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Current studies in plants suggest that the content of the coenzyme NAD is variable and potentially important in determining cell fate. In cases that implicate NAD consumption, re-synthesis must occur to maintain dinucleotide pools. Despite information on the pathways involved in NAD synthesis in plants, the existence of a mitochondrial nicotinamide mononucleotide adenylyltransferase (NMNAT) activity which catalyses NAD synthesis from nicotinamide mononucleotide (NMN) and ATP has not been reported. To verify the latter assumed pathway, experiments with purified and bioenergetically active mitochondria prepared from tubers of Jerusalem artichoke (Helianthus tuberosus L.) were performed. To determine whether NAD biosynthesis might occur, NMN was added to Jerusalem artichoke mitochondria (JAM)...

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4-methylumbelliferone (4-MU) is a hyaluronic acid (HA) synthesis inhibitor with anticancer properties; the mechanism of its anticancer effects is unknown. We evaluated the effects of 4-MU on...Full Text Available

UK PubMed Central (United Kingdom)

Transformed Drosophila Kc cell lines, resistant to methotrexate, an inhibitor of de novo purine and pyrimidine synthesis, have been obtained by calcium phosphate transfection of plasmids containing...Full Text Available

DEFF Research Database (Denmark)

The notes describe in detail primary and secondary galvanic cells, fuel cells, electrochemical synthesis and electroplating processes, corrosion: measurments, inhibitors, cathodic and anodic protection, details of metal dissolution reactions, Pourbaix diagrams and purification of waste water from galvanic industries.

British Library Electronic Table of Contents (United Kingdom)

With collaboration between chemistry, X-ray crystallography, and molecular modeling, we designed and synthesized a series of novel piperazine sulfonamide BACE1 inhibitors. Iterative exploration of the non-prime side and S2prime sub-pocket of the enzyme culminated in identification of an analog that potently lowers peripheral Ab40 in transgenic mice with a single subcutaneous dose.

Science.gov (United States)

Indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) are tryptophan-degrading enzymes. Mammalian IDO expression is induced by cytokines and has antimicrobial and immunomodulatory effects. A major role of mammalian TDO is to supply nicotinamide adenine dinucleotide (NAD(+)). In fungi, the IDO homologue is thought to be expressed constitutively and supply NAD(+), as TDO is absent from their genomes. Here, we reveal the distribution of IDO genes among fungal species and characterize their enzymatic activity. The yeast, Saccharomyces cerevisiae has only one IDO gene, whereas the koji-mold, Aspergillus oryzae has two genes, IDO? and IDO?. The A. oryzae IDO? showed more similar enzymatic properties to those of S. cerevisiae IDO than IDO?, suggesting that the A. oryzae IDO? is a functional homologue of the S. cerevisiae IDO. From the IDO? gene, two isoforms, IDO? and IDO?(+) could be generated by alternative splicing. The latter ...

UK PubMed Central (United Kingdom)

Silent information regulators are potent NAD⁺-dependent protein deacetylases, which have been shown to regulate gene silencing, muscle differentiation and DNA damage repair. Here,...Full Text Available

UK PubMed Central (United Kingdom)

The cofactor nicotinamide adenine dinucleotide (NAD+) has emerged as a key regulator of metabolism, stress resistance and longevity. Apart from its role as ...Full Text Available

UK PubMed Central (United Kingdom)

A two-step purification protocol was used in an attempt to separate the constitutive NAD(P)H-nitrate reductase [NAD(P)H-NR, pH 6.5; EC 1.6.6.2] activity from the nitric oxide and nitrogen dioxide (NO_(x))...Full Text Available

British Library Electronic Table of Contents (United Kingdom)

A novel class of pyrrolidinyl-acetyleneic thieno[3,2-d]pyrimidines has been identified which potently inhibit the EGFR and ErbB-2 receptor tyrosine kinases. Synthetic modifications of the pyrrolidine carbamate moiety result in a range of effects on enzyme and cellular potency. In addition, the impact of the absolute stereochemical configuration on cellular potency and oral mouse pharmacokinetics is described.

International Nuclear Information System (INIS)

1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) is an anti-inflammatory agent with a propenone moiety and chemically synthesized recently. In this study, we examined the chemopreventive effect of FPP-3 on 7,12-dimethylbenz[a]anthracene (DMBA)-induced genotoxicity in MCF-7 cells. FPP-3 reduced the formation of the DMBA-DNA adduct. DMBA-induced CYP1A1 and CYP1B1 gene expression and enzyme activity were inhibited by FPP-3. It inhibited DMBA-induced aryl hydrocarbon receptor (AhR) transactivation and DMBA-inducible nuclear localization of the AhR. Induction of detoxifying phase II genes by chemopreventive agents represents a coordinated protective response against oxidative stress and neoplastic effects of carcinogens. Transcription factor NF-E2 related factor 2 (Nrf2) regulates antioxidant response element (ARE) of phase II detoxifying and antioxidant enzymes, such as glutathione S-transferase (GST) and NAD(P)H:quinone oxidoreductase (QR). FPP-3 increased the expression ...

British Library Electronic Table of Contents (United Kingdom)

Conformationally constrained analogue synthesis was undertaken to aid in pharmacophore mapping and 3D-QSAR analysis of nitrobenzylmercaptopurine riboside (NBMPR) congeners as equilibriative nucleoside transporter 1 (ENT1) inhibitors. In our previous study [J. Med. Chem. 2003, 46, 831-837], novel regioisomeric nitro-1,2,3,4-tetrahydroisoquinoline conformationally constrained analogues of NBMPR were synthesized and evaluated as ENT1 ligands. 7-NO2-1,2,3,4-Tetrahydroisoquino-2-yl purine riboside was identified as the analogue with the nitro group in the best orientation at the NBMPR binding site of ENT1. In the present study, further conformational constraining was introduced by synthesizing 5prime-O,8-cyclo derivatives. The flow cytometrically determined binding affinities indicated that the...

International Nuclear Information System (INIS)

Continuous freestanding SiC(Al) films were fabricated by melt spinning the aluminum-containing polycarbosilane (A-PCS) precursor. The results showed that the films contained #beta#-SiC crystals, #alpha#-SiC nano-crystals, C clusters and small amount of Al_4O_4C and Al_4SiC_4. The Al atoms in the films played important roles as both sintering aids and grain growth inhibitor. The PL spectrum showed a wide luminescence band from 320 nm to 440 nm, and the origin of PL centered at 385 nm might be related to the #alpha#-SiC nano-crystals using quantum size effects. The obtained films are expected to have important applications in MEMS for the environment of high temperature and optoelectronic devices.

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Culturing human prostate PC-3 cells for 4, 24, or 72 h in the presence of 5,8,11,14-eicosatetraynoic acid (ETYA), an inhibitor of arachidonic acid metabolism and cholesterol biosynthesis, markedly altered the morphology and reduced the number of mitochondria in the treated cells. Using quantitative electron microscopic morphometry, we documented changes in the number, form, area, matrix density, and integrity of the cristae and limiting membranes of mitochondria in cells cultured with ETYA. The inhibition of cholesterol synthesis or the substitution of ETYA for polyunsaturated fatty acids in the inner membrane may participate in the disruption of the mitochondria, which resembles the morphologic sequelae of oxidative stress. If sufficiently extensive, these changes could contribute to the inhibition of cellular proliferation by ETYA.

UK PubMed Central (United Kingdom)

NADPH nitrate reductase activity in higher plants has been attributed to the presence of NAD(P)H bispecific nitrate reductases and to the presence of phosphatases capable of hydrolyzing NADPH to NADH....Full Text Available

UK PubMed Central (United Kingdom)

Sirtuins are highly conserved NAD⁺-dependent protein deacetylases and/or ADP-ribosyltransferases that can extend the lifespan of several lower model organisms including yeast, worms and flies....Full Text Available

UK PubMed Central (United Kingdom)

The sirtuin Sirt6 is a NAD-dependent histone deacetylase that is implicated in gene regulation and lifespan control. Sirt6 can interact with the stress-responsive transcription factor NF-κB...Full Text Available

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Ethylene is a plant hormone that elicits a wide variety of responses in plant tissue. Among these responses are the hastening of abscission, ripening and senescence. In 1979 it was discovered that 1-amino-1-cyclopropane carboxylic acid is the immediate biosynthetic precursor to ethylene. Given the obvious economic significance of ethylene production the authors concentrated their studies on the conversion of ACC to ethylene. They delved into mechanistic aspects of ACC oxidation and they studied potential inhibitors of ethylene forming enzyme (EFE). They synthesized various analogs of ACC and found that EFE shows good stereodiscrimination among alkyl substituted ACC analogs with the 1R, 2S stereoisomer being processed nine times faster than the 1S, 2R isomer in the MeACC series. They also synthesized 2-cyclopropyl ACC which is a good competitive inhibitor of EFE. This compound also causes time dependent loss of EFE activity leading us to believe ...

Science.gov (United States)

... R OFFICIAL FILE COPY SYNTHESIS OF PERFLUOROALIPHATIC ETHER MONOMERS PCR, Inc. ... Synthesis of Perfluoroaliphatic Ether Monomers ...

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A decrease of inhibitor concentration in a medium is always desirable even if the inhibitor is not toxic. In this connection, a sharp increase in the protective effect of certain corrosion inhibitors when cathodic polarization was applied to the metal is reviewed. The importance of a simultaneous account of the chemical structure of inhibitor and the nature of the metal corrosion under cathodic polarization is outlined. Some examples of applying this combined protection of metals are discussed.

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The need exists for rapid and inexpensive methods to determine the health effects of environmental contaminants on biological systems. One of the current research approaches for assessing cytotoxicity is to monitor the respiratory activity of the mitochondrion, a sensitive, nonspecific subcellular target site. Detected changes in mitochondrial function after the addition of a test chemical could be correlated to toxic effects. Mitochondrial respiration can be characterized by three indices: state 3 and state 4 respiratory rates, and the respiratory control ratio (RCR). State 4, the idle or resting state, results when coupled mitochondrial respire in a medium containing inorganic phosphate and a Kreb's cycle substrate in the absence of a phosphate acceptor such as adenosine diphosphate (ADP). In the presence of ADP the respiration rate increases to a maximum (state 3), accompanied by phosphorylation of ADP to adenosine triphosphate (ATP). The ratio of state 3 to state 4, or ...

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3T3 - L1 cells can be induced to differentiate by exposing cell culture to a medium containing 3-isobutyl-1-methyl-xanthine together with insulin and dexamethasone. They have observed that oxalomalate (OMA) which inhibits aconitase thus blocking the citric cycle, also favours differentiation to adipocytes leading to fatty acids accumulation and increased synthesis of specific proteins. They compared the effects of 3-isobutyl-1-methyl-xanthine-insulin-dexamethasone and OMA on the steady-state levels of mRNA of c / EBP, H-ferritin and aconitase / IRE-BP. OMA does not affect the steady-state mRNA amount of C / EBP, H-ferritin and aconitase / IRE-BP but the 3-isobutyl-1-methyl-xanthine-insulin-dexamethasone mixture is able to induce a five-fold increase of mRNA levels for aconitase / IRE-BP. This is the first finding correlating iron metabolism to adipocyte differentiation. Further studies will clarify a possible role for the aconitase inhibitor ...

UK PubMed Central (United Kingdom)

Background and purpose:Diphenyleneiodonium (DPI) is often used as an NADPH oxidase inhibitor, but is increasingly being found to have unrelated side effects. We investigated its...Full Text Available

UK PubMed Central (United Kingdom)

Chemical genetics is an emerging approach to investigate the biology of host-pathogen interactions. We screened several inhibitors of ATP-dependent DNA motors and detected the gyrase B inhibitor coumermycin...Full Text Available

International Science & Technology Center (ISTC)

The Production of Highly Active Human Blood Plasma Butyrylcholinesterase Preparation by Gene Engineering Methods to Create Protective Means against Poisoning by Organophosphorous Cholinesterase Inhibitors

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The authors have found that heat-inactivated serum (57/sup 0/C for 1 hour) from normal chickens reduces the proliferation of mitogen-stimulated chicken and murine splenocytes as well as some transformed mammalian lymphoblastoid cell lines. Greater than a 50% reduction in /sup 3/H-thymidine incorporation was observed when concanavalin A (Con A)-activated chicken splenocytes that were cultured in the presence of 10% autologous or heterologous serum were compared to mitogen-stimulated cells cultured in the absence of serum. Normal chicken serum (10%) also caused greater than 95% suppression of /sup 3/H-thymidine incorporation by bovine (EBL-1 and BL-3) and gibbon ape (MLA 144) transformed lymphoblastoid cell lines. The only cell line tested that was not inhibited by chicken serum was an IL-2-dependent, murine cell line. Chicken serum also inhibited both /sup 3/H-thymidine incorporation and IL-2 synthesis by Con A-activated murine splenocytes. Suppression was caused by ...

UK PubMed Central (United Kingdom)

Glucose metabolism through glycolysis and hexosamine pathway has been shown to be altered in type 2 diabetes. However, its fate through the pentose phosphate pathway (PPP) is currently unclear....Full Text Available

UK PubMed Central (United Kingdom)

Several cDNA clones encoding Δ¹-pyrroline-5-carboxylate reductase (P5CR, l-proline:NAD[P]⁺ 5-oxidoreductase, EC 1.5.1.2), which catalyzes the terminal step in...Full Text Available

KoreaScience (Korea)

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Treatment Induced Hypertension

DEFF Research Database (Denmark)

Udgivelsesdato: 2008-Jul-15

British Library Electronic Table of Contents (United Kingdom)

The acid corrosion inhibition process of mild steel in 1M HCl by 1-butyl-3-methylimidazolium chlorides (BMIC) and 1-butyl-3-methylimidazolium hydrogen sulfate ([BMIM]HSO4) has been investigated using electrochemical impedance, potentiodynamic polarization and weight loss measurements. Potentiodynamic polarization studies indicate the studied inhibitors are mixed type inhibitors. For both inhibitors, the inhibition efficiency increased with increase in the concentration of the inhibitor and the effectiveness of the two inhibitors are in the order [BMIM]HSO4>BMIC. The adsorption of the inhibitors on mild steel surface obeyed the Langmuirs adsorption isotherm. The effect of temperature on the corrosion behavior in the presence of 5x10-3M of inhibitors was studied in the temperature range of 3...

UK PubMed Central (United Kingdom)

The stereocontrolled total synthesis of 4-hydroxydictyolactone (4), a member of the xenicane diterpene family of natural products, is described. These studies feature the development...Full Text Available

International Nuclear Information System (INIS)

Short communication.

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Not Available

British Library Electronic Table of Contents (United Kingdom)

Histone deacetylase (HDAC) inhibitors have been actively exploited as potential anticancer agents. To identify gene targets of HDAC inhibitors, we found that HDAC inhibitors such as sodium butyrate, scriptaid, apicidin and oxamflatin induced the expression of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), a potential cyclooxygenase-2 (COX-2) antagonist and tumor suppressor, in a time and concentration dependent manner in A549 and H1435 lung adenocarcinoma cells. Detailed analyses indicated that HDAC inhibitors activated the 15-PGDH promoter-luciferase reporter construct in transfected A549 cells. A representative HDAC inhibitor, scriptaid, and its negative structural analog control, nullscript, were further evaluated at the chromatin level. Scriptaid but not nullscript induced a signific...

International Nuclear Information System (INIS)

Cultures of 3T3-L1 cells were incubated with either 10 ng/ml cholera toxin or 10 ng/ml pertussis toxin from 4 days prior to the initiation of differentiation and throughout the subsequent incubation. Toxin concentrations were sufficient to completely prevent the labelling of alpha-subunits with ["3"2P]NAD"+ and pertussis toxin and to prevent by more than 90% the labelling with ["3"2P]NAD"+ and cholera toxin in membranes prepared from these cells. Neither toxin prevented the differentiation to the adipocyte phenotype. Neither toxin prevented the increases in the relative amounts of G-proteins which occur upon differentiation. Both toxins dramatically decreased the amount of beta-subunits. As measured by quantitative immunoblotting with antisera specific for both the 35 kDa and 36 kDa beta-subunits, levels of beta-subunit were decreased by more than 50% of steady-state level of control cells. Thus, bacterial toxins which modifies G-protein ...

UK PubMed Central (United Kingdom)

ObjectiveThe objective of this study was to identify patterns of brain activation elicited by erotic visual stimuli in patients treated with either Selective Serotonin Reuptake Inhibitors...Full Text Available

UK PubMed Central (United Kingdom)

Reactive blue 2 (RB-2) had been characterized as a relatively potent ectonucleoside triphosphate diphosphohydrolase (E-NTPDase) inhibitor with some selectivity for NTPDase3. In search for the pharmacophore...Full Text Available

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AimsTo assess the tolerability and pharmacokinetic profile of single and repeat doses of the oral matrix metalloproteinase inhibitor marimastat in healthy male volunteers.Full Text Available

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BackgroundSerine proteinase inhibitors (Serpins) are a large superfamily of structurally related, but functionally diverse proteins that control essential proteolytic pathways in...Full Text Available

UK PubMed Central (United Kingdom)

AimsTo describe the pharmacokinetic–pharmacodynamic (PK–PD) characteristics of the direct thrombin inhibitor dabigatran in hip replacement patients by assessing coagulation...Full Text Available

International Nuclear Information System (INIS)

Interleukin 2 (IL-2) is a T-cell-derived lymphokine critical in the activation and proliferation of T cells, B cells, and lymphokine-activated killer cells. It is a glycoprotein of #approx#15,500 daltons that is synthesized and secreted after activation by antigen or mitogen. By using the analogs 8-azidoadensoine 5'-[#gamma#-"3"2P]triphosphate ([#gamma#-"3"2P]8N_3ATP) and nicotinamide 2-azidoadenine [adenylate-"3"2P]dinucleotide ([#alpha#-"3"2P]2N_3NAD"+) as photoaffinity probes, the authors have detected specific, metal ion-requiring nucleotide binding sites on recombinant human IL-2 (rhIL-2). The specificity of these nucleotide interactions with rhIL-2 was demonstrated by saturation effects and by competition by the parent nucleotides at physiologically relevant concentrations. Saturation of photoinsertion into rhIL-2 occurred at 50 #mu#M [#gamma#-"3"2P]8N_3ATP. Saturation of photoinsertion with [#alpha#-"3"2P]2N_3NAD"+ was observed at 180 ...

KoreaScience (Korea)

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The inhibitor action of unbranched polyamines on corrosion of low-carbon steel in 0.5 M sulfuric acid is studied through potentiostatic polarization curves. It is shown that the inhibitor efficiency I depends on the polyamine concentration and molecular structure. The quantum-mechanical calculations of molecular properties are accomplished through the MNDO method. Correlation between the measured I and physicochemical properties of the polyamine inhibitors in protonized and nonprotonized form is found with application of the general perturbation theory

UK PubMed Central (United Kingdom)

The serpin ZPI is a protein Z (PZ)-dependent specific inhibitor of membrane-associated factor Xa (fXa) despite having an unfavorable P1 Tyr. PZ accelerates the inhibition reaction ∼2000-fold...Full Text Available

International Nuclear Information System (INIS)

The acid corrosion inhibition process of mild steel in 1 M HCl by 1-butyl-3-methylimidazolium chlorides (BMIC) and 1-butyl-3-methylimidazolium hydrogen sulfate ([BMIM]HSO_4) has been investigated using electrochemical impedance, potentiodynamic polarization and weight loss measurements. Potentiodynamic polarization studies indicate the studied inhibitors are mixed type inhibitors. For both inhibitors, the inhibition efficiency increased with increase in the concentration of the inhibitor and the effectiveness of the two inhibitors are in the order [BMIM]HSO_4 > BMIC. The adsorption of the inhibitors on mild steel surface obeyed the Langmuir's adsorption isotherm. The effect of temperature on the corrosion behavior in the presence of 5 x 10"-"3 M of inhibitors was studied in the temperature range of 303-333 K. The associated activation ...

UK PubMed Central (United Kingdom)

Three photaffinity labeled derivatives of epothilone D were prepared by total synthesis, using efficient novel asymmetric synthesis methods for the preparation of two important synthetic building...Full Text Available

Science.gov (United States)

Robert A. Martock. Cleveland State University, Cleveland, Ohio. Synthesis and Structural Characterization of a. Novel Indium Mercapto Derivative. [Clln(SCH. 2 ...

UK PubMed Central (United Kingdom)

A one-pot multicomponent procedure for the synthesis of highly functionalized pyrrolidine rings through a domino...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

DOE installations possessing sufficient quantities of fissile material to potentially constitute a critical mass, such that the excessive exposure of personnel to radiation from a nuclear accident is possible, are required to provide nuclear accident dosimetry services. This document describes the personal nuclear accident dosimeter (PNAD) used by SNL and prescribes methodologies to initially screen, and to process PNAD results. In addition, this report describes PNAD dosimetry results obtained during the Nuclear Accident Dosimeter Intercomparison Study (NAD23), held during 12-16 June 1995, at Los Alamos National Laboratories. Biases for reported neutron doses ranged from -6% to +36% with an average bias of +12%.

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The effect of sodium gluconate anion (SG) on the corrosion and scale inhibition of ordinary steel in simulated cooling water has been studied using weight loss, polarisation curves, electrochemical impedance spectroscopy (EIS) and scanning electron microscopy (SEM) techniques. SG was studied in concentration from 10{sup -4} M to 10{sup -1} M. Results obtained reveal that SG perform excellently as corrosion and scaling inhibitor for ordinary steel in simulated cooling water. An increase of SG concentration leads to the increase of the corrosion potential towards the positive direction. The inhibition efficiency was a low temperature dependence. The inhibitor mechanism was treated as an adsorption process according to Langmuir adsorption isotherm. The SEM/EDAX data show that was a corrosion and scale inhibitor.

Science.gov (United States)

(NaMBT) inhibitor in ethylene glycol-water solutions. The improved method must be faster and more accur- ate than wet chemical techniques. ...

DEFF Research Database (Denmark)

Raltegravir is the first integrase inhibitor approved for treatment of HIV-infected patients harboring multiresistant viruses.

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KoreaScience (Korea)

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The heterogeneous solid catalyst, mercaptopropylsilica (MPS), has been prepared by a modified procedure in water and its structure confirmed by solid state carbon-13 CP-MAS NMR spectrum. This catalyst has been efficiently utilized for the synthesis of a wide variety of tri-, tetrasubstituted imidazoles and their bis-analogues at room temperature. The protocol was further explored for the synthesis of the drug trifenagrel.

DEFF Research Database (Denmark)

ATPase, endoplasmic reticulum, calcium, ischaemia

International Nuclear Information System (INIS)

... odd nuclei organic compounds radiation effects radioisotopes synthesis

UK PubMed Central (United Kingdom)

BackgroundThe most recent ESC guidelines for percutaneous coronary intervention (PCI) recommend the use of glycoprotein IIb/IIIa inhibitors (GPI) in high risk patients with non-ST-segment...Full Text Available

Science.gov (United States)

There are about fifty SET domain protein methyltransferases (PMTs) in the human genome, that transfer a methyl group from S-adenosyl-L-methionine (SAM) to substrate lysines on histone tails or other peptides. A number of structures in complex with cofactor, substrate, or inhibitors revealed the mechanisms of substrate recognition, methylation state specificity, and chemical inhibition. Based on these structures, we review the structural chemistry of SET domain PMTs, and propose general concepts towards the development of selective inhibitors.

UK PubMed Central (United Kingdom)

BackgroundRecent studies have suggested that the Src inhibitor dasatinib preferentially inhibits the growth of breast cancer cells of the basal-like subtype. To clarify this finding...Full Text Available

UK PubMed Central (United Kingdom)

1. Ro 15-8081 (Hoffmann-La Roche, Basle, Switzerland) is a novel mixed 5-HT/noradrenaline uptake inhibitor producing potent antinociceptive effects in animal pain models. 2. In healthy man, two models...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundUpon CD95/Fas ligation, the initiator caspase-8 is known to activate effector caspases leading to apoptosis. In the presence of zVAD-fmk, a broad-spectrum caspase inhibitor,...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

Field and laboratory work sponsored by the Gas Research Institute (GRI) and the Department of Energy (DOE) have shown that calcium-carbonate scale formation in waters produced with natural gas and oil can be prevented by injection of phosphonate inhibitor into the formation, even if the formation is sandstone without calcite binding material. Inhibitor squeeze jobs have been carried out on DOE's geopressured-geothermal Gladys MaCall brine-gas well and GRI's co-production wells in the Hitchcock field. Following the inhibitor squeeze on Gladys McCall, the well produced over five million barrels of water at a rate of approximately 30,000 BPD without calcium-carbonate scaling. Before the inhibitor squeeze, the well could not be produced above 15,000 BPD without significant scale formation. In the GRI brine-gas co-production field tests, inhibitor squeezes have been ...

UK PubMed Central (United Kingdom)

The t-butyldimethylsilyl group is shown to be an ideal protecting group for the 2T-hydroxyl function of ribonucleosides during the synthesis of ribonucleotides using any of nine commonly used condensing...Full Text Available

UK PubMed Central (United Kingdom)

The accepted model of retroviral reverse transcription includes a circular DNA intermediate which requires strand displacement synthesis for linearization and creation of an integration-competent, long...Full Text Available

International Nuclear Information System (INIS)

There is renewed interest in the +6 oxidation state of iron, ferrate (VI) (FeVIO42-), because of its potential as a benign oxidant for organic synthesis, as a chemical in developing cleaner ('greener') technology for remediation processes, and as an alternative for environment-friendly battery cathodes. This interest has led many researchers to focus their attention on the synthesis of ferrate(VI). Of the three synthesis methods, electrochemical, wet chemical and thermal, electrochemical synthesis has received the most attention due to its ease and the high purity of the product. Moreover, electrochemical processes use an electron as a so-called clean chemical, thus avoiding the use of any harmful chemicals to oxidize iron to the +6 oxidation state. This paper reviews the development of electrochemical methods to synthesize ferrate(VI). The approaches chosen by different laboratories to overcome some of ...

UK PubMed Central (United Kingdom)

A new strategy is presented for the synthesis of graft copolymers using only the ring-opening metathesis polymerization (ROMP). From a ROMP-derived main chain, pendant maleimide functional groups...Full Text Available

UK PubMed Central (United Kingdom)

Cell suspension cultures of tomato, Lycopersicon esculentum Mill. cv VFNT-Cherry, produce phytochelatins (poly[γ-glutamylcysteinyl]glycines) when exposed to cadmium. The synthesis...Full Text Available

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Research programs, presented at the contractor's review meeting on indirect liquefaction, are presented on the following topics: oxygenates (methanol) synthesis; Fischer-Tropsch synthesis; product upgrading; and process support engineering evaluations. A total of 18 reports are included. Individual projects are processed separately for the data bases. (CBS)

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Adenosine triphosphate (ATP) is an indicator of living biomass in marine particulates. This report details the method used by Lawrence Berkeley Laboratory to analyze particulate ATP in samples taken from oligotrophic, tropical ocean waters. It represents a synthesis of previously published methods.

UK PubMed Central (United Kingdom)

This study examined the hypothesis that solid surfaces may stimulate attached bacteria to produce exopolymers. Addition of sand to shake-flask cultures seemed to induce exopolymer synthesis by a number...Full Text Available

UK PubMed Central (United Kingdom)

The accumulation of α-1,4-polyglucans is an important strategy to cope with transient starvation conditions in the environment. In bacteria and plants, the synthesis of glycogen and starch occurs...Full Text Available

Science.gov (United States)

Research continued on the synthesis of model compounds for coal liquefaction research. This report covers the actual laboratory investigation performed during the reporting period in order to attain the stated objective of the project, viz, the synthesis of a model compound containing tetrahydronaphthalene, naphthalene and phenyl moieties linked by methylene, ethylene and ether bonds. The overall synthetic approach aimed at obtaining the end product has been broken down into three major steps that involve the synthesis of three key reactive intermediates. These are: (1) 3,5-dimethyl-5-bromobenzyl chloride, (2) 1-chloromethylene-2-hydroxytetralin and (3) 2-chloromethylene-1-hydroxynaphthalene.

KoreaScience (Korea)

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International Nuclear Information System (INIS)

A mixture of aminoacids was irradiated by a scattered proton beam, its energy varying from 4 to 6.6 MeV, by doses up to 5 x 10"1"1 proton/cm"2 for studying the potentiality of abiogenic synthesis of biologically important compounds in space. It was ascertained that increase in the radiation dose and reduction of proton energy involve increase in effectiveness both of destruction of the initial aminoacid (tryptophan, tyrosine, glycine) and synthesis of the relevant dipeptide. Essential influence of mineral substrate on abiogenic synthesis of natural nucleotides under the action of diverse energy sources was pointed out

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No abstract prepared.

British Library Electronic Table of Contents (United Kingdom)

The effect of sodium gluconate anion (SG) on the corrosion and scale inhibition of ordinary steel in simulated cooling water has been studied using weight loss, polarisation curves, electrochemical impedance spectroscopy (EIS) and scanning electron microscopy (SEM) techniques. SG was studied in concentration from 10-4M to 10-1M. Results obtained reveal that SG perform excellently as corrosion and scaling inhibitor for ordinary steel in simulated cooling water. An increase of SG concentration leads to the increase of the corrosion potential towards the positive direction. The inhibition efficiency was a low temperature dependence. The inhibitor mechanism was treated as an adsorption process according to Langmuir adsorption isotherm. The SEM/EDAX data show that was a corrosion and scale inhi...

British Library Electronic Table of Contents (United Kingdom)

Vanadium carbide is the most effective grain growth inhibitor for ultrafine WC-Co composites due to its high solubility and mobility in the cobalt phase at relatively low temperatures; however, there are still some debates over the best way to introduce it into the WC-Co formulation. In this paper, the differences between admixed and chemically doped grain growth inhibitors on the microstructural development and properties of an ultrafine WC-10Co composite are discussed. The densification rate of chemically doped samples is slower in the early stage of sintering and the WC grain sizes of the sintered alloys are finer than those of admixed samples, leading to the increase of hardness and transverse rupture strength of the sintered alloys. The effectiveness of the chemically doped inhibitor ...

British Library Electronic Table of Contents (United Kingdom)

A study of the ordinary mild steel/cooling water interface, with and without inhibitor, was carried out using electrochemical impedance spectroscopy (EIS). EIS spectra in uninhibited medium reveal that a layer of corrosion and scale products is formed naturally and evolves with the immersion time. Monosaccharides derivatives were used as corrosion inhibitors. Most of them exhibit good behaviour against corrosion of ordinary steel in simulated water systems. Their inhibiting efficiency increases with concentration rise and depends on molecular structure especially -OH groups' position on two adjacent carbons and their number. In addition, the effect of MoO4^2^- on the corrosion inhibition in the presence of the best inhibitor was also studied by EIS. The addition of MoO4^2^- enhanced the in...

British Library Electronic Table of Contents (United Kingdom)

Total synthesis of cis-solamin A was accomplished without using protecting groups starting from (-)-muricatacin in 11 steps with an overall yield of 4.5%. The backbone of cis-solamin A was constructed by olefin cross-metathesis between the tetrahydrofuran moiety and g-lactone moiety. An enzymatic kinetic transesterification procedure was successfully applied to the synthesis of an optically pure g-lactone moiety.

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We have found that the methionine repression of the ..beta..-subunit gene expression is not due to degradation of the ..beta..-subunit but is due to an effect on synthesis of the ..beta..-subunit. The effect of methionine on the synthesis of the ..beta..-is due to an inhibition of ..beta..-subunit mRNA synthesis. 3 references, 1 figure.

British Library Electronic Table of Contents (United Kingdom)

A novel, one-pot, multicomponent synthesis of 4-arylidene-3-methyl-1-(4-arylthiazol-2-yl)-1H-pyrazol-5(4H)-ones is described using phenacyl bromides, thiosemicarbazide, ethylacetoacetate, and aryl aldehydes. This synthesis involves simultaneous formation of two heterocycles like thiazole and pyrazolone along with condensation of active methylene group by aldehydes via Knoevenagel reaction. The methodology is mild, efficient, and high yielding. GRAPHICAL ABSTRACT[image omitted

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A calorimetric microliter plate assay for ethanol amplified by aldehyde dehydrogenase (ALDH) was developed. In the assay ethanol from a sample took part in a chain-reaction catalyzed by alcohol dehydrogenase (ADH) and amplified by ALDH in the presence of NAD{sup +}, diaphorase, and p-ibdonitrotetrazolium-violet (INT-violet)(a precursor of red product). The resultant reaction gave a red color, the intensity of which was proportional to the amount of ethanol present. Using the technique, the content of activity from peanuts of differing maturity and curing stages were determined respectively. Data showed that immature peanuts had a higher level of ethanol and a lower ADH activity than mature peanuts, and that the level of ethanol and ADH activity decreased with the curing time. This indicates that peanut maturity and curing have an effect on ethanol. Also, this implies that other peanut volatiles could be affected in the same way as ethanol, a major volatile in ...

UK PubMed Central (United Kingdom)

Background: Patients with a typical depression are more likely to respond to monoamine oxidase inhibitors than to tricyclic antidepressants. They are frequently offered psychotherapy...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundFinasteride, a 5 alpha reductase inhibitor, is an established treatment for benign prostatic hyperplasia. The recommended dosage is 5 mg a day, however case reports have...Full Text Available

UK PubMed Central (United Kingdom)

Dominant mutations in sarcomere protein genes cause hypertrophic cardiomyopathy, an inherited human disorder with increased ventricular wall thickness, myocyte hypertrophy, and disarray. To understand...Full Text Available

UK PubMed Central (United Kingdom)

The treatment for erectile dysfunction (ED) was revolutionized with the development of phosphodiesterase type 5 (PDE5) inhibitors. Tadalafil (Cialis^®; Eli Lilly and Company, Indianapolis,...Full Text Available

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BackgroundUnderstanding the interactions between ion channels and blockers remains an important goal that has implications for delineating the basic mechanisms of ion channel function...Full Text Available

UK PubMed Central (United Kingdom)

Rapamycin inhibits the mTOR (target of rapamycin) pathway and extends lifespan in multiple species. The tuberous sclerosis complex (TSC) protein is a negative regulator of mTOR. In humans, loss of the...Full Text Available

UK PubMed Central (United Kingdom)

Dimethyl sulfoxide (DMSO) is commonly used in biological studies to dissolve drugs and enzyme inhibitors with low solubility. While DMSO is generally thought of as being relatively inert, it...Full Text Available

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In the adult mammalian CNS, the growth inhibitors oligodendrocyte-myelin glycoprotein (OMgp) and the reticulon RTN4 (Nogo) are broadly expressed in oligodendrocytes and neurons. Nogo and OMgp...Full Text Available

UK PubMed Central (United Kingdom)

Treating brain tumors using inhibitors of angiogenesis is extensively researched and tested in clinical trials. Although anti-angiogenic treatment holds a great potential for treating primary and secondary...Full Text Available

UK PubMed Central (United Kingdom)

Flavone and isoflavone phytoestrogens are plant chemicals and are known to be competitive inhibitors of cytochrome P450 aromatase with respect to the androgen substrate. Aromatase is the enzyme that...Full Text Available

UK PubMed Central (United Kingdom)

Glycoprotein 60 (gp60) is a normal plasma protein (mean concentration in normal serum 34 micrograms/ml) that is present in increased levels (mean concentration 97 micrograms/ml) in the sera of patients...Full Text Available

UK PubMed Central (United Kingdom)

Auxin modulates diverse plant developmental pathways through direct transcriptional regulation and cooperative signaling with other plant hormones. Genetic and biochemical approaches have clarified...Full Text Available

UK PubMed Central (United Kingdom)

Bortezomib/PS-341/Velcade, a proteasome inhibitor, is widely used to treat multiple myeloma. While several mechanisms of the cytotoxicity of the drug were proposed, the actual mechanism remains elusive....Full Text Available

Science.gov (United States)

of a tethered dimer of HIV-1 proteinase complexed with an inhibitor. Bhat TN, Baldwin ET, Liu B, Cheng YS, Erickson JW. Nat Struct Biol. 1994 Aug;1(8):552-6. Abstract End...

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Moenomycin A (MmA) belongs to a family of natural products that inhibit peptidoglycan biosynthesis by binding to the peptidoglycan glycosyltransferases (PGTs), the enzymes that make the glycan...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

In this work, a new class of thiadiazole derivatives, namely 3,5-bis(2-thienyl)-1,3,4-thiadiazole (2-TTH) and 3,5-bis(3-thienyl)-1,3,4-thiadiazole (3-TTH), have been studied as possible corrosion inhibitors for mild steel in molar hydrochloric acid (1M HCl). Polarisation curves and AC impedance methods have been used. These studies have shown that the thiadiazole derivatives were very good inhibitors for mild steel in 1M HCl. Comparison of results showed that 3-TTH was the best inhibitor. The potential of zero charge (PZC) of mild steel was studied by ac impedance method, and the mechanism of adsorption has been predicted. X-ray photoelectron spectroscopy surface analysis with thiadiazole derivatives shows that it chemisorbed at the mild steel/HCl interface. The adsorption of these inhibitors followed Langmuir's adsorption isotherm. The electronic properties of 2-TTH and 3-TTH, obtained using ...

UK PubMed Central (United Kingdom)

Restenosis remains the main complication of balloon angioplasty and/or stent implantation. Preclinical testing of new pharmacologic agents preventing restenosis largely rely on porcine models, where...Full Text Available

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The p21-activated kinases (PAKs), immediate downstream effectors of the small G-proteins of the Rac/cdc42 family, are critical mediators of signaling pathways regulating cellular behaviors and...Full Text Available

UK PubMed Central (United Kingdom)

Terfestatin A (TrfA), terphenyl-β-glucoside, was isolated from Streptomyces sp. F40 in a forward screen for compounds that inhibit the expression of auxin-inducible...Full Text Available

UK PubMed Central (United Kingdom)

Oligopeptidic drugs such as β-lactams and angiotensin-converting enzyme inhibitors share the same carriers in humans and animals, which results in possible pharmacokinetic interactions. To model...Full Text Available

UK PubMed Central (United Kingdom)

Selective phosphodiesterase type 5 inhibitors (PDE5Is) have revolutionized the treatment of erectile dysfunction (ED) in men. As an on-demand treatment, PDE5Is have excellent efficacy and safety in...Full Text Available

UK PubMed Central (United Kingdom)

OBJECTIVES: Although the tricyclic antidepressant amitriptyline is extensively used in the prophylactic treatment of chronic tension-type headache, only few studies have investigated the efficacy of...Full Text Available

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Inhibition efficiency of some water-soluble hydrazones for C-steel corrosion in hydrochloric acid has been tested by weight loss, polarisation measurements and open circuit technique. The inhibition effect was attributed to the adsorption of the additives on the C-steel surface as supported by adsorption measurements at Pt electrode using cyclic voltammetry. Electrochemical measurements indicated that all the additives behave as cathodic-type inhibitors. The data obtained fit well to both the Temkin adsorption isotherm and the kinetic-thermodynamic model. The inhibition behaviour and its order were explained with the help of the proposed skeletal representation.

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Nitrite is to be used to inhibit pitting corrosion during Extended Sludge Processing (ESP) at the Savannah River Plant. The required nitrite concentrations are expressed as a function of the slurries` nitrate ion concentration and temperature. In the most dilute slurries, the nitrite inhibitor requirement is independent of the nitrate ion concentration and depends only on the temperature of the waste. The nitrate-independent concentration ensures that there is sufficient inhibitor, in sludge slurries whose nitrate has been depleted by radiolysis, to prevent pitting corrosion induced by other corrosive anions (e.g., sulfate and chloride). The threshold nitrate concentration at which the nitrite level is expressed as a function only of temperature is 0.02 M.

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A chromium-free conversion coating for magnesium alloys were described. The conversion coating could be obtained when AZ31D magnesium alloy was immersed in a solution containing a manganese salt, phosphate and an inhibitor. Corrosion resistance of the chemical conversion coating was evaluated by anodizing polarization curve and salt immersion. XRD analysis showed that the conversion coating was mainly composed of Mn{sub 3}(PO{sub 4}){sub 2}. The morphology of the coating is observed by using SEM. The effect of electrolyte pH and concentration of inhibitor on coating growth are investigated. (orig.)

Science.gov (United States)

Calcium-activated chloride channels (CaCCs) are widely expressed in mammalian tissues, including intestinal epithelia, where they facilitate fluid secretion. Potent, selective CaCC inhibitors have not been available. We established a high-throughput screen for identification of inhibitors of a human intestinal CaCC based on inhibition of ATP/carbachol-stimulated iodide influx in HT-29 cells after lentiviral infection with the yellow fluorescent halide-sensing protein YFP-H148Q/I152L. Screening of 50,000 diverse, drug-like compounds yielded six classes of putative CaCC inhibitors, two of which, 3-acyl-2-aminothiophenes and 5-aryl-2-aminothiazoles, inhibited by >95% iodide influx in HT-29 cells in response to multiple calcium-elevating agonists, including thapsigargin, without inhibition of calcium elevation, calcium-calmodulin kinase II activation, or cystic fibrosis transmembrane conductance regulator chloride channels. ...

International Nuclear Information System (INIS)

Single-crystalline cadmium selenide nanoparticles were obtained using high-temperature solution phase synthesis (HTSPS) synthesis. X-Ray powder diffraction and transmission electron microscopy were used to confirm the crystallinity and morphology of the resulting nanoparticles. To study the action of CdSe on antioxidant activity, we selected two biotechnological important strains of microalgae: cyanobacteria Spirulina platensis and red microalgae Porphyridium cruentum. In the case of Porphyridium cruentum, the obtained results demonstrated an increase in the productivity. For Spirulina platensis, the presence of the compound in the cultivating medium decreased the productivity of cyanobacteria.

British Library Electronic Table of Contents (United Kingdom)

Cyst nematodes are troublesome parasites that live on, and destroy, a range of important host vegetable plants. Damage caused by the potato cyst nematode has now been reported in over 50 countries. One approach to eliminating the problem is to stimulate early hatching of the nematodes, but key hatching stimuli are not naturally available in sufficient quantities to do so. Here, we report the first chemical synthesis of solanoeclepin A, the key hatch-stimulating substance for potato cyst nematode. The crucial steps in our synthesis are an intramolecular cyclization reaction for construction of the highly strained tricyclo[5.2.1.01,6]decane skeleton (DEF ring system) and an intramolecular Diels???Alder reaction of a furan derivative for the synthesis of the ABC carbon framework. The present ...

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Iodine-125 labelled vinyl and aryl iodides are formed via the reaction of sodium iodide-125 with vinyl- and arylboronic acids. Good yields of isomerically pure products are obtained.

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No abstract prepared.

International Nuclear Information System (INIS)

Short communication.

KoreaScience (Korea)

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...Synthesis of low-temperature, fast, single-firing body for porcelain stoneware tiles with coal gangue Synthesis of low-temperature, fast, single-firing body for porcelain stoneware ... tiles with coal gangue Synthesis of low-temperature, fast, single-firing body for porcelain stoneware tiles with coal gangue Wei et al.,... Article Synthesis of low-temperature, fast, single-firing body for porcelain stoneware tiles with coal gangue Qiangwei Wei1, Wenyuan Gao1*, and Xinguo ...According to phase diagram theory, a low-temperature, fast, single-firing body mix for porcelain stoneware tiles was designed in the quaternary system CaO-MgO-Al2O3-SiO2, using ...

CERN Document Server

Proteins are polymers of amino acids. These macromolecules are synthesized by intracellular machines called {\\it ribosome}. Although, traditionally, the experimental investigation of protein synthesis has been an active area of research in molecular cell biology, important quantitative models of this phenomenon have been reported mostly in the research journals devoted to statistical physics and related interdisciplinary topics. From the perspective of a physicist, protein synthesis is a phenomenon of {\\it classical transport of interacting ribosomes on a messenger RNA (mRNA) template} that dictates the sequence of the amino acids on the protein. Here we bring this frontier area of contemporary research into the classroom by appropriate simplification of the models and methods. In particular, we develope a simple toy model and analyze it by some elementary techniques of non-equilibrium statistical mechanics to predict the average rate of ...

UK PubMed Central (United Kingdom)

Synthesis of wild-type Neurospora crassa assimilatory nitrate reductase is induced in the presence of nitrate ions and repressed in the presence of ammonium ions. Effects of several...Full Text Available

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... 0.2 ml each were taken. The reaction was stopped by the addition of 1 ml LO% trichloracetic acid (TCA) in 0.1 mole of pyrophosphate ...

Science.gov (United States)

Current models of DNA repair of biological damage are reviewed correlating the similarity between carcinogenesis and mutagenesis theories. (PCS)

Science.gov (United States)

Cambridge scientists in the late 1980's. This same team, then headed by Professor John Baldwin, built the world's first separated-element optical/infrared aperture synthesis...

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The objective of this work was to investigate the efficiency of imidazole and its derivatives 4-methylimidazone, 4-methyl-5-hydroxymethylimidazone, 1-phenyl-4-methylimidazone, and 1-(p-tolyl)-4-methylimidazole for corrosion inhibition of copper in 0.5 M hydrochloric acid. Corrosion inhibition was studied using potentiodynamic methods. These studies have shown that 1-(p-tolyl)-4-methylimidazole has the best inhibitory efficiency. Activation energies were obtained by measuring the temperature dependence of the corrosion current. The activation energies in the presence of the various inhibitors are low (3--5 kJ/mol), with the best inhibitor showing the highest value. The adsorptive behavior of the imidazole derivatives on the copper electrode surface follows a Freundlich-type isotherm. The standard free energies of adsorption are also low (14--16 kJ/mol), indicating that imidazole and its derivatives physisorb on the copper surface. Possible ...

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Tissue factor pathway inhibitor (TFPI), a protease inhibitor that circulates in association with plasma lipoproteins (VLDL, LDL and HDL), helps to regulate the extrinsic blood coagulation cascade. The authors have cloned a 125-kb genomic region containing the entire human TFPI gene on six overlapping cosmids and prepared a restriction map of this contig to clarify gene structure. More than half (45 kb) of the 85-kb gene is occupied with 5[prime] noncoding elements: coding begins at exon 3. A HindIII RFLP identified with one cosmid was genotyped in the CEPH panel of 559 reference families. Linkage analysis using markers on human chromosome 2 located the TFPI gene on 2q, 36 cM proximal to D2S43(pYNZ15) and 13 cM distal to the crystalline [gamma]-polypeptide locus CRYGP1(p5G1). 31 refs., 3 figs., 3 tabs.

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Corrosion in drilling and well stimulation is described in relation to acid corrosion inhibition, acid inhibitors, acetylenic inhibitors, synergistic blends, metallurgy, wellbore tubulars, coiled tubing, and high alloy tubular materials. Acidizing is a procedure for stimulating oil and gas wells. Factors that have an important influence on the reaction rate and the way in which acid reacts with rock include temperature, acid concentration, acid volume, injection velocity, acid viscosity, and fluid loss properties of the formation. The cost of drill pipe failures are $1 per fot of hole drilled, which is a significant fraction of the drilling cost. Steps in a test procedure are listed, as well as factors which determine the extent of acid corrosion in a given situation including acid type and strength, metal type, temperature, contact time; pressure, and volume/surface area ratio. Underbalanced drilling is a method for completing oil and gas ...

British Library Electronic Table of Contents (United Kingdom)

Pulses are rich in nutrients. The existence of anti-nutritional components and the length of time required for preparation have, however, limited their frequency of use compared to recommended intake levels. Anti-nutritional components in pulses can be largely removed by heat treatment. Additionally pre-treatment of pulses with heat and processing of seeds into flour could further enhance their use by decreasing processing and preparation times. In this study, trypsin inhibitor activity, functional properties, and microstructural characteristics of flours prepared from different varieties of lentil, chickpea, and pea as affected by roasting and boiling were evaluated. Both thermal treatments resulted in significant reduction (p<0.05) in trypsin inhibitor activity ranging from -95.6% to -37...

British Library Electronic Table of Contents (United Kingdom)

Reactive blue 2 (RB-2) had been characterized as a relatively potent ectonucleoside triphosphate diphosphohydrolase (E-NTPDase) inhibitor with some selectivity for NTPDase3. In search for the pharmacophore and to analyze structure-activity relationships we synthesized a series of truncated derivatives and analogs of RB-2, including 1-amino-2-sulfo-4-ar(alk)ylaminoanthraquinones, 1-amino-2-methyl-4-arylaminoanthraquinones, 1-amino-4-bromoanthraquinone 2-sulfonic acid esters and sulfonamides, and bis-(1-amino-4-bromoanthraquinone) sulfonamides, and investigated them in preparations of rat NTPDase1, 2, and 3 using a capillary electrophoresis assay. Several 1-amino-2-sulfo-4-ar(alk)ylaminoanthraquinone derivatives inhibited E-NTPDases in a concentration-dependent manner. The 2-sulfonate group ...

British Library Electronic Table of Contents (United Kingdom)

Eight selected sulfonamide drugs were investigated as inhibitors of heat shock protein 90 (Hsp90). The investigation included simulated docking experiments to fit the selected compounds within the binding pocket of Hsp90. The selected molecules were found to readily fit within the ATP-binding pocket of Hsp90 in low-energy poses. The sulfonamides torsemide, sulfathiazole, and sulfadiazine were found to inhibit the ATPase activity of Hsp90 with IC50 values of 1.0, 2.6, and 1.5 mM, respectively. Our results suggest that these well-established sulfonamides can be good leads for subsequent optimization into potent Hsp90 inhibitors.

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We quantified the resistance levels of transgenic rice plants, expressing Myxococcus xanthus protoporphyrinogen oxidase (PROTOX) in chloroplasts and mitochondria, to PROTOX inhibitors, acifluorfen, oxyfluorfen, carfentrazone-ethyl, and oxadiazon. We also determined whether active oxygen species-scavenging enzymes are involved in the resistance mechanism of transgenic rice. The transgenic rice line M4 was about >200-fold more resistant to oxyfluorfen than the wild-type (WT). M4 was also resistant to acifluorfen, carfentrazone-ethyl, and oxadiazon, but did not show multiple resistance to imazapyr and paraquat, which have different target sites. Acifluorfen, oxyfluorfen, carfentrazone-ethyl, and oxadiazon reduced the chlorophyll content in leaves of WT, but had minimal or no effect on M4. The...

Science.gov (United States)

Penile rehabilitation therapy following radical prostatectomy is a much debated topic. Erectile dysfunction is still a significant contributor to postoperative morbidity following radical prostatectomy, despite meticulous nerve-sparing technique. Secondary smooth muscle changes in the penis have been identified as the underlying causes of penile atrophy, veno-occlusive dysfunction, and fibrosis. Initial observations that intracavernous injection therapies used on a regular basis postoperatively resulted in improvements in the return of spontaneous erectile function led to the development of penile rehabilitation protocols. Chronic dosing of PDE-V inhibitors is now commonly used by urologists after radical prostatectomy. Despite the current enthusiasm of penile rehabilitation therapy, current scientific evidence with clinical trials is still limited. PMID:19255627

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Some N-containing or S-containing organic substances and some acetylenic alcohols were tested as inhibitors of the corrosive attack suffered by Fe-based metallic glasses in deaerated 0.1 N sulfuric acid (H{sub 2}SO{sub 4}) solution at 25 C. It was verified that the specific action these compounds exerted on the corrosion process of the amorphous alloys was similar to the one these compounds exerted on polycrystalline iron. The most efficient substances were those containing a sulfur atom with available lone pairs, which chiefly inhibited the anodic reaction of both metal specimens. Owing to the chemical and physical homogeneity of the amorphous alloy, the chemisorbed inhibitor film that formed on the glassy surface was more stable and protective than that formed on the polycrystalline iron.

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...comAbstract: Hepatocellular carcinoma (HCC), once thought to be a rare tumor in North America, is a rapidly increasing type of cancer in recent years in the United States. Current treatment modalities to halt the disease progression are only marginally effective. The mainstay treatment ...In addition, NM was shown to down-regulate urokinase plasminogen activator (by fibrin zymography) and up-regulate tissue inhibitors of metalloproteinases (by reverse zymography) in another HCC cell line, Sk-Hep-1. MMP-2 and MMP-9 activities were further modulated by cytokines, inducers and inhibitors, including NM. In ... Our results suggest that NM is an excellent candidate for therapeutic use in the treatment HCC by inhibiting critical parameters in cancer development and progression, such as proliferation, invasion and metastasis, and by inducing apoptosis. Last update: 2 September 2011 JavaScript seems ...

British Library Electronic Table of Contents (United Kingdom)

Summary Background:- Cholinesterase inhibitors form the mainstay of treatment for persons with mild-to-moderate Alzheimer-s disease (AD). The rivastigmine patch may increase compliance and the proportion of patients maintaining an efficacious dose compared with oral cholinesterase inhibitors. Objective:- To investigate the proportion of patients who reached and maintained the target rivastigmine patch dose compared with the target rivastigmine capsule dose reported in clinical trials. Methods:- This was a multicentre, 24-week, open-label study in persons with probable AD and a Mini-Mental State Examination (MMSE) score of --10 and --26. The primary outcome was the proportion of patients (ITT population) treated with 9.5-mg/24-h rivastigmine patch for at least 8-weeks at week 24. Secondary ...

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Synthesis of silver nanoparticles based on a polyol process and variable frequency microwave (VFM) was investigated. Comparing to a thermal method, the reaction by VFM radiation was much faster. The effects of silver nitrate concentration, poly(N-vinylpyrrolidone) (PVP) concentration, reaction time and reaction temperature were studied. It was found that the higher concentration of silver nitrate, longer reaction time and higher temperature increased the particle size while the higher concentration of PVP decreased the particle size.

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A decoupled characteristic between the damping of a specific swing mode and the stabilizer gain of the corresponding machine in multimachine power systems is identified. Using this decoupled characteristic a power system stabilizer (PSS) synthesis approach which is based on the phase compensation concept is verified on a 9-machine system and the dynamic performance of this system is significantly improved. This method is proved to be effective, simple and it can provide useful guidance for the PSS field tuning.

International Nuclear Information System (INIS)

Synthesis of the azido substituted non-steroidal anti-inflammatory drug 2-(2,6-dichloroanilino)phenylacetic acid and isotope labeling of this compound have been performed and are described. Initial evaluation of the binding ability and photoreactivity indicates that this compound has potential for photoaffinity labeling as well as enzyme selectivity studies. (author).

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The synthesis of (/sup 14/C)-10,11-Epoxy-(2E,6E)-farnesyl diazoacetate in one vessel, starting from (/sup 14/C)-glyoxylic acid, is described. This compound is useful as a potential photoaffinity labeling agent for juvenile hormone binding sites.

International Nuclear Information System (INIS)

We recently found that injection of 2 mCi of yttrium 90 (90Y; approximately 23,000 rads) into normal canine knees stimulated glycosaminoglycan (GAG) synthesis by femoral condylar cartilage. The present investigation was conducted to determine whether radiation affects cartilage metabolism directly. Rates of GAG synthesis and degradation in normal canine articular cartilage were studied following irradiation. Cultured synovium from the same knees was treated similarly, to determine the effects of irradiation on hyaluronic acid synthesis. Twenty-four hours after exposure to 1,000 rads, 10,000 rads, or 50,000 rads, 35S-GAG synthesis by the cartilage was 93%, 69%, and 37%, respectively, of that in control, nonirradiated cartilage. The effect was not rapidly reversible: 120 hours after exposure to 50,000 rads, GAG synthesis remained at only 28% of the control level. Autoradiography ...

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Stable strange quark matter produced in the QCD phase transition in the early universe will trap neutrons and repel protons, thus reducing primordial helium production, Ysub(p). For reasonable values of Ysub(p), the radius of strange droplets must exceed 10/sup 6/ cm if strange matter shall solve the dark-matter problem without spoiling Big Bang helium synthesis. (orig.).

UK PubMed Central (United Kingdom)

The rates of synthesis of a class of both secreted and intracellular degradative enzymes in Bacillus subtilis are controlled by a signal transduction pathway defined by at least four regulatory genes:...Full Text Available

UK PubMed Central (United Kingdom)

The endogenous reverse transcriptase reaction of equine infectious anemia virus (EIAV) has been studied, and conditions allowing synthesis of full-length minus-strand DNA have been determined. In contrast...Full Text Available

UK PubMed Central (United Kingdom)

Expression of brome mosaic virus (BMV) coat protein and internal genes of many other positive-strand RNA viruses requires initiation of subgenomic mRNA synthesis from specific internal sites on minus-strand...Full Text Available

Science.gov (United States)

We have used a cell-free polymerase I transcription system derived from HeLa cells to study the regulation of human rRNA synthesis. Analysis of deletion mutants spanning the start site of transcription at nucleotide +1 indicates that the control region affecting initiation of human rRNA synthesis is contained within sequences from nucleotides -158 to +18. This promoter region can be subdivided into (i) a central segment of approximately 40 base pair that is required for transcription and (ii) flanking sequences that influence the efficiency of transcription in vitro. We have examined the in vitro transcriptional activity of the human extract under various conditions that are thought to modulate rRNA synthesis in vivo. Cell-free extracts prepared from HeLa cells infected with adenovirus 2 synthesize human rRNA at levels greatly decreased relative to uninfected cell extracts. By contrast, in vitro transcription of human rRNA ...

International Nuclear Information System (INIS)

Effect of helium and hydrogen production on radiation-hardening of F82H irradiated by dual or triple beam condition were investigated. The specimens used were four types of ferritic martensitic steels of F82H-std (Fe-8Cr-2W-0.2V-0.04Ta-0.1C) steels tempered at 750degC for 60 minutes, 20% cold worked F82H steel, F82H tempered for 10 minutes and non-tempered F82H steels. The irradiation was performed at 450degC to 50 dpa under simultaneous dual beams of 10.5 MeV Fe"3"+ and 1.05 MeV He"+ or triple beams of those and 380 keV H"+ ions. The ratios of He (appm)/dpa and H(appm)/dpa were 15 nad 15 (or 150) for dual and triple ion beams. The hardness of the irradiated specimens measured at room temperature using a micro indentation after the irradiations. The hardness in these F82H steels irradiated at 450degC to 18 dpa under triple beam irradiation was harder than that under dual beam irradiation. Irradiation softening and hardening under dual beams was observed in F82H ...

UK PubMed Central (United Kingdom)

BackgroundThe status of estrogen receptor-α (ERα) is critical to the clinical prognosis and therapeutic approach in breast cancer. ERα-negative breast cancer...Full Text Available

UK PubMed Central (United Kingdom)

Two novel crystal structures of Zea mays protein kinase CK2α catalytic subunit, one in complex with the specific inhibitor 4,5,6,7-tetrabromobenzotriazole (TBB) and another...Full Text Available

International Nuclear Information System (INIS)

Azobenzene dyes are effective inhibitors for austenitic 304 L and 316 L stainless steel corrosion in high acidic medium up to 7N. A good efficiency is obtained from weight loss and electrochemical Rsub(p) measurements in hydrochloric acid, while no inhibition is observed in sulfuric solutions. Transformation from the primarily azobenzene to other compounds give rise to enhanced protection of steel samples, and probable structures of the inhibiting species are proposed in view of our results.

UK PubMed Central (United Kingdom)

Hematopoietic stem cells are resistant to HIV-1 infection. Here, we report a novel mechanism by which the cyclin-dependent kinase inhibitor (CKI) p21^{Waf1/Cip1/Sdi1} (p21), a known regulator...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

Current information suggests that chemical carcinogenesis is a multistep process with one of the best studied models in this regard being the two-stage carcinogenesis system using mouse skin. The effects of several carcinogens and tumor promoters in various sequences of application were studied to examine the nature of the process. The actions of several tumor inhibitors were compared. (ACR)

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In the aim to fight against tubes corrosion of geothermal wells which exploit the aquifer of Dogger reservoir in the Parisian basin, injection of corrosion inhibitors in the geothermal fluid has been generalized since 1989 by using an additive injection tube in the bottom of the well, allowing the protection of the two wells from the geothermal doublet. 3 annexes. 46 refs. 13 tabs. 9 figs.

UK PubMed Central (United Kingdom)

N-Hydroxy-N′-(4-n-butyl-2-methylphenyl)formamidine (HET0016) is a potent inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) formation by specific cytochrome P450 (CYP) isoforms....Full Text Available

Science.gov (United States)

Inhibition of the phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) pathway is an appealing method for decreasing the immunoresistance and augmenting T cell-mediated immunotherapy. A major impediment to this strategy is the impact of conventional PI3K/mTOR pathway inhibitors on T cell function. In particular, rapamycin, is a well-known immunosuppressant that can decrease the activity of the PI3K/mTOR pathway in tumor cells, but also has a profound inhibitory effect on T cells. Here we show that Honokiol, a natural dietary product isolated from an extract of seed cones from Magnolia grandiflora, can decrease PI3K/mTOR pathway-mediated immunoresistance of glioma, breast and prostate cancer cell lines, without affecting critical proinflammatory T cell functions. Specifically, we show that at doses sufficient to down-regulate levels of phospho-S6 and the negative immune regulator B7-H1 in tumor cells, Honokiol does not significantly impair T cell ...

UK PubMed Central (United Kingdom)

The p90 ribosomal S6 kinases (RSKs) also known as MAPKAP-Ks are serine/threonine protein kinases that are activated by ERK or PDK1 and act as downstream effectors of mitogen-activated protein kinase...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundPulmonary vascular structure remodeling (PVSR) is a hallmark of pulmonary hypertension. P27^kip1, one of critical cyclin-dependent kinase inhibitors, has been...Full Text Available

UK PubMed Central (United Kingdom)

Barley (Hordeum vulgare L. cv Golden Promise) plants were grown in a continuous culture system in which the root and shoot ammonia and amino acid levels were constant over a 6-hour...Full Text Available

UK PubMed Central (United Kingdom)

1,1-Dichloroethylene is reported to produce renal tumors in male mice. It is an hepatotoxin in fasted rats after inhalation. We found that trichloropropane epoxide, an inhibitor of epoxide hydrase,...Full Text Available

British Library Electronic Table of Contents (United Kingdom)

Plants use multiple defence mechanisms comprising both constitutive and inducible barriers to prevent entering of phytopathogenic micro-organisms. In many plant species one of the most efficient responses to combat attacking microbes is the rapid synthesis of antimicrobial low molecular weight phytoalexins, for example, resveratrol, 3,5,4prime-trihydroxystilbene (1). Resveratrol and its natural derivatives, however, display only moderate antimicrobial effects. Nevertheless, resveratrol may be a useful lead structure for the chemical synthesis of antimicrobials. In this study, several series of stilbenes have been synthesized, starting from the aldehydes using Wittig reactions to access the corresponding styrenes that were subjected to Mizoroki-Heck reactions to yield the stilbenes in good ...

International Nuclear Information System (INIS)

The use of Sialon ceramics has been restricted by the high temperature required for synthesis and the expense of the pure oxide and nitride raw materials required. For refractory applications the purity required is less demanding and it has been possible to exploit the outstanding durability of the Sialons at moderate cost. New low cost manufacturing routes are being developed by nitriding silicon metal powder at relatively low temperature with clay and various additives depending on the Sialon required. For example the introduction of carbon or fine silicon carbide allows the preparation of beta Sialons and alpha Sialons which can be stabilised by including the appropriate cations. A wide range of composite Sialon bodies with diverse properties can be prepared by a one step process. Current projects developing the synthesis routes are aimed, in the first instance, at refractory manufacture but are showing promise for more sophisticated ...

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Super light and high performance Mg{sub 2}Si/Mg composites, which had excellent mechanical properties, were developed via the combination of solid-state synthesis and hot extrusion process. In this study, cold compacting (CP) and repeated plastic working (RPW) were firstly carried out for the mixture of Mg-Si powders, and the refinement of both Mg grains and dispersoids. Each specimen was evaluated by observation of microstructure and tensile test. As a result, it was understood that Mg{sub 2}Si dispersoids were refined and dispersed into Mg matrix, and were flowed along extrusion direction. And their mechanical properties were higher than the conventional die casting alloys. Also the effect of RPW as the improvement of properties and the decrease of synthesis temperature were confirmed. (orig.)

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Replication of plus-strand RNA viruses depends on host factors that are recruited into viral replicase complexes. Previous studies showed that eukaryotic translation elongation factor (eEF1A) is one...Full Text Available

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Electricity generation from natural gas in gas turbine units can be made substantially more efficient by preliminary methane conversion to a synthesis gas containing hydrogen and carbon monoxide and/or by the use of some of the synthesis gas produced in industry. An alternative improvement involves the introduction of solid oxide fuel cells (SOFCs) and the use of the synthesis gas in them. In this study, a modified scheme of gas turbine cycle that includes an SOFC, a membrane reactor (instead of a traditional combustion chamber), and a catalytic reactor to perform methane conversion to produce hydrogen (synthesis gas) is proposed. Variations of the energy and exergy efficiencies of the integrated system with operating conditions are provided, showing, for example, that SOFC efficiency is enhanced if the fuel cell active area is augmented. The SOFC stack efficiency can be maximized by reducing the steam ...

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Previous work has provided evidence that plants may require boron to maintain adequate levels of pyrimidine nucleotides, suggesting that the state of boron deficiency may actually be one of pyrimidine...Full Text Available

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... Technology; Warsaw (Poland) 978-83-909690-8-4 221 p. RADIOLOGY AND

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In many dinoflagellate species, the plastid genome has been proposed to exist as a limited number of single-gene minicircles, and many genes normally found in the plastid genome are nuclear-encoded....Full Text Available

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The purpose of this study was to synthesize biocompatible polyvinylpyrrolidone (PVP)-coated iron oxide (PVP-IO) nanoparticles and to evaluate their efficacy as a magnetic resonance imaging (MRI)...Full Text Available

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The changes in protein species synthesized during early Drosophila embryogenesis were characterized by two-dimensional electrophoresis. Of the 261 proteins scored, 68 (26%) show dramatic changes in...Full Text Available

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Interleukin 12 (IL-12) activates natural killer (NK) and T cells with the secondary synthesis and release of interferon-gamma (IFN-gamma) and other cytokines. IL-12-induced organ alterations are reported...Full Text Available

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Carbon nanotubes (CNTs) are considered one of the most promising materials in nanotechnology, with attractive properties for many technologic applications. The different synthesis, purification, and...Full Text Available

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BackgroundGlucocorticoids down-regulate cytokine synthesis and suppress inflammatory responses. The glucocorticoid receptor (GR) antagonist RU486 may exacerbate the inflammatory...Full Text Available

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Increased intrauterine prostaglandin (PG) production is crucial for the initiation of parturition. To investigate the mechanisms controlling intrauterine PG synthesis, we examined the expression of...Full Text Available

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The high-yield, stereoselective conversion of geraniol (3,7-dimethyl-trans-2,6-octadien-1-ol) to the insect juvenile hormone, methyl 12,14-dihomojuvenate (methyl cis-10-epoxy-3,11-dimethyl-7-ethyl-trans,...Full Text Available

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The in vitro response of melatonin synthesis was assessed by incubation of individual whole pineal glands for 4 hr without or with different concentrations of isoproterenol in the medium. Pineals were taken either at the end of the 14-hr light phase (day)...

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Nucleoside 3'-phosphoramidite and chlorophosphite reagents have been found to react with the lactam function of guanine. This reaction caused unsatisfactory results when oligodeoxyribonucleotides containing...Full Text Available

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Salamanders regenerate their appendages after amputation and nerves are required for this process. Experiments were designed to test the idea that one way nerves could affect blastema cell proliferation is by influencing the metabolism of extracellular matrix (ECM) components and to identify neurotrophic factors which promote blastema cell mitosis. Temporal and spatial differences of glycosaminoglycans (GAGs) synthesis is innervated and denervated limbs were examined. Hyaluronic acid (HA) was found to be the major GAG produced during the proliferative period and chondroitin sulfate during differentiation. Denervation reduced synthesis of both these components by half. Dorsal root ganglia and fibroblast growth factor (FGF), a brain-derived mitogen, similarly doubled GAG synthesis in cultured blastemas, the FGF-effect being primarily on HA production. Histochemical and autoradiographical results confirmed the biochemical ...

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In the past, the fermentation activity of Saccharomyces cerevisiae in substrates with a high concentration of sucrose (HSuc), such as sweet bread doughs, has been linked inversely to invertase activity...Full Text Available

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A mutation in a new gene, molR, prevented the synthesis in Escherichia coli of molybdoenzymes, including the two formate dehydrogenase isoenzymes, nitrate reductase and trimethylamine-N-oxide reductase....Full Text Available

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Though the genetic background of ischaemic and haemorrhagic stroke is often polygenetic or multifactorial, it can in some cases result from a monogenic disease, particularly in young adults. Besides...Full Text Available

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In the synthesis of the peptidyl-polymer corresponding to the sequence (57-100) of the ..beta.. chain of human hemoglobin on Teflon with radiationally grafted polystyrene a comparative study was made of different methods of fragment condensation. It was shown that the most effective methods are azide condensation and condensation with the use of complex F.

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... of Viscous Liquids, Glasses, and Crystalline Materials Under Extremes of Pressure and Temperature ... Materials 9624724 ENG AZ U of Arizona Gervay Jacquelyn Synthesis of Novel Materials Utilizing Sialic ...

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Lumbricus terrestris (Annelid, Oligocheta) is capable of cellular- and humoral-specific reactions against natural antigens. Is this earthworm able to elaborate a response of antibody type against a...Full Text Available

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AIM: To analyze the antiviral mechanism of Epigallocatechin gallate (EGCG) against hepatitis B virus (HBV) replication.METHODS: In this research, the HBV-replicating cell line HepG2.117 was used...Full Text Available

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Glutathione (GSH) depletion sensitizes human lung carcinoma (A549-T27) cells to the cytotoxic effects of Cd++. The effects of GSH depletion on Cd++ accumulation and Cd++-induced metallothionein (MT) content were investigated to determine the possible role of these Cd++ responses in the sensitization process. Cellular GSH was depleted to 20% to 25% of control levels with buthionine sulfoximine (BSO), or diethyl maleate (DEM), respectively. Neither treatment significantly affected Cd++-induced accumulation of exogenous 35s-cysteine into intracellular MT in a dose-dependent fashion. The results indicate that neither enhanced Cd++ accumulation nor reduced MT synthesis plays a primary role in affecting enhanced Cd++ cytotoxicity in A549 cells with reduced GSH levels. Although BSO inhibition of GSH synthesis enhanced MT synthesis, it sensitized the cells to Cd++, which suggests an additive effect of GSH and MT in cadmium ...

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Mice lacking acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1), an enzyme that catalyzes the terminal step in triacylglycerol synthesis, have enhanced insulin sensitivity and are protected from...Full Text Available

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The effect of plant water deficit on ethylene production by intact plants was tested in three species, beans (Phaseolus vulgaris L.), cotton (Gossypium hirsutum L.)...Full Text Available

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The syntheses and applications of two metallointercalators, Rh(bpy)₂(chrysi)³⁺ and Rh(bpy)₂(phzi)³⁺, that target single base mismatches in DNA are...Full Text Available

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CF-23“The biggest stumbling block for biological sciences turned out to be synthetic organic chemistry” – Elias A. Zerhouni, Former NIH Director in Chemical...Full Text Available

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BackgroundWax esters are important ingredients in cosmetics, pharmaceuticals, lubricants and other chemical industries due to their excellent wetting property. Since the naturally...Full Text Available

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A balanced application of chemiosmosis to plant mitochondria is presented. Electron transport carriers are sequenced to achieve proton translocation across the inner membrane. The processes of proton translocation, use, and release are integrated to yield a description of the effective proton gradient available for metabolite transport and ATP synthesis. 27 references, 6 figures.

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Zinc modulates the activity of glutamic acid decarboxylase, the rate limiting enzyme in the synthesis of gamma-aminobutyric acid (GABA), which is a major inhibitory neurotransmitter. Low cerebrospinal...Full Text Available

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Gerard, G. and Papirno, R. , "Ductility Ratio of Aged Beta Titanium Alloy,. I t. Transactions of the ASM, VO~. 55, NO. 3, pp. 373-388, Sept. 1962. ...