igf1r kinase inhibitor: Topics by WorldWideScience.org

P-glycoprotein and breast cancer resistance protein in acute myeloid leukaemia cells treated with the Aurora-B Kinase Inhibitor barasertib-hQPA

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

2007-12-01

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Development of small-molecule inhibitors of the group I p21-activated kinases, emerging therapeutic targets in cancer

BackgroundAurora kinases play an essential role in orchestrating chromosome alignment, segregation and cytokinesis during mitotic progression, with both aurora-A and B frequently...Full Text Available

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CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway

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

2010-09-01

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Activation of fat cell adenylate cyclase by protein kinase C

Recently, CID755673 was reported to act as a highly selective inhibitor of protein kinase D (PKD). In the course of experiments using CID755673, we noticed that it exerted unexpected stimulatory...Full Text Available

2010-01-01

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Predictive and prognostic markers for epidermal growth factor receptor inhibitor therapy in non-small cell lung cancer

Purified protein kinase C (C-kinase) from guinea pig pancreas and rat brain stimulated adenylate cyclase activity in purified rat adipocyte membranes. Cyclase stimulation occurred over 100 to 1000 mU/ml of C-kinase activity, required greater than 10 ..mu..M calcium, proceeded without a lag, was not readily reversible, and required no exogenous phospholipid. Moreover, C-kinase inhibitors, such as chlorpromazine and palmitoyl carnitine, inhibited selectively adenylate cyclase which was activated by C-kinase and calcium. Depending on assay conditions, 10 nM 12-0-tetradecanoylphorbol-13-acetate (TPA) either enhanced or was required for kinase action on cyclase. Also, TPA plus calcium promoted the quantitative association of C-kinase with membranes. Adenylate cyclase activation by C-kinase was seen both ...

1986-05-01

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H-1152 Effects on Intraocular Pressure and Trabecular Meshwork Morphology of Rat Eyes

Epidermal growth factor receptor (EGFR) related therapies – mainly tyrosine kinase inhibitors (TKIs) such as erlotinib and gefitinib, but also monoclonal antibodies targeting EGFR, for example,...Full Text Available

2009-11-01

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c-JUN N-TERMINAL KINASE MODULATES OXIDANT STRESS AND PEROXYNITRITE FORMATION INDEPENDENT OF INDUCIBLE NITRIC OXIDE SYNTHASE IN ACETAMINOPHEN HEPATOTOXICITY

AbstractPurposeThe aim of this study was to elucidate the effects of the Rho-kinase inhibitor, H-1152, on cultured human trabecular meshwork (HTM) cells, TM morphology,...Full Text Available

2008-08-01

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Structural features underlying selective inhibition of protein kinase CK2 by ATP site-directed tetrabromo-2-benzotriazole

Acetaminophen (APAP) overdose, which causes liver injury in animals and humans, activates c-jun N-terminal kinase (JNK). Although it was shown that the JNK inhibitor SP600125 effectively reduced...Full Text Available

2010-07-01

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Adverse cutaneous reactions secondary to tyrosine kinase inhibitors including imatinib mesylate, nilotinib, and dasatinib

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

2001-11-01

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British Library Electronic Table of Contents (United Kingdom)

Abstract Imatinib mesylate is the first of a novel group of drugs that specifically target protein tyrosine kinases, which are central to the pathogenesis of human cancer. It has been approved for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumor and has been found efficacious in other neoplastic diseases. Nilotinib and dasatinib, a second-generation of tyrosine kinase inhibitors (TKIs), were developed in response to findings of emerging imatinib resistance or intolerance to the drug. Cutaneous reactions are the most common nonhematologic side effect of these drugs, and their management is challenging especially in the absence of alternative anticancer agents. The present review focuses on the clinical characteristics and the hypothesized molecular pathogenesis o...

2011-01-01

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Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors

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.

2009-01-01

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Primitive hematopoietic cells resist HIV-1 infection via p21^{Waf1/Cip1/Sdi1}

Multistage skin tumor promotion: involvement of a protein kinase

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

2007-02-01

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Beta-estradiol attenuates hypoxic pulmonary hypertension by stabilizing the expression of p27^kip1in rats

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)

1980-01-01

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Involvement of protein kinase C in the mechanism of action of Escherichia coli heat-stable enterotoxin (STa) in a human colonic carcinoma cell line, COLO-205

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

2010-01-01

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Cloning and mapping of the mouse {alpha}7-neuronal nicotinic acetylcholine receptor

The present study was undertaken to determine the involvement of calcium-protein kinase C pathway in the mechanism of action of Escherichia coli heat stable enterotoxin (STa) apart from STa-induced activation of guanylate cyclase in human colonic carcinoma cell line COLO-205, which was used as a model cultured cell line to study the mechanism of action of E. coli STa. In response to E. coli STa, protein kinase C (PKC) activity was increased in a time-dependent manner with its physical translocation from cytosol to membrane. Inhibition of the PKC activity in membrane fraction and inhibition of its physical translocation in response to IP_3-mediated calcium release inhibitor dantrolene suggested the involvement of intracellular store depletion in the regulation of PKC activity. Among different PKC isoforms, predominant involvement of calcium-dependent protein kinase C (PKC#alpha#) was specified using ...

2005-08-01

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A novel small-molecule inhibitor of NF-#kappa#B signaling

We report the isolation of cDNA clones for the mouse {alpha}7 neuronal nicotinic acetylcholine receptor subunit (gene symbol Acra7), the only nicotinic receptor subunit known to bind a-bungarotoxin in mammalian brain. This gene may have relevance to nicotine sensitivity and to some electrophysiologic findings in schizophrenia. The mouse {alpha}7 subunit gene encodes a protein of 502 amino acids with substantial identity to the rat (99.6%), human (92.8%), and chicken (87.5%) amino acid sequences. The {alpha}7 gene was mapped to mouse chromosome 7 near the p locus with the following gene order from proximal to distal: Myod1-3.5 {+-}1.7 cM-Gas2-0.9 cM {+-} 0.9 cM-D7Mit70-1.8 {+-} 1.2 cM- Acra7-4.4 {+-}1.0 cM-Hras1-ps11/Igf1r/Snrp2a. The human gene was confirmed to map to the homologous region of human chromosome 15q13-q14. 26 refs., 3 figs.

1995-03-20

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Cyclin-Dependent Kinase Inhibitor p16 and p21 Expression, and Cell Cycle Change in Human Lens Epithelial Cell Line SRA 01/04 following Contact Inhibition in Normal Culture

The inducible transcription factor NF-#kappa#B regulates divergent signaling pathways including inflammatory response and cancer development. Selective inhibitors for NF-#kappa#B signaling are potentially useful for treatment of inflammation and cancer. NF-#kappa#B is canonically activated by preferential disposal of its inhibitory protein; I#kappa#B, which suppresses the nuclear translocation of NF-#kappa#B. I#kappa#B#alpha# (a major member of I#kappa#B family proteins) is phosphorylated with an I#kappa#B kinase (IKK) and subsequently polyubiquitylated by SCF"#beta#"T"r"C"P"1 ubiquitin-ligase in the presence of E1 and E2 prior to proteasomal degradation. Here, we describe a novel inhibitor termed GS143, which suppressed I#kappa#B#alpha# ubiquitylation, but not I#kappa#B#alpha# phosphorylation, MDM2-directed p53 ubiquitylation, and proteasome activity in vitro. GS143 markedly suppressed the destruction of I#kappa#B#alpha# ...

2008-04-18

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British Library Electronic Table of Contents (United Kingdom)

Abstract Purpose: To describe the pattern of expression of the cyclin-dependent kinase inhibitors (CDKIs) p16, p21 and p27, and the cell cycle in SRA 01/04 cells relative to contact inhibition. Methods: SRA 01/04 cells were grown to overconfluence under normal conditions. At various phases of the cell growth, cells were assayed by flow cytometry and Western blotting for the expression of CDKIs. Results: Expression of p16 was detected from early logarithmic growth to stationary phases, during which the number of cells in G0/G1 increased from 46 to 69%. Expression of p21 was detected only during the overgrowth phase, when 60% of the cells were in G0/G1. Expression of p27 was not observed in SRA 01/04 cells. Conclusions: p16 expression was likely mediated by G0/G1 arrest to induce contact inh...

2011-01-01

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ERK-dependent and -independent pathways trigger human neural progenitor cell migration

Small-molecule screen identifies inhibitors of a human intestinal calcium-activated chloride channel.

Besides differentiation and apoptosis, cell migration is a basic process in brain development in which neural cells migrate several centimeters within the developing brain before reaching their proper positions and forming the right connections. For identifying signaling events that control neural migration and are therefore potential targets of chemicals to disturb normal brain development, we developed a human neurosphere-based migration assay based on normal human neural progenitor (NHNP) cells, in which the distance is measured that cells wander over time. Applying this assay, we investigated the role of the extracellular signal-regulated kinases 1 and 2 (ERK1/2) in the regulation of NHNP cell migration. Exposure to model substances like ethanol or phorbol 12-myristate 13-acetate (PMA) revealed a correlation between ERK1/2 activation and cell migration. The participation of phospho-(P-) ERK1/2 was confirmed by exposure of the cells to the MEK ...

2007-05-15

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Rapid inhibition of vasoconstriction in renal afferent arterioles by aldosterone

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 ...

2007-12-14

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Phosphorylation of proteins in Clostridium thermohydrosulfuricum

Aldosterone has been suggested to elicit vessel contraction via a nongenomic mechanism. We tested this proposal in microdissected, perfused rabbit renal afferent arterioles. Aldosterone had no effect on internal diameter in concentrations from 10(-10) to 10(-5) mol/L, but aldosterone abolished the ability of 100 mmol/L KCl to induce vascular contraction. The inhibitory effect of aldosterone was observed from 1 pmol/L. The inhibitory effect was significant after 5 minutes and maximal after 20 minutes and was fully reversible. Actinomycin D (10(-6) mol/L) prolonged the effect of aldosterone. The effect was abolished by the mineralocorticoid receptor antagonist spironolactone (10(-7) mol/L) but not by the glucocorticoid receptor antagonist mifepristone (10(-6) mol/L). The K+-mediated increase of intracellular calcium concentration in afferent arterioles was not affected by aldosterone. Mineralocorticoid receptor was detected by reverse transcription-polymerase chain reaction and ...

2003-01-01

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Calmodulin Kinase II Interacts with the Dopamine Transporter C Terminus to Regulate Amphetamine-Induced Reverse Transport

Cell extracts of the thermophile Clostridium thermohydrosulfuricum catalyzed the phosphorylation by (..gamma..-/sup 32/P)ATP of several endogenous proteins with M/sub r/s between 13,000 and 100,000. Serine and tyrosine were the main acceptors. Distinct substrate proteins were found in the soluble (e.g., proteins p66, p63, and p53 of M/sub r/s 66,000, 63,000, and 53,000, respectively) and particulate (p76 and p30) fractions, both of which contained protein kinase and phosphatase activity. The soluble fraction suppressed the phosphorylation of particulate proteins and contained a protein kinase inhibitor. Phosphorylation of p53 was promoted by 10..mu..M fructose 1,6-bisphosphate or glucose 1,6-bisphosphate and suppressed by hexose monophosphates, whereas p30 and p13 were suppressed by 5 ..mu..M brain (but not spinach) calmodulin. Polyamines, including the odd polyamines characteristic of thermophiles, modulated the labeling ...

1986-02-01

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VASCULARIZATION INHIBITOR

Efflux of dopamine through the dopamine transporter (DAT) is critical for the psychostimulatory properties of amphetamines, but the underlying mechanism is unclear. Here we show that Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) plays a key role in this efflux. CaMKIIalpha bound to the distal C terminus of DAT and colocalized with DAT in dopaminergic neurons. CaMKIIalpha stimulated dopamine efflux via DAT in response to amphetamine in heterologous cells and in dopaminergic neurons. CaMKIIalpha phosphorylated serines in the distal N terminus of DAT in vitro, and mutation of these serines eliminated the stimulatory effects of CaMKIIalpha. A mutation of the DAT C terminus impairing CaMKIIalpha binding also impaired amphetamine-induced dopamine efflux. An in vivo role for CaMKII was supported by chronoamperometry measurements showing reduced amphetamine-induced dopamine efflux in response to the CaMKII inhibitor KN93. Our data suggest that ...

2006-01-01

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J-STORE (Japan)

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2008-01-25

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Accumulation, Activity and Localization of Cell Cycle Regulatory Proteins and the Chloroplast Division Protein FtsZ in the Alga Scenedesmus quadricauda under Inhibition of Nuclear DNA Replication

British Library Electronic Table of Contents (United Kingdom)

Synchronized cultures of the green alga Scenedesmus quadricauda were grown in the absence (untreated cultures) or in the presence (FdUrd-treated cultures) of 5-fluorodeoxyuridine, the specific inhibitor of nuclear DNA replication. The attainment of commitment points, at which the cells become committed to nuclear DNA replication, mitosis and cellular division, and the course of committed processes themselves were determined for cell cycle characterization. FdUrd-treated cultures showed nearly unaffected growth and attainment of the commitment points, while DNA replication(s), nuclear division(s) and protoplast fission(s) were blocked. Interestingly, the FdUrd-treated cells possessed a very high mitotic histone H1 kinase activity in the absence of any nuclear division(s). Compared with the ...

2008-01-01

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Honokiol-mediated inhibition of PI3K/mTOR pathway: a potential strategy to overcome immunoresistance in glioma, breast, and prostate carcinoma without impacting T cell function.

A modified immunoblot method to identify substrates of protein kinases

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 ...

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Transforming growth factor-b induces CD44 cleavage that promotes migration of MDA-MB-435s cells through the up-regulation of membrane type 1-matrix metalloproteinase

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British Library Electronic Table of Contents (United Kingdom)

CD44, a transmembrane receptor for hyaluronic acid, is implicated in various adhesion-dependent cellular processes, including cell migration, tumor cell metastasis and invasion. Recent studies demonstrated that CD44 expressed in cancer cells can be proteolytically cleaved at the ectodomain by membrane type 1-matrix metalloproteinase (MT1-MMP) to form soluble CD44 and that CD44 cleavage plays a critical role in cancer cell migration. Here, we show that transforming growth factor-b (TGF-b), a multifunctional cytokine involved in cell proliferation, differentiation, migration and pathological processes, induces MT1-MMP expression in MDA-MB-435s cells. TGF-b-induced MT1-MMP expression was blocked by the specific extracellular regulated kinase-1/2 (ERK1/2) inhibitor PD98059 and the specific pho...

2009-01-01

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Salicylate Treatment Improves Age-Associated Vascular Endothelial Dysfunction: Potential Role of Nuclear Factor kB and Forkhead Box O Phosphorylation

British Library Electronic Table of Contents (United Kingdom)

We hypothesized that I kappa B kinase (IKK)-mediated nuclear factor kappa B and forkhead BoxO3a phosphorylation will be associated with age-related endothelial dysfunction. Endothelium-dependent dilation and aortic protein expression/phosphorylation were determined in young and old male B6D2F1 mice and old mice treated with the IKK inhibitor, salicylate. IKK activation was greater in old mice and was associated with greater nitrotyrosine and cytokines. Endothelium-dependent dilation, nitric oxide (NO), and endothelial NO synthase phosphorylation were lower in old mice. Endothelium-dependent dilation and NO bioavailability were restored by a superoxide dismutase mimetic. Nuclear factor kappa B and forkhead BoxO3a phosphorylation were greater in old and were associated with increased express...

2011-01-01

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Proteomic Analysis of Proteins Secreted by HepG2 Cells Treated with Butyl Benzyl Phthalate

British Library Electronic Table of Contents (United Kingdom)

Proteomic changes in proteins secreted by human hepatocellular carcinomas (HepG2) cells exposed to butyl benzyl phthalate (BBP) were evaluated. HepG2 cells were treated with three different concentrations of BBP (0, 10, or 25 ?M) for 24 or 48 h. Following incubation, the cells were subjected to proteomic analysis using two different pI ranges (4-7 and 6-9) and large-size two-dimensional gel electrophoresis. Results showed resolution of a total of 2776 protein spots. Of these, 29, including 19 upregulated and 10 downregulated proteins, were identified by electrospray ionization-mass spectrometry-mass spectrometry (ESI-MS/MS). Among these, the identities of cystatin C, Rho guanine nucleotide dissociation inhibitor, gelsolin, DEK protein, Raf kinase inhibitory protein, triose phosphate ...

2010-01-01

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Internal medical therapy of gastrointestinal stroma tumors; Internistische Therapie gastrointestinaler Stromatumoren

Rapid detection of epidermal growth factor receptor mutations with multiplex PCR and primer extension in lung cancer

Until recently no active treatment for advanced or metastatic gastrointestinal stroma tumors (GIST) was available. The tyrosine kinase inhibitor imatinib has revolutionized the treatment of this disease and the median overall survival now reaches 5 years. The standard dose of imatinib is 400 mg per day. Locally advanced GIST should be treated with systemic therapy prior to surgical resection. Imatinib was recently licensed for adjuvant therapy following complete surgical removal of GIST in patients with a significant risk of recurrence. (orig.) [German] Bis vor einigen Jahren existierte keine wirksame systemische Therapie fuer fortgeschrittene oder metastasierte gastrointestinale Stromatumoren (GIST). Der Tyrosinkinaseinhibitor Imatinib hat die Behandlung dieser Tumoren revolutioniert, die mediane Ueberlebenszeit liegt heute bei etwa 5 Jahren. Die Standarddosierung von Imatinib betraegt initial 400 mg/Tag. Lokal fortgeschrittene Tumoren werden ...

2009-12-15

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Epidermal growth factor receptor (EGFR) kinase domain mutations hyperactivate the kinase and confer kinase addiction of the non-small-cell lung cancer (NSCLC) tumor...Full Text Available

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EhMAPK, the Mitogen-Activated Protein Kinase from Entamoeba histolytica Is Associated with Cell Survival

The activity of Src-related protein-tyrosine kinases is repressed by the phosphorylation of a conserved carboxyl-terminal tyrosine by another cytoplasmic protein-tyrosine kinase termed p50csk. In this...Full Text Available

1994-05-24

35

Cardiac Myosin Is a Substrate for Zipper-interacting Protein Kinase (ZIPK)*

Mitogen Activated Protein Kinases (MAPKs) are a class of serine/threonine kinases that regulate a number of different cellular activities including cell proliferation, differentiation, survival and...Full Text Available

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AMP-Activated Protein Kinase: A Stress-Responsive Kinase with Implications for Cardiovascular Disease

Zipper-interacting protein kinase (ZIPK) is a member of the death-associated protein kinase family associated with apoptosis in nonmuscle cells where it phosphorylates myosin regulatory light chain...Full Text Available

2010-02-19

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Phosphorylation of Annexin A1 by TRPM7 Kinase: A Switch Regulating the Induction of an ?-Helix

AMP-activated protein kinase (AMPK) was initially viewed as energy sensor and activated by increased intracellular concentrations of AMP following nutrient deprivation. Physiological or pathological...Full Text Available

2010-04-01

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Structure and Function of NtCDPK1, a Calcium-dependent Protein Kinase in Tobccco

TRPM7 is an unusual bifunctional protein consisting of an α-kinase...Full Text Available

2011-03-29

39

Gamma interferon induces rapid and coordinate activation of mitogen-activated protein kinase (extracellular signal-regulated kinase) and calcium-independent protein kinase C in human monocytes.

Full Text Available

2000-05-01

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Corrosion Inhibitors Equipment on Environmental Expert

Gamma interferon plays an important role in regulating the functional properties of mononuclear phagocytes. In the present study, the role of activated protein kinases in the mechanism of action of...Full Text Available

1994-07-01

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Wastenet

... Corrosion Inhibitors Equipment on Environmental Expert Find and compare a variety of corrosion inhibitors equipment on the world's largest environmental industry portal. View ...

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Phosphorylation of sites 3 and 2 in rabbit skeletal muscle glycogen synthase by a multifunctional protein kinase (ATP-citrate lyase kinase)

Detection of a Quorum-Sensing Inhibitor from the Natural Products

A multifunctional protein kinase, purified from rat liver as ATP-citrate lyase kinase, has been identified as a glycogen synthase kinase. This kinase catalyzed incorporation of up to 1.5 mol of and)2numberSPO4/mol of synthase subunit associated with a decrease in the glycogen synthase activity ratio from 0.85 to a value of 0.15. Approximately 65-70% of the TUPO4 was incorporated into site 3 and 30-35% into site 2 as determined by reverse phase high performance liquid chromatography. This multifunctional kinase was distinguished from glycogen synthase kinase-3 on the basis of nucleotide and protein substrate specificities. Since the phosphate contents in glycogen synthase of sites 3 and 2 are altered in diabetes and by insulin administration, the possible involvement of the multifunctional kinase was explored. Glycogen synthase purified from ...

1985-10-05

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Insulin-induced decrease in protein phosphorylation in rat adipocytes not explained by decreased A-kinase activity

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2008-02-01

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The impact of a repeated bout of eccentric exercise on muscular strength, muscle soreness and creatine kinase.

In isolated rat adipocytes, insulin inhibits lipolysis to a greater extent than would be predicted by the decrease in (-/+)cAMP activity ratio of cAMP-dependent protein kinase (A-kinase), from which it was speculated that insulin promotes the dephosphorylation of hormone-sensitive lipase. They have examined the phosphorylation state of cellular proteins under conditions of varying A-kinase activities in the presence and absence of insulin. Protein phosphorylation was determined by SDS-PAGE electrophoresis of extracts from /sup 32/P-loaded cells; glycerol and A-kinase activity ratios were measured in the cytosolic extracts from control, non-radioactive cells. Increased protein phosphorylation in general occurred over the same range of A-kinase activity ratios, 0.1-0.3, associated with increased glycerol release. The insulin-induced decrease in lipolysis was associated with a decrease ...

1987-05-01

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Syk Tyrosine Kinase Acts as a Pancreatic Adenocarcinoma Tumor Suppressor by Regulating Cellular Growth and Invasion

The purpose of this study was to determine if there were any beneficial or detrimental effects regarding delayed onset muscle soreness (DOMS), serum creatine kinase (CK), and maximum concentric strength...Full Text Available

1994-12-01

46

Separation, Purification, and Comparative Properties of Chloroplast and Cytoplasmic Phosphoglycerate Kinase from Barley Leaves ¹

We have identified the nonreceptor tyrosine kinase syk as a marker of differentiation/tumor suppressor in pancreatic ductal adenocarcinoma (PDAC). Syk expression is lost in poorly differentiated PDAC...Full Text Available

2009-12-01

47

Phosphoglycerate kinase and triosephosphate isomerase from the hyperthermophilic bacterium Thermotoga maritima form a covalent bifunctional enzyme complex.

The chloroplast and cytoplasmic isoenzymes of phosphoglycerate kinase (PGK) (EC. 2.7.2.3) from Hordeum vulgare leaves have been separated and purified for the first time to apparent...Full Text Available

1990-06-01

48

Involvement of AMP-activated-protein-kinase (AMPK) in neuronal amyloidogenesis

Phosphoglycerate kinase (PGK) from the hyperthermophilic bacterium Thermotoga maritima has been purified to homogeneity. A second larger enzyme with PGK activity and identical N-terminal sequence was...Full Text Available

1995-02-01

49

Immunolocalization of phospho-S6 kinases: a new way to detect mitosis in tissue sections and in cell culture

AMP-activated-protein-kinase (AMPK) is a key sensor and regulator of cellular and whole-body energy metabolism and plays a key role in regulation of lipid metabolism. Since lipid metabolism...Full Text Available

2010-09-03

50

Expression and Characterization of the Mycobacterium tuberculosis Serine/Threonine Protein Kinase PknB

During a study on the mTor pathway in the rat kidney we observed a striking increase of the phosphorylation of the S6 kinase in mitosis. In cryostat sections of perfusion-fixed tissue mitotic cells...Full Text Available

2007-02-01

51

EFFECT OF AGE ON THE ROLE OF RHO-KINASE IN SHORT TERM PARTIAL BLADDER OUTLET OBSTRUCTION

PknB is a member of the newly discovered eukaryotic-like protein serine/threonine kinase (PSTK) family of proteins. The pknB gene was cloned and expressed in Escherichia coli....Full Text Available

1999-11-01

52

Deficiency of Phosphoinositide 3-Kinase Enhancer Protects Mice From Diet-Induced Obesity and Insulin Resistance

ObjectivesWe examined the expression of Rho Kinase (ROK) isoforms in young and old rabbit’s detrusor smooth muscles (SM) during the progression of short term...Full Text Available

2008-03-01

53

Chronic inflammation and estradiol interact through MAPK activation to affect TMJ nociceptive processing by trigeminal caudalis neurons

OBJECTIVEPhosphoinositide 3-kinase enhancer A (PIKE-A) is a proto-oncogene that promotes tumor growth and transformation by enhancing Akt activity. However, the physiological functions...Full Text Available

2010-04-01

54

Autoantibodies to BRAF, a new family of autoantibodies associated with rheumatoid arthritis

The mitogen-activated protein kinase/extracellular regulated kinase (MAPK/ERK) pathway plays a key role in mediating estrogen actions in the brain and neuronal sensitization during inflammation....Full Text Available

2009-12-29

55

Antisense Expression of the CK2 ?-Subunit Gene in Arabidopsis. Effects on Light-Regulated Gene Expression and Plant Growth1

IntroductionBRAF (v raf murine sarcoma viral oncogene homologue B1) is a serine-threonine kinase involved in the mitogen-activated protein kinase (MAPK) signalling pathway, known...Full Text Available

2010-01-01

56

Allosteric regulation of glycerol kinase by enzyme IIIglc of the phosphotransferase system in Escherichia coli and Salmonella typhimurium.

The protein kinase CK2 (formerly casein kinase II) is thought to be involved in light-regulated gene expression in plants because...Full Text Available

1999-03-01

57

AMP-activated protein kinase (AMPK) cross-talks with canonical Wnt signaling via phosphorylation of ?-catenin at Ser 552

The mechanism by which enzyme IIIglc of the bacterial phosphotransferase system regulates the activity of crystalline glycerol kinase from Escherichia coli has been studied, and the inhibitory effects...Full Text Available

1985-05-01

58

c-Jun N-terminal Kinase 2 Regulates Multiple Receptor Tyrosine Kinase Pathways in Mouse Mammary Tumor Growth and Metastasis

AMP-activated protein kinase (AMPK) is a key regulator of energy metabolism; its activity is regulated by a plethora of physiological conditions, exercises and many anti-diabetic drugs. Recent...Full Text Available

2010-04-23

59

The Protein Kinase SnRK2.6 Mediates the Regulation of Sucrose Metabolism and Plant Growth in Arabidopsis^[W]^[OA]

c-Jun N-terminal kinase 2 (JNK2) isoforms are transcribed from the jnk2 gene and are highly homologous with jnk1 and jnk3 transcriptional products....Full Text Available

2011-01-01

60

Canonical and Alternative Pathways in Cyclin-Dependent Kinase 1/Cyclin B Inactivation upon M-Phase Exit in Xenopus laevis Cell-Free Extracts

In higher plants, three subfamilies of sucrose nonfermenting-1 (Snf1)-related protein kinases have evolved. While the Snf1-related protein kinase 1 (SnRK1) subfamily has been shown to share pivotal...Full Text Available

2010-05-01

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Combined protection of metals by cathodic polarization and inhibitors

Cyclin-Dependent Kinase 1 (CDK1) is the major M-phase kinase known also as the M-phase Promoting Factor or MPF. Studies performed during the last decade have shown many details of how CDK1 is regulated...Full Text Available

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The NADPH oxidase inhibitor diphenyleneiodonium is also a potent inhibitor of cholinesterases and the internal Ca²⁺ pump

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.

1996-12-01

63

Organophosphate acetylcholine esterase inhibitor poisoning from a home-made shampoo

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

2009-10-01

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Gyrase B Inhibitor Impairs HIV-1 Replication by Targeting Hsp90 and the Capsid Protein*

Organophosphate acetylcholine esterase inhibitor poisoning is a major health problem in children. We report an unusual cause of organophosphate acetylcholine esterase inhibitor poisoning. Two children...Full Text Available

2011-07-01

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Cholinesterase for Prophylactics of Poisoning by Organophosphorous Inhibitors

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

2010-12-10

66

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

67

Disruption of contact inhibition in rat liver epithelial cells by various types of AhR ligands

Screening and Extraction Condition of Anti-skin Aging Elastase Inhibitor from Medicinal Plants

The maintenance of a balance between cell gain and cell loss is essential for proper liver function. The exact role of aryl hydrocarbon receptor (AhR) in regulating cell proliferation and apoptosis of liver cells remains unclear, since ligand-dependent activation of AhR has been shown to induce cell cycle arrest, proliferation, differentiation or apoptosis, depending on the cellular model used. AhR can directly interact with retinoblastoma protein in hepatic cells, forming protein complexes that can efficiently block cell cycle progression by inducing G1 arrest, or to induce the expression of inhibitors of cyclin-dependent kinases, such as p271. On the other hand, it has been suggested that AhR could play a stimulatory role in cell proliferation, either directly or by mediating a release from contact inhibition. It is now generally accepted that progenitor cells exist in the liver, are activated in various liver diseases and can form a ...

2004-09-15

68

Purification and Characterization of Angiotensin I-Converting Enzyme Inhibitors from Sinapis alba L.

Full Text Available

2005-12-01

69

Pilot Study of the Treatment of VEGF-Signaling Pathway Inhibitor-Induced Hypertension

Full Text Available

2000-06-01

70

High Throughput Screening on Angiogenesis Inhibitor and Promoter of Medicinal Plants using a Protein Microarray Chip

Treatment Induced Hypertension

2011-01-19

71

Hepatocyte growth factor activator inhibitor-1 has a complex subcellular itinerary.

Full Text Available

2007-04-01

72

A study of matrix metalloproteinase-9 inhibitor in Hovenia dulcis Thunberg

Udgivelsesdato: 2008-Jul-15

2008-01-01

73

Corrosion inhibition of mild steel by alkylimidazolium ionic liquids in hydrochloric acid

Full Text Available

2011-04-01

74

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...

2009-01-01

75

Inhibitors of steel corrosion in hydrochloric acid at high temperature

Phospholemman: A Novel Cardiac Stress Protein

A proposed inhibitor for steel corrosion in hydrochloric acid consists essentially of 0.5% of an inhibitor called BA-6, 0.25-0.5% of 1-hexynol-3, and about 0.02% of potassium iodide (calculated on the amount of acid). The inhibitor DA-6 is produced by condensing benzylamine with utrotropine. 1-Hexynol-3, secondary alcohol, is obtained from butyraldehyde and acetylene in the presence of caustic potash. The increase of potassium iodide concentration from 0.02-0.1% increases the protective action of the inhibitor. Hexynol, dipropargyl ester, and potassium iodide must be introduced in HC1 before injection of the latter into the well.

1965-01-07

76

Cardiac Enzymes, Renal Failure and Renal Transplantation

Phospholemman (PLM), a member of the FXYD family of regulators of ion transport, is a major sarcolemmal substrate for protein kinases A and C in cardiac and skeletal muscle. In the heart, PLM...Full Text Available

2010-08-01

77

Up-Regulation of the RhoA/Rho-Kinase Signaling Pathway in Corpus Cavernosum from Endothelial Nitric-Oxide Synthase (NOS), but Not Neuronal NOS, Null Mice

Diagnostic accuracy of the currently available serum markers of cardiac injury, such as myoglobin, creatine kinase and its myocardial isoform, are altered in patients with renal failure. It is shown...Full Text Available

2006-03-01

78

Selective control of amino acid metabolism by the GCN2 eIF2 kinase pathway in Saccharomyces cerevisiae

We tested the hypothesis that the basal release of nitric oxide (NO) from endothelial cells modulates contractile activity in the corpus cavernosum (CC) via inhibition of the RhoA/Rho-kinase signaling...Full Text Available

2010-04-01

79

Phosphorylation of ?6-Tubulin by Protein Kinase C? Activates Motility of Human Breast Cells*

BackgroundWhen eukaryotic cells are deprived of amino acids, uncharged tRNAs accumulate and activate the conserved GCN2 protein kinase. Activated Gcn2p up-regulates the general amino...Full Text Available

80

Kappa-opioid receptor activation during reperfusion limits myocardial infarction via ERK1/2 activation in isolated rat hearts

Engineered overexpression of protein kinase Cα (PKCα) was previously shown to endow nonmotile MCF-10A human breast cells with aggressive motility. A traceable mutant of PKCα...Full Text Available

2009-06-26

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81

Involvement of stress-activated protein kinase and p38 mitogen-activated protein kinase in mIgM-induced apoptosis of human B lymphocytes

BackgroundWe investigated whether p42/p44 extracellular signal-regulated kinases (ERK1/2) and/or phosphatidylinositol-3-OH kinase (PI3K)-Akt play a crucial role in cardioprotection...Full Text Available

2011-05-01

82

Evolution of a bifunctional enzyme: 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase.

Despite intensive efforts, the intracellular signaling pathways that mediate apoptosis remain unclear. The human B lymphoma cell line, B104, possesses characteristics that make it an attractive model...Full Text Available

1996-11-26

83

A New Metal-Binding Site for Yeast Phosphoglycerate Kinase as Determined by the Use of a Metal-ATP Analog

The bifunctional rat liver enzyme 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (ATP:D-fructose-6-phosphate 2-phosphotransferase/D-fructose-2,6-bisphosphate 2-phosphohydrolase, EC 2.7.1.105/EC...Full Text Available

1989-12-01

84

(-)-Epigallocatechin Gallate Regulates CD3-mediated T Cell Receptor Signaling in Leukemia through the Inhibition of ZAP-70 Kinase*

Suicide substrate β, γ-bidentate Rh(III)ATP (RhATP) was used to map the metal ion-binding site in yeast phosphoglycerate kinase (PGK). Cleavage of the RhATP-inactivated enzyme with...Full Text Available

1997-02-01

85

Histone deacetylase inhibitors and transforming growth factor-b induce 15-hydroxyprostaglandin dehydrogenase expression in human lung adenocarcinoma cells

The ζ chain-associated 70-kDa protein (ZAP-70) of tyrosine kinase plays a critical role in T cell receptor-mediated signal transduction and the immune response. A high level of ZAP-70 expression...Full Text Available

2008-10-17

86

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...

2006-01-01

87

Treatment with Selective Serotonin Reuptake Inhibitors and Mirtapazine Results in Differential Brain Activation by Visual Erotic Stimuli in Patients with Major Depressive Disorder

The Pseudoreceptor BMP and Activin Membrane-bound Inhibitor Positively Modulates Wnt/?-Catenin Signaling*

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

2009-06-01

88

Structure-activity relationships of anthraquinone derivatives derived from bromaminic acid as inhibitors of ectonucleoside triphosphate diphosphohydrolases (E-NTPDases)

The canonical Wnt/β-catenin pathway plays a pivotal role in regulating embryogenesis and tumorigenesis by promoting cell proliferation. BAMBI (BMP and activin membrane-bound inhibitor) has...Full Text Available

2008-11-28

89

Results of single and repeat dose studies of the oral matrix metalloproteinase inhibitor marimastat in healthy male volunteers

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

2009-03-01

90

Ixodes scapularis tick serine proteinase inhibitor (serpin) gene family; annotation and transcriptional analysis

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

1998-01-01

91

Intravenous proton pump inhibitors for peptic ulcer bleeding: Clinical benefits and limits

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

92

Effects of the direct thrombin inhibitor dabigatran on ex vivo coagulation time in orthopaedic surgery patients: a population model analysis

Peptic ulcer bleeding is a common disease and recurrent bleeding is an independent risk factor of mortality. Infusion with proton pump inhibitors (PPIs) prevents recurrent bleeding after successful...Full Text Available

2011-03-16

93

ANTITUMOR ACTIVITY OF HYALURONIC ACID SYNTHESIS INHIBITOR 4-METHYLUMBELLIFERONE IN PROSTATE CANCER CELLS

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

2006-11-01

94

A Review of the Pathophysiology and Novel Treatments for Erectile Dysfunction

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

2010-04-01

95

Wrapped Laminated Felted Monolithic Combustible Cartridge ...

Erectile dysfunction (ED) affects up to 50% of men between the ages of 40 and 70. Treatment with PDE-5 inhibitors is effective in the majority of men with ED. However, PDE-5 inhibitors are not effective...Full Text Available

2010-01-01

96

Effect of Resveratrol on the Induction of Cdk Inhibitor p21 and Pro-apoptotic Bax Expression by amyloid-? in Astroglioma C6 Cells

... ordnance requirements. Descriptors : *Combustible cartridge cases, *Patents, Laminates, Felts, Flame inhibitors, Films. Subject ...

1975-08-26

97

Quantum mechanical interpretation for the role of polyamines in acid corrosion inhibition

Full Text Available

2005-04-01

98

Criteria for the selection of corrosion inhibitors for Arctic and subsea high velocity flowlines

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

99

Basis for the Specificity and Activation of the Serpin Protein Z-dependent Proteinase Inhibitor (ZPI) as an Inhibitor of Membrane-associated Factor Xa*

Qualifying corrosion inhibitors for use in high velocity multiphase flowlines in arctic or subsea environments is discussed. The tests include high velocity flow loop corrosion tests, pumpability through 0.125 (0.318 cm) inch capillary at low temperatures, compatibility with Nylon 11, emulsion tendency testing, and partitioning characteristics. Laboratory and field data show the importance for using the above criteria for inhibitor selection.

1999-11-01

100

The hippo pathway in biological control and cancer development

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

2010-06-25

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101

British Library Electronic Table of Contents (United Kingdom)

Abstract The Hippo pathway is an evolutionally conserved protein kinase cascade involved in regulating organ size in vivo and cell contact inhibition in vitro by governing cell proliferation and apoptosis. Deregulation of the Hippo pathway is linked to cancer development. Its first core kinase Warts was identified in Drosophila more than 15 years ago, but it gained much attention when other core components of the pathway were identified 8 years later. Major discoveries of the pathway were made during past several years. The core kinase components Hippo, Salvador, Warts, and Mats in the fly and Mst1/2, WW45, Lats1/2, and Mob1 in mammals phosphorylate and inactivate downstream transcriptional co-activators Yorkie in the fly, Yes-associated protein (YAP) and transcriptional co-activator with ...

2011-01-01

102

Phorbol esters, protein kinase C, and thyroxine 5 prime -deiodinase in brown adipocytes

Inhibition of the heterotetrameric K++ channel KCNQ1/KCNE1 by the AMP-activated protein kinase

Protein kinase C activity has been identified in the rat brown adipocyte. About 60% of this activity is found in the cytosolic fraction under basal conditions, and 12-O-tetradecanoylphorbol 13-acetate (TPA) causes a rapid shift from the cytosol to the particulate fraction. Norepinephrine and phenylephrine causes a similar redistribution that can be blocked by prazosin but not by alprenolol. {alpha}{sub 1}-Adrenergic agonists cause three- to fivefold stimulation of type 2 iodothyronine 5{prime}-deiodinase activity in brown adipocytes. TPA has no effect on basal deiodinase activity and reduces the response of the enzyme to {alpha}{sub 1}-adrenergic agonists. These results suggest that the translocation of protein kinase C from cytosol to particulate fraction is not sufficient to increase deiodinase activity but can modulate the {alpha}{sub 1}-adrenergic agonist-mediated responses in these cells.

1988-03-01

103

British Library Electronic Table of Contents (United Kingdom)

Abstract The heterotetrameric K++-channel KCNQ1/KCNE1 is expressed in heart, skeletal muscle, liver and several epithelia including the renal proximal tubule. In the heart, it contributes to the repolarization of cardiomyocytes. The repolarization is impaired in ischemia. Ischemia stimulates the AMP-activated protein kinase (AMPK), a serine/threonine kinase, sensing energy depletion and stimulating several cellular mechanisms to enhance energy production and to limit energy utilization. AMPK has previously been shown to downregulate the epithelial Na++ channel ENaC, an effect mediated by the ubiquitin ligase Nedd4-2. The present study explored whether AMPK regulates KCNQ1/KCNE1. To this end, cRNA encoding KCNQ1/KCNE1 was injected into Xenopus oocytes with and without additional injection o...

2011-01-01

104

Corrosion inhibition of mild steel by alkylimidazolium ionic liquids in hydrochloric acid

Corrosion inhibition of mild steel by alkylimidazolium ionic liquids in hydrochloric acid

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{sub 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{sub 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{sup -3} M of inhibitors was studied in the temperature range of 303-333 K. ...

2009-02-15

105

Brine chemistry and control of adverse chemical reactions with natural gas production. Annual report, January-December 1984

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 ...

2009-02-15

106

skittles, a Drosophila phosphatidylinositol 4-phosphate 5-kinase, is required for cell viability, germline development and bristle morphology, but not for neurotransmitter release.

Monitoring brine chemistry to determine the extent of potential adverse reactions was simplified by the development of a field brine test kit and a series of nomographs. Results of the kit analyses serve as input to the nomographs, which provide a graphic means of determining the scaling tendency (Saturation Index value) of a brine. Brines that do not tend to form scale may be corrosive. Saturation Index values have been correlated with various processes using data from geopressured wells in the Gulf Coast area. Control of scale in surface equipment of geopressured wells by chemical inhibitors has been successful. Downhole treatment with inhibitors to prevent scale formation in the production tubing is being investigated. Laboratory simulations indicate that an inhibitor squeeze treatment may be successful at the Gladys McCall No. 1 well. Inhibitor mixtures exhibit additive behavior at minimum ...

1985-01-01

107

Use of clopidogrel in the reduction of myocardial damage during percutaneous coronary intervention

The phosphatidylinositol pathway is implicated in the regulation of numerous cellular functions and responses to extracellular signals. An important branching point in the pathway is the phosphorylation...Full Text Available

1998-12-01

108

The Receptor Tyrosine Kinase FGFR4 Negatively Regulates NF-kappaB Signaling

It is estimated that approximately a quarter of patients undergoing coronary intervention may have significant post-procedural creatinine (CK)/creatinine kinase myocardial band (CK-MB) elevations and...Full Text Available

2009-01-01

109

The Dynamical Mechanism of Auto-Inhibition of AMP-Activated Protein Kinase

BackgroundNFκB signaling is of paramount importance in the regulation of apoptosis, proliferation, and inflammatory responses during human development and homeostasis, as...Full Text Available

110

The Cytokinin Receptors of Arabidopsis Are Located Mainly to the Endoplasmic Reticulum¹^[W]^[OA]

We use a novel normal mode analysis of an elastic network model drawn from configurations generated during microsecond all-atom molecular dynamics simulations to analyze the mechanism of auto-inhibition...Full Text Available

2011-07-01

111

Serotype- and strain- dependent contribution of the sensor kinase CovS of the CovRS two-component system to Streptococcus pyogenes pathogenesis

The plant hormone cytokinin is perceived by membrane-located sensor histidine kinases. Arabidopsis (Arabidopsis thaliana) possesses three cytokinin receptors: ARABIDOPSIS HISTIDINE...Full Text Available

2011-08-01

112

Role of bile salt in regulating Mcl-1 phosphorylation and chemoresistance in hepatocellular carcinoma cells

BackgroundThe Streptococcus pyogenes (group A streptococci, GAS) two-component signal transduction system CovRS has been described to be important for pathogenesis...Full Text Available

113

Regulation of hyaluronan secretion into rabbit synovial joints in vivo by protein kinase C

BackgroundGlycochenodeoxycholate (GCDA) is one of the major human bile salts. Bile salts stimulate cell survival and proliferation through the mitogen-activated protein kinase, but...Full Text Available

114

Regulation of ROMK1 Channels by Protein-tyrosine Kinase and -tyrosine Phosphatase*

Hyaluronan (HA) is important for joint cavitation, lubrication, volume regulation and synovial fluid drainage but little is known about the regulation of joint HA synthesis/secretion in vivo....Full Text Available

2003-07-15

115

Regulation of Mixed Lineage Kinase 3 is Required for Neurofibromatosis-2-Mediated Growth Suppression in Human Cancer

We have used the two-electrode voltage clamp technique and the patch clamp technique to investigate the regulation of ROMK1 channels by protein-tyrosine phosphatase (PTP) and protein-tyrosine...Full Text Available

2001-03-09

116

Rapamycin inhibits trypanosome cell growth by preventing TOR complex 2 formation

The Neurofibromatosis-2 (NF2) tumor suppressor merlin negatively regulates cell proliferation in numerous cell types. We have previously shown that the NF2...Full Text Available

2011-02-17

117

PtdIns 3-Kinase Orchestrates Autophagosome Formation in Yeast

Target of rapamycin (TOR) kinases control cell growth through two functionally distinct multiprotein complexes. TOR complex 1 (TORC1) controls temporal cell growth and is sensitive to rapamycin, whereas...Full Text Available

2008-09-23

118

PKC expression is regulated by dietary K intake and mediates internalization of SK channels in the CCD

Eukaryotic cells can massively transport their own cytoplasmic contents into a lytic compartment, the vacuole/lysosome, for recycling through a conserved system called autophagy. The key process in...Full Text Available

2011-01-01

119

Oligomycin-induced Bioenergetic Adaptation in Cancer Cells with Heterogeneous Bioenergetic Organization

We have used Western blot analysis and immunocytochemistry to determine the effect of dietary K intake on the expression of protein kinase C (PKC) isoforms in the kidney. Western blot has demonstrated...Full Text Available

2004-06-01

120

Neutral endopeptidase inhibits prostate cancer cell migration by blocking focal adhesion kinase signaling

Cancer cells constantly adapt to oxidative phosphorylation (OXPHOS) suppression resulting from hypoxia or mitochondria defects. Under the OXPHOS suppression, AMP-activated protein kinase (AMPK) regulates...Full Text Available

2010-04-23

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121

Neurotensin Receptor 1 Is Expressed in Gastrointestinal Stromal Tumors but Not in Interstitial Cells of Cajal

Neutral endopeptidase 24.11 (NEP, CD10) is a cell-surface enzyme expressed by prostatic epithelial cells that cleaves and inactivates neuropeptides implicated in the growth of androgen-independent prostate...Full Text Available

2000-12-01

122

Lnk constrains myeloproliferative diseases in mice

Gastrointestinal stromal tumors (GIST) are thought to derive from the interstitial cells of Cajal (ICC) or an ICC precursor. Oncogenic mutations of the KIT or PDGFRA receptor tyrosine kinases are present...Full Text Available

123

Light-Dependent Regulation of Cyanobacterial Phytochrome Expression

Hematopoietic stem and progenitor cell (HSPC) expansion is regulated by intrinsic signaling pathways activated by cytokines. The intracellular kinase JAK2 plays an essential role in cytokine signaling,...Full Text Available

2010-06-01

124

Elevated c-Src tyrosine kinase activity in premalignant epithelia of ulcerative colitis.

A histidine kinase protein (Cph1) with sequence homology and spectral characteristics very similar to those of the plant phytochrome has been recently identified in the cyanobacterium Synechocystis...Full Text Available

2000-01-01

125

Effects of norepinephrine infusion on myocardial high-energy phosphate content and turnover in the living rat.

Ulcerative colitis (UC) is a chronic inflammatory disease of the colon with a high incidence of colon cancer. Dysplasia is a precursor to carcinoma and a predictor of malignant potential; epithelia...Full Text Available

1994-02-01

126

DosT and DevS are oxygen-switched kinases in Mycobacterium tuberculosis

Using 31P-nuclear magnetic resonance, we studied the relationship between myocardial high-energy phosphate content and flux values for the creatine kinase reaction in the living rat under inotropic...Full Text Available

1987-06-01

127

Differential Regulation of Mitogen-Activated Protein Kinase Pathways by Acetaminophen and Its Nonhepatotoxic Regioisomer 3?-Hydroxyacetanilide in TAMH Cells

Exposure of Mycobacterium tuberculosis to hypoxia is known to alter the expression of many genes, including ones thought to be involved in latency, via the transcription factor DevR...Full Text Available

2007-08-01

128

DNA replication in vertebrates requires a homolog of the Cdc7 protein kinase

Acetaminophen (APAP), a widely used analgesic and antipyretic that is considered to be relatively safe at recommended doses, is the leading cause of drug-induced liver failure in the United States....Full Text Available

2010-07-01

129

Cytokinin-Dependent Photorespiration and the Protection of Photosynthesis during Water Deficit1[W][OA

CDC7 is an essential gene required for DNA replication in Saccharomyces cerevisiae. Cdc7p homologs have recently been identified in vertebrates, but their role in DNA...Full Text Available

1999-03-16

130

Co-Induction of LTP and LTD and Its Regulation by Protein Kinases and Phosphatases

We investigated the effects of P_SARK∷IPT (for Senescence-Associated Receptor Kinase∷Isopentenyltransferase) expression and cytokinin production...Full Text Available

2009-07-01

131

Chemical activation of MEK1 - a redox trigger for evaluating the effects of phosphorylation.

The cellular properties of long-term potentiation (LTP) following pairing of pre- and postsynaptic activity were examined at a known glutamatergic synapse in the leech, specifically between the pressure...Full Text Available

2010-05-01

132

Calcium/Calmodulin-Dependent Protein Kinase II Mediates Hippocampal Glutamatergic Plasticity During Benzodiazepine Withdrawal

An approach to generate mimics of phosphorylated serine proteins chemically through site-specific sulfonation of cysteine is presented. This chemical modification is reversible in the presence of reducing agent and therefore is analogous to the kinase/phosphatase system used in nature. PMID:21717004

2011-06-30

133

Beyond AICA Riboside: In Search of New Specific AMP-activated Protein Kinase Activators

Benzodiazepine withdrawal anxiety is associated with potentiation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor (AMPAR) currents in hippocampal CA1 pyramidal...Full Text Available

2010-08-01

134

Autophosphorylation Within the Atg1 Activation Loop Is Required for Both Kinase Activity and the Induction of Autophagy in Saccharomyces cerevisiae

Summary5-Aminoimidazole-4-carboxamide-1-β-d-ribofuranoside (AICA riboside) has been extensively used in vitro and in vivo to...Full Text Available

2009-01-01

135

ATM-Dependent Phosphorylation of ATF2 Is Required for the DNA Damage Response

Autophagy is an evolutionarily conserved degradative pathway that has been implicated in a number of physiological events important for human health. This process was originally identified as a response...Full Text Available

2010-07-01

136

AICAR inhibits adipocyte differentiation in 3T3L1 and restores metabolic alterations in diet-induced obesity mice model

SummaryActivating transcription factor 2 (ATF2) is regulated by JNK/p38 in response to stress. Here, we demonstrate that the protein kinase ATM phosphorylates ATF2 on serines...Full Text Available

2005-05-27

137

A Conserved Role for Phosphoinositide-3-Kinase but Not Akt Signaling in Mitochondrial Adaptations that Accompany Physiological Cardiac Hypertrophy

BackgroundObesity is one of the principal causative factors involved in the development of metabolic syndrome. AMP-activated protein kinase (AMPK) is an energy sensor that regulates...Full Text Available

138

?Activation of the mitogen-activated protein kinase pathways by heat shock

Physiological cardiac hypertrophy is associated with mitochondrial adaptations that are characterized by activation of PGC-1α and increased fatty acid oxidative (FAO) capacity. It is...Full Text Available

2007-10-01

139

Use of integrin-linked kinase to extend function of encapsulated pancreatic tissue

In addition to inducing new transcriptional activities that lead within a few hours to the accumulation of heat shock proteins (Hsps), heat shock activates within minutes the major signaling transduction...Full Text Available

2002-04-01

140

Functions of mammalian Cdc7 kinase in initiation/monitoring of DNA replication and development

We have studied the impact of overexpression of an intracellular signaling protein, integrin-linked kinase (ILK), on the survival and function of encapsulated islet tissue used for the treatment of type 1 diabetes. The dimensions of the encapsulated tissue can impact the stresses placed on the tissue and ILK overexpression shows the ability to extend function of dissociated cells as well as intact islets. These results suggest that lost cell-extracellular matrix interactions in cell encapsulation systems can lead to decreased insulin secretion and ILK signaling is a target to overcome this phenomenon. (communication)

2010-12-15

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141

Cdc7 kinase plays an essential role in firing of replication origins by phosphorylating components of the replication complexes. Cdc7 kinase has also been implicated in S phase checkpoint signaling downstream of the ATR and Chk1 kinases. Inactivation of Cdc7 in yeast results in arrest of cell growth with 1C DNA content after completion of the ongoing DNA replication. In contrast, conditional inactivation of Cdc7 in undifferentiated mouse embryonic stem (ES) cells leads to growth arrest with rapid cessation of DNA synthesis, suggesting requirement of Cdc7 functions for continuation of ongoing DNA synthesis. Furthermore, loss of Cdc7 function induces recombinational repair (nuclear Rad51 foci) and G2/M checkpoint responses (inhibition of Cdc2 kinase). Eventually, p53 becomes highly activated and the cells undergo massive p53-dependent apoptosis. Thus, defective origin activation in mammalian cells can ...

2003-11-27

142

Heat storage composition

Sodium gluconate as corrosion and scale inhibitor of ordinary steel in simulated cooling water

A heat storage compostion comprises sodium sulfate decahydrate as main component, a supercooling inhibitor, and a solid-liquid separation inhibitor. The composition is characterized in that hydraulic calcium sulfate and/or calcium sulfate dihydrate is contained as the solid-liquid separation inhibitor in an amount of 2-15 wt% base on the whole weight of the composition, whereby the solid-liquid separation, i.e. the sedimentation of the anhydrous sodium sulfate during the phase transition, is effectively prevented and the long-term stability is improved. The long-term stabilty of the composition can be more improved by addition of a silcia series of thickener.

1987-05-05

143

Possible association of lower rate of postherpetic neuralgia in patients on anti-tumor necrosis factor-

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.

2008-06-15

144

British Library Electronic Table of Contents (United Kingdom)

Abstract Recently, a study of patients with rheumatoid arthritis who developed herpes zoster while taking a tumor necrosis factor (TNF)- inhibitor reported a decreased incidence of postherpetic neuralgia. The objective of this study was to investigate whether patients on TNF- inhibitors who developed herpes zoster have a lower incidence of subsequent development of postherpetic neuralgia. A retrospective review of herpes zoster patients on TNF- inhibitors (infliximab, etanercept, or adalimumab) was conducted in 12 dermatology clinics. Medical records of such patients were reviewed thoroughly to confirm herpes zoster and TNF- inhibitors and any subsequent development of postherpetic neuralgia (pain score -3 out of 10 after 90 days of shingles onset) was noted. A total of 206 cases were revi...

2011-01-01

145

NASA TECH BRIEF - NASA Technical Report Server (NTRS)

Inhibitor for aqueous acid solutions

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

146

Clinical, virological and immunological responses in Danish HIV patients receiving raltegravir as part of a salvage regimen

An organic inhibitor for acid corrosion inhibition is described. The inhibitor is a condensation product of a mixture of diethyl- and dibutyl-thiourea with hexamethylenetatramine. This condensation product is preferably made by reacting a mixture of diethyl- and dibutyl-thiourea, in a weight ratio of from 1:5 to 5:1, with 0.1 to 1 mole of hexamethylene tetramine per mole of the thiourea mixture, at temperatures of from 100 to 150 C. It is possible to modify this by using other organic thiourea derivatives containing organic radicals (aliphatic or aromatic) having up to 10 carbon atoms, for example, ditoluyl-thiourea, in addition to the mixture of diethyl- and dibutyl-thiourea, but the amount by weight of these other derivatives must not exceed 20% of the diethyl-dibutyl-thiourea mixture. The advantages of the inhibitor are observed mainly when it is used in hydrofluoric acid solutions. 6 claims.

1978-07-18

147

Use of platelet glycoprotein IIb/IIIa inhibitors in diabetics undergoing PCI for non-ST-segment elevation acute coronary syndromes: impact of clinical status and procedural characteristics

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

2010-01-01

148

Synergistic activity of the proteasome inhibitor PS-341 with non-myeloablative 153-Sm-EDTMP skeletally targeted radiotherapy in an orthotopic model of multiple myeloma

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

2010-06-01

149

Structural Chemistry of Human SET Domain Protein Methyltransferases

Multiple myeloma is a highly radiosensitive skeletal malignancy, but bone-seeking radionuclides have not yet found their place in disease management. We previously reported that the proteasome inhibitor...Full Text Available

2006-05-15

150

Side chain SAR of bicyclic [beta]-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem

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.

2011-08-22

151

Preferential antitumor effect of the Src inhibitor dasatinib associated with a decreased proportion of aldehyde dehydrogenase 1-positive cells in breast cancer cells of the basal B subtype

Bridged monobactam {beta}-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C {beta}-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.

2010-09-17

152

Piperazine sulfonamide BACE1 inhibitors: Design, synthesis, and in vivo characterization

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

153

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.

2010-01-01

154

Pharmacokinetics and pharmacodynamics of terbogrel, a combined thromboxane A₂ receptor and synthase inhibitor, in healthy subjects

Effects of graded oral doses of a new 5-hydroxytryptamine/noradrenaline uptake inhibitor (Ro 15-8081) in comparison with 60 mg codeine and placebo on experimentally induced pain and side effect profile in healthy men.

AimsTo characterize the pharmacokinetics of terbogrel, a new combined thromboxane A₂ (TxA₂) receptor and synthase inhibitor, in healthy human subjects after...Full Text Available

2004-07-01

155

Clavulanic Acid, a Novel Inhibitor of ?-Lactamases

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

1987-11-01

156

Caspase-10-Dependent Cell Death in Fas/CD95 Signalling Is Not Abrogated by Caspase Inhibitor zVAD-fmk

Clavulanic acid, Z-(2R,5R)-3-(β-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0] heptane-2-carboxylic acid, has been shown to be an effective inhibitor of the β-lactamases of the...Full Text Available

1978-11-01

157

Brine chemistry and control of adverse chemical reactions with natural gas production. Annual report, January-December 1986

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

158

Dietary turmeric modulates DMBA-induced p21ras, MAP kinases and AP-1/NF-?B pathway to alter cellular responses during hamster buccal pouch carcinogenesis

Monitoring brine chemistry to determine the extent of potential adverse reactions has been simplified by the development of a field-brine test kit and a series of nomographs. Results of the kit analyses serve as input to the nomographs, which provide a graphic means of determining the scaling tendency (Saturation Index value) of a brine. Brines that do not tend to form scale may be corrosive. Saturation Index values were correlated with various processes using data from geopressured wells in the Gulf Coast area. Control of scale in surface equipment with chemical inhibitors has been successful. Numerous laboratory simulations of inhibitor squeeze operations were completed using core material with calcite present and absent. The corresponding wells were squeezed with phosphorous-containing inhibitors, and the flowback of brine was monitored for phosphorous concentrations vs time. A new procedure to measure the concentration ...

1987-01-01

159

British Library Electronic Table of Contents (United Kingdom)

The chemopreventive efficacy of turmeric has been established in experimental systems. However, its mechanism(s) of action are not fully elucidated in vivo. The present study investigates the mechanism of turmeric-mediated chemoprevention in 7,12-dimethylbenz(a)anthracene (DMBA)-induced hamster buccal pouch (HBP) carcinogenesis at 2, 4, 6, 10 and 12?weeks. Dietary turmeric (1%) led to decrease in DMBA-induced tumor burden and multiplicity, and enhanced the latency period in parallel, to its modulatory effects on oncogene products and various cellular responses during HBP tumorigenesis. DMBA-induced expression of ras oncogene product, p21 and downstream target, the mitogen-activated protein kinases were significantly decreased by turmeric during HBP carcinogenesis. Turmeric also diminished ...

2008-01-01

160

Use of inhibitors for scale control in brine-producing gas and oil wells

Primary structures of four trypsin inhibitor E homologs from venom of Dendroaspis angusticeps: structure-function comparisons with other dendrotoxin homologs.

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 ...

1986-01-01

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161

Tomato 14-3-3 Protein 7 Positively Regulates Immunity-Associated Programmed Cell Death by Enhancing Protein Abundance and Signaling Ability of MAPKKK ?^[C]^[W]

Four trypsin inhibitor homologs, the first known from Dendroaspis angusticeps venom, were characterized using a combination of gel filtration, cation exchange, reverse-phase liquid chromatography, Edman degradation and mass spectrometry. The four toxins comprise two 57 residue and two 59 residue isoforms. The long toxins possess a Lys-Gln N-terminal extension lacked by the short toxins. The only other structural difference is an Arg/His replacement at position 55. The long Arg55 variant is identical to trypsin inhibitor E from the venom of Dendroaspis polylepis. The name epsilon-dendrotoxin is suggested so as to follow the nomenclature of Benishin, C.G., Sorensen, R.G., Brown, W.E., Krueger, B.K., Blaustein, M.P., 1988. Four polypeptide components of green mamba venom selectively block certain potassium channels in rat brain synaptosomes. Mol. Pharmacol. 34, 152-159. Among snake venom protease inhibitors, the ...

2002-03-01

162

The direct interaction between ASH2, a Drosophila trithorax group protein, and SKTL, a nuclear phosphatidylinositol 4-phosphate 5-kinase, implies a role for phosphatidylinositol 4,5-bisphosphate in maintaining transcriptionally active chromatin.

Programmed cell death (PCD) is triggered when Pto, a Ser-Thr protein kinase, recognizes either the AvrPto or AvrPtoB effector from Pseudomonas syringae pv tomato. This...Full Text Available

2010-01-01

163

Targeting AMP-activated protein kinase in adipocytes to modulate obesity-related adipokine production associated with insulin resistance and breast cancer cell proliferation

The products of trithorax group (trxG) genes maintain active transcription of many important developmental regulatory genes, including homeotic genes. Several trxG proteins have been shown to act in...Full Text Available

2004-07-01

164

Synergistic Activation of Glucose-6-Phosphate Dehydrogenase and NAD(P)H oxidase by Src kinase Elevates Superoxide in Type 2 Diabetic, Zucker fa/fa, Rat Liver

BackgroundAdipokines, e.g. TNFα, IL-6 and leptin increase insulin resistance, and consequent hyperinsulinaemia influences breast cancer progression. Beside its mitogenic...Full Text Available

165

Selective Expression in Carotid Body Type I Cells of a Single Splice Variant of the Large Conductance Calcium- and Voltage-activated Potassium Channel Confers Regulation by AMP-activated Protein Kinase*

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

2009-08-01

166

Scyl1 Facilitates Nuclear tRNA Export in Mammalian Cells by Acting at the Nuclear Pore Complex

Inhibition of large conductance calcium-activated potassium (BK_Ca) channels mediates, in part, oxygen sensing by carotid body type I cells. However, BK_Ca channels remain active...Full Text Available

2011-04-08

167

ReSETting PP2A tumour suppressor activity in blast crisis and imatinib-resistant chronic myelogenous leukaemia

Scyl1 is an evolutionarily conserved N-terminal protein kinase-like domain protein that plays a role in COP1-mediated retrograde protein trafficking in mammalian cells. Furthermore, loss of Scyl1 function...Full Text Available

2010-07-15

168

Overexpression of Partner of Numb Induces Asymmetric Distribution of the PI4P 5-Kinase Skittles in Mitotic Sensory Organ Precursor Cells in Drosophila

The deregulated kinase activity of p210-BCR/ABL oncoproteins, hallmark of chronic myelogenous leukaemia (CML), induces and sustains the leukaemic phenotype, and contributes to disease progression....Full Text Available

2006-10-09

169

Nucleotide sequence and genetic analysis of a 13.1-kilobase-pair Pseudomonas denitrificans DNA fragment containing five cob genes and identification of structural genes encoding Cob(I)alamin adenosyltransferase, cobyric acid synthase, and bifunctional cobinamide kinase-cobinamide phosphate guanylyltransferase.

Unequal segregation of cell fate determinants at mitosis is a conserved mechanism whereby cell fate diversity can be generated during development. In Drosophila, each sensory organ...Full Text Available

170

NPM-ALK and the JunB transcription factor regulate the expression of cytotoxic molecules in ALK-positive, anaplastic large cell lymphoma

A 13.1-kb DNA fragment carrying Pseudomonas denitrificans cob genes has been sequenced. The nucleotide sequence and genetic analysis revealed that this fragment contained five different cob genes named...Full Text Available

1991-10-01

171

Mutational Analysis of the Carboxy-Terminal (YGX)₄ Repeat Domain of CpsD, an Autophosphorylating Tyrosine Kinase Required for Capsule Biosynthesis in Streptococcus pneumoniae

Anaplastic lymphoma kinase-positive, anaplastic large cell lymphoma (ALK+ ALCL) is an aggressive non-Hodgkin lymphoma of T/null immunophenotype that is most prevalent in children and young adults. The...Full Text Available

2011-02-15

172

Mobilization of the genetically engineered plasmid pHSV106 from Escherichia coli HB101(pHSV106) to Enterobacter cloacae in drinking water.

In Streptococcus pneumoniae, CpsB, CpsC, and CpsD are essential for encapsulation, and mutants containing deletions of cpsB, cpsC, or cpsD...Full Text Available

2003-05-01

173

Mechano-transduction in Osteoblastic Cells Involves Strain-regulated Estrogen Receptor ?-mediated Control of Insulin-like Growth Factor (IGF) I Receptor Sensitivity to Ambient IGF, Leading to Phosphatidylinositol 3-Kinase/AKT-dependent Wnt/LRP5 Receptor-independent Activation of ?-Catenin Signaling*

We have used triparental matings to demonstrate transfer (mobilization) of the nonconjugative genetically engineered plasmid pHSV106, which contains the thymidine kinase gene of herpes simplex virus...Full Text Available

1991-01-01

174

Magnesium Sensitizes Slow Vacuolar Channels to Physiological Cytosolic Calcium and Inhibits Fast Vacuolar Channels in Fava Bean Guard Cell Vacuoles1

The capacity of bones to adjust their mass and architecture to withstand the loads of everyday activity derives from the ability of their resident cells to respond appropriately to the strains engendered....Full Text Available

2010-03-19

175

Isoform-Specific Functions of Phosphoinositide 3-Kinases: p110? but Not p110? Promotes Optimal Allergic Responses In Vivo1

Vacuolar ion channels in guard cells play important roles during stomatal movement and are regulated by many factors including Ca²⁺, calmodulin, protein kinases, and phosphatases....Full Text Available

1999-11-01

176

Insulin-like growth factor II receptor is phosphorylated by a tyrosine kinase in adipocyte plasma membranes

The leukocyte-enriched p110γ and p110δ isoforms of PI3K have been shown to control in vitro degranulation of mast cells induced by cross-linking...Full Text Available

2008-02-15

177

Forkhead Box Transcription Factor FOXO3a Regulates Estrogen Receptor Alpha Expression and Is Repressed by the Her-2/neu/Phosphatidylinositol 3-Kinase/Akt Signaling Pathway

Incorporation of /sup 32/P from (gamma-32P)ATP into tyrosine residues of the insulin-like growth factor (IGF)-II receptor was observed in a Triton X-100-insoluble fraction of rat adipocyte plasma membranes. IGF-II receptor phosphorylation proceeded to a stoichiometry of approximately 0.5 mol of phosphate/IGF-II binding site after 10 min of incubation at 4 degrees C. A Km for ATP of 6 microM was calculated for this phosphorylation reaction. Addition of IGF-II caused an approximately 2-fold increase in tyrosine phosphorylation of the IGF-II receptor in this preparation. In contrast, phosphorylation of angiotensin II by the Triton X-100 washed membranes was not stimulated by IGF-II. Incubation of purified receptor immobilized on IGF-II agarose or of receptor-enriched low density microsomal membranes with (gamma-32P)ATP did not result in appreciable incorporation of (/sup 32/P)phosphate into the IGF-II receptor nor into exogenous substrates. These data suggest that the IGF-II receptor is ...

1986-06-15

178

Cordycepin Blocks Lung Injury-Associated Inflammation and Promotes BRCA1-Deficient Breast Cancer Cell Killing by Effectively Inhibiting PARP

The expression status of the estrogen receptor alpha (ERα) and that of the epidermal growth factor receptor Her-2/neu frequently correlate inversely in breast cancers. While ERα-dependent...Full Text Available

2004-10-01

179

Alterations in Adenylate Kinase Activity in Human PBMCs after In Vitro Exposure to Electromagnetic Field: Comparison between Extremely Low Frequency Electromagnetic Field (ELF) and Therapeutic Application of a Musically Modulated Electromagnetic Field (TAMMEF)

Cordycepin has been shown to interfere with a myriad of molecular processes from RNA elongation to kinase activity, and prevents numerous inflammatory processes in animal models. Here we show in a mouse...Full Text Available

2011-09-01

180

Sodium gluconate as corrosion and scale inhibitor of ordinary steel in simulated cooling water

This study investigated the effects of electromagnetic fields on enzymes involved in purine metabolism in human peripheral blood mononuclear cells in vitro. Cells were obtained from 20 volunteers. We...Full Text Available

2009-01-01

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181

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...

2008-01-01

182

Scale prevention with special reference to threshold treatment

Microstructure and properties of ultrafine WC-10Co composites with chemically doped VC

Various chemical, physical, and mechanical methods to prevent unwanted deposition of mineral scale are described. The suitability of the different methods, which largely depends on the specific features and requirements of the system involved, is discussed. Special emphasis is placed upon the threshold treatment, where the growth process is retarded by the addition of trace amounts of growth inhibitors. Growth experiments have been performed on barium sulfate and calcium sulfate dihydrate seed crystals, suspended in a supersaturated solution with and without organic bisphosphonates as inhibitors. Two methods are selected for the analysis of the growth data. A degree of inhibition is defined to obtain a quantitative description of the influence of a growth inhibitor on the growth rate of the crystals. In addition the influence of the molecular structure of various bisphosphonates with different substituents is shown. The ...

1983-01-01

183

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 ...

2011-01-01

184

Inhibition of barium sulfate deposition by polycarboxylates of various molecular structures

Corrosion and scale processes and their inhibition in simulated cooling water systems by monosaccharides derivatives

To establish a relationship between the molecular structure of polycarboxylates and their growth-retarding influence on barium sulfate, seeded-suspension-growth experiments were performed at various inhibitor concentrations and pH values. Two types of polycarboxylates with a molecular structure based on their polyacrylic or maleic acid were studied. The molecular structure of these compounds were varied by particle substitution with monomers containing hydroxyl, amide, and sulfonic acid, as well as hydrophobic groups. Hydrophobic groups are detrimental to good inhibitor performance, whereas the introduction of OH, NH {sub 2}, or SO {sub 3} H groups presents opportunities to enhance the inhibitor effectiveness. The sequence in performance of the compounds on barium sulfate was compared with the sequence formerly obtained for calcium sulfate dihydrate.

1990-02-01

185

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...

2009-01-01

186

Bortezomib induces apoptosis in T lymphoma cells and natural killer lymphoma cells independent of Epstein-Barr virus infection

British Library Electronic Table of Contents (United Kingdom)

Abstract Epstein-Barr virus (EBV), which infects not only B cells, but also T cells and natural killer (NK) cells, is associated with multiple lymphoid malignancies. Recently, the proteasome inhibitor bortezomib was reported to induce apoptosis of EBV-transformed B cells. We evaluated the killing effect of this proteasome inhibitor on EBV-associated T lymphoma cells and NK lymphoma cells. First, we found that bortezomib treatment decreased the viability of multiple T and NK cell lines. No significant difference was observed between EBV-positive and EBV-negative cell lines. The decreased viability in response to bortezomib treatment was abrogated by a pan-caspase inhibitor. The induction of apoptosis was confirmed by flow cytometric assessment of annexin V staining. Additionally, cleavage o...

2011-01-01

187

Wounding Nicotiana tabacum Leaves Causes a Decline in Endogenous Indole-3-Acetic Acid ¹

Vectors containing a prokaryotic dihydrofolate reductase gene transform Drosophila cells to methotrexate-resistance.

We have previously observed that auxin can act as a repressor of the wound-inducible activation of a chimeric potato proteinase inhibitor II-CAT chimeric gene (pin2-CAT) in transgenic...Full Text Available

1991-07-01

188

Treatment of atypical depression with cognitive therapy or phenelzine: a double-blind, placebo-controlled trial.

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

1983-01-01

189

The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects

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

1999-05-01

190

The effectiveness of reducing the daily dose of finasteride in men with benign prostatic hyperplasia

Hypoxia inducible factor-1 (HIF-1) promotes tumor cell adaptation to microenvironmental stress. HIF-1 is up-regulated in irradiated tumors and serves as a promising target for radiosensitization....Full Text Available

2009-04-01

191

The antihypertensive efficacy and tolerability of a low dose combination of ramipril and felodipine ER in mild to moderate essential hypertension.

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

192

The L-type calcium channel inhibitor diltiazem prevents cardiomyopathy in a mouse model

1. The antihypertensive efficacy and tolerability of a low dose combination of the angiotensin converting enzyme inhibitor ramipril (2.5 mg) and the extended release formulation of the dihydropyridine...Full Text Available

1993-10-01

193

The Effect of 5?-Reductase Inhibition With Dutasteride and Finasteride on Bone Mineral Density, Serum Lipoproteins, Hemoglobin, Prostate Specific Antigen and Sexual Function in Healthy Young Men

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

2002-04-15

194

Tadalafil in the treatment of erectile dysfunction

PurposeDutasteride and finasteride are 5α-reductase inhibitors that dramatically decrease serum levels of dihydrotestosterone. Because androgens...Full Text Available

2008-06-01

195

Synthesis and characterization of a biotinylated organophosphorus ester for detection and affinity purification of a brain serine esterase: neuropathy target esterase.

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

2008-12-01

196

Skin permeation mechanism and bioavailability enhancement of celecoxib from transdermally applied nanoemulsion

We have synthesized a novel stable precursor, saligenin phosphorotrichloridate, which, on reaction with N-monobiotinyldiamines, generates a series of biotinylated covalent inhibitors of serine esterases....Full Text Available

1994-07-15

197

Selection of Inhibitor-Resistant Viral Potassium Channels Identifies a Selectivity Filter Site that Affects Barium and Amantadine Block

BackgroundCelecoxib, a selective cyclo-oxygenase-2 inhibitor has been recommended orally for the treatment of arthritis and osteoarthritis. Long term oral administration of celecoxib...Full Text Available

198

Reconstruction of the complete human cytomegalovirus genome in a BAC reveals RL13 to be a potent inhibitor of replication

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

199

Potential of mTOR inhibitors for the treatment of subependymal giant cell astrocytomas in tuberous sclerosis complex

Human cytomegalovirus (HCMV) in clinical material cannot replicate efficiently in vitro until it has adapted by mutation. Consequently, wild-type HCMV differ fundamentally from the passaged strains...Full Text Available

2010-09-01

200

Peptides of human bronchial mucus glycoproteins. Size determination by electron microscopy and by biosynthetic experiments.

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

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201

Pathogenic Role of NKT and NK Cells in Acetaminophen-Induced Liver Injury is Dependent on the Presence of DMSO

Secreted human bronchial mucins, directly collected from macroscopically healthy bronchial mucosa, were prepared in the presence of six proteinase inhibitors, and analysed by electron microscopy. These...Full Text Available

1987-11-15

202

Oligodendrocyte-Myelin Glycoprotein and Nogo Negatively Regulate Activity-Dependent Synaptic Plasticity

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

2008-09-01

203

New Insights into the Design of Inhibitors of Human S-Adenosylmethionine Decarboxylase: Studies of Adenine C[superscript 8] Substitution in Structural Analogues of S-Adenosylmethionine

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

2010-09-15

204

Nano to micro delivery systems: targeting angiogenesis in brain tumors

S-Adenosylmethionine decarboxylase (AdoMetDC) is a critical enzyme in the polyamine biosynthetic pathway and depends on a pyruvoyl group for the decarboxylation process. The crystal structures of the enzyme with various inhibitors at the active site have shown that the adenine base of the ligands adopts an unusual syn conformation when bound to the enzyme. To determine whether compounds that favor the syn conformation in solution would be more potent AdoMetDC inhibitors, several series of AdoMet substrate analogues with a variety of substituents at the 8-position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. The biochemical analysis indicated that an 8-methyl substituent resulted in more potent inhibitors, yet most other 8-substitutions provided no benefit over the parent compound. To understand these results, we used computational modeling and X-ray crystallography to study C{sup ...

2009-04-02

205

Mycophenolic acid inhibits activation of inducible nitric oxide synthase in rodent fibroblasts

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

206

Molecular basis of the inhibition of human aromatase (estrogen synthetase) by flavone and isoflavone phytoestrogens: A site-directed mutagenesis study.

Mycophenolate mofetil (MMF) is an immunosuppressive drug that acts as a selective inhibitor of inosine monophosphate dehydrogenase (IMPDH). MMF has recently been shown to inhibit the enzymatic activity...Full Text Available

2003-05-01

207

Method and composition for acidizing subterranean formations

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

1998-02-01

208

Mechanism of action of an inhibitor of complement-mediated prevention of immune precipitation.

The present invention relates to a method of acidizing a subterranean formation or well bore employing an acidic solution containing a corrosion inhibitor composition comprising an inhibiting effective amount of an acetylenic alcohol, a quaternary ammonium compound, an aromatic hydrocarbon and an antimony compound.

1985-02-12

209

Inhibitors of RecA Activity Discovered by High-Throughput Screening: Cell-Permeable Small Molecules Attenuate the SOS Response in Escherichia coli

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

1990-06-01

210

Identification of inhibitors of auxin transcriptional activation by means of chemical genetics in Arabidopsis

The phenomenon of antibiotic resistance has created a need for the development of novel antibiotic classes with non-classical cellular targets. Unfortunately, target-based drug discovery against...Full Text Available

2009-10-01

211

Identification of a Novel Inhibitor of Coactivator-associated Arginine Methyltransferase 1 (CARM1)-mediated Methylation of Histone H3 Arg-17*

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

2004-10-12

212

Identification of Genes Affecting the Toxicity of Anti-Cancer Drug Bortezomib by Genome-Wide Screening in S. pombe

Methylation of the arginine residues of histones by methyltransferases has important consequences for chromatin structure and gene regulation; however, the molecular mechanism(s) of methyltransferase...Full Text Available

2010-03-05

213

Habituation of unconditioned fear can be attenuated by the presence of a safe stimulus: Assessment using the neophobic response of the rat

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

214

Protection from extinction of conditioned fear has been demonstrated when a conditioned inhibitor of fear is presented during extinction treatment. The present study assessed if similar results...Full Text Available

2008-01-01

215

HIV Structural Database

Functional and Structural Analysis of a Key Region of the Cell Wall Inhibitor Moenomycin

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...

2011-09-25

216

Finasteride-Its Impact on Sexual Function and Prostate Cancer

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

2010-07-16

217

Enhanced corrosion resistance of mild steel in hydrochloric acid solution by new thiadiazole derivatives: Electrochemical, theoretical and XPS studies

Finasteride, a specific and competitive inhibitor of 5α-reductase enzyme Type 2, inhibits the conversion of testosterone to dihydrotestosterone (DHT). In adults, DHT acts as primary androgen...Full Text Available

2009-01-01

218

Electrochemical Processes : Lecture Notes for a course in Applied Inorganic Chemistry

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 ...

2004-07-01

219

Effects of cyclooxygenase inhibitors on the alterations in lung mechanics caused by endotoxemia in the unanesthetized sheep.

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.

1997-01-01

220

Effects of an Alpha-4 Integrin Inhibitor on Restenosis in a New Porcine Model Combining Endothelial Denudation and Stent Placement

The effects of Escherichia coli endotoxin on lung mechanics, hemodynamics, gas exchange, and lung fluid and solute exchange were studied in 12 chronically instrumented unanesthetized sheep. A possible...Full Text Available

1983-07-01

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221

Effects of Leupeptin on Proteinase and Germination of Castor Beans ¹

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

222

Citalopram is not Effective Therapy for Non-Depressed Patients with Irritable Bowel Syndrome

Leupeptin, a tripeptide inhibitor of some proteinases, was shown previously to maintain the stability of several enzymes (isocitrate lyase, fumarase, and catalase) in crude extracts of castor bean endosperm....Full Text Available

1981-10-01

223

Characterization of Terfestatin A, a New Specific Inhibitor for Auxin Signaling1[w

Background & AimsData are conflicting on the benefit of selective serotonin reuptake inhibitors (SSRIs) for patients with irritable bowel syndrome (IBS);...Full Text Available

2010-01-01

224

Analysis of the Pharmacokinetic Interaction between Cephalexin and Quinapril by a Nonlinear Mixed-Effect Model

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

2005-10-01

225

An Arabidopsis Mutant Resistant to Thaxtomin A, a Cellulose Synthesis Inhibitor from Streptomyces SpeciesW?

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

1998-06-01

226

Acute change in the cyclic AMP content of rat mammary acini in vitro. Influence of physiological and pharmacological agents.

Thaxtomin A is a phytotoxin produced by Streptomyces scabies and other Streptomyces species, the causative agents of common scab disease in potato and other taproot...Full Text Available

2003-08-01

227

A once-daily dose of tadalafil for erectile dysfunction: compliance and efficacy

The cyclic AMP content of acini, freshly prepared from mammary tissue of lactating rats, was measured during incubation in vitro. Neither adrenergic agonists nor cyclic AMP phosphodiesterase inhibitors...Full Text Available

1985-08-15

228

A non-selective (amitriptyline), but not a selective (citalopram), serotonin reuptake inhibitor is effective in the prophylactic treatment of chronic tension-type headache.

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

229

A Vasculature-Targeting Regimen of Pre-Operative Docetaxel with or without Bevacizumab for Locally Advanced Breast Cancer

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

1996-09-01

230

The use of water-soluble hydrazones as inhibitors for the corrosion of C-steel in acidic medium

PurposeTaxanes have effects on angiogenesis causing difficulties in separating biologic effects of chemotherapy from those due to angiogenesis inhibitors. This randomized...Full Text Available

2009-05-15

231

Revised minimum nitrite concentration for ESP

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.

2007-09-15

232

Revised minimum nitrite concentration for ESP

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.

1992-10-26

233

Hideout return testing from support crevices

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.

1992-10-26

234

Corrosion and protection of magnesium alloy AZ31D by a new conversion coating

The objectives of the project were to develop operational techniques for promoting contaminant hideout return from tube support crevices and to identify the effect of chemical inhibitor application on corrodent transport. The implementation of routine procedures for promoting the return of sequestered corrodents could retard the progression of denting or other corrosion processes and improve steam generator availability. Tests also quantified the effect of inhibitor application on crevice hideout and hideout return processes, with the intention of developing a better understanding of the inhibition mechanism. By carefully monitoring the hideout and hideout return inventories, the program also has provided the opportunity to study steam generator concentration processes in general.

1985-03-01

235

Susceptibility of the human retrovirus XMRV to antiretroviral inhibitors

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.)

2003-07-01

236

Corrosion inhibition of steel in crude oil storage tanks

BackgroundXMRV (xenotropic murine leukemia virus-related virus) is the first known example of an exogenous gammaretrovirus that can infect humans. A limited number of reports suggest that XMRV is intrinsically resistant to many of the antiretroviral drugs used to treat HIV-1 infection, but is sensitive to a small subset of these inhibitors. In the present study, we used a novel marker transfer assay to directly compare the antiviral drug sensitivities of XMRV and HIV-1 under identical conditions in the same host cell type.ResultsWe extend the findings of previous studies by showing that, in addition to AZT and tenofovir, XMRV and HIV-1 are equally sensitive to AZddA (3'-azido-2',3'-dideoxyadenosine), AZddG (3'-azido-2',3'-dideoxyguanosine) and adefovir. These results indicate that specific 3'-azido or acyclic nucleoside analog inhibitors of HIV-1 reverse transcriptase (RT) also block XMRV infection with comparable efficacy in vitro. Our data ...

2010-08-31

237

Polyphenol rich botanicals used as food supplements interfere with EphA2-ephrinA1 system

The corrosion behavior of steel in water from certain oil fields with various organic inhibitors was studied by applying potentiodynamic technique at pH 5.9. The inhibitors which were used include 2-methylbenzimidazole (I), 2-mercaptobenzimidazole (II), 2-mercapto-5-methylbenzimidazole (III), and 2-mercaptothiazole (IV). The inhibiting efficiency of the different additives was evaluated from their anodic and cathodic polarization curves at different temperatures. A comparative study of curve fitting procedures using the kinetic thermodynamic model and those utilizing well-known adsorption isotherms was undertaken. Three types of isotherms were used, Langmuir, Frumkin and Flory-Huggins isotherm. The results show that the kinetic-thermodynamic model and Flory-Huggins isotherms are more suitable to fit the data for the four inhibitors, at all applied temperatures. From the values of binding constants, K, the order of ...

2003-04-01

238

British Library Electronic Table of Contents (United Kingdom)

The Eph tyrosine kinase receptors and their ephrin ligands play a central role in several human cancers and their deregulated expression or function promotes tumorigenesis, inducing aggressive tumor phenotypes. Green tea extracts (GTE) have been recently found to inhibit Eph-kinase phosphorylation. In order to evaluate the potential contribution of edible and medicinal plants on EphA2-ephrinA1 modulation, 133 commercially available plant extracts used as food supplements, essential and fixed oils were screened with an ELISA-based binding assay. Nine plant extracts, rich of polyphenols, reversibly inhibited binding in a dose-dependent manner (IC"5"0 0.83-24@mg/ml). Functional studies on PC3 prostate adenocarcinoma cells revealed that active extracts antagonized ephrinA1-Fc-induced EphA2-pho...

2011-01-01

239

Mechanism of adenylate kinase. Dose adenosine 5'-triphosphate bind to the adenosine 5'-monophosphate site

In vivo phosphorylation of histones H1 and H5 in calf thymus and chicken erythrocytes as studied by /sup 31/P nuclear magnetic resonance spectroscopy

Although the subtrate binding properties of adenylate kinase (AK) have been studied extensively by various biochemical and biophysical techniques, it remains controversial whether uncomplexed adenosine 5'-triphosphate (ATP) binds to the adenosine 5'-monophosphate (AMP) site of AK. The authors present two sets of experiments which argue against binding of ATP to the AMP site. (a) /sup 31/P nuclear magnetic resonance titration of ATP with AK indicated a 1:1 stoichiometry on the basis of changes in coupling constants and line widths. This ruled out binding of ATP to both sites. (b) ATP and MgATP were found to behave similarly by protecting AK from spontaneous inactivation while AMP showed only a small degree of protection. Such inactivation could also be protected or reversed by dithioerythritol and is most likely due to oxidation of sulfhydryl groups, one of which (cysteine-25) is located near the MgATP site. The results support binding of ATP to ...

1987-10-06

240

Gene discovery in the Acanthamoeba castellanii genome

The /sup 31/P NMR method was first applied to characterize in vivo phosphorylation of H1 and H5 in calf thymus and chicken erythrocytes as well as in vitro phosphorylation of H1 and H5 by cAMP-dependent protein kinase. The amino acid residues phosphorylated in vivo in the histones were exclusively serine residues, and the mole fraction of phosphoserine was estimated to be 0.34 and 0.27 per molecule of calf thymus H1 and chicken erythrocyte H5, respectively. Interestingly, chicken erythrocyte H1 was not phosphorylated in vivo. Three H1 subtypes from calf thymus H1 varied in the /sup 31/P NMR spectra, and the bisected fragments of calf thymus H1 and chicken erythrocyte H5 exhibited characteristic spectral patterns, indicating that there are considerable diversities of the degree of phosphorylation and phosphorylation sites in very-lysine-rich histones. Furthermore, it was found that the microenvironment of phosphoserine residues phosphorylated in vivo in calf thymus ...

1987-08-01

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241

GROWTH REGULATION IN ROUS SARCOMA VIRUS INFECTED CHICKEN EMBRYO FIBROBLASTS: THE ROLE OF THE src GENE

Acanthamoeba castellanii is a free-living amoeba found in soil, freshwater, and marine environments and an important predator of bacteria. Acanthamoeba castellanii is also an opportunistic pathogen of clinical interest, responsible for several distinct diseases in humans. In order to provide a genomic platform for the study of this ubiquitous and important protist, we generated a sequence survey of approximately 0.5 x coverage of the genome. The data predict that A. castellanii exhibits a greater biosynthetic capacity than the free-living Dictyostelium discoideum and the parasite Entamoeba histolytica, providing an explanation for the ability of A. castellanii to inhabit adversity of environments. Alginate lyase may provide access to bacteria within biofilms by breaking down the biofilm matrix, and polyhydroxybutyrate depolymerase may facilitate utilization of the bacterial storage compound polyhydroxybutyrate as a food source. Enzymes for the synthesis and breakdown of cellulose were ...

2005-08-01

242

Changes in intracellular Ca2+ levels induced by cytokines and P2 agonists differentially modulate proliferation or commitment with macrophage differentiation in murine hematopoietic cells.

We report here a study of the mechanisms leading to loss of growth control in chicken embryo fibroblasts transformed by Rous sarcoma virus (RSV). We have been particularly concerned with the role of the src gene in this process, and have used RSV mutants temperature sensitive (ts) for transformation to investigate the nature of the growth regulatory lesion. The two principal findings were (1) the stationary phase of the cell cycle (G{sub 1}) in chick embryo fibroblasts seems to have two distinct regulatory compartments (using the terminology of Brooks et al. we refer to these as 'Q' and 'A' states). When rendered stationary at 41.5 C by serum deprivation, normal cells enter a Q state, but cells infected with the ts-mutant occupy an A state. (2) Whereas normal cells can occupy either state depending on culture conditions, the ts-infected cells, at 41.5 C, do not seem to enter Q even though a known src gene product, a kinase, is ...

1980-07-01

243

The ATG1/ATG13 Protein Kinase Complex Is Both a Regulator and a Target of Autophagic Recycling in Arabidopsis.

The role of intracellular Ca2+ (Ca2+i) on hematopoiesis was investigated in long term bone marrow cultures using cytokines and agonists of P2 receptors. Cytokines interleukin 3 and granulocyte/macrophage colony stimulator factor promoted a modest increase in Ca2+i concentration ([Ca2+]i) with activation of phospholipase Cgamma, MEK1/2, and Ca2+/calmodulin kinase II. Involvement of protein kinase C was restricted to stimulation with interleukin 3. In addition, these cytokines promoted proliferation (20 times) and an increase in the Gr-1(-)Mac-1+ population with participation of gap junctions (GJ). Nevertheless ATP, ADP, and UTP promoted a large increase in [Ca2+]i, moderate proliferation (6 times), a reduction in the primitive Gr-1(-)Mac-1(-)c-Kit+ population, and differentiation into macrophages without participation of GJ. It is likely that Ca2+i participates as a regulator of hematopoietic signaling: moderate increases in [Ca2+]i would be ...

2008-09-05

244

Friend Spleen Focus-Forming Virus Activates the Tyrosine Kinase sf-Stk and the Transcription Factor PU.1 to Cause a Multi-Stage Erythroleukemia in Mice.

Autophagy is an intracellular recycling route in eukaryotes whereby organelles and cytoplasm are sequestered in vesicles, which are subsequently delivered to the vacuole for breakdown. The process is induced by various nutrient-responsive signaling cascades converging on the Autophagy-Related1 (ATG1)/ATG13 kinase complex. Here, we describe the ATG1/13 complex in Arabidopsis thaliana and show that it is both a regulator and a target of autophagy. Plants missing ATG13 are hypersensitive to nutrient limitations and senesce prematurely similar to mutants lacking other components of the ATG system. Synthesis of the ATG12-ATG5 and ATG8-phosphatidylethanolamine adducts, which are essential for autophagy, still occurs in ATG13-deficient plants, but the biogenesis of ATG8-decorated autophagic bodies does not, indicating that the complex regulates downstream events required for autophagosome enclosure and/or vacuolar delivery. Surprisingly, levels of the ATG1a and ATG13a ...

2011-10-01

245

Synthesis of alkylated deoxyno irimycin and 1,5-dideoxy-1,5-iminoxylitol analogues: : Polar side-chain modification, sulfonium and selenonium heteroatom variants, conformational analysis, and evaluation as glycosidase inhibitors

HEMATOLOGICAL MALIGNANCIES IN HUMANS TYPICALLY INVOLVE TWO TYPES OF GENETIC CHANGES: those that promote hematopoietic cell proliferation and survival (often the result of activation of tyrosine kinases) and those that impair hematopoietic cell differentiation (often the result of changes in transcription factors). The multi-stage erythroleukemia induced in mice by Friend spleen focus-forming virus (SFFV) is an excellent animal model for studying the molecular basis for both of these changes. Significant progress has been made in understanding the molecular basis for the multi-stage erythroleukemia induced by Friend SFFV. In the first stage of leukemia, the envelope protein encoded by SFFV interacts with and activates the erythropoietin (Epo) receptor and the receptor tyrosine kinase sf-Stk in erythroid cells, causing their Epo-independent proliferation, differentiation and survival. In the second stage, SFFV integration into the Sfpi1 locus ...

2010-10-11

246

In situ studies of imidazole and its derivatives as copper corrosion inhibitors. I. Activation energies and thermodynamics of adsorption

The syntheses of N-alkylated deoxynojirimycin and 1,5-dideoxy-1,5-iminoxylitol derivatives having either a D- or an L-erythritol-3-sulfate functionalized N-substituent are reported. The alkylating agent used was a cyclic sulfate derivative, whereby selective attack of the nitrogen atom at the least hindered primary center afforded the desired ammonium salt. In aqueous solution, these salts were configurationally labile at the ammonium center. Sulfonium and/or selenonium analogues of the ammonium salts were prepared by analogous reactions. The chalcogen salts were obtained as mixtures of diastereomers, separable in some cases, differing only in the stereochemistry at the configurationally stable sulfur or selenium atoms. Proof of configuration and conformation of each compound was obtained by detailed NMR experiments. The compounds are six-membered ring analogues of salacinol, a known sulfonium-salt glucosidase inhibitor. Evaluation of the target compounds for ...

2004-01-01

247

In situ and ex situ studies of imidazole and its derivatives as copper corrosion inhibitors. 2. AC impedance, XPS, and SIMS studies

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 ...

2000-02-01

248

Human tissue factor pathway inhibitor (TFPI) gene: Complete genomic structure and localization on the genetic map of chromosome 2q

The objective of this work was to investigate the efficiency of imidazole derivatives for corrosion inhibition of copper in 0.5 M hydrochloric acid. Corrosion inhibition was studied using impedance spectroscopy. Imidazole and its derivatives 4-methylimida-zole, 4-methyl-5-hydroxymethylimidazole, 1-phenyl-4-methylimidazole, 1-(p-tolyl)-4-methylimidazole were investigated. These studies have shown that 1-(p-tolyl)-4-methylimidazole is the best inhibitor in this series and that it acts as mixed inhibitor. The nature of the chemical interaction between these molecules and the copper surface was investigated by Cu exposed to solutions having two very different pH values: 0.5 M HCl and unbuffered purified water. X-ray photoelectron spectroscopy and secondary ion mass spectrometry were used to explore the nature of the interaction. Possible mechanisms of corrosion inhibition for these molecules are discussed.

2000-03-01

249

Effect of halogens and inhibitors on the external stress corrosion cracking of Type 304 austenitic stainless steel

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.

1993-08-01

250

Corrosion in drilling and well stimulation

The methodology of the drip procedure of the Standard Test Method for Evaluating the Influence of Thermal Insulation on External Stress Corrosion Cracking Tendency of Austenitic Stainless Steel (ASTM C 692-95a) was used to research the effect of halogens and inhibitors on the external stress corrosion cracking (ESCC) of Type 304 stainless steel as it applies to the insulation industry. Simulated insulation extraction solutions were made with pure chemical reagents for the halogens and inhibitors. The results indicated that sodium silicate compounds that were higher in sodium were more effective for preventing chloride-induced ESCC in Type 304 austenitic stainless steel. Potassium silicate was not as effective as sodium silicate. Fluoride, bromide, and iodide may cause ESCC but they were much less active than chloride and could be effectively inhibited by sodium silicate compound. The addition of fluoride ions to the chloride/sodium silicate ...

1997-11-01

251

Vascular ATP-sensitive potassium channels are over-expressed and partially regulated by nitric oxide in experimental septic shock

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 ...

1999-07-01

252

British Library Electronic Table of Contents (United Kingdom)

Purpose To study the activation and expression of vascular (aorta and small mesenteric arteries) potassium channels during septic shock with or without modulation of the NO pathway. Methods Septic shock was induced in rats by peritonitis. Selective inhibitors of vascular KATP (PNU-37883A) or BKCa [iberiotoxin (IbTX)] channels were used to demonstrate their involvement in vascular hyporeactivity. Vascular response to phenylephrine was measured on aorta and small mesenteric arteries mounted on a wire myograph. Vascular expression of potassium channels was studied by PCR and Western blot, in the presence or absence of 1400W, an inducible NO synthase (iNOS) inhibitor. Aortic activation of the transcriptional factor nuclear factor-kappaB (NF-?B) was assessed by electrophoretic mobility shift as...

2011-01-01

253

Thermal processing effects on the functional properties and microstructure of lentil, chickpea, and pea flours

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...

2011-01-01

254

TEM and ToF-SIMS studies on the corrosion behavior of vanadium and chromium containing WC-Co hard metals in alkaline solutions

British Library Electronic Table of Contents (United Kingdom)

The corrosion behavior of hard metals with VC and Cr3C2 grain growth inhibitors was investigated in alkaline solutions by electrochemical methods. The two inhibitors have opposite effects on the corrosion behavior: Cr3C2 significantly improves the corrosion behavior, whereas VC-containing alloys show a poor resistance. Time-of-flight secondary ion mass spectrometry (ToF-SIMS) and analytical transmission electron microscopy (TEM) analyses of the distributions of Cr and V in the composite material, as well as in the surface layers formed during corrosion were employed to clarify the influence of these elements on the corrosion behavior. The measurements showed that VC is precipitated mostly along the WC/binder interface after the liquid-phase sintering process, while Cr3C2 is almost homogene...

2011-01-01

255

Structure-activity relationships of anthraquinone derivatives derived from bromaminic acid as inhibitors of ectonucleoside triphosphate diphosphohydrolases (E-NTPDases)

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 ...

2009-01-01

256

Strain differences in the responsiveness between Sprague-Dawley and Fischer rats to nephropathy induced by FYX-051, a xanthine oxidoreductase inhibitor

British Library Electronic Table of Contents (United Kingdom)

To determine a rat strain appropriate for carcinogenicity testing of FYX-051, a xanthine oxidoreductase inhibitor, we performed a 4-week oral toxicity study by administering 0.3, 1 and 3?mg/kg, and 1, 3 and 10?mg/kg of FYX-051 to male Sprague-Dawley (SD) and Fischer (F344) rats, respectively. Histopathology revealed that the degree of FYX-051-induced nephropathy was 3-fold stronger in SD rats than in F344 rats. Our previous study demonstrated that the key factor of species differences in FYX-051-induced nephropathy is purine metabolism. This observation led us to examine the involvement of purine metabolism in differences among two strains of rats. However, purine metabolism was proven not to be implicated as an important factor. Subsequently, other factors responsible for the strain diffe...

2006-01-01

257

Some sulfonamide drugs inhibit ATPase activity of heat shock protein 90: investigation by docking simulation and experimental validation

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.

2011-01-01

258

SYNERGISTIC EFFECT OF N,N-BIS(PHOSPHONOMETHYL) GLYCINE AND ZINC IONS IN CORROSION CONTROL OF CARBON STEEL IN COOLING WATER SYSTEMS

British Library Electronic Table of Contents (United Kingdom)

A protective film has been developed on the surface of carbon steel in low chloride aqueous environment using a synergistic mixture of an environmentally friendly phosphonic acid, N,N-bis(phosphonomethyl) glycine (BPMG), and zinc ions. Impedance studies of the metal/solution interface indicated that the surface film is highly protective against the corrosion of carbon steel in the chosen environment. Potentiodynamic polarization studies showed that the inhibitor is a mixed inhibitor. X-ray photoelectron spectroscopic analysis (XPS) of the film showed the presence of the elements iron, phosphorus, nitrogen, oxygen, carbon, and zinc. Deconvolution spectra of these elements in the surface film showed the presence of oxides/hydroxides of iron(III), Zn(OH)2, and [Zn(II)-BPMG] complex. This infe...

2011-01-01

259

Resistance pattern and antioxidant enzyme profiles of protoporphyrinogen oxidase (PROTOX) inhibitor-resistant transgenic rice

British Library Electronic Table of Contents (United Kingdom)

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...

2008-01-01

260

Practical applications and feasibility of efflux pump inhibitors in the clinic-A vision for applied use

British Library Electronic Table of Contents (United Kingdom)

The world of antibiotic drug discovery and development is driven by the necessity to overcome antibiotic resistance in common Gram-positive and Gram-negative pathogens. However, the lack of Gram-negative activity among both recently approved antibiotics and compounds in the developmental pipeline is a general trend despite the fact that the plethora of covered drug targets are well-conserved across the bacterial kingdom. Such intrinsic resistance in Gram-negative bacteria is largely attributed to the activity of multidrug resistance (MDR) efflux pumps. Moreover, these pumps also play a significant role in acquired clinical resistance. Together, these considerations make efflux pumps attractive targets for inhibition in that the resultant efflux pump inhibitor (EPI)/antibiotic combination d...

2006-01-01

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261

Penile rehabilitation therapy with PDE-V inhibitors following radical prostatectomy: proceed with caution.

Knowledge-Based Identification of the ERK2/STAT3 Signal Pathway as a Therapeutic Target for Type 2 Diabetes and Drug Discovery

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

2009-01-25

262

British Library Electronic Table of Contents (United Kingdom)

Many existing agents for diabetes therapy are unable to restore or maintain normal glucose homeostasis or prevent the eventual emergence of hyperglycemia-related complication. Therefore, agents based on novel mechanisms are sought to complement and extend the current therapeutic approaches. Based on the initial paper research, we focused on active STAT3 as an attractive pharmacological target for type 2 diabetes. The subsequent text mining with a unique query to identify suppressors but not activators of STAT3 revealed the ERK2/STAT3 pathway as a novel diabetes target. The description of ERK2 inhibitors as diabetes target had not been found in our text mining research at present. The mechanism-based peptide inhibitor for ERK2 was identified using the knowledge of the KIM sequence, which ha...

2011-01-01

263

Influence of organic additives on the corrosion of iron-based amorphous alloys in dilute sulfuric acid solution

Improving protein quality of soybean through induced mutations

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.

1999-07-01

264

Cancers | Special Issue: Advances and Research Progress in Hepatocellular Carcinoma

Soybean is one of the most economical and nutritious food packed with basic nutrients that combat diseases stemming from mal- and under-nutrition. Despite its rich nutritional profile, use of soybean in food has been limited because soybean proteins are often associated with compounds, which could exert a negative impact on the nutritional quality of the protein. Trypsin inhibitor (TI) is one of the important anti-nutritional factors that exert negative effect by causing growth inhibition. Soybean cultivar VLS-2 was irradiated with 250 Gy gamma rays in a gamma cell (200) with 60Co source installed at BARC to induce mutations for low trypsin inhibitor content. Three mutants with lower levels of TI content were identified and can be utilized for developing elite varieties of soybean. (author)

2011-02-22

265

Wastenet

...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 ...

266

A 24-week, multicentre, open evaluation of the clinical effectiveness of the rivastigmine patch in patients with probable Alzheimer-s disease

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 ...

2011-01-01

267

Synergistic epigenetic reactivation of estrogen receptor-? (ER?) by combined green tea polyphenol and histone deacetylase inhibitor in ER?-negative breast cancer cells

Structure-function studies on inhibitory activity of Bungarus multicinctus protease inhibitor-like protein on matrix metalloprotease-2, and invasion and migration of human neuroblastoma SK-N-SH cells.

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

268

Stainless steel acid corrosion inhibition by organic dyes

In view of the findings that several Kunitz-type protein inhibitors suppress tumor invasion and metastasis, the aim of the present study is to explore whether Bungarus multicinctus protease inhibitor-like protein-2 (PILP-2) and PILP-3 exhibit anti-tumor activity. Although approximately 28% of amino acid substitutions occurred between PILP-2 and PILP-3, molecular modeling suggested that PILP-2 and PILP-3 shared similar folded structures. Unlike PILP-2, PILP-3 showed a notable activity in abolishing migration and invasion of human neuroblastoma SK-N-SH cells. The ability of PILP-3 to inhibit matrix metalloprotease-2 (MMP-2) activity was higher than that of PILP-2. Pull-down assay revealed protein-protein interaction between PILP-3 and MMP-2. In contrast to mutation on N-terminal region, replacement of amino acids at C-terminus attenuated notably the ability of PILP-3 to inhibit cell invasion, cell migration and MMP-2 activity as well as the ...

2009-08-23

269

Stainless steel acid corrosion inhibition by organic dyes

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.

1983-10-01

270

Spectrophotometric technique quantitatively determines NaMBT inhibitor in ethylene glycol-water solutions

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.

271

Prevention of physostigmine-, DFP-, and diazinon-induced acute toxicity by monoethylcholine and N-aminodeanol.

Spectrophotometric method, using a ratio-recording ultraviolet-absorption spectrophotometer, permits analysis of NaMBT in ethylene glycol-water solutions with high accuracy. It reduces analysis time, requires smaller samples, and is able to detect extremely small concentrations of mercaptobenzothiazole.

1967-01-01

272

Photolysis of the novel inotropes EMD 57033 and EMD 57439: evidence that Ca2+ sensitization and phosphodiesterase inhibition depend upon the same enantiomeric site.

1. Choline, and the choline analogues monoethylcholine (MEC) and N-aminodeanol (NAD) were examined for prophylactic activity in acute acetylcholinesterase inhibitor toxicity in mice. The rank order of potency of the compounds was MEC greater than NAD greater than choline. 2. Simultaneous administration of MEC (60 mg kg-1) or NAD (200 mg kg-1) with physostigmine reduced lethality to 17 and 13% respectively. MEC (60 mg kg-1) completely protected against disopropylfluorophosphate (DFP) and diazinon toxicity, and NAD reduced lethality to 17% for both agents. Choline (200 mg kg-1) exhibited only negligible antidotal activity against the inhibitors. 3. In vitro concentrations of choline, MEC, and NAD, similar to the estimated concentration obtained in vivo in the acute toxicity study, produced mixed inhibition of mouse brain acetylcholinesterase. The inhibition was dose-related and was additive to the inhibition produced by the cholinesterase ...

1989-06-01

273

Optimization of amide-based inhibitors of soluble epoxide hydrolase with improved water solubility.

1. We studied the effects of flash photolysis on the novel enantiomeric cardiac inotropes EMD 57033 (a calcium sensitizer) and EMD 57439 (a phosphodiesterase III inhibitor) in rat isolated ventricular...Full Text Available

1996-08-01

274

Molecular, functional and structural properties of the prolyl oligopeptidase of Trypanosoma cruzi (POP Tc80), which is required for parasite entry into mammalian cells

Soluble epoxide hydrolase (sEH) plays an important role in the metabolism of endogenous chemical mediators involved in the regulation of blood pressure and inflammation. 1,3-Disubstituted ureas with a polar group located on the fifth atom from the carbonyl group of urea function are active inhibitors of sEH both in vitro and in vivo. However, their limited solubility in water and relatively high melting point lead to difficulties in formulating the compounds and poor in vivo efficacy. To improve these physical properties, the effect of structural modification of the urea pharmacophore on the inhibition potencies, water solubilities, octanol/water partition coefficients (log P), and melting points of a series of compounds was evaluated. For murine sEH, no loss of inhibition potency was observed when the urea pharmacophore was modified to an amide function, while for human sEH 2.5-fold decreased inhibition was obtained in the amide compounds. In addition, a NH group ...

2005-05-19

275

We have demonstrated that the 80 kDa POP Tc80 (prolyl oligopeptidase of Trypanosoma cruzi) is involved in the process of cell invasion, since specific inhibitors block parasite...Full Text Available

2005-05-15

276

Manual corrosion

MMP-9 Gene Ablation and TIMP-4 Mitigate PAR-1-Mediated Cardiomyocyte Dysfunction: A Plausible Role of Dicer and miRNA

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.

1994-09-01

277

Intravenous Formulation of HET0016 for Inhibition of Rat Brain 20-Hydroxyeicosatetraenoic Acid (20-HETE) Formation

Although matrix metalloproteinase-9 (MMP-9) is involved in cardiomyocytes contractility dysfunction, tissue inhibitor of metalloproteinase-4 (TIMP-4) mitigates the effect of MMP-9, and proteinase-activated...Full Text Available

2010-07-01

278

Interplay of Reverse Transcriptase Inhibitor Therapy and Gag p6 Diversity in HIV Type 1 Subtype G and CRF02_AG

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

2008-11-01

279

Effect of WC particle size on grain growth inhibition in the WC-xVC-Co system

AbstractThe gag p6 region of HIV-1 has various nonsubstitutionary mutations, including insertions, duplications, deletions, and premature stop codons. Studies have linked gag p6 mutations...Full Text Available

2008-09-01

280

Comparative In Vitro Activity Profiles of Novel Bis-Indole Antibacterials against Gram-Positive and Gram-Negative Clinical Isolates?

The effect of WC particle size with the addition of VC as a grain growth inhibitor was investigated during the liquid phase sintering of WC-Co system. With increasing WC particle size at the same VC content, the effect of grain growth inhibition was increased. Also, with increasing the VC content, the grain shape of WC was changed from the faceted shape to the distorted shape, and the step density of the WC grain was increased. (orig.)

2003-07-01

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281

Assessment of Glucagon-Like Peptide-1 Analogue and Renin Inhibitor on the Binding and Regulation of GLP-1 Receptor in Type 1 Diabetic Rat Hearts

Antimicrobial susceptibilities of 233 Gram-positive and 180 Gram-negative strains to two novel bis-indoles were evaluated. Both compounds were potent inhibitors of Gram-positive bacteria, with MIC₉₀...Full Text Available

2010-09-01

282

Action of Inhibitors of Ammonia Assimilation on Amino Acid Metabolism in Hordeum vulgare L. (cv Golden Promise) 1

This study focuses on the effects of long-term renin-angiotensin system suppression and/or incretin mimetic therapies on the regulation and binding affinity of GLP-1 to its receptor in the coronary...Full Text Available

2011-01-01

283

5'-Azido-[3,6-3H2]-1-napthylphthalamic acid, a photoactivatable probe for naphthylphthalamic acid receptor proteins from higher plants: identification of a 23-kDa protein from maize coleoptile plasma membranes.

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

1983-03-01

284

1,1-Dichloroethylene hepatotoxicity: Proposed mechanism of action and distribution and binding of ¹⁴C radioactivity following inhalation exposure in rats

1-Naphthylphthalamic acid (NPA) is a specific inhibitor of polar auxin transport that blocks carrier-mediated auxin efflux from plant cells. To allow identification of the NPA receptor thought to be...Full Text Available

1992-01-15

285

Tungsten Effects on Phosphate-Dependent Biochemical Pathways are Species and Liver Cell Line Dependent

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

1977-12-01

286

British Library Electronic Table of Contents (United Kingdom)

Tungsten, in the form of tungstate, polymerizes with phosphate, and as extensive polymerization occurs, cellular phosphorylation and dephosphorylation reactions may be disrupted, resulting in negative effects on cellular functions. A series of studies were conducted to evaluate the effect of tungsten on several phosphate-dependent intracellular functions, including energy cycling (ATP), regulation of enzyme activity (cytosolic protein tyrosine kinase [cytPTK] and tyrosine phosphatase), and intracellular secondary messengers (cyclic adenosine monophosphate [cAMP]). Rat noncancerous hepatocyte (Clone-9), rat cancerous hepatocyte (H4IIE), and human cancerous hepatocyte (HepG2) cells were exposed to 1-1000 mg/l tungsten (in the form of sodium tungstate) for 24 h, lysed, and analyzed for the ab...

2010-01-01

287

Tissue-specific expression of Fgfr2b and Fgfr2c isoforms, Fgf10 and Fgf9 in the developing chick mandible

British Library Electronic Table of Contents (United Kingdom)

SummaryExperimental evidence has demonstrated the importance of FGF signalling in morphogenesis of the mandibular processes. FGFs transmit their signals through four tyrosine kinase transmembrane receptors (FGFRs). Alternative splicing in FGFRs including FGFR2 generates different isoforms that exhibit different ligand-specificities, exclusive tissue distributions and specific biological functions. Despite extensive information regarding the isoform-specific patterns of expression Fgfr2c and Fgfr2b during morphogenesis of many organs, a comparative analysis of these specific isoforms in the chick mandible has not been reported. To better understand the function of FGFR2 in mandibular morphogenesis, we have analysed the expression Fgfr2b, Fgfr2c and their putative ligands Fgf10 and Fgf9, in ...

2006-01-01

288

Submitochondrial distribution of cAMP in its incubation with rat liver mitochondria

Small heat shock protein 20 (HspB6) in cardiac hypertrophy and failure

When labeled cAMP is incubated with isolated mitochondria from rat liver, it penetrates not only through the outer membrane of the mitochondria but also into the mitoplasts, where it is accumulated chiefly in the matrix. Damage to the mitochondrial membrane by freezing-thawing promotes not an influx but an efflux of cAMP out of the mitoplasts. A substantial part of the labeled nucleotide in all the investigated submitochondrial fractions was identified as intact cAMP by the method of thin-layer chromatography. The transport of cAMP into the mitochondria can explain the activation of their functions by the hormones that activate cytoplasmic adenylate cyclase and by extramitochondrial (cytosol) cAMP, as well as the presence of cAMP-dependent protein kinase and cAMP-phosphodiesterase in the mitochondria.

1986-03-20

289

British Library Electronic Table of Contents (United Kingdom)

Hsp20, referred to as HspB6, is constitutively expressed in various tissues. Specifically, HspB6 is most highly expressed in different types of muscle including vascular, airway, colonic, bladder, and uterine smooth muscle; cardiac muscle; and skeletal muscle. It can be phosphorylated at Ser-16 by both cAMP- and cGMP-dependent protein kinases (PKA/PKG). Recently, Hsp20 and its phosphorylation have been implicated in multiple physiological and pathophysiological processes including smooth muscle relaxation, platelet aggregation, exercise training, myocardial infarction, atherosclerosis, insulin resistance and Alzheimer's disease. In the heart, key advances have been made in elucidating the significance of Hsp20 in contractile function and cardioprotection over the last decade. This mini-rev...

2011-01-01

290

Rapamycin (sirolimus) protects against hypoxic damage in primary heart cultures via Na^+/Ca^2^+ exchanger activation

British Library Electronic Table of Contents (United Kingdom)

Aims: Rapamycin (sirolimus) is an antibiotic that inhibits protein synthesis through mammalian targeting of rapamycin (mTOR) signaling, and is used as an immunosuppressant in the treatment of organ rejection in transplant recipients. Rapamycin confers preconditioning-like protection against ischemic-reperfusion injury in isolated mouse heart cultures. Our aim was to further define the role of rapamycin in intracellular Ca^2^+ homeostasis and to investigate the mechanism by which rapamycin protects cardiomyocytes from hypoxic damage. Main methods: We demonstrate here that rapamycin protects rat heart cultures from hypoxic-reoxygenation (H/R) damage, as revealed by assays of lactate dehydrogenase (LDH) and creatine kinase (CK) leakage to the medium, by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-d...

2011-01-01

291

Metabolic and molecular stress responses of gilthead seam bream Sparus aurata during exposure to low ambient temperature: an analysis of mechanisms underlying the winter syndrome

British Library Electronic Table of Contents (United Kingdom)

The winter syndrome in the gilthead sea bream Sparus aurata indicates that the species is exposed to critically low temperatures in Mediterranean aquaculture in winter. The present study of metabolic patterns and molecular stress responses during cold exposure was carried out to investigate this ?disease?, in light of the recent concept of oxygen and capacity limited thermal tolerance. The metabolic profile of fuel oxidation was examined by determining the activities of the enzymes hexokinase (HK), aldolase (Ald), pyruvate kinase (PK), l-lactate dehydrogenase (l-LDH), citrate synthase (CS), malate dehydrogenase (MDH) and 3-hydroxyacyl CoA dehydrogenase (HOAD) in heart, red and white muscle after exposure to temperatures of 10, 14 and 18?C. Especially, the increase in LDH activity combined ...

2010-01-01

292

Mechanism of Dephosphorylation of the SR Protein ASF/SF2 by Protein Phosphatase 1

British Library Electronic Table of Contents (United Kingdom)

SR proteins are essential splicing factors whose function is controlled by multi-site phosphorylation of a C-terminal domain rich in arginine-serine repeats (RS domain). The protein kinase SRPK1 has been shown to polyphosphorylate the N-terminal portion of the RS domain (RS1) of the SR protein ASF/SF2, a modification that promotes nuclear entry of this splicing factor and engagement in splicing function. Later, dephosphorylation is required for maturation of the spliceosome and other RNA processing steps. While phosphates are attached to RS1 in a sequential manner by SRPK1, little is known about how they are removed. To investigate factors that control dephosphorylation, we monitored region-specific mapping of phosphorylation sites in ASF/SF2 as a function of the protein phosphatase PP1. W...

2010-01-01

293

Degradation of leucine zipper-positive isoform of MYPT1 may contribute to development of nitrate tolerance

British Library Electronic Table of Contents (United Kingdom)

Aims A depressed cGMP-dependent protein kinase (PKG) activity is implicated in nitrate tolerance. The present study determines whether the leucine zipper-positive (LZ+) isoform of myosin phosphatase target subunit 1 (MYPT1), a key target protein for PKG actions, is involved in the development of nitrate tolerance. Methods and results Nitrate tolerance in in vitro preparations was obtained by a 24 h incubation with nitroglycerin (NTG). Nitrate tolerance in in vivo preparations was obtained by subcutaneous injection of mice with NTG, and the aortas were used. Protein levels of total MYPT1, MYPT1 (LZ+), PP1Cd, myosin light chain (MLC), and phosphorylated MLC were determined by Western blot analysis. Isometric vessel tension was determined by an organ chamber technique. Protein levels of MYPT1...

2010-01-01

294

Decreased dendritic spine density and abnormal spine morphology in Fyn knockout mice

British Library Electronic Table of Contents (United Kingdom)

Fyn is a Src-family tyrosine kinase that affects long term potentiation (LTP), synapse formation, and learning and memory. Fyn is also implicated in dendritic spine formation both in vitro and in vivo. However, whether Fyn's regulation of dendritic spine formation is brain-region specific and age-dependent is unknown. In the present study, we systematically examined whether Fyn altered dendritic spine density and morphology in the cortex and hippocampus and if these effects were age-dependent. We found that Fyn knockout mice trended toward a decrease in dendritic spine density in cortical layers II/III, but not in the hippocampus, at 1month of age. Additionally, Fyn knockout mice had significantly decreased dendritic spine density in both the cortex and hippocampus at 3months and 1year, an...

2011-01-01

295

Cyclosporine metabolic side effects: association with the WNK4 system

British Library Electronic Table of Contents (United Kingdom)

Abstract Background- Cyclosporine is used for treatment of transplanted patients and for immune-mediated diseases. Cyclosporine is known to cause a combination of metabolic side effects including hypertension, hyperkalemia, hypercalciuria and hypomagnesemia. These side effects except for hypomagnesemia are the cardinal features of familial hyperkalemia and hypertension (FHHt), also called pseudohypoaldosteronism type II (PHA II). FHHt is caused by mutations in the kinases WNK1 and WNK4 resulting in an increase in renal Na-Cl cotransporter (NCC) apical distribution and function. Therefore, we studied whether cyclosporine-s metabolic side effects are mediated by WNK4 and NCC. Design- Sprague-Dawley (SD) rats were treated by cyclosporine 25-mg-kg-1 subcutaneously for 14-days. Blood pressure, ...

2011-01-01

296

BzpF is a CREB-like transcription factor that regulates spore maturation and stability in Dictyostelium

British Library Electronic Table of Contents (United Kingdom)

The cAMP response element-binding protein (CREB) is a highly conserved transcription factor that integrates signaling through the cAMP-dependent protein kinase A (PKA) in many eukaryotes. PKA plays a critical role in Dictyostelium development but no CREB homologue has been identified in this system. Here we show that Dictyostelium utilizes a CREB-like protein, BzpF, to integrate PKA signaling during late development. bzpF^- mutants produce compromised spores, which are extremely unstable and germination defective. Previously, we have found that BzpF binds the canonical CRE motif in vitro. In this paper, we determined the DNA binding specificity of BzpF using protein binding microarray (PBM) and showed that the motif with the highest specificity is a CRE-like sequence. BzpF is necessary to ...

2011-01-01

297

Mechanism of enzyme-catalyzed phospho group transfer

Differential regulation of the biosynthesis of glucose transporters by the PI3-K and MAPK pathways of insulin signaling by treatment with novel compounds from Liriope platyphylla.

To understand more fully the mechanism of enzyme-catalyzed phospho group transfer, the stereochemical course at phosphorus of four enzymes has been determined. First, using adenosine (..gamma..-(S)-/sup 16/O, /sup 17/O, /sup 18/O)triphosphate as the substrate, the reaction catalyzed by creatine kinase has been found to proceed with overall inversion of configuration at phosphorus. Second, using adenosine (..beta..-(S)-/sup 16/O, /sup 17/O, /sup 18/O)diphosphate as the substrate, the reaction catalyzed by adenylate kinase has been found also to proceed with overall inversion. Third, the reaction catalyzed by phosphoenolpyruvate carboxylase has been studied using ((S/sub p/)-/sup 16/O, /sup 17/O)thiophospoenolpyruvate as the substrate in H/sub 2/ /sup 18/O. Fourth, using adenosine 5'-O-((..gamma..S/sub p/)-..beta gamma..-/sup 17/O,..gamma..-/sup 17/O,/sup 18/O)(3-thiotriphosphate) as the substrate, the reaction catalyzed by pyruvate ...

1986-01-01

298

Cysteinyl peptides of rabbit muscle pyruvate kinase labeled by the affinity label 8-((4-bromo-2,3-dioxobutyl)thio)adenosine 5 prime -triphosphate

The insulin signaling pathway, involving protein kinase B (PKB) and mitogen-activated protein kinase (MAPK), mediates the biological response to insulin and several growth factors and cytokines. To investigate the correlation between glucose transporter (Glut) biosynthesis and the insulin signaling pathway activated by novel compounds of Liriope platyphylla (LP9M80-H), alterations in Glut and key protein expression in the insulin signaling pathway were analyzed in the liver and brain of ICR mice treated with LP9M80-H. An in vitro assay showed that the highest level of insulin concentration was observed in the LP9M80-H-treated group, followed by the LP-H, LP-M, LP-E, and LP9M80-C-treated groups. Therefore, LP9M80-H was selected for use in studying the detailed mechanism of the insulin signaling pathway in animal systems. In an in vivo experiment, LP9M80-H induced a significant increase in glucose levels and a decrease of insulin concentration in ...

2010-12-14

299

Characterization of the major phosphoprotein and its kinase on the surface of the rat adipocyte

The affinity label 8-((4-bromo-2,3-dioxobutyl)thio)adenosine 5{prime}-triphosphate (8-BDB-TA-5{prime}-TP) reacts covalently with rabbit muscle pyruvate kinase, incorporating 2 mol of reagent/mol of enzyme subunit upon complete inactivation. Protection against inactivation is provided by phosphoenolpyruvate, K{sup +}, and Mn{sup 2+} and only 1 mol of reagent/mol of subunit is incorporated. The authors have now identified the resultant modified residues. After reaction with 8-BDB-TA-5{prime}-TP at pH 7.0, modified enzyme was incubated with ({sup 3}H)NaBH{sub 4} to reduce the carbonyl groups of enzyme-bound 8-BDB-TA-5{prime}-TP and to introduce a radioactive tracer into the modified residues. Following carboxymethylation and digestion with trypsin, the radioactive peptides were separated on a phenylboronate agarose column followed by reverse-phase high-performance liquid chromatography in 0.1% trifluoroacetic acid with an acetonitrile gradient. Gas-phase sequencing ...

1990-03-13

300

The growth factor from plerocercoids of Spirometra mansonoides is both a growth hormone agonist and a cysteine proteinase.

Intact rat fat cell exposed to 12.5 ..mu..M (..gamma..-32P)ATP incorporate label into specific proteins within minutes. By solubilizing the reaction mixture with SDS which bypasses the subcellular fractionation steps, the labeled proteins can be identified in autoradiographs of SDS-PAGE gels. The most prominently labeled protein has an M/sub r/ of 42,000. Localization of this component to the cell surface can be made on the basis of inhibition of phosphorylation by addition of a protein derived from the rat brain with protein kinase inhibitory property, susceptibility of the phosphorylated protein to the tryptic digestion, inhibition of phosphorylation of this protein after brief exposure to melittin. To rule out the possibility that the cell surface protein might be a mitochondrial contaminant from broken cells, /sup 32/Pi-labeled and (..gamma..-/sup 32/P)ATP-labeled cells were chromatographed on a rabbit anti-pyruvate dehydrogenase antibody-Sepharose 4B column. A ...

1986-12-01

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301

T-2 mycotoxin inhibits mitochondrial protein synthesis

Plerocercoids of the tapeworm Spirometra mansonoides produce a substance that stimulates growth of experimental hosts. We report purification of plerocercoid growth factor (PGF) to homogeneity by a process involving isolation and solubilization of plerocercoid membranes, isoelectric point selection by chromatofocusing chromatography or preparative isoelectric focusing, and anion-exchange chromatography. A radioreceptor assay (RRA) for human growth hormone (hGH) was used to detect PGF and purity of the 27.5-kDa protein was judged by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). Proteolytic activity was detected in the 27.5-kDa protein by gelatin substrate PAGE. Characterization of PGF as a neutral cysteine proteinase was based on substrate and inhibitor specificities and dependence on pH and thiol-containing reagents. The association of hGH agonist and proteinase activities was shown by comparing RRA and hydrolytic activities in the presence ...

1996-04-01

302

Preclinical evidence for the benefits of penile rehabilitation therapy following nerve-sparing radical prostatectomy.

The authors investigated the effect of T-2 toxin on rat liver mitochondrial protein synthesis. Isolated rat liver mitochondria were supplemented with an S-100 supernatant from rat liver and an external ATP-generating system. An in-vitro assay employing cycloheximide, and inhibitor of cytoplasmic protein synthesis, and chloramphenicol, and inhibitor of mitochondrial protein synthesis, to distinguish mitochondrial protein synthesis from the cytoplasmic process. Amino acid incorporation into mitochondria was dependent on the concentration of mitochondria and was inhibited by chloramphenicol. The rate of uptake of tritium leucine into mitochondrial protein was unaffected by the addition of T-2 toxin and was not a rate-limiting step in incorporation. However, 0.02 micrograms/ml of T-2 toxin decreased the rate of protein synthesis inhibition correlated with the amount of T-2 toxin taken up by the mitochondria. While T-2 toxin is known to inhibit ...

1988-01-01

303

Metal cation inhibitors for controlling denting corrosion in steam generators. Final report. [PWR

Erectile dysfunction following radical prostatectomy remains a frequent problem despite the development of nerve-sparing techniques. This erectile dysfunction is believed to be neurogenic, enhanced by hypoxia-induced structural changes which result in additional veno-occlusive dysfunction. Recently, daily use of intracavernous vasoactive substances and oral use of PDE5-inhibitors have been clinically studied for treatment of postprostatectomy erectile dysfunction. Since these studies showed benefits of "penile rehabilitation therapy," these effects have been studied in a preclinical setting. We reviewed experimental literature on erectile tissue preserving and neuroregenerative treatment strategies, and found that preservation of the erectile tissue by the use of intracavernous nitric oxide donors or vasoactive substances, oral PDE5-inhibitors, and hyperbaric oxygen therapy improved erectile function by antifibrotic effects and preservation of ...

2008-01-01

304

Inhibition of corrosion resistant alloys in hot hydrochloric acid solutions

Metal cations of arsenic, antimony, tin, manganese, zinc, cadmium, indium, and thallium have been evaluated in a preliminary way as possible3 inhibitors for controlling denting corrision observed in steam generators used with pressurized water reactors (PWR). The rationale for this approach was based upon the well-known inhibition effects of metal cations on corrosion rates in electrolyte/metal systems. A review of corrosion inhibition by metal cations (H. Leidheiser, Jr., Corrosion 36, 339 (1982)) has identified eleven inhibition mechanisms. The major test methods used for this evaluation were: (1) Isothermal capsule tests of carbon/steel/Inconel 600 tube bulging rates at temperatures up to 288/sup 0/C in seawater/copper-nickel chloride bulge-accelerating solutions. (2) Immersion weight-loss tests of steel coupled to Inconel 600 in boiling (102/sup 0/C) 3% sodium chloride solutions. In addition, electrochemical measuremens and surface analyses were performed. The ...

1982-12-01

305

Influence of thin oxide films on pitting corrosion of CrNi steels. Beeintraechtigung der Lochkorrosionsbestaendigkeit von CrNi-Staehlen durch duenne Oxidschichten

Weight loss measurements were performed in 20% and 28% hydrochloric acid at 90/sup 0/C on carbon steel, 22Cr5Ni duplex stainless steel, and two superaustenitic steels - 27Cr31Ni3Mo and 19Cr25Ni4Mo -, in presence of organic substances used singly or mixed. The organic substances examined were quaternary ammonium salts (1-4-pyridyl)-pyridinium chloride hydrochloride, dodecylpyridiniumchloride, benzyldimethylstearylammonium chloride, and dodecyltrimethylammonium bromide), alkynols (1-octyn-3-ol, propargyl alcohol) and trans-cinnamaldehyde. The synergistic effect of potassium iodide on the inhibitive efficiency of the organic substances was studied. The variations of corrosion rate during the test time (normally six hours) were recorded by means of polarization resistance measurements. Polarization curves were also recorded. The results showed that the corrosion rates of the four steels examined can be reduced to less than 1 mg/cm/sup -2/ . h/sup -1/ using ternary ...

1988-12-01

306

Genetic organization of Bungarus multicinctus protease inhibitor-like proteins.

Chloride-induced pitting corrosion of stainless steel (Materials No. 1.4301 and 1.4571) was investigated with the aid of chronopotentiostatic tests. Oxide films upon the surface (temper colours), addition of inhibitors (sulphate and nitrate) and temperature were the testing variables. Two different critical pitting potentials have been found, which give information on the potential ranges for stable passivity, latent and stable pitting corrosion. The results only indicate a small effect of Mo content of the material and test temperature. The inhibitors (sulphate and nitrate) have a marked effect. Specimens with a clean surface produced by pickling are markedly more resistant against pitting corrosion than specimens with a yellow temper colour, whereas the difference in corrosion resistance between yellow and blue films is relatively small. The width of the critical potential range for pitting corrosion generally increases with increasing oxide ...

1993-09-01

307

Effect of some tripodal bipyrazolic compounds on C38 steel corrosion in hydrochloric acid solution

The structural organization of the genes encoding Bungarus multicinctus protease inhibitor-like proteins (PILPs), PILP-1, PILP-2 and PILP-3, are reported in this study. Unlike PILP-2 and PILP-3, recombinant PILP-1 exhibited inhibitory activity on trypsin. PILP genes and B chain genes shared identical organization with three exons interrupted by two introns in similar positions. On the contrary, intron 1 of these genes had a similar size, a notable variation with the size of intron 2 was observed. It was found that two regions at the second intron of B1 chain and B2 chain genes were absent in that of PILP genes. Noticeably, intronic insertion in the second intron of B chain genes appeared in the promoter region of PILP-1 gene, but not in that of PILP-2 and PILP-3 genes. Comparative analyses of PILP genes and B chain genes showed that the protein-coding regions of the exons are more diverse than introns, except for in the signal peptide domain. These results suggest ...

2008-03-27

308

British Library Electronic Table of Contents (United Kingdom)

The corrosion inhibition of C38 steel in molar HCl by N,N-bis[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]buthylamine (P1) and 5-{N,N-bis[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl] amino} pentanol (P2) has been investigated at 308?K using electrochemical and weight loss measurements. Measurements show that these compounds act as good inhibitors without changing the mechanism of the corrosion process. Moreover, the inhibiting efficiency increases with the increase in concentration of the studied inhibitors. Compound P2 showed better protection properties even at relatively higher temperatures when compared to P1. The associated activation corrosion and free adsorption energies have been determined. P1 and P2 are adsorbed on the C38 steel surface according to a Langmuir isotherm adsorption model.

2010-01-01

309

Easy access to 6-membered iminoalditols - important glycosidase inhibitors

Application of the histone deacetylase inhibitors for the treatment of endometriosis: histone modifications as pathogenesis and novel therapeutic target.

Stereoselective methods for synthesising iminoalditols are still needed, as this class of compounds is known to contain strong glycosidase inhibitors. We have for some time investigated (1) the possibilities for using 2-amino-6-bromo-2,6-dideoxy-aldonolactones as starting materials for such compounds, since a substitution at C-6 by the 2-amino group should lead to the target molecules. We have found that treatment of mentioned 2-aminolacones with aqueous base gave 5- or 6-membered iminoalditols depending of the stereochemistry of the lactone, while under non aqueous conditions only formation of 6-membered iminoalditols were observed. The use of triethylamine in methanol thus gave methylesters of 6-membered iminouronic acids. Reduction of the ester group with sodium borohydride gave the target compounds. The mechanisms of the reactions will be discussed as well as specific results obtained. (1) Lundt, I. Top. Curr. Chem. 1997, 187, 117-156

310

Antihemostatic molecules from saliva of blood-feeding arthropods.

BACKGROUND Accumulating evidence suggests that various epigenetic aberrations play definite roles in the pathogenesis of endometriosis. We investigated the histone acetylation status in endometriosis and the application of the histone deacetylase inhibitors (HDACIs) for the treatment of endometriosis. METHODS The levels of acetylated histones in the endometriotic cyst stromal cells (ECSCs) and normal endometrial stromal cells (NESCs) were evaluated. The effects of the HDACIs on cell proliferation, the cell cycle, apoptosis of ECSCs and NESCs, and the expression of genes related to these cellular events were investigated. The effects of HDACIs on histone acetylation in chromatin of the promoter region of the cell cycle regulatory genes in ECSCs were also investigated. RESULTS The acetylated histone levels were significantly lower in ECSCs than in NESCs (P endometriosis and that HDACIs reactivated epigenetically silenced genes, resulting in the suppression of cell ...

2011-06-29

311

Antifungal thiopeptide cyclothiazomycin B1 exhibits growth inhibition accompanying morphological changes via binding to fungal cell wall chitin

The ability to feed on vertebrate blood has evolved many times in various arthropod clades. Each time this trait evolves, novel solutions to the problem posed by vertebrate hemostasis are generated. Consequently, saliva of blood-feeding arthropods has proven to be a rich source of antihemostatic molecules. Vasodilators include nitrophorins (nitric oxide storage and transport heme proteins), a variety of peptides that mimic endogenous vasodilatory neuropeptides, and proteins that catabolize or sequester endogenous vasoconstrictors. A variety of platelet aggregation inhibitors antagonize platelet responses to wound-generated signals, including ADP, thrombin, and collagen. Anticoagulants disrupt elements of both the intrinsic and extrinsic pathways. Molecular approaches (termed 'sialomics') to characterize the full inventory of mRNAs transcribed in salivary glands have revealed a surprising level of complexity within a single species. Multiple salivary proteins may be ...

2005-01-01

312

British Library Electronic Table of Contents (United Kingdom)

Cyclothiazomycin B1 (CTB1) is an antifungal cyclic thiopeptide isolated from the culture broth of Streptomyces sp. HA 125-40. CTB1 inhibited the growth of several filamentous fungi including plant pathogens along with swelling of hyphae and spores. The antifungal activity of CTB1 was weakened by hyperosmotic conditions, and hyphae treated with CTB1 burst under hypoosmotic conditions, indicating increased cell wall fragility. CTB1-sensitive fungal species contain high levels of cell wall chitin and/or chitosan. Unlike nikkomycin Z, a competitive inhibitor of chitin synthase (CHS), CTB1 did not inhibit CHS activity. Although CTB1 inhibited CHS biosynthesis, the same result was also obtained with a non-specific proteins inhibitor, cycloheximide, which did not reduce cell wall rigidity. These ...

2011-01-01

313

A rapid, radiometric assay for sucrose synthase

A low temperature synthesized NbC as grain growth inhibitor for WC-Co composites

Investigations of sucrose synthase in maize root tips have required development of a means to circumvent the rapid decline of activity observed after extraction dialysis and either synthetic or degradative assays. Several protease inhibitors were tested; although PMSF increased initial activity, no inhibitor prevented the drop in activity with time. Western blot analysis indicated that activity decline was not associated with protein degradation. Therefore, a procedure was developed which (1) shortened extraction-to-assay period from ca. 24 hours to 7 minutes, (2) simplified previous assays and (3) reduced the amount of tissue required. Extract was desalted with spun columns and the {sup 14}C-UDPG product recovered with DEAE ion exchange paper. The minute quantities of product recovered can be concealed by the presence of trace impurities in the {sup 14}C-sucrose utilized. DEAE ion exchange paper was used to remove interfering radio-labelled ...

1990-05-01

314

Temperature Dependences of Leakage Currents of ZnO Varistors Doped with Rare-Earth Oxides

Niobium carbide can be used to inhibit WC grain growth in hardmetal. The performance of a NbC powder produced at low temperature by solid-gas reaction (an experimental powder) as WC grain growth inhibitor is compared with that of a commercial NbC powder. It is verified that NbC effectively inhibits heterogeneous WC coarsening. This results in an increase in hardness. The commercial and experimental NbC powders exhibit a comparable performance in inhibiting the WC grain coarsening, in spite of a significant difference in particle size and shape. The commercial NbC powder is very fine while the experimental one is coarse and porous, but its crystallites are finer than those of the commercial product. The milling procedure used to prepare the alloys is able to reduce the particle size of the experimental NbC, and thus guarantee a dispersion of the particles with a quality level comparable to that found for the alloy prepared with the commercial NbC. (orig.)

2000-11-30

315

British Library Electronic Table of Contents (United Kingdom)

Rare-earth oxides are doped into ZnO varistors as grain growth inhibitors for increasing the varistors' voltage gradients. However, their leakage currents become large and their nonlinear coefficients decrease at the same time. The reasonable explanation for such a phenomenon has not yet been available. In this paper, the temperature dependences of varistor samples' leakage currents are investigated, which reveal that the increased leakage currents of ZnO varistors with Y2O3 doping are mainly due to the bypass paths through the intergranular materials at grain corners.

2010-01-01

316

Stress corrosion cracking susceptibility of #beta# titanium alloy 38-6-44

Reduced levels of MMP-2 and TIMP-1 in dyssegmental dysplasia.

The threshold stress intensities for stress corrosion crack propagation in beta titanium alloy 38-6-44, Ti3Al-8V-6Cr-4Mo-4Zr, has been determined in salt water and methanolic solutions. The alloy was immune to stress corrosion cracking (SCC) in aqueous sodium chloride solutions (marine atmosphere). However, in methanolic solutions, the alloy was very susceptible to SCC. This marked susceptibility in methanolic solutions can be mitigated by the addition of an inhibitor: sodium nitrate. Crack extension in the alloy was transgranular and failure occurred by brittle quasi-cleavage in methanolic solutions.

317

Process to eliminate the deposits formed in a steam generator of a pressurized water nuclear reactor

Matrix metalloproteinases (MMPs) and tissue inhibitors of metalloproteinases (TIMPs) were measured in a mild case of dyssegmental dysplasia. X-ray pictures of a female baby born vaginally at 39 weeks of gestation showed short, bent, dumbbell-shaped long bones of the limbs and profound dyssegmental ossification in the spine, findings characteristic of dyssegmental dysplasia. When the levels of MMP-1, MMP-2, MMP-9, TIMP-1, and TIMP-2 were measured, the levels of MMP-2 and TIMP-1 were significantly reduced. This case might provide a clue to disclose the etiology of dyssegmental dysplasia. PMID:12568417

2003-02-01

318

Phytic acid doped nanoparticles for green anticorrosion coatings

The present process allows to eliminate the corrosion products formed on the tube plates and in the interstices of plate-tube crosspieces of a PWR steam generator in order to avoid a corrosion phenomenon which may cause denting by presence of oxides. The process consists in applying on these oxides at about 50-100 degrees, an aqueous solution containing 6-8% of gluconic acid, 3-5% of citric acid, about 0.5% of a corrosion inhibitor and ammonia until a pH of 3-9.5 is obtained.

1984-04-05

319

British Library Electronic Table of Contents (United Kingdom)

In this paper, an environmentally friendly metal corrosion inhibitor, phytic acid, was assembled into the walls of silica nanoparticles via layer-by-layer self-assembly technique (LbL) with poly(allylamine hydrochloride). Such functionalized nanoparticles were uniformly distributed into sol-gel films for metal anticorrosion. The films showed very pronounced and lasting protective efficiency in concentrated salt aqueous solutions as indicated by electrochemical impedance spectroscopy (EIS) measurement. These results may provide a new route for the preparation of environment-friendly anticorrosion coatings.

2010-01-01

320

Phase formation in gas-phase combustion and pyrolysis reactions under spark and radio-frequency discharge conditions

British Library Electronic Table of Contents (United Kingdom)

Doped ultrafine silicon dioxide powder with a narrow particle size distribution was obtained by RF discharge-stimulated dichlorosilane (SiH2C) oxidation at a low pressure using isobutylene as the combustion inhibitor and chromium hexacarbonyl (Cr(CO)6) as the dopant. The formation and morphology of the ultrafine particles are governed by the parameters of the RF discharge and by the chemical mechanism of the combustion reaction yielding the aerosol. Submicron-sized filamentous carbon structures can be obtained by isobutylene decomposition under spark discharge conditions in the presence of a molybdenum metal catalyst.

2009-01-01

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321

Microstructure of spray converted nanostructured tungsten carbide-cobalt composite

Influence of wood extractives in the polymerization of methyl methacrylate by gamma irradiation

This paper reports the presence of face centered cubic cobalt precipitates inside tungsten carbide in nanocomposite of WC-Co synthesized by spray conversion processing. EDS was used to identify the presence and micro-diffraction was employed to determine the nature of the precipitates. There is entrapment of cobalt in tungsten carbide during the spray conversion process used to form WC/Co powder. During consolidation, at high temperatures, the cobalt attains enough mobility to precipitate inside WC. A vanadium containing compound was seen at the interfaces in samples which incorporated VC as a grain growth inhibitor. (orig.)

1996-05-01

322

Influence of anaerobic microbial activity on biosorption of 2,4-dichlorophenol

Those materials that can be extracted from pine or oak by ether, ethanol, methyl methacrylate (MMA), or benzene--alcohol all act as inhibitors in the #gamma# polymerization of MMA--wood composites. It was found that preirradiation of either the wood or of the wood--monomer combination reduces or eliminates the inhibitory effect. The most practical industrial solution to this problem is to increase the dose, thereby achieving high molecular polymer in the composite. However, the presence of a maximum in the molecular weight--dose curves means that each wood--monomer pair may have a different optimum dose.

1975-01-01

323

Exact solution to NO/sub 2/ absorption

Biosorption is an important removal mechanism in treating hydrophobic toxic organics in biological reactors. Equilibrium sorption isotherms and sorption kinetics of 2,4-dichlorophenol on live and chemically inactive anaerobic granules were studied. A metabolic inhibitor was used to inactivate the biological activity of the biomass. Results showed that the difference in the biosorption of live and chemically inactive anaerobic granules is not significant. This would suggest that anaerobic biosorption is mainly a physical-chemical process and that metabolic-mediated diffusion in the process is negligible. 12 refs., 3 tabs., 7 figs.

1995-12-31

324

Electrochemical behavior of nickel in nitric acid and its corrosion inhibition using some thiosemicarbazone derivatives

This paper describes an exact solution to the problem of absorbing nitrogen dioxide into aqueous solution, in which case the nitrogen dioxide concentration is allowed to vary over a wide range. The authors have worked on the rate of calcium sulfate dihydrate scale formation on the reverse osmosis membrane and find this phenomena can be treated by the crystallization theory. The authors performed long-term experiments using calcium sulfate dihydrate solution with addition of sodium hexametaphosphate (SHMP) and commercially available organophosphates and investigated the mechanism of the inhibitor's action quantitatively.

1984-04-01

325

British Library Electronic Table of Contents (United Kingdom)

The adsorption and corrosion inhibition behavior of three selected thiosemicarbazone derivatives, namely 3-pyridinecarboxaldehyde thiosemicarbazone (META), isonicotinaldehyde thiosemicarbazone (PARA) and 2-pyridinecarboxaldehyde thiosemicarbazone (ORTHO) at the nickel surface were studied electrochemically by Tafel and impedance methods and computationally by carrying out Monte Carlo searches of configurational space on nickel/thiosemicarbazone derivative system. Electrochemical measurements showed that the inhibition efficiency of these compounds increased with increase in their concentration. The recorded inhibition efficiencies of the three tested thiosemicarbazone increase in the order: META>PARA>ORTHO. Polarization studies showed that these compounds act as mixed-type inhibitors for n...

2010-01-01

326

Effect of porosity on the superplasticity of an alumina

Development of time-resolved laser fluorescence spectrometry for on-line uranium checking in solutions of the Purex reprocessing process; Developpement de la spectrofluorimetrie laser a resolution temporelle pour le controle en ligne de l`uranium dans les solutions du procede de retraitement purex

To evaluate the effect of porosity on superplasticity behavior, it is essential to use materials of similar initial grain sizes. This can be achieved by HIPing, which provides an effective way of reducing initial porosity while avoiding appreciable grain growth; various levels of porosity can be achieved for similar grain sizes. This note is concerned with the influence of porosity on superplasticity tensile deformation of a fine grained high-purity alumina doped with copper oxide and containing a grain growth inhibitor. Specimens were prepared by slip casting to net-shape and sintering; some presintered specimens were HIPed to reduce porosity. The subsequent superplasticity behavior is related to porosity in the material.

1994-02-01

327

Corrosion 2003. Conference papers on CD-ROM

The Purex process and the fluorescence spectrometry are first recalled, then uranyl fluorescence is studied in a pure nitric medium without other elements to establish a theoretical model, allowing the description of uranium fluorescence signal with a general equation. The influence of different parameters (temperature, inhibitors, dynamic quenching of iron and cerium) is investigated to develop the model. A quantitative analysis method without addition of reagents is proposed to validate the model.

1992-02-25

328

Acid corrosion inhibition of copper by mangrove tannin

Papers are presented under 38 symposia. Subjects included reinforced concrete, protective coatings and linings, cathodic/anodic protection, chemical cleaning of boilers, managing corrosion with plastics, water treatment, HRSG boiler tube failure analysis, corrosion in oil and gas production, corrosion in petroleum refining and gas, processing, pipelines and tanks, high temperature materials, chemical process industry, aerospace equipment, materials technology developments for incinerators and waste fuel-fired processors, materials and corrosion in fossil-fuels conversion and combustion, corrosion in nuclear systems, marine corrosion, building systems, corrosion mechanisms, corrosion inhibitors and corrosion monitoring and measurement.

2003-07-01

329

British Library Electronic Table of Contents (United Kingdom)

Purpose - The purpose of this paper is to evaluate the corrosion inhibition potential of mangrove (Rhizopora apiculata) tannin in hydrochloric acid medium on copper with the view of developing a natural corrosion inhibitor. Design/methodology/approach - The mangrove tannin was extracted from the mangrove bark and its anticorrosion potential was studied by weight loss, electrochemical and scanning electron microscopy (SEM) analysis. Findings - It has been found that the mangrove tannin effectively inhibits the corrosion on copper metal in hydrochloric acid solution. The results of the electrochemical and weight loss methods showed that the inhibition efficiency of mangrove tannin increases with increasing its concentration. Inhibition is achieved through the adsorption of tannin molecules o...

2011-01-01

330

A low temperature synthesized NbC grain growth inhibitor in WC-Co hardmetal alloy

Structures of trihydroxynaphthalene reductase-fungicide complexes: implications for structure-based design and catalysis

The efficiency of NbC on WC grain coarsening in a WC-10wt.%Co hardmetal alloy was demonstrated by hardness measurement and WC granulation observation. The heterogeneous and overall grain growth were controlled. A low temperature experimentally produced NbC was used and compared to the inhibition potential of a commercial NbC powder. The results were the same in terms of structural fineness and hardness. The dispersion of the experimental NbC was not a problem, in spite of its size. The experimental NbC has very large particles, formed by agglomerates of small crystallites. During milling these agglomerates could be broken down. (orig.)

2001-07-01

331

Mechanistic studies of ethylene biosynthesis in higher plants

Trihydroxynaphthalene reductase catalyzes two intermediate steps in the fungal melanin biosynthetic pathway. The enzyme, a typical short-chain dehydrogenase, is the biochemical target of three commercial fungicides. The fungicides bind preferentially to the NADPH form of the enzyme. Three X-ray structures of the Magnaporthe grisea enzyme complexed with NADPH and two commercial and one experimental fungicide were determined at 1.7 {angstrom} (pyroquilon), 2.0 {angstrom} (2,3-dihydro-4-nitro-1H-inden-1-one, 1), and 2.1 {angstrom} (phthalide) resolutions. The chemically distinct inhibitors occupy similar space within the enzyme's active site. The three inhibitors share hydrogen bonds with the side chain hydroxyls of Ser-164 and Tyr-178 via a carbonyl oxygen (pyroquilon and 1) or via a carbonyl oxygen and a ring oxygen (phthalide). Active site residues occupy similar positions among the three structures. A buried water molecule that is ...

2010-03-08

332

Influence of photodynamic therapy on cell cycle perturbations of the HT-29 cells with modulated 5-lipoxygenase pathway

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 ...

1986-01-01

333

Effect of phlorizin on sugar uptake by broadbean leaf discs. [Vica faba L

One rationale proposals to increase the efficiency of PDT is to combine photo-sensitization with other treatment modalities, including modulation of arachidonic acid metabolism. In combine treatment we examined the effects of 48 h and 24 h pre-treatment of cells with 5- lipoxygenase inhibitor MK-886 prior to photoactivation of hypericin on cell cycle distribution and DNA synthesis. All parameters were examined 24 hours after hypericin activation. Pre-treatment of HT-29 with 5-lipoxygenase inhibitor MK-886 followed by PDT resulted in most significant effects on cell cycle perturbations. Administration of MK-886 alone as well as combination of low doses MK-886 with hypericin induced S phase accumulation. Increasing of MK-886 concentration induced massive changes in the cell cycle progression. Pre-treatment of HT-29 cells with MK-886 alone (15 #mu#M; - 48 h) caused accumulation of cells in S-phase (58 % in S-phase and 36 % in G_0/G_1 phase). ...

2006-05-01

334

A DNA methyltransferase inhibitor and all-trans retinoic acid reduce oral cavity carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide.

Phlorizin is a competitive inhibitor of Na/sup +//glucose symport in animal cells and of H/sup +//3-O-methylglucose (3-O-MeG) symport in liverworts. The effects of this compound on the uptake of (U-/sup 14/C) sucrose and of (/sup 14/C) 3-O-MeG by broadbean (Vicia faba L.) leaf discs were studied. Leaf discs without lower epidermis were preincubated in the dark for 30 min (fresh discs) or for 12 h (aged discs) on a medium buffered at pH 5.0 containing mannitol as an osmoticum. They were then incubated for 30 min in the light on a similar solution added with 1 mM (/sup 14/C) sucrose or (/sup 14/C) 3-O-MeG and 5 mM phlorizin. Phlorizin inhibited uptake of 3-O-MeG by 37 and 50% respectively in fresh and aged discs. Sucrose uptake was more sensitive to the inhibitor than 3-O-MeG uptake and was also more inhibited in aged than in fresh discs (76% inhibition vs 54%). Kinetic studies showed that the inhibition exerted by phlorizin in fresh material is ...

1986-04-01

335

Transforming growth factor-b induces nerve growth factor expression in pancreatic stellate cells by activation of the ALK-5 pathway

The transcriptional silencing of some cell cycle inhibitors and tumor suppressors, such as p16 and retinoic acid receptor beta(2), by DNA hypermethylation at CpG islands is commonly found in human oral squamous carcinoma cells. We examined the effects of the DNA methyltransferase inhibitor 5-Aza-2'-deoxycytidine (5-Aza; 0.25 mg/kg body weight), all-trans retinoic acid (RA; given at 100 microg/kg body weight and 1 mg/kg body weight), and the combination of 5-Aza and the low-dose RA on murine oral cavity carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide (4-NQO) in a mouse model. All the drug treatments were done for 15 weeks after a 10-week 4-NQO treatment. Mice in all drug treatment groups showed decreases in the average numbers of neoplastic tongue lesions. The combination of 5-Aza and RA effectively attenuated tongue lesion severity. Although all drug treatments limited the increase in the percentage of proliferating cell ...

2009-12-01

336

British Library Electronic Table of Contents (United Kingdom)

Nerve growth factor (NGF), a survival factor for neurons enforces pain by sensitizing nociceptors. Also in the pancreas, NGF was associated with pain and it can stimulate the proliferation of pancreatic cancer cells. Hepatic stellate cells (HSC) respond to NGF with apoptosis. Transforming growth factor (TGF)-b, one of the strongest pro-fibrogenic activators of pancreatic stellate cells (PSC) induced NGF and its two receptors in an immortalized human cell line (ihPSC) and primary rat PSC (prPSC) as determined by RT-PCR, western blot, and immunofluorescence. In contrast to HSC, PSC expressed both NGF receptors, although p75NTR expression was weak in prPSC. In contrast to ihPSC TGF-b activated both Smad signaling cascades in prPSC. NGF secretion was diminished by the activin-like kinase (ALK)...

2009-01-01

337

Nuclear Targeting of Methyl-Recycling Enzymes in Arabidopsis thaliana Is Mediated by Specific Protein Interactions.

Mutations in cyr1 and pat1 reveal pheromone-induced G1 arrest in the fission yeast Schizosaccharomyces pombe

Numerous transmethylation reactions are required for normal plant growth and development. S-adenosylhomocysteine hydrolase (SAHH) and adenosine kinase (ADK) act coordinately to recycle the by-product of these reactions, S-adenosylhomocysteine (SAH) that would otherwise competitively inhibit methyltransferase (MT) activities. Here, we report on investigations to understand how the SAH produced in the nucleus is metabolized by SAHH and ADK. Localization analyses using green fluorescent fusion proteins demonstrated that both enzymes are capable of localizing to the cytoplasm and the nucleus, although no obvious nuclear localization signal was found in their sequences. Deletion analysis revealed that a 41-amino-acid segment of SAHH (Gly(150)-Lys(190)) is required for nuclear targeting of this enzyme. This segment is surface exposed, shows unique sequence conservation patterns in plant SAHHs, and possesses additional features of protein-protein interaction motifs. ADK ...

2011-10-01

338

Loss of PINK1 function decreases PP2A activity and promotes autophagy in dopaminergic cells and a murine model

Investigations into sexual differentiation and pheromone response in the fission yeast Schizosaccharomyces pombe are complicated by the need to first starve the cells of nitrogen. Most mating-related experiments are therefore performed on non-dividing cells. Here we overcome this problem by using two mutants that bypass the nutritional requirements and respond to the M-factor mating pheromone in rich medium. The first mutant lacks the cyr1 gene which encodes adenylate cyclase and these cells contain no measurable amounts of cAMP. When M-factor is added to a growing h+ cyr1- strain it causes a transient G1 arrest of cell division, transcription of mat1-Pm, and elongation of the cells to form shmoos. The second mutant contains the temperature-sensitive pat1-114 allele. At 30 degrees C this mutant was previously shown not only to bypass the nutritional signal but also to stop growing in a state derepressed for pheromone-controlled functions. We now report that an h+ pat1-114 strain ...

1994-01-01

339

British Library Electronic Table of Contents (United Kingdom)

Parkinson's disease (PD) is the most common neurodegenerative movement disorder. Mutations in PTEN-induced kinase 1 (PINK1) are a frequent cause of recessive PD. Autophagy, a pathway for clearance of protein aggregates or impaired organelles, is a newly identified mechanism for PD development. However, it is still unclear what molecules regulate autophagy in PINK1-silenced cells. Here we report that autophagosome formation is promoted in the early phase in response to PINK1 gene silencing by lentivirus transfer vectors expressed in mouse striatum. Reduced PP2A activity and increased phosphorylation of PP2A at Y307 (inactive form of PP2A) were observed in PINK1-knockdown dopaminergic cells and striatum tissues. Treatment with C2-ceramide (an agonist of PP2A) reduced autophagy levels in PINK...

2011-01-01

340

Influence of valency and labelling chemistry on in vivo targeting using radioiodinated HER2-binding Affibody molecules

British Library Electronic Table of Contents (United Kingdom)

Purpose HER2 is a transmembrane tyrosine kinase, which is overexpressed in a number of carcinomas. The Affibody molecule ZHER2:342 is a small (7?kDa) affinity protein binding to HER2 with an affinity of 22?pM. The goal of this study was to evaluate the use of ((4-hydroxyphenyl)ethyl)maleimide (HPEM) for radioiodination of ZHER2:342 and to compare the targeting properties of monomeric and dimeric forms of ZHER2:342. Methods The biodistribution of different radioiodinated derivatives of ZHER2:342 was studied in BALB/C nu/nu mice bearing HER2-expressing SKOV-3 xenografts. Biodistributions of 125I-PIB-ZHER2:342 and site-specifically labelled 125I-HPEM-ZHER2:342-C were compared. Biodistributions of monomeric 131I-HPEM-ZHER2:342-C and dimeric 125I-HPEM-(ZHER2:342)2-C were evaluated using a paire...

2009-01-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

341

Increase in phorbol ester binding in liver microsomes after chronic administration of phenobarbital

Identification of protein phosphorylation sites within Ser/Thr-rich cluster domains using site-directed mutagenesis and hybrid linear quadrupole ion trap Fourier transform ion cyclotron resonance mass spectrometry

The effect of chronic administration of phenobarbital on the binding of phorbol-12,13-dibutyrate (({sup 3}H)PDBu), an activator of protein kinase C (PKC), was examined in rat liver microsomes. A significant increase in the number of binding sites was observed in microsomes of Fisher 344 rats. However, no change appeared in liver cytosol binding of PDBu. Consequently, a translocation process of PKC is unlikely. The increase in ({sup 3}H)PDBu binding in liver microsomes is significant 24 h. after one injection of phenobarbital and reaches its maximum in 2 days. In other strains of rats (ACI and lean Zucker), significant differences were found in the increase of ({sup 3}H)PDBu binding in microsomes. Fisher 344 were the most sensitive, lean Zucker rats, the least sensitive. Those results parallel the pentoxy-resorufin O demethylase activity in the microsomes of the same animals. EC{sub 50} values for inhibition of ({sup 3}H)PDBu binding by pentobarbital were determined ...

1991-03-15

342

British Library Electronic Table of Contents (United Kingdom)

We describe a method for the analysis of multi-site phosphorylation in serine/threonine (Ser/Thr)-rich protein sequences. Site-specific mutagenesis was used to introduce tryptic cleavage sites in the serine glutamine/threonine glutamine cluster domain (SCD) of the human checkpoint protein kinase (Chk2). The mutant proteins were shown to autophosphorylate on residues that are inducibly phosphorylated when mammalian cells are exposed to ionizing radiation (serine 33/35, serine 516, threonine 68 and threonine 432). Five Ser/Thr clusters within the SCD were flanked by arginine or lysine residues to produce tryptic peptides for nanospray liquid chromatography (nanoLC)/linear quadrupole ion trap Fourier transform ion cyclotron resonance mass spectrometry. Phosphorylation sites were assigned usin...

2007-01-01

343

Final report of the specific research. Investigations on the analysis of bio-protective factors against radiation. 1998-2000 FY (Research Group of NIRS)

Enhanced MALDI-TOF MS Analysis of Phosphopeptides Using an Optimized DHAP/DAHC Matrix

This report concerns investigations in the title conducted by 8 groups of National Institute of Radiological Sciences (NIRS) during the period of 1998-2000. The groups are for investigation of: Effects of p53 tumor suppressor gene in radiation-induced leukemia, Role of atm-gene in dose rate effect of ionizing radiation, Function of DNA-dependent protein kinase catalytic subunit (DNA-PK{sub cs}), Functional complementation of radiation-sensitive mutant M10 cell line by human XRCC4 cDNA expression, Role of radiation-induced apoptosis in digital defects in embryonic mice, Functional analysis of S-phase specific novel nuclear protein NP95 by gene targeting, Role of chemokine in T cell development and lymphomagenesis, and establishment of production techniques of gene-modified mice using embryonic stem cells for genetic analysis of radiation-sensitive genes. The groups describe summaries of their studies and published original articles are also given. (N.I.)

2002-03-01

344

Development of a novel mouse tk{sup +/-} embryonic stem cell line for use in mutagenicity studies

Selecting an appropriate matrix solution is one of the most effective means of increasing the ionization efficiency of phosphopeptides in matrix-assisted laser-desorption/ionization time-of-flight mass spectrometry (MALDI-TOF-MS). In this study, we systematically assessed matrix combinations of 2, 6-dihydroxyacetophenone (DHAP) and diammonium hydrogen citrate (DAHC), and demonstrated that the low ratio DHAP/DAHC matrix was more effective in enhancing the ionization of phosphopeptides. Low femtomole level of phosphopeptides from the tryptic digests of ?-casein and ?-casein was readily detected by MALDI-TOF-MS in both positive and negative ion mode without desalination or phosphopeptide enrichment. Compared with the DHB/PA matrix, the optimized DHAP/DAHC matrix yielded superior sample homogeneity and higher phosphopeptide measurement sensitivity, particularly when multiple phosphorylated peptides were assessed. Finally, the DHAP/DAHC matrix was applied to identify phosphorylation sites ...

2010-01-01

345

In vitro evaluation of herpes simplex virus type 1 thymidine kinase reporter system in dynamic studies of transcriptional gene regulation

A tk{sup +/-} mouse embryonic stem (ES) cell line, designated 1G2, has been created in which one allele of the thymidine kinase (tk) gene was inactivated by targeted homologous recombination. This line is an analog of the mouse lymphoma tk{sup +/-} L5178Y cell line, which is used widely to assess the mutagenicity of chemical agents. Treatment of 1G2 cells with the alkylating agent N-ethyl-N-nitrosourea (ENU) resulted in a dose-related increase in tribluorothymidine-resistant colonies. Mutant frequencies of 152 and 296 per 10{sup 6} cells were determined for 0.1 and 0.3 mg/ml doses of ENU, compared with a spontaneous mutant frequency of 15 per 10{sup 6} cells. The data indicate that tk{sup +/-} 1G2 ES cells may be useful for the creation of a transgenic mouse model for assessing in vivo mutation using an endogenous autosomal gene. 45 refs., 2 figs., 1 tab.

1996-12-31

346

WC-TiC-Ni cemented carbide with enhanced properties

The herpes simplex virus type 1 thymidine kinase (HSV1-TK) reporter system is being used to directly and indirectly monitor therapeutic gene expression, immune cell trafficking and protein-protein interactions in various living animals. However, the issues of HSV1-TK enzyme stability in living cells and whether this reporter system is optimal for dynamic studies of gene expression events in genetic imaging have not be addressed. The purpose of the present study was to evaluate the application of this reporter system in dynamic studies of transcriptional gene regulation. To achieve this purpose, we established two tetracycline-inducible murine sarcoma cell lines, tetracycline-turn-off HSV1-tk-expressing cell line (NG4TL4/tet-off-HSV1-tk) and tetracycline-turn-off Luc-expressing cell line (NG4TL4/tet-off-Luc), to create an artificially regulated gene expression model in vitro. The dynamic transcriptional events mediating a series of doxycycline (Dox) inductions were ...

2006-07-15

347

British Library Electronic Table of Contents (United Kingdom)

In the paper, the effect of Ni content, WC grain size and Mo2C addition on WC-6.25wt%TiC-9.3wt%Ni cemented carbide were investigated to improve the properties of Ni-bonded cemented carbides. The results show that the decrease of Ni content will result in the decrease of transverse rupture strength and increase of hardness; with the decrease of WC particle size, hardness increases due to the refinement of WC grains, however, the transverse rupture strength decrease due to the decrease of Ni binder thickness; Mo2C proves to be an effective grain growth inhibitor. With the increase of Mo2C content, the WC grains are refined and the hardness and transverse rupture strength are improved. Generally, when the Ni content is decreased to 8.4wt%, 13.45mm WC is used and 1.2wt% Mo2C is added, a higher...

2008-01-01

348

Variation of surface composition and sintering of binary Pd{sub 7}Ag{sub 3} nanoparticles

Variation of surface composition and sintering of binary Pd_7Ag_3 nanoparticles

The variation of surface composition and sintering of the binary Pd{sub 7}Ag{sub 3} nanoparticles prepared by chemical reduction were studied. The composition of the as-prepared Pd{sub 7}Ag{sub 3} nanoparticles across the diameter is inhomogeneous due to different reduction potentials of Pd and Ag. Upon heating, Ag will migrate to the surface because of its lower surface energy. Surface modification results in variation of surface composition during the sintering process. Stearic acid acts as a grain growth inhibitor. The migration of Ag to the surface is suppressed and the sintering is retarded. Modification by polyethylene glycol leads to more migration of Ag atoms from the core to the surface. This makes the nanoparticles easier to sinter.

2006-05-18

349

VC- and Cr{sub 3}C{sub 2}-doped WC-NbC-Co hardmetals

The variation of surface composition and sintering of the binary Pd_7Ag_3 nanoparticles prepared by chemical reduction were studied. The composition of the as-prepared Pd_7Ag_3 nanoparticles across the diameter is inhomogeneous due to different reduction potentials of Pd and Ag. Upon heating, Ag will migrate to the surface because of its lower surface energy. Surface modification results in variation of surface composition during the sintering process. Stearic acid acts as a grain growth inhibitor. The migration of Ag to the surface is suppressed and the sintering is retarded. Modification by polyethylene glycol leads to more migration of Ag atoms from the core to the surface. This makes the nanoparticles easier to sinter.

2006-05-18

350

The contribution of ear photosynthesis to grain filling in bread wheat (Triticum aestivum L.)

This study compares the microstructure and mechanical properties of plain and 0.9 or 3.6 wt% VC- or Cr{sub 3}C{sub 2}-doped WC-12 wt% Co hardmetals with 40 wt% NbC, prepared by pulsed electric current sintering (PECS) in the solid state for 4 min at 1240 deg. C and conventional pressureless liquid phase sintering (CS) for 1 h at 1420 deg. C. The addition of VC or Cr{sub 3}C{sub 2} was found to inhibit grain growth of the residual WC grains, whereas the size of the solid solution (Nb,W,V/Cr)C grains was hardly influenced. The type of grain growth inhibitor and densification temperature however, strongly influenced the composition of the NbC solid solution formed, which was thermodynamically and experimentally assessed.

2008-09-22

351

British Library Electronic Table of Contents (United Kingdom)

The contribution of ear photosynthesis to grain filling in wheat (Triticum aestivum L.) is not well known. The main objective of this work was to evaluate this contribution through three different experimental approaches: (1) ear photosynthesis was reduced by removing awns or shading the ears (in combination with a defoliation treatment), (2) grain weight per ear was compared in an 'all shaded' crop versus plants where only the vegetative parts were shaded ('ear emerging'), and (3) ear photosynthesis was reduced with DCMU (3-(3,4-dichlorophenyl)-1,1-dimethylurea), a specific inhibitor of photosystem II. In field experiments in La Plata (Argentina), cultivars Klein Escudo and BioINTA 3000 were subjected to awn removal and ear shading treatments, with or without severe defoliation, and to 'a...

2010-01-01

352

Synthesis and photoluminescence properties of continuous freestanding SiC(Al) films derived from aluminum-containing polycarbosilane

Synergistic effect of iodide ion and polyacrylic acid on corrosion inhibition of iron in H2SO4 investigated by electrochemical techniques

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.

2010-10-01

353

British Library Electronic Table of Contents (United Kingdom)

Corrosion inhibition of iron in H2SO4 by polyacrylic acid (PAA) was investigated using electrochemical techniques at 30degreeC. Results obtained indicate that PAA inhibited the corrosion of iron in the acid medium. Inhibition efficiency increases with increase in PAA concentration and synergistically enhanced on addition of iodide ions. Potentiodynamic polarization results suggest that PAA functions as a modest cathodic inhibitor. The adsorption of PAA onto the iron surface followed Temkin adsorption isotherm. FTIR analysis revealed that the synergistic effect due to co-adsorption of iodide ions and PAA is co-operative in nature.

2010-01-01

354

Study of phosphonate addition and hydrodynamic conditions on ordinary steel corrosion inhibition in simulated cooling water

British Library Electronic Table of Contents (United Kingdom)

The effect of phosphonate anion (PHOS) on the corrosion of ordinary steel in simulated cooling water has been studied using weight loss, polarization curves and electrochemical impedance spectroscopy measurements. PHOS was studied in the concentration range from 7.5x10^-^5 to 10^-^3M. The results obtained reveal that PHOS perform excellently as corrosion inhibitor for ordinary steel in simulated cooling water. The inhibition efficiency of PHOS was increased with increasing both its concentration and water circulation velocity. These two factors seem to promote the adsorption of phosphorus and oxygen ions on the metal surface, leading to the formation of a protective layer with a greater charge transfer resistance and lower permeability. The inhibition efficiency decreased slightly with tem...

2010-01-01

355

Sodium monocarboxylates as inhibitors of AZ31 alloy corrosion in a synthetic cooling water

Role of Intravenous Omeprazole in Patients with High-Risk Peptic Ulcer Bleeding After Successful Endoscopic Epinephrine Injection: A Prospective Randomized Comparative Trial

This research investigated the inhibiting effects that sodium salts of linear monocarboxylic acids displayed towards the corrosion process of AZ31 Mg alloy in ASTM D 1387 saline solution (a synthetic industrial cooling water). The length of the aliphatic chain of the acids ranged between 7 and 15 carbon atoms. The inhibiting action of these salts can be related to the precipitation of an insoluble magnesium salt, which mainly affected the anodic reaction. The aliphatic chain length controlled the anion solubility and the reaction rate of magnesium carboxylate formation. For all the salts, an optimum concentration was experienced: 10{sup -2} M for sodium decanoate (caprate), 10{sup -3} M for sodium dodecanoate (laurate), 10{sup -4} M for sodium tetradecanoate (myristate); when this concentration was exceeded, a diminution (even a disappearance) in the inhibiting action was found. (Abstract Copyright [2009], Wiley Periodicals, Inc.)

2009-03-15

356

British Library Electronic Table of Contents (United Kingdom)

BACKGROUND: Epinephrine injection is the most common endoscopic therapy for peptic ulcer bleeding. Controversy exists concerning the optimal dose of proton pump inhibitors (PPI) for patients with bleeding peptic ulcers after successful endoscopic therapy. The objective of this study was to determine the optimal dose of PPI after successful endoscopic epinephrine injection in patients with bleeding peptic ulcers. METHODS: A total of 200 peptic ulcer patients with active bleeding or nonbleeding visible vessels (NBVV) who had obtained initial hemostasis with endoscopic injection of epinephrine were randomized to receive omeprazole 40 mg infusion every 6 h, omeprazole 40 mg infusion every 12 h or cimetidine (CIM) 400 mg infusion every 12 h. Outcomes were checked at 14 days after enrollment. RE...

2006-01-01

357

Resveratrol causes COX-2- and p53-dependent apoptosis in head and neck squamous cell cancer cells

British Library Electronic Table of Contents (United Kingdom)

Cyclooxygenase-2 (COX-2) content is increased in many types of tumor cells. We have investigated the mechanism by which resveratrol, a stilbene that is pro-apoptotic in many tumor cell lines, causes apoptosis in human head and neck squamous cell carcinoma UMSCC-22B cells by a mechanism involving cellular COX-2. UMSCC-22B cells treated with resveratrol for 24 h, with or without selected inhibitors, were examined: (1) for the presence of nuclear activated ERK1/2, p53 and COX-2, (2) for evidence of apoptosis, and (3) by chromatin immunoprecipitation to demonstrate p53 binding to the p21 promoter. Stilbene-induced apoptosis was concentration-dependent, and associated with ERK1/2 activation, serine-15 p53 phosphorylation and nuclear accumulation of these proteins. These effects were blocked by ...

2008-01-01

358

Reductive metabolism of the dinitrobenzamide mustard anticancer prodrug PR-104 in mice

British Library Electronic Table of Contents (United Kingdom)

Purpose PR-104, a bioreductive prodrug in clinical trial, is a phosphate ester which is rapidly metabolized to the corresponding alcohol PR-104A. This dinitrobenzamide mustard is activated by reduction to hydroxylamine (PR-104H) and amine (PR-104M) metabolites selectively in hypoxic cells, and also independently of hypoxia by aldo-keto reductase (AKR) 1C3 in some tumors. Here, we evaluate reductive metabolism of PR-104A in mice and its significance for host toxicity. Methods The pharmacokinetics of PR-104, PR-104A and its reduced metabolites were investigated in plasma and tissues of mice (with and without SiHa or H460 tumor xenografts) and effects of potential oxidoreductase inhibitors were evaluated. Results Pharmacokinetic studies identified extensive non-tumor reduction of PR-104A to t...

2011-01-01

359

Ramiprilate Inhibits Functional Matrix Metalloproteinase Activity in Crohn-s Disease Fistulas

British Library Electronic Table of Contents (United Kingdom)

Abstract:- Increased expression of matrix metalloproteinase (MMP)-2, -3 and -9 has been demonstrated in Crohn-s disease fistulas, but it is unknown whether these enzymes are biologically active and represent a therapeutic target. Therefore, we investigated the proteolytic activity of MMPs in fistula tissue and examined the effect of inhibitors, including clinically available drugs that beside their main action also suppress MMPs. Fistula specimens were obtained by surgical excision from 22 patients with Crohn-s disease and from 10 patients with fistulas resulting from other causes. Colonic endoscopic biopsies from six controls were also included. Total functional MMP activity was measured by a high-pressure liquid chromatography (HPLC)-based, fluorogenic MMP-substrate cleavage assay, and t...

2011-01-01

360

Preparation and photocatalytic property of pyrochlore Bi2Ti2O7 and (Bi, La) 2Ti2O7 films

British Library Electronic Table of Contents (United Kingdom)

Dopant-free Bi2Ti2O7 thin films with pyrochlore structure and La-doped bismuth titanate thin films have been fabricated by means of chemical solution decomposition, and characterized by X-ray diffraction, atomic force microscopy, scanning electron microscopy and UV?Vis spectrophotometry in this study. Their photocatalytic activities have been evaluated by photodegrading methyl orange solution, and the optimum processing parameters for the highest photocatalytic activity have been found. Moreover, the effects of La-doping on the phase transformation and the photocalalytic activity have been studied. It has been deduced from the experiment result that substituted La3+ ions can act as a stabilizer of Aurivillus phase BLT and a grain?growth inhibitor in BLT thin films.

2008-01-01

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361

Polarity of prismatic facets delimiting WC grains in WC-Co alloys

British Library Electronic Table of Contents (United Kingdom)

This study reports a determination of the polarity of WC facets in WC-Co alloys sintered at the liquid state. In these alloys, WC grains are delimited by basal facets and two sets of {101 0} prismatic facets, one set of facets being much more developed than the other. A variation of the shape is observed as a function of the composition of the alloy. High resolution transmission electron microscopy is used to investigate the polarity of the prismatic facets owing to the typical triangular patterns appearing on the images. The effect of the composition is investigated using two alloys with different carbon potentials and one containing VC and Cr3C2 as grain growth inhibitors. The interpretation of the images shows that in all cases, the same set of prismatic planes is favoured.

2010-01-01

362

Pharmacokinetic and pharmacodynamic properties of an oral formulation of the histone deacetylase inhibitor Belinostat (PXD101)

British Library Electronic Table of Contents (United Kingdom)

Purpose The primary objective of this sub-study, undertaken as an extension to the previously reported phase-I study, was to explore the feasibility, tolerability and pharmacokinetics (PK) of belinostat when administered by the oral route. Preliminary pharmacodynamic (PD) studies were also performed to enable comparison of the biological effects of the oral and intravenous formulations. Patients and methods Oral belinostat was administered in a range of doses and schedules (once, twice or thrice daily), on either day 1 or days 1?5, of the second or a subsequent treatment cycle in 15 patients who were included in the phase-I trial of intravenous belinostat. Serial blood samples were collected for PK and PD (histone acetylation) analyses, and the results compared with corresponding analyses ...

2011-01-01

363

Nanostructured nickel ferrite: A liquid petroleum gas sensor

British Library Electronic Table of Contents (United Kingdom)

The present investigation deals with the synthesis of nanostructured nickel ferrite (NiFe2O4) and their liquid petroleum gas-sensing characteristics. The 15-20nm size nickel ferrite has been synthesized at 700degreeC by a simple molten-salt route using sodium chloride as grain growth inhibitor. These nanoparticles exhibit significantly high response towards liquid petroleum gas (LPG) in comparison with ethanol vapor, hydrogen sulfide, ammonia and hydrogen. The gas response towards various gases at their 200ppm concentrations is investigated at 200-450degreeC. Different characterization techniques have been employed, such as differential thermal analysis, X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and high resolution transmission elec...

2009-01-01

364

Microstructure-property relationships in beryllia-ceramics sintered to near theoretical density

Methanogen community structure in the rumens of farmed sheep, cattle and red deer fed different diets

The use of selective additives such as MgO as a sintering aid and a rare earth oxide as a grain growth inhibitor, has allowed the manufacture of beryllia ceramics having close to theoretical density. The grain size and grain size distribution can be controlled by an optimum firing schedule leaving a remnant porosity which is extremely fine (0.2 {mu}m). This structure is compared with conventional BeO ceramics, densified by liquid phase sintering, which develops a glassy grain boundary and retains large pores up to 3 {mu}m. The significantly improved strength properties, extremely fine pores,the 'pinning effect' of rare earth oxide, and the superior surface finish both in the as-fired and polished state are discussed in relation to the micro-structure. (orig.).

1989-01-01

365

British Library Electronic Table of Contents (United Kingdom)

Abstract Development of inhibitors and vaccines that mitigate rumen-derived methane by targeting methanogens relies on knowledge of the methanogens present. We investigated the composition of archaeal communities in the rumens of farmed sheep (Ovis aries), cattle (Bos taurus) and red deer (Cervus elaphus) using denaturing gradient gel electrophoresis (DGGE) to generate fingerprints of archaeal 16S rRNA genes. The total archaeal communities were relatively constant across species and diets, and were less variable and less diverse than bacterial communities. There were diet- and ruminant-species-based differences in archaeal community structure, but the same dominant archaea were present in all rumens. These were members of three coherent clades: species related to Methanobrevibacter ruminan...

2011-01-01

366

Kinetics of inhibition of green crab (Scylla serrata) alkaline phosphatase by sodium (2,2'-bipyridine) oxodiperoxovanadate.

Involvement of Rh blood group polypeptides in the maintenance of aminophospholipid asymmetry

Green crab (Scylla serrata) alkaline phosphatase (EC 3.1.3.1) is a metalloenzyme, which catalyzes the nonspecific hydrolysis of phosphate monoesters. The kinetics of inhibition of the enzyme by sodium (2, 2'-bipyridine) oxodiperoxovanadate, pV(bipy), has been studied. The time course of the hydrolysis of p-nitrophenyl-phosphate catalyzed by the enzyme in the presence of different pV(bipy) concentrations showed that at each pV(bipy) concentration, the rate decreased with increasing time until a straight line was approached, the straight line slopes are the same for all concentrations. The results suggest that the inhibition of the enzyme by pV(bipy) is a slow, reversible reaction with fractional remaining activity. The microscopic rate constants are determined for the reaction of inhibitor with the enzyme. PMID:10691182

1999-10-01

367

Inhibitor effect on corrosion of titanium alloys in muriatic solutions of titanium-magnesium production

The human erythrocyte (RBC) Rh blood group system consists of a complex of distinct integral membrane polypeptides with physical properties common to the aminophospholipid transporter responsible for the transbilayer movement of phosphatidylserine (PS) in RBC. To assess the involvement of Rh polypeptides in PS translocation, the aminophospholipid translocase was labeled with a photoactivatable PS analogue, "1"2"5I-azido-PS, and with an inhibitor of PS transport, "1"2"5I-labeled 2-(2-pyridyldithio)ethylamine. The ability of monoclonal Rh antibodies to immunoprecipitate the labeled transporter was determined. Immunoprecipitated Rh polypeptides were found to be labeled with the aminophospholipid translocase markers, suggesting that Rh proteins are involved in the transbilayer movement of PS.

368

Inhibition of Metabolism of Diethylene Glycol Prevents Target Organ Toxicity in Rats

Corrosion tests of titanium alloys VTI-0, OT4, VT5-1 and steel Kh18N1OT in 10% and 18% HCl with additions of carnallite at 40 deg C have been carried out. It has been established that titanium alloys in 10% and 18% HCl containing 5 and 10% carnallite are sufficiently corrosion resistant in the presence of 0.1-1% FeCl or HNO_3 and can be used for manufacturing the equipment of recirculation gas scrubbers. Steel Kh18N10T is unstable in all the media tested. It is subjected to intensive pitting. Specimens of steel Kh18N10T have also revealed edge cracking.

369

British Library Electronic Table of Contents (United Kingdom)

Diethylene glycol (DEG) is an industrial chemical, the misuse of which has led to numerous epidemic poisonings worldwide. The mechanism of its toxicity has not been defined as to the precise relationship between the metabolism of DEG and target organ toxicity. The purpose of this study was to investigate the mechanism for the acute toxicity of DEG, and the effect of the alcohol dehydrogenase inhibitor 4-methylpyrazole (fomepizole), by determining the relationship between accumulation of DEG or its metabolites and the resulting kidney and liver toxicity. Rats were treated by oral gavage with water, 2 g/kg DEG (low dose), 10 g/kg DEG (high dose), or 10 g/kg DEG + fomepizole, and blood and urine were collected over 48 h. Rats treated with high-dose DEG had metabolic acidosis, increased BUN an...

2010-01-01

370

Inhibition effects on fermentation of hardwood extracted hemicelluloses by acetic acid and sodium

British Library Electronic Table of Contents (United Kingdom)

Extraction of hemicellulose from hardwood chips prior to pulping is a possible method for producing ethanol and acetic acid in an integrated forest bio-refinery, adding value to wood components normally relegated to boiler fuel. Hemicellulose was extracted from hardwood chips using green liquor, a pulping liquor intermediate consisting of aqueous NaOH, Na2CO3, and Na2S, at 160degreeC, held for 110min in a 20L rocking digester. The extracted liquor contained 3.7% solids and had a pH of 5.6. The organic content of the extracts was mainly xylo-oligosaccharides and acetic acid. Because it was dilute, the hemicellulose extract was concentrated by evaporation in a thin film evaporator. Concentrates from the evaporator reached levels of up to 10% solids. Inhibitors such as acetic acid and sodium ...

2010-01-01

371

In vitro atrazine-exposure inhibits human natural killer cell lytic granule release

British Library Electronic Table of Contents (United Kingdom)

The herbicide atrazine is a known immunotoxicant and an inhibitor of human natural killer (NK) cell lytic function. The precise changes in NK cell lytic function following atrazine exposure have not been fully elucidated. The current study identifies the point at which atrazine exerts its affect on the stepwise process of human NK cell-mediated lyses of the K562 target cell line. Using intracellular staining of human peripheral blood lymphocytes, it was determined that a 24-h in vitro exposure to atrazine did not decrease the level of NK cell lytic proteins granzyme A, granzyme B or perforin. Thus, it was hypothesized that atrazine exposure was inhibiting the ability of the NK cells to bind to the target cell and subsequently inhibit the release of lytic protein from the NK cell. To test t...

2007-01-01

372

Impact of Cr3C2/VC addition on the dry sliding friction and wear response of WC-Co cemented carbides

British Library Electronic Table of Contents (United Kingdom)

Two grades of WC-10wt.%Co cemented carbide with or without addition of Cr3C2/VC grain growth inhibitor during liquid phase sintering were produced with the goal to investigate their reciprocating sliding friction and wear behaviour against WC-6wt.%Co cemented carbide under unlubricated conditions. The tribological characteristics were obtained on a Plint TE77 tribometer using distinctive normal contact loads. The generated wear tracks were analyzed by scanning electron microscopy and quantified topographically using surface scanning equipment. The post-mortem obtained wear volumes were compared to the online assessed wear. Correlations between wear volume, wear rate and coefficient of friction on the one hand and sliding distance and microstructural properties on the other hand were determ...

2009-01-01

373

Immunosuppressant calcineurin inhibitors phase shift circadian rhythms and inhibit circadian responses to light

British Library Electronic Table of Contents (United Kingdom)

PP2B is a Ca2+/calmodulin-dependent protein phosphatase that is ubiquitously expressed in mammals. Among other actions, it is an effector mechanism in NMDA-mediated glutamate neurotransmission as well as a regulator of GSK3? and MAPK signaling cascades. Because all of these mechanisms have demonstrable roles in the control of circadian rhythyms, we hypothesized that PP2B would be a key regulator of rhythm generation and entrainment, and that through inhibition of its phosphatase activity, the circadian system would be affected by immunosuppressant drug therapy. We report here that immunosuppressant drugs (cyclosporin A, FK506) (1) block the circadian responses to light that underlie photic entrainment; (2) produce circadian phase shifts with a characteristic nonphotic profile; and (3) disr...

2008-01-01

374

IL-1b enhances the antibacterial activity of astrocytes by activation of NF-kB

British Library Electronic Table of Contents (United Kingdom)

Astrocytes have important immune functions in CNS, and astrocytes stimulated by interferon-g were showed to have direct antimicrobial function. However whether astrocytes without the stimulation of cytokines have antibacterial function, and how this function is regulated are still largely unknown. In this study, we found that primary cultured astrocytes inhibited the growth of both gram-negative and gram-positive bacteria. Further more, we showed that interleukin-1b (IL-1b) enhanced the antibacterial effect in a dose-dependent manner, and the antibacterial effect of astrocytes from IL-1b receptor-deficient mice failed to be enhanced by IL-1b. IL-1b stimulated IkBa degradation, NF-kB nuclear translocation, and transactivation in astrocytes. NF-kB inhibitors blocked NF-kB activation and the ...

2010-01-01

375

Epigenetic regulation of Myc on retinoic acid receptor beta and PDLIM4 in RWPE1 cells

British Library Electronic Table of Contents (United Kingdom)

BACKGROUND Hypermethylation of CpG islands is a common epigenetic alteration associated with cancer. Tumor suppressor genes retinoic acid receptor beta (RARb) and PDLIM4 are hypermethylated and silenced in prostate cancer (PCa) tissues and PCa cell lines compared to normal prostate cells. METHODS In this study, a benign prostate epithelial cell line RWPE1 was used as a model to study the epigenetic regulation of Myc on the RARb and PDLIM4 promoters. Forced Myc overexpression inhibited the RARb and PDLIM4 expression. RESULTS Pyrosequencing study showed that Myc overexpression increased methylation in several CpG sites of both promoters. A DNA methylation inhibitor 5-aza-2prime-deoxycytidine reversed the epigenetic alteration effect of Myc on both RARb and PDLIM4. CONCLUSION The epigenetic r...

2009-01-01

376

Electrochemical noise in corrosion

Efficacy and Safety of Galantamine in Patients with Dementia with Lewy Bodies: A 24-Week Open-Label Study

By varying different variables (potential, chloride content, surface pretreatment etc.) it is possible to show the effect of increasingly harsher corrosion conditions on passive-layer stability. These changes will not be detected by conventional methods e.g. measurement of passive current density, until a very late stage. Electrochemical noise measurement will allow the action of inhibitors to be detected in a rapid and effective manner. High-alloy steels and titanium claddings subjected to pitting corrosion in chloride-containing media demonstrate how to use this method for problem solutions and to open up new practical applications. The effect of mechanical stresses (natural, tensile) on the corrosion system can be detected by electrochemical noise which opens up new methods for crack corrosion studying and monitoring. (orig./DG).

1993-10-07

377

British Library Electronic Table of Contents (United Kingdom)

Abstract Background: Dementia with Lewy bodies (DLB) is a common dementia of the elderly. A significant cholinergic deficit has been demonstrated that may be responsive to treatment by cholinesterase inhibitors (ChEIs). Methods: A 24-week, open-label study was designed to assess the efficacy and safety of a ChEI, galantamine, in 50 patients with DLB. Results: This study showed beneficial effects with galantamine in 2 of the 3 primary efficacy parameters. The scores on the Neuropsychiatric Inventory (NPI-12) improved by 8.24 points from baseline (p = 0.01) especially in visual hallucinations and nighttime behaviors (p = 0.004). The scores on the Clinician's Global Impression of Change improved by 0.5 points from baseline (p = 0.01). The third primary efficacy parameter, the Cognitive Drug R...

2007-01-01

378

Corrosion: Understanding the basics

Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity

This new book presents a practical how to approach to understanding and solving the problems of corrosion of structural materials. Although it is written mainly for those having a limited technical background in corrosion, it also provides more experienced engineers with a useful overview of the principles of corrosion and can be used as a general guide for developing a corrosion-control program. Contents include: the effects and economic impact of corrosion; basic concepts important to corrosion; principles of aqueous corrosion; forms of corrosion: recognition and prevention; types of corrosive environments; corrosion characteristics of structural materials; corrosion control by proper design; corrosion control by materials selection; corrosion control by protective coatings and inhibitors; corrosion control by cathodic and anodic protection; corrosion testing and monitoring; techniques for diagnosis of corrosion failures; and glossary of corrosion-related terms.

2000-07-01

379

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...

2008-01-01

380

Considerations referring to chemical descaling of filmed carbon steels

Cleaning steam generators off-line (soaking) with chelants. Final report. [PWR

Under operational conditions in nuclear power plants, the carbon steel components of the primary and secondary circuits react with high temperature cooling agent forming several iron oxides and oxyhydroxides. These deposits can result in tubes' constrictions, pitting and intergranular corrosion and finally to heat transfer reducing and increasing of radiation fields around the circuits, as well. The descaling process involves the chemical dissolution of the corrosion deposits by means of diluted organic acidic solutions containing usually a carboxylic acid, a reductant and one or more corrosion inhibitors. To evaluate the removing rates of these superficial films two types of methods were used, the gravimetric and potentiodynamic techniques. By correlating the experimental results, we established the chemical composition of descaling solution and two models of mechanisms applicable to our specific conditions. (authors)

2009-10-12

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381

Cleaning steam generators off-line (soaking) with chelants. Final report

This report discusses the work done on EPRI program S149-1. In this program the feasibility of cleaning steam generators off line with organic chelants as a means of arresting denting corrosion was investigated. The rationale behind this program is to make use of those periods during which nuclear steam generators are in cold shutdown or wet layup to carry out a low-temperature soak with a combined chelant-inhibitor solution in order to dissolve some of the magnetite which has built up in crevices and to concomitantly remove entrained corrodents such as chloride ion. It was hoped that these soaks would be effective in reducing carbon steel support plate corrosion which produces tube denting.

1983-02-01

382

Beyond Acid Suppression: New Pharmacologic Approaches for Treatment of GERD

This report discusses the work done on EPRI program S149-1. In this program the feasibility of cleaning steam generators off line with organic chelants as a means of arresting denting corrosion was investigated. The rationale behind this program is to make use of those periods during which nuclear steam generators are in cold shutdown or wet layup to carry out a low-temperature soak with a combined chelant-inhibitor solution in order to dissolve some of the magnetite which has built up in crevices and to concomitantly remove entrained corrodents such as chloride ion. It was hoped that these soaks would be effective in reducing carbon steel support plate corrosion which produces tube denting.

383

British Library Electronic Table of Contents (United Kingdom)

Proton pump inhibitors are highly successful in treating gastroesophageal reflux disease, but a significant proportion of patients have persistent symptoms from weakly or nonacidic reflux. Transient lower esophageal sphincter relaxation (TLESR) represents the dominant mechanism of gastroesophageal reflux and has therefore become the most intensely investigated therapeutic target. The triggering of TLESR involve the vagal pathways and the ?-aminobutyric type B (GABA(B)) and metabotropic glutamate type 5 (mGluR5) receptors. Baclofen is a GABA(B) receptor agonist that is effective in inhibiting TLESR and reducing the number of reflux episodes, but is associated with significant central nervous system (CNS) side effects. The newer GABA(B) agonists, such as AZD9343 and AZD3355, and mGluR5 antag...

2010-01-01

384

Assuring both quality and creativity in basic research

Application of zeolite-based catalyst to hydrocracking of coal-derived liquids

How does one assure that both quality and creativity are obtained in basic research environments QA theoreticians have attempted to develop workable definitions of quality, but in more reflective moments, these definitions often fail to capture the deeper essence of the idea of quality.'' This paper asserts that creativity (as a product of the human mind) is a concrete interface between perfunctory definitions of quality (conformance to specifications) and more philosophical speculations about the nature of quality- related ultimates'' like elegance or beauty. In addition, we describe the distinction between creative ideas and creative acts and highlight one of the major inhibitors of creativity, fear. Finally we show that highly creative people often have an irreverent attitude toward boundaries and established authority, and discuss how one can allow for this when designing a QA program in a basic research environment.

1990-04-12

385

Antioxidant activity in banana peel extracts: Testing extraction conditions