followed function and remodeling through the aging process, up to 20 months. Mice with inhibitor-1 had normal survival and similar function to WTs. There was no overt remodeling as evidenced by measures of left ventricular end-systolic and diastolic diameters and posterior wall dimensions, heart weight to tibia length ratio, and histology. Higher phosphorylation of phospholamban at both Ser16 and Thr17 was maintained in aged hearts with active inhibitor-1, potentially offsetting the effects of elevated Ser2815-phosphorylation in ryanodine receptor, as there were no increases in arrhythmias under stress conditions in 20-month old mice. Furthermore, long-term expression of active inhibitor-1 via recombinant adeno-associated virus type 9 gene transfer in rats with pressure-overload induced heart failure improved function and prevented remodeling, associated with increased phosphorylation of phospholamban at Ser16 and Thr17. Thus, chronic inhibition of protein phosphatase 1, through increases in active inhibitor-1, does not accelerate age-related cardiomyopathy and gene transfer of this molecule in vivo improves function and halts remodeling in the long term.

Screening Marker Components Of Tyrosinase Inhibitor From Xylocarpus Granatum Stem

Directory of Open Access Journals (Sweden)

Latifah K Darusman

2017-03-01

Full Text Available The aim of our research was to screen the marker components of tyrosinase inhibitor from Xylocarpus granatum stem collected from Pulau Sebuku, South Kalimantan, Indonesia.  The screening method started from selection of part of X. granatum, stem or stem bark.  Stem and stem bark of X. granatum were dried and grounded before submitted to methanol.  The stem extracts is more potent as tyrosinase inhibitor (IC50 for monophenolase is 45.12 μg/ml and diphenolase is 31.59μg/ml compared to the bark extracts. The IC50 values of kojic acid as positive control are 17.43μg/ml for monophenolase and 20.69 μg/ml for diphenolase. The stem extract then separated with silica gel column chromatography and preparative thin layer chromatography.  The results showed that component with Rf 0,25 and 0.63 (TLC analysis with stationary phase silica gel GF254 and mobile phase ethyl acetic: methanol (8:2 are the marker components as tyrosinase inhibitor for X. granatum.

Pnserpin: A Novel Serine Protease Inhibitor from Extremophile Pyrobaculum neutrophilum

Directory of Open Access Journals (Sweden)

Huan Zhang

2017-01-01

Full Text Available Serine protease inhibitors (serpins are native inhibitors of serine proteases, constituting a large protein family with members spread over eukaryotes and prokaryotes. However, only very few prokaryotic serpins, especially from extremophiles, have been characterized to date. In this study, Pnserpin, a putative serine protease inhibitor from the thermophile Pyrobaculum neutrophilum, was overexpressed in Escherichia coli for purification and characterization. It irreversibly inhibits chymotrypsin-, trypsin-, elastase-, and subtilisin-like proteases in a temperature range from 20 to 100 °C in a concentration-dependent manner. The stoichiometry of inhibition (SI of Pnserpin for proteases decreases as the temperature increases, indicating that the inhibitory activity of Pnserpin increases with the temperature. SDS-PAGE (sodium dodecyl sulfate polyacrylamide gel electrophoresis showed that Pnserpin inhibits proteases by forming a SDS-resistant covalent complex. Homology modeling and molecular dynamic simulations predicted that Pnserpin can form a stable common serpin fold. Results of the present work will help in understanding the structural and functional characteristics of thermophilic serpin and will broaden the current knowledge about serpins from extremophiles.

New global electron density observations from GPS-RO in the D- and E-Region ionosphere

Science.gov (United States)

Wu, Dong L.

2018-06-01

A novel retrieval technique is developed for electron density (Ne) in the D- and E-region (80-120 km) using the high-quality 50-Hz GPS radio occultation (GPS-RO) phase measurements. The new algorithm assumes a slow, linear variation in the F-region background when the GPS-RO passes through the D- and E-region, and extracts the Ne profiles at 80-130 km from the phase advance signal caused by Ne. Unlike the conventional Abel function, the new approach produces a sharp Ne weighting function in the lower ionosphere, and the Ne retrievals are in good agreement with the IRI (International Reference Ionosphere) model in terms of monthly maps, zonal means and diurnal variations. The daytime GPS-RO Ne profiles can be well characterized by the α-Chapman function of three parameters (NmE, hmE and H), showing that the bottom of E-region is deepening and sharpening towards the summer pole. At high latitudes the monthly GPS-RO Ne maps at 80-120 km reveal clear enhancement in the auroral zones, more prominent at night, as a result of energetic electron precipitation (EEP) from the outer radiation belt. The D-/E-region auroral Ne is strongly correlated with Kp on a daily basis. The new Ne data allow further comprehensive analyses of the sporadic E (Es) phenomena in connection with the background Ne in the E-region. The layered (2-10 km) and fluctuated (Layer than Ne_Pert, are extracted with respect to the background Ne_Region on a profile-by-profile basis. The Ne_Layer component has a strong but highly-refined peak at ∼105 km, with an amplitude smaller than Ne_Region approximately by an order of magnitude. The Ne_Pert component, which was studied extensively in the past, is ∼2 orders of magnitude weaker than Ne_Layer. Both Ne_Layer and Ne_Pert are subject to significant diurnal and semidiurnal variations, showing downward progression with local time in amplitude. The 11-year solar cycle dominates the Ne interannual variations, showing larger Ne_Region and Ne_Layer but smaller

Multimerized CHR-derived peptides as HIV-1 fusion inhibitors.

Science.gov (United States)

Nomura, Wataru; Hashimoto, Chie; Suzuki, Takaharu; Ohashi, Nami; Fujino, Masayuki; Murakami, Tsutomu; Yamamoto, Naoki; Tamamura, Hirokazu

2013-08-01

To date, several HIV-1 fusion inhibitors based on the carboxy-terminal leucine/isoleucine heptad repeat (CHR) region of an HIV-1 envelope protein gp41 have been discovered. We have shown that a synthetic peptide mimetic of a trimer form of the CHR-derived peptide C34 has potent inhibitory activity against the HIV-1 fusion mechanism, compared to a monomer C34 peptide. The present study revealed that a dimeric form of C34 is evidently structurally critical for fusion inhibitors, and that the activity of multimerized CHR-derived peptides in fusion inhibition is affected by the properties of the unit peptides C34, SC34EK, and T20. The fluorescence-based study suggested that the N36-interactive sites of the C34 trimer, including hydrophobic residues, are exposed outside the trimer and that trimerization of C34 caused a remarkable increase in fusion inhibitory activity. The present results could be useful in the design of fusion inhibitors against viral infections which proceed via membrane fusion with host cells. Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.

Small-Molecule Inhibitors of the Type III Secretion System

Directory of Open Access Journals (Sweden)

Lingling Gu

2015-09-01

Full Text Available Drug-resistant pathogens have presented increasing challenges to the discovery and development of new antibacterial agents. The type III secretion system (T3SS, existing in bacterial chromosomes or plasmids, is one of the most complicated protein secretion systems. T3SSs of animal and plant pathogens possess many highly conserved main structural components comprised of about 20 proteins. Many Gram-negative bacteria carry T3SS as a major virulence determinant, and using the T3SS, the bacteria secrete and inject effector proteins into target host cells, triggering disease symptoms. Therefore, T3SS has emerged as an attractive target for antimicrobial therapeutics. In recent years, many T3SS-targeting small-molecule inhibitors have been discovered; these inhibitors prevent the bacteria from injecting effector proteins and from causing pathophysiology in host cells. Targeting the virulence of Gram-negative pathogens, rather than their survival, is an innovative and promising approach that may greatly reduce selection pressures on pathogens to develop drug-resistant mutations. This article summarizes recent progress in the search for promising small-molecule T3SS inhibitors that target the secretion and translocation of bacterial effector proteins.

Nucleotide sequence of a cDNA coding for the barley seed protein CMa: an inhibitor of insect α-amylase

DEFF Research Database (Denmark)

Rasmussen, Søren Kjærsgård; Johansson, A.

1992-01-01

The primary structure of the insect alpha-amylase inhibitor CMa of barley seeds was deduced from a full-length cDNA clone pc43F6. Analysis of RNA from barley endosperm shows high levels 15 and 20 days after flowering. The cDNA predicts an amino acid sequence of 119 residues preceded by a signal...... peptide of 25 amino acids. Ala and Leu account for 55% of the signal peptide. CMa is 60-85% identical with alpha-amylase inhibitors of wheat, but shows less than 50% identity to trypsin inhibitors of barley and wheat. The 10 Cys residues are located in identical positions compared to the cereal inhibitor...

The flotation of Roşia Poieni copper ore in column machine, with non-polar oils addition

Directory of Open Access Journals (Sweden)

Ciocani V.

2005-11-01

Full Text Available The most important natural resource of copper in Romania is the ore deposit of Roşia Poieni. At present, the utilization of Roşia Poieni poorphyry copper ore is possible by extraction in quarry of the mass ore and mineral processing into a technological flux with modest results for the value of metal recovery in concentrate 70-72 % and an average contents of 16,5 % Cu. Our researches were directed to studies regarding test and utilisation of special procedure of flotation – addition of the non-polar oil – applied to advanced grinding ore with column type machines.

The effect of MEP pathway and other inhibitors on the intracellular localization of a plasma membrane-targeted, isoprenylable GFP reporter protein in tobacco BY-2 cells [v1; ref status: indexed, http://f1000r.es/yx

Directory of Open Access Journals (Sweden)

Michael Hartmann

2013-08-01

Full Text Available We have established an in vivo visualization system for the geranylgeranylation of proteins in a stably transformed tobacco BY-2 cell line, based on the expression of a dexamethasone-inducible GFP fused to the carboxy-terminal basic domain of the rice calmodulin CaM61, which naturally bears a CaaL geranylgeranylation motif (GFP-BD-CVIL. By using pathway-specific inhibitors it was demonstrated that inhibition of the methylerythritol phosphate (MEP pathway with known inhibitors like oxoclomazone and fosmidomycin, as well as inhibition of the protein geranylgeranyltransferase type 1 (PGGT-1, shifted the localization of the GFP-BD-CVIL protein from the membrane to the nucleus. In contrast, the inhibition of the mevalonate (MVA pathway with mevinolin did not affect the localization. During the present work, this test system has been used to examine the effect of newly designed inhibitors of the MEP pathway and inhibitors of sterol biosynthesis such as squalestatin, terbinafine and Ro48-8071. In addition, we also studied the impact of different post-prenylation inhibitors or those suspected to affect the transport of proteins to the plasma membrane on the localization of the geranylgeranylable fusion protein GFP-BD-CVIL.

La construcción de un modelo de control de la Hacienda en el primer tercio del siglo XVIII. El proyecto de José Patiño (1724-1726

Directory of Open Access Journals (Sweden)

Anne Dubet

2012-07-01

Full Text Available Este texto pretende contribuir al estudio de la cultura de los grupos dirigentes del siglo XVIII centrándose en las representaciones de los que gobiernan la Hacienda real. Se aborda el caso de José Patiño, estudiando su estrategia de acceso a la Secretaría del Despacho de la Hacienda en 1724-1726 y la construcción de su proyecto de gobierno de la Hacienda. En los años 1720, el gobierno de la Hacienda es objeto de debates y rivalidades. Mi hipótesis es que Patiño y su entorno no se distinguen tanto de sus adversarios por su proyecto económico como por su concepción del control financiero, estrechamente vinculada a la definición de las competencias del ministro y de las relaciones a mantener con los hombres de negocios. Patiño no es más moderno que su época; tampoco es original, pero tiene una visión global y coherente de la Hacienda y sabe ganarse apoyos útiles a la promoción de su proyecto.

Anti-Ro and anti-La autoantibodies induce TNF-α production by human salivary gland cells: an in vitro study

Directory of Open Access Journals (Sweden)

V. Mitolo

2011-09-01

Full Text Available Obiettivo: Lo scopo di questo studio è stato valutare la produzione di TNF-α, induttore della via estrinseca del processo apoptotico, in seguito al trattamento con gli autoanticorpi anti-Ro ed anti-La isolati da pazienti con sindrome di Sjögren primaria in un modello sperimentale rappresentato dalla linea cellulare di ghiandole salivari umane, A- 253. È stata, inoltre, valutata la presenza sulla superficie di tali cellule di recettori specifici per tale induttore, TNFR1 e TNFR2. Materiali e metodi: Gli autoanticorpi anti-La ed anti-Ro sono stati purificati su una colonna cromatografia ad alta affinità. Le metodiche utilizzate per la valutazione della produzione di TNF-α e lo studio dei recettori di superficie sono state immunofluorescenza, RT-PCR e saggi immunoenzimatici. Risultati: I nostri risultati hanno dimostrato che le cellule A-253 esprimono in superficie i recettori TNFR1 e TNFR2 e che gli autoanticorpi anti-Ro e anti-La sono in grado di indurre la produzione di TNF-α nelle stesse cellule. Conclusioni: Il trattamento con gli autoanticorpi anti-Ro ed anti-La induce la produzione di TNF-α in cellule di ghiandole salivari umane e questo potrebbe spiegare la attivazione della via estrinseca della apoptosi.

Treatment of vitiligo with the topical Janus kinase inhibitor ruxolitinib.

Science.gov (United States)

Rothstein, Brooke; Joshipura, Deep; Saraiya, Ami; Abdat, Rana; Ashkar, Huda; Turkowski, Yana; Sheth, Vaneeta; Huang, Victor; Au, Shiu Chung; Kachuk, Courtney; Dumont, Nicole; Gottlieb, Alice B; Rosmarin, David

2017-06-01

Existing therapies for vitiligo are limited in efficacy and can be associated with undesirable side effects. Topical Janus kinase inhibitors may offer a new therapeutic option for vitiligo. We sought to assess the role of topical ruxolitinib 1.5% cream, a Janus kinase inhibitor, in vitiligo treatment. This 20-week, open-label, proof-of-concept trial of twice-daily topical ruxolitinib 1.5% cream was conducted in 12 patients with a minimum of 1% affected body surface area of vitiligo. The primary outcome was percent improvement in Vitiligo Area Scoring Index from baseline to week 20. Of 12 patients screened, 11 were enrolled and 9 completed the study (54.5% men; mean age, 52 years). Four patients with significant facial involvement at baseline had a 76% improvement in facial Vitiligo Area Scoring Index scores at week 20 (95% confidence interval, 53-99%; P = .001). A 23% improvement in overall Vitiligo Area Scoring Index scores was observed in all enrolled patients at week 20 (95% confidence interval, 4-43%; P = .02). Three of 8 patients responded on body surfaces and 1 of 8 patients responded on acral surfaces. Adverse events were minor, including erythema, hyperpigmentation, and transient acne. Limitations of the study include the small sample size and open-label study design. Topical ruxolitinib 1.5% cream provided significant repigmentation in facial vitiligo and may offer a valuable new treatment for vitiligo. Copyright © 2017 American Academy of Dermatology, Inc. Published by Elsevier Inc. All rights reserved.

In vivo trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors.

Science.gov (United States)

Bacchi, C J; Brun, R; Croft, S L; Alicea, K; Bühler, Y

1996-01-01

A series of novel aromatic derivatives based on the structure of methylglyoxal bis(guanylhydrazone) (MGBG) was examined for trypanocidal activities in human and veterinary trypanosomes of African origin. One agent, CGP 40215A, a bicyclic analog of MGBG which also resembles the diamidines diminazene (Berenil) and pentamidine, was curative of infections by 19 isolates of Trypanosoma brucei subspecies as well as a Trypanosoma congolense isolate. Several of these isolates were resistant to standard trypanocides. Curative doses were < or = 25 mg/kg of body weight/day for 3 days in these acute laboratory model infections. In addition, CGP 40215A also cured a model central nervous system infection in combination with the ornithine decarboxylase inhibitor DL-alpha-difluoromethylornithine (DFMO; Ornidyl, eflornithine). Curative combinations were 14 days of oral 2% DFMO (approximately 5 g/kg/day) plus 5, 10, or 25 mg/kg/day for 3 or 7 days given by intraperitoneal injection or with a miniosmotic pump. Combinations were most effective if CGP 40215A was given in the second half or at the end of the DFMO regimen. MGBG has modest activity as an inhibitor of trypanosome S-adenosylmethionine decarboxylase (50% inhibitory concentration [IC50]. 130 microM), while CGP 40215A was a more active inhibitor (IC50, 20 microM). Preincubation of trypanosomes with CGP 40215A for 1 h caused a reduction in spermidine content (36%) and an increase in putrescine content (20%), indicating that one possible mechanism of its action may be inhibition of polyamine biosynthesis. PMID:8726018

Phosphodiesterase-5 inhibitor sildenafil preconditions adult cardiac myocytes against necrosis and apoptosis. Essential role of nitric oxide signaling.

Science.gov (United States)

Das, Anindita; Xi, Lei; Kukreja, Rakesh C

2005-04-01

We investigated the effect of sildenafil in protection against necrosis or apoptosis in cardiomyocytes. Adult mouse ventricular myocytes were treated with sildenafil (1 or 10 microM) for 1 h before 40 min of simulated ischemia (SI). Necrosis was determined by trypan blue exclusion and lactate dehydrogenase release following SI alone or plus 1 or 18 h of reoxygenation (RO). Apoptosis was assessed by terminal deoxynucleotidyl transferase-mediated nick end labeling assay and mitochondrial membrane potential measured using a fluorescent probe 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolyl-carbocyanine iodide (JC-1). Sildenafil reduced necrosis as indicated by decrease in trypan blue-positive myocytes and leakage of lactate dehydrogenase compared with untreated cells after either SI or SI-RO. The number of terminal deoxynucleotidyl transferase-mediated nick end labeling-positive myocytes or loss of JC-1 fluorescence following SI and 18 h of RO was attenuated in the sildenafil-treated group with concomitant inhibition of caspase 3 activity. An early increase in Bcl-2 to Bax ratio with sildenafil treatment was also observed in myocytes after SI-RO. The increase of Bcl-2 expression by sildenafil was inhibited by nitric-oxide synthase (NOS) inhibitor, L-nitro-amino-methyl-ester. The drug also enhanced mRNA and protein content of inducible NOS (iNOS) and endothelial NOS (eNOS) in the myocytes. Sildenafil-induced protection against necrosis and apoptosis was absent in the myocytes derived from iNOS knock-out mice and was attenuated in eNOS knock-out myocytes. The up-regulation of Bcl-2 expression by sildenafil was also absent in iNOS-deficient myocytes. Reverse transcription-PCR, Western blots, and immunohistochemical assay confirmed the expression of phosphodiesterase-5 in mouse cardiomyocytes. These data provide strong evidence for a direct protective effect of sildenafil against necrosis and apoptosis through NO signaling pathway. The results may have possible

Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives.

Science.gov (United States)

Li, C S; Black, W C; Chan, C C; Ford-Hutchinson, A W; Gauthier, J Y; Gordon, R; Guay, D; Kargman, S; Lau, C K; Mancini, J

1995-12-08

The recent discovery of an alternative form cyclooxygenase (cyclooxygenase-2, COX-2), which has been proposed to play a significant role in inflammatory conditions, may provide an opportunity to develop anti-inflammatory drugs with fewer side effects than existing non-steroidal anti-inflammatory drugs (NSAIDs). We have now identified 6-[(2,4-difluorophenyl)-thio]-5-methanesulfonamido-1-indanone++ + (20) (L-745,337) as a potent, selective, and orally active COX-2 inhibitor. The structure-activity relationships in this series have been extensively studied. Ortho- and para-substituted 6-phenyl substitutents are optimal for in vitro potency. Replacement of this phenyl ring by a variety of heterocycles gave compounds that were less active. The methanesulfonamido group seems to be the optimal group at the 5-position of the indanone system. Compound 20 has an efficacy profile that is superior or comparable to that of the nonselective COX inhibitor indomethacin in animal models of inflammation, pain, and fever and appears to be nonulcerogenic within the dosage ranges required for functional efficacy. Although 20 and its oxygen linkage analog 2 (flosulide) are equipotent in the in vitro assays, compound 20 is more potent in the rat paw edema assay, has a longer t1/2 in squirrel monkeys, and seems less ulcergenic than 2 in rats.

Assay for inhibitors of nucleoside transport based upon the use of 5-125I]Iodo-2-deoxyuridine as permeant

International Nuclear Information System (INIS)

Mahony, W.B.; Zimmerman, T.P.

1986-01-01

5[ 125 I]Iodo-2-deoxyuridine (IdUrd) has been shown to serve as a permeant for the nucleoside transport system of human erythrocytes and to be metabolically inert in these cells. Linear initial velocities were obtained at 20 0 C for 125 IdUrd transport, yielding a K/sub m/ of 73 +/- 18 μM (n = 6). Low-affinity inhibitors of 125 IdUrd transport, such as adenosine (K/sub i/ = 32 +/- 2 μM, n = 2), could be characterized by Michaelis-Menten kinetics. However, high-affinity inhibitors, such as 6-[4-nitrobenzyl)thio]9-β-D-ribofuranosylpurine, caused nonlinear initial velocities when added to the cells simultaneously with 125 IdUrd. Conditions were defined (viz., 20-min pretreatment of cells with test compound followed by 5.0-min incubation with 1.0 μM 125 IdUrd, all at 20 0 C) whereby high-affinity inhibitors of IdUrd transport can be identified and evaluated according to their 50% inhibitory concentrations. The use of 125 IdUrd as permeant greatly expedites the testing of compounds as inhibitors of nucleoside transport by allowing the cell pellets generated in these assays to be monitored directly in a gamma spectrometer, thereby circumventing the solubilization and decolorization of cell pellets required by assays that use 3 H- or 14 C-labeled nucleoside permeants

20 let Oddělení environmentální geografie Ústavu geoniky AV ČR, v.v.i

Czech Academy of Sciences Publication Activity Database

Frantál, Bohumil; Kirchner, Karel; Klusáček, Petr

2013-01-01

Roč. 32, č. 2 (2013), s. 54-56 ISSN 1213-1075 Institutional support: RVO:68145535 Keywords : Department of environmental geography * 20 years of founding * Brno Subject RIV: DE - Earth Magnetism, Geodesy, Geography

nNOS inhibitors attenuate methamphetamine-induced dopaminergic neurotoxicity but not hyperthermia in mice.

Science.gov (United States)

Itzhak, Y; Martin, J L; Ail, S F

2000-09-11

Methamphetamine (METH)-induced dopaminergic neurotoxicity is associated with hyperthermia. We investigated the effect of several neuronal nitric oxide synthase (nNOS) inhibitors on METH-induced hyperthermia and striatal dopaminergic neurotoxicity. Administration of METH (5 mg/kg; q. 3 h x 3) to Swiss Webster mice produced marked hyperthermia and 50-60% depletion of striatal dopaminergic markers 72 h after METH administration. Pretreatment with the nNOS inhibitors S-methylthiocitrulline (SMTC; 10 mg/kg) or 3-bromo-7-nitroindazole (3-Br-7-NI; 20 mg/kg) before each METH injection did not affect the persistent hyperthermia produced by METH, but afforded protection against the depletion of dopaminergic markers. A low dose (25 mg/kg) of the nNOS inhibitor 7-nitroindazole (7-NI) did not affect METH-induced hyperthermia, but a high dose (50 mg/kg) produced significant hypothermia. These findings indicate that low dose of selective nNOS inhibitors protect against METH-induced neurotoxicity with no effect on body temperature and support the hypothesis that nitric oxide (NO) and peroxynitrite have a major role in METH-induced dopaminergic neurotoxicity.

Effect of flow on corrosion in catenary risers and its corrosion inhibitor performance

Energy Technology Data Exchange (ETDEWEB)

Ferreira, Pedro Altoe; Magalhaes, Alvaro Augusto Oliveira; Silva, Jussara de Mello [PETROBRAS S.A., Rio de Janeiro, RJ (Brazil); Kang, Cheolho; More, Parimal P. [Det Norske Veritas (DNV), Oslo (Norway)

2009-07-01

In oil and gas production, multiphase flow is often encountered and a range of different flow patterns can be experienced in pipelines. The flow regime transition and flow characteristics can be changed with the change of pipeline topography, which affects the corrosion and the performance of corrosion inhibitor in these multiphase pipelines. This paper outlines on the effect of inclination on the flow characteristics and their subsequent effect on corrosion rates. Also, this paper presents on the performance of three candidate corrosion inhibitors under severe slugging conditions at low water cut. For the simulation of offshore flow lines and risers, the experiments were carried out in a 44 m long, 10 cm diameter, three different pipeline inclinations of 0, 3 and 45 degrees. Light condensate oil with a viscosity of 2.5 cP at room temperature was used and water cut was 20%. The results indicated that the baseline corrosion rate in 45 degrees showed higher than other inclinations. Each corrosion inhibitor showed a different inhibitor performance. (author)

Thapsigargin, an inhibitor of the endoplasmic reticulum Ca2+ ATPase, is an inducer of IFN-gamma

Czech Academy of Sciences Publication Activity Database

Kmoníčková, Eva; Potměšil, Petr; Farghali, H.; Harmatha, Juraj; Zídek, Z.

2005-01-01

Roč. 15, č. 10 (2005), s. 280 ISSN 1001-0602. [Annual meeting of International Society for Interferon and Cytokine Research. 20.10.2005-24.10.2005, Shanghai] R&D Projects: GA ČR(CZ) GA305/05/2425 Institutional research plan: CEZ:AV0Z50390512; CEZ:AV0Z40550506 Keywords : Thapsigargin * sesquiterpene lactone Subject RIV: CC - Organic Chemistry

Ibrutinib interferes with the cell-mediated anti-tumor activities of therapeutic CD20 antibodies: implications for combination therapy

Science.gov (United States)

Roit, Fabio Da; Engelberts, Patrick J.; Taylor, Ronald P.; Breij, Esther C.W.; Gritti, Giuseppe; Rambaldi, Alessandro; Introna, Martino; Parren, Paul W.H.I.; Beurskens, Frank J.; Golay, Josée

2015-01-01

The novel Bruton tyrosine kinase inhibitor ibrutinib and phosphatidyl-4-5-biphosphate 3-kinase-δ inhibitor idelalisib are promising drugs for the treatment of chronic lymphocytic leukemia and B-cell non-Hodgkin lymphoma, either alone or in combination with anti-CD20 antibodies. We investigated the possible positive or negative impact of these drugs on all known mechanisms of action of both type I and type II anti-CD20 antibodies. Pretreatment with ibrutinib for 1 hour did not increase direct cell death of cell lines or chronic lymphocytic leukemia samples mediated by anti-CD20 antibodies. Pre-treatment with ibrutinib did not inhibit complement activation or complement-mediated lysis. In contrast, ibrutinib strongly inhibited all cell-mediated mechanisms induced by anti-CD20 antibodies rituximab, ofatumumab or obinutuzumab, either in purified systems or whole blood assays. Activation of natural killer cells, and antibody-dependent cellular cytotoxicity by these cells, as well as phagocytosis by macrophages or neutrophils were inhibited by ibrutinib with a half maximal effective concentration of 0.3–3 μM. Analysis of anti-CD20 mediated activation of natural killer cells isolated from patients on continued oral ibrutinib treatment suggested that repeated drug dosing inhibits these cells in vivo. Finally we show that the phosphatidyl-4-5-biphosphate 3-kinase-δ inhibitor idelalisib similarly inhibited the immune cell-mediated mechanisms induced by anti-CD20 antibodies, although the effects of this drug at 10 μM were weaker than those observed with ibrutinib at the same concentration. We conclude that the design of combined treatment schedules of anti-CD20 antibodies with these kinase inhibitors should consider the multiple negative interactions between these two classes of drugs. PMID:25344523

Inhibitors of pan PI3K signaling synergize with BRAF or MEK inhibitors to prevent BRAF-mutant melanoma cell growth

Directory of Open Access Journals (Sweden)

Melanie eSweetlove

2015-06-01

Full Text Available BRAF and MEK inhibitors have improved outcomes for patients with BRAF-mutant melanoma, but their efficacy is limited by both intrinsic and acquired resistance. Activation of the PI3K pathway can mediate resistance to these agents, providing a strong rationale for combination therapy in melanoma. Here, a panel of 9 low passage human metastatic melanoma cell lines with BRAF mutations were tested in cell proliferation and protein expression assays for sensitivity to inhibitors of MEK (selumetinib and BRAF (vemurafenib as single agents and in combination with inhibitors of pan-PI3K (ZSTK474, pan-PI3K/mTOR (BEZ235, individual PI3K isoforms (p110α, A66; p110β, TGX-221; p110γ, AS-252424; p110δ, idelalisib, or mTORC1/2 (KU-0063794. Selumetinib and vemurafenib potently inhibited cell proliferation in all cell lines, especially in those that expressed low levels of pAKT. ZSTK474 and BEZ235 also inhibited cell proliferation in all cell lines and enhanced the antitumor activity of selumetinib and vemurafenib in the majority of lines by either interacting synergistically or additively to increase potency or by inducing cytotoxicity by significantly increasing the magnitude of cell growth inhibition. Furthermore, ZSTK474 or BEZ235 combined with selumetinib to produce robust inhibition of pERK, pAKT and pS6 expression and synergistic inhibition of NZM20 tumor growth. The inhibitors of individual PI3K isoforms or mTORC1/2 were less effective at inhibiting cell proliferation either as single agents or in combination with selumetinib or vemurafenib, although KU-0063794 synergistically interacted with vemurafenib and increased the magnitude of cell growth inhibition with selumetinib or vemurafenib in certain cell lines. Overall, these results suggest that the sensitivity of BRAF-mutant melanoma cells to BRAF or MEK inhibitors is at least partly mediated by activation of the PI3K pathway and can be enhanced by combined inhibition of the BRAF/MEK and PI3K

Health, Sanitary and Economic Evaluation of Home-like Systems of Water Treatment (Reverse Osmosis, RO in Qom City

Directory of Open Access Journals (Sweden)

Mohammadreza Jafaripour

2011-07-01

Full Text Available Reverse Osmosis (RO is one of the most useful techniques to improve the elimination of organic and mineral Substances from ground and surface water after primary purification processes such as coagulation, sedimentation and filtration.This System provides the required water quality characteristics to somehow.  However, in selection RO systems civil management decision and general public opinion along with cost and health impact must be considered. This study was done in 2010. Statistical methods have used to gather data about of families who used RO In their private homes and mode of eliminate of the wastewater generated by this process. The results indicated that in the normal operational conditions such as pressure 6- 10 kg / cm2 the, optimum recovery % 30 and flow rate 1lit/min , and water temperature 4- 38C°, an Amount of 14191200 kwh of power energy have been consumed to produce 157680 m3 / year treated water required for 36000 families. This has also generated 367920 m3 / year of wastewater being disposed without any management and environmental considerations. Apart from that more than 198000 of filters have been ejected to the environment. Also regarding health aspects, reducing the hardness and fluoride levels in treated water could be undesirable. It could be concluded that increasing the number of local water distribution points and speeding up the water supplying project from Dez river toQom can decrease the investment on RO system.

Design, Synthesis, and Evaluation of Dihydrobenzo[cd]indole-6-sulfonamide as TNF-alpha Inhibitors

Science.gov (United States)

Deng, Xiaobing; Zhang, Xiaoling; Tang, Bo; Liu, Hongbo; Shen, Qi; Liu, Ying; Lai, Luhua

2018-04-01

Tumor necrosis factor-α (TNF-α) plays a pivotal role in inflammatory response. Dysregulation of TNF can lead to a variety of disastrous pathological effects, including auto-inflammatory diseases. Antibodies that directly targeting TNF-α have been proven effective in suppressing symptoms of these disorders. Compared to protein drugs, small molecule drugs are normally orally available and less expensive. Till now, peptide and small molecule TNF-α inhibitors are still in the early stage of development, and much more efforts should be made. In a previously study, we reported a TNF-α inhibitor, EJMC-1 with modest activity. Here, we optimized this compound by shape screen and rational design. In the first round, we screened commercial compound library for EJMC-1 analogs based on shape similarity. Out of the 68 compounds tested, 20 compounds showed better binding affinity than EJMC-1 in the SPR competitive binding assay. These 20 compounds were tested in cell assay and the most potent compound was 2-oxo-N-phenyl-1,2-dihydrobenzo[cd]indole-6-sulfonamide (S10) with an IC50 of 14 M, which was 2.2-fold stronger than EJMC-1. Based on the docking analysis of S10 and EJMC-1 binding with TNF-α, in the second round, we designed S10 analogues, purchased 7 of them and synthesized 7 new compounds. The best compound, 4e showed an IC50 value of 3 M in cell assay, which was 14-fold stronger than EJMC-1. 4e was among the most potent TNF-α organic compound inhibitors reported so far. Our study demonstrated that 2-oxo-N-phenyl-1,2-dihydrobenzo[cd]indole-6-sulfonamide analogues could be developed as potent TNF-α inhibitors. 4e can be further optimized for its activity and properties. Our study provides insights into designing small molecule inhibitors directly targeting TNF-α and for protein-protein interaction inhibitor design.

Saururus cernuus lignans-Potent small molecule inhibitors of hypoxia-inducible factor-1

International Nuclear Information System (INIS)

Hossain, Chowdhury Faiz; Kim, Yong-Pil; Baerson, Scott R.; Zhang Lei; Bruick, Richard K.; Mohammed, Kaleem A.; Agarwal, Ameeta K.; Nagle, Dale G.; Zhou Yudong

2005-01-01

Hypoxia-inducible factor-1 (HIF-1) represents an important tumor-selective therapeutic target for solid tumors. In search of novel small molecule HIF-1 inhibitors, 5400 natural product-rich extracts from plants, marine organisms, and microbes were examined for HIF-1 inhibitory activities using a cell-based reporter assay. Bioassay-guided fractionation and isolation, followed by structure elucidation, yielded three potent natural product-derived HIF-1 inhibitors and two structurally related inactive compounds. In a T47D cell-based reporter assay, manassantin B 1 , manassantin A, and 4-O-methylsaucerneol inhibited hypoxia-induced HIF-1 activation with IC 50 values of 3, 3, and 20 nM, respectively. All three compounds are relatively hypoxia-specific inhibitors of HIF-1 activation, in comparison to other stimuli. The hypoxic induction of HIF-1 target genes CDKN1A, VEGF, and GLUT-1 were also inhibited. These compounds inhibit HIF-1 by blocking hypoxia-induced nuclear HIF-1α protein accumulation without affecting HIF-1α mRNA levels. In addition, preliminary structure-activity studies suggest specific structural requirements for this class of HIF-1 inhibitors

Cyclic GMP-mediated memory enhancement in the object recognition test by inhibitors of phosphodiesterase-2 in mice.

Science.gov (United States)

Lueptow, Lindsay M; Zhan, Chang-Guo; O'Donnell, James M

2016-02-01

Cyclic nucleotide phosphodiesterase-2 (PDE2) is a potential therapeutic target for the treatment of cognitive dysfunction. Using the object recognition test (ORT), this study assessed the effects of two PDE2 inhibitors, Bay 60-7550 and ND7001, on learning and memory, and examined underlying mechanisms. To assess the role of PDE2 inhibition on phases of memory, Bay 60-7550 (3 mg/kg) was administered: 30 min prior to training; 0, 1, or 3 h after training; or 30 min prior to recall testing. To assess cyclic nucleotide involvement in PDE2 inhibitor-enhanced memory consolidation, either the nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester (L-NAME; 20 mg/kg; intraperitoneal (IP)), soluble guanylyl cyclase inhibitor 1H-[-1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one (ODQ; 20 mg/kg; IP), protein kinase G inhibitor KT5823 (2.5 μg; intracerebroventricular (ICV)), or protein kinase A inhibitor H89 (1 μg; ICV) was administered 30 min prior to the PDE2 inhibitor Bay 60-7550 (3 mg/kg) or ND7001 (3 mg/kg). Changes in the phosphorylation of 3'5'-cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) at Ser-133 and vasodilator-stimulated phosphoprotein (VASP) at Ser-239 were determined to confirm activation of cAMP and 3'5'-cyclic guanosine monophosphate (cGMP) signaling. Bay 60-7550 (3 mg/kg) enhanced memory of mice in the ORT when given 30 min prior to training, immediately after training, or 30 min prior to recall. Inhibitors of the cGMP pathway blocked the memory-enhancing effects of both Bay 60-7550 (3 mg/kg) and ND7001 (3 mg/kg) on early consolidation processes. Bay 60-7550 (3 mg/kg) enhanced phosphorylation of CREB and VASP, both targets of cGMP-dependent protein kinase (PKG). These results confirm a potential of PDE2, or components of its signaling pathway, as a therapeutic target for drug discovery focused on restoring memory function.

Transient behaviour and coupling aspects of a hybrid MSF-RO nuclear desalination plant

International Nuclear Information System (INIS)

Tewari, P.K.; Misra, B.M.

1998-01-01

BARC is setting up a 6300 M 3 /day (1.4 MGD) hybrid MSF-RO nuclear desalination plant for sea water desalination at Madras Atomic Power Station (MAPS) coupled to a 170 MWe Pressurised Heavy Water Reactor (PHWR). The transient behaviour and coupling aspects of this dual purpose plant has been discussed. A hybrid desalination plant appears to offer high availability factor. (author)

Perioceutics: Matrix metalloproteinase inhibitors as an adjunctive therapy for inflammatory periodontal disease

Directory of Open Access Journals (Sweden)

Esther Nalini Honibald

2012-01-01

Full Text Available Matrix metalloproteinases (MMPs form a group of more than 20 zinc-dependent enzymes that are crucial in the degradation of the main components in the extracellular matrix, and thereby play important roles in cell migration, wound healing, and tissue remodeling. MMPs have outgrown the field of extracellular matrix biology and have progressed toward being important regulatory molecules in inflammation, and hence are key components in the pathogenesis of periodontitis. This rise in status has led to the development of MMP inhibitors which can act as switches or delicate tuners in acute and chronic inflammation and the regenerative phase after inflammation. The new challenge in MMP research is to better understand the complex role these enzymes play in periodontal disease and to design inhibitors that are successful in the clinic. Perioceutics or the use of the pharmacological agents specifically developed to manage periodontitis is an interesting and emerging aid in the management of periodontal diseases along with mechanical debridement. The purpose of this review is to provide an introduction to MMPs and their inhibitors, the pathologic effects of a disturbance in the functions of enzyme cascades in balance with natural inhibitors, and highlight on the adjunctive use of MMP inhibitors in periodontal therapy and some of the current challenges with an overview of what has been achieved till date.

The Modified Fouling Index Ultrafiltration constant flux for assessing particulate/colloidal fouling of RO systems

KAUST Repository

Salinas-Rodriguez, Sergio G.; Amy, Gary L.; Schippers, Jan C.; Kennedy, Maria D.

2015-01-01

that remain on the surface of membrane) were measured in a full-scale plant ranging between 0.2 and 0.5. The concept of “safe MFI” is presented as a guideline for assessing pre-treatment for RO systems.

Changes of seizure susceptibility during benzodiazepine withdrawal in immature rats: comparison of clonazepam and partial benzodiazepine agonist Ro 19-8022

Czech Academy of Sciences Publication Activity Database

Kubová, Hana

2006-01-01

Roč. 47, č. S4 (2006), s. 221-221 ISSN 0013-9580. [Annual Meeting of the American Epilepsy Society and Canadian League against Epilepsy. 01.12.2006-05.12.2006, San Diego, CA] R&D Projects: GA MŠk(CZ) LC554 Institutional research plan: CEZ:AV0Z50110509 Keywords : PTZ-induced seizures * clonazepam * agonist Ro 19-8022 Subject RIV: ED - Physiology

Yaacov Ro´i, Boris Morozov, eds, The Soviet Union and the June 1967 Six Day War

OpenAIRE

Rey, Marie-Pierre

2009-01-01

L’ouvrage coordonné par Yaacov Ro´i et Boris Morozov réunit neuf contributions qui, émanant de chercheurs américains, russes et israéliens et toutes fondées sur des archives depuis peu accessibles, éclaire de manière nouvelle et convaincante la question de l’engagement et du rôle de l’Union soviétique durant la guerre des Six Jours. Cinq articles présentés dans le volume traitent directement de l’attitude soviétique à l’heure du conflit. Le premier, rédigé par Yaacov Ro´i, traite de l’engagem...

Effects of the angiotensin-receptor blocker telmisartan on cardiovascular events in high-risk patients intolerant to angiotensin-converting enzyme inhibitors: a randomised controlled trial

DEFF Research Database (Denmark)

NN, NN; Yusuf, S; Teo, K

2008-01-01

BACKGROUND: Angiotensin-converting enzyme (ACE) inhibitors reduce major cardiovascular events, but are not tolerated by about 20% of patients. We therefore assessed whether the angiotensin-receptor blocker telmisartan would be effective in patients intolerant to ACE inhibitors with cardiovascular...

State of the art of the production and utilization of biogas using the NawaRo plant; Stand der Technik bei der Erzeugung und Nutzung von Biogas unter Einsatz von NawaRo-Anlagen

Energy Technology Data Exchange (ETDEWEB)

Weiland, P.; Rieger, C.; Schroeder, J. [Bundesforschungsanstalt fuer Landwirtschaft (FAL), Braunschweig (Germany); Kissel, R.; Bachmaier, H. [LfL, Freising (Germany); Plogsties, V. [ATB, Potsdam (Germany); Vogtherr, J. [Hohenheim Univ., Stuttgart (Germany)

2007-07-01

With amending the Renewable Energy Law (EEG) in August 2004 the fundamentals for the utilization of renewable raw materials in biological gas facilities were created. Since that time the number of installed plants processing energy plants grew very fast, although at the time of amending only few experiences with NawaRo plants were present. Therefore, in order to attain secured informations about the current state of the art in the production and utilization of fermentation gas to, in the context of a country wide measuring program, NawaRo plants are examined and evaluated according to technical and economic criteria. The results determined so far show that due to the intensified employment by energy plants completely new dosing systems and agitating systems are applied, and also pure fermentation techniques for solids increasingly are used for the mono fermentation of renewable raw materials. Although the common generation of current and heat in cogeneration plants dominate, new use routes like the feed of bio methane in the natural gas grid as well as the utilization of the gas as fuel gain in importance.

ÜRO rahuvalvajatel lasub taas laste ahistamise süüdistus / Oliver Tiks, Hendrik Vosman

Index Scriptorium Estoniae

Tiks, Oliver

2008-01-01

Ilmunud ka: Postimees : na russkom jazõke 28. mai 2008, lk. 5. Briti heategevusorganisatsiooni Save the Children raport avalikustas, et maailma kriisipiirkondades on lapsed sattunud neid turvama saadetud ÜRO rahuvalvajate ja abitöötajate seksuaalse kuritarvitamise ohvriks. Lisa: Seksiskandaalid

Effect of Semen on Vaginal Fluid Cytokines and Secretory Leukocyte Protease Inhibitor

Directory of Open Access Journals (Sweden)

Kathy J. Agnew

2008-01-01

Methods: 138 pregnant women had vaginal fluid collected for Gram stain, acid phosphatase detection by colorimetric assay, and interleukin 1-Beta, interleukin-6, interleukin-8, and secretory leukocyte protease inhibitor measurement by enzyme immunoassay. Results for women with and without acid phosphatase were compared by Mann-Whitney test. Results: of 138 subjects, 28 (20% had acid phosphatase detected; of these, only 19 (68% reported recent intercourse and 3 (11% had sperm seen on Gram stain. There were no significant differences in proinflammatory cytokine concentrations; however, secretory leukocyte protease inhibitor concentrations were significantly higher among women with acid phosphatase. Conclusions: proinflammatory cytokine measurement does not appear to be affected by the presence of semen, but secretory leukocyte protease inhibitor is significantly higher when semen is present. Detection of semen by acid phosphatase was associated with higher vaginal SLPI concentrations, however, the presence of semen did not appear to influence vaginal proinflammatory cytokine concentrations.

Influence of B-Complex Vitamins on the Pharmacokinetics of Ginsenosides Rg1, Rb1, and Ro After Oral Administration.

Science.gov (United States)

Zheng, Peihe; Chen, Yinbin; Fu, Yangyang; Wang, Hecheng; Wang, Jia; Zheng, Siwen; Xiao, Shengyuan; Wang, Yingping

2017-11-01

After cultivation of ginseng, ginsenosides, which are the major active ingredients of gingeng, were approved for use by the food industry, and began to be used as added functional ingredients to try to improve the quality and price of functional foods. However, the interaction between different types of ginsenosides and nutrients needs further study. We investigated the effect of B-complex vitamins (which are essential nutrients) on the pharmacokinetics of the ginsenosides protopanaxatriol-type saponin Rg 1 , protopanaxadiol-type saponin Rb 1 , and oleanolic acid-type saponin Ro after oral administration. Ginsenosides Rg 1 , Rb 1 , and Ro, with or without B-complex vitamins, respectively, were administered orally to rats to evaluate their pharmacokinetics. The concentration of ginsenosides in plasma was determined by liquid chromatography/tandem mass spectrometry. Pharmacokinetic parameters were fitted using WinNonlin v6.2. After oral coadministration with B-complex vitamins, the area under the concentration-time curve from zero to infinity (AUC 0-∞ ) of ginsenoside Rg 1 was reduced by 70%, that of ginsenoside Rb 1 was reduced by 43%, and that of ginsenoside Ro was reduced by 34%. The AUC 0-∞ of ginsenosides Rg 1 and Rb 1 showed significant differences between different treatments, but the AUC 0-∞ of ginsenoside Ro did not. These results suggest significant ginsenoside-nutrient interactions between ginsenosides Rg 1 , Rb 1 , and B-complex vitamins.

Allosteric small-molecule kinase inhibitors

DEFF Research Database (Denmark)

Wu, Peng; Clausen, Mads Hartvig; Nielsen, Thomas E.

2015-01-01

current barriers of kinase inhibitors, including poor selectivity and emergence of drug resistance. In spite of the small number of identified allosteric inhibitors in comparison with that of inhibitors targeting the ATP pocket, encouraging results, such as the FDA-approval of the first small...

Plasmin substrate binding site cooperativity guides the design of potent peptide aldehyde inhibitors.

Science.gov (United States)

Swedberg, Joakim E; Harris, Jonathan M

2011-10-04

Perioperative bleeding is a cause of major blood loss and is associated with increased rates of postoperative morbidity and mortality. To combat this, antifibrinolytic inhibitors of the serine protease plasmin are commonly used to reduce bleeding during surgery. The most effective and previously widely used of these is the broad range serine protease inhibitor aprotinin. However, adverse clinical outcomes have led to use of alternative serine lysine analogues to inhibit plasmin. These compounds suffer from low selectivity and binding affinity. Consequently, a concerted effort to discover potent and selective plasmin inhibitors has developed. This study used a noncombinatorial peptide library to define plasmin's extended substrate specificity and guide the design of potent transition state analogue inhibitors. The various substrate binding sites of plasmin were found to exhibit a higher degree of cooperativity than had previously been appreciated. Peptide sequences capitalizing on these features produced high-affinity inhibitors of plasmin. The most potent of these, Lys-Met(sulfone)-Tyr-Arg-H [KM(O(2))YR-H], inhibited plasmin with a K(i) of 3.1 nM while maintaining 25-fold selectivity over plasma kallikrein. Furthermore, 125 nM (0.16 μg/mL) KM(O(2))YR-H attenuated fibrinolysis in vitro with an efficacy similar to that of 15 nM (0.20 μg/mL) aprotinin. To date, this is the most potent peptide inhibitor of plasmin that exhibits selectivity against plasma kallikrein, making this compound an attractive candidate for further therapeutic development.

Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase

Science.gov (United States)

Hutchinson, Jonathan P.; Rowland, Paul; Taylor, Mark R. D.; Christodoulou, Erica M.; Haslam, Carl; Hobbs, Clare I.; Holmes, Duncan S.; Homes, Paul; Liddle, John; Mole, Damian J.; Uings, Iain; Walker, Ann L.; Webster, Scott P.; Mowat, Christopher G.; Chung, Chun-Wa

2017-06-01

Kynurenine-3-monooxygenase (KMO) is a key FAD-dependent enzyme of tryptophan metabolism. In animal models, KMO inhibition has shown benefit in neurodegenerative diseases such as Huntington's and Alzheimer's. Most recently it has been identified as a target for acute pancreatitis multiple organ dysfunction syndrome (AP-MODS); a devastating inflammatory condition with a mortality rate in excess of 20%. Here we report and dissect the molecular mechanism of action of three classes of KMO inhibitors with differentiated binding modes and kinetics. Two novel inhibitor classes trap the catalytic flavin in a previously unobserved tilting conformation. This correlates with picomolar affinities, increased residence times and an absence of the peroxide production seen with previous substrate site inhibitors. These structural and mechanistic insights culminated in GSK065(C1) and GSK366(C2), molecules suitable for preclinical evaluation. Moreover, revising the repertoire of flavin dynamics in this enzyme class offers exciting new opportunities for inhibitor design.

Biodegradation of Azo Dye RO16 in Different Reactors by Immobilized Irpex lacteus

Czech Academy of Sciences Publication Activity Database

Tavčar, M.; Svobodová, Kateřina; Kuplenk, J.; Novotný, Čeněk; Pavko, A.

2006-01-01

Roč. 53, - (2006), s. 338-343 ISSN 1318-0207 R&D Projects: GA MŠk(CZ) 1P05ME828; GA AV ČR(CZ) IAA6020411; GA ČR(CZ) GP526/06/P102 Institutional research plan: CEZ:AV0Z50200510 Keywords : irpex lacteus * dye decolorization * trickle bed reactor Subject RIV: EE - Microbiology, Virology Impact factor: 0.703, year: 2006

Stavovi medicinskih sestara u Hrvatskoj o primarnom oživljavanju prijevremeno rođene novorođenčadi

OpenAIRE

Bilić, Iva; Prpić, Igor; Radić, Jelena; Vukelić, Petar; Petrović, Ana; Juretić, Emilija; Furlan, Ivanka

2008-01-01

CILJ: Cilj istraživanja bilo je ispitati stavove medicinskih sestara u Hrvatskoj o primarnom oživljavanju prijevremeno rođene djece. METODE: Pisanom anketom ispitivana je dob, roditeljstvo, radno iskustvo i mjesto rada te stavovi medicinskih sestara iz Hrvatske o primarnom oživljavanju prijevremeno rođene djece. Anketirano je 174 medicinskih sestara; 49 zaposlenih u rađaonici ili na mjestima rada sa trudnicama (Rađ/Tr), 79 u pedijatrijskim/ neonatološkim jedinicama intenzivnog liječenja (...

The antimalarial drug, Ro 42-1611 (arteflene), does not affect cytoadherence and cytokine-inducing properties of Plasmodium falciparum malaria parasites

DEFF Research Database (Denmark)

Jakobsen, P H; Staalsø, T; Bendtzen, K

1995-01-01

The purpose of this study was to investigate the ability of the antimalarial drug, Ro 42-1611 to block parasite mediated cytokine induction in vitro as well as cytoadherence of infected erythrocytes to melanoma cells in vitro. The biological activity of Ro 42-1611 was confirmed as it blocked...... to melanoma cells. The therapeutic effect of To 42-1611 appears to be confined to its parasite killing activity....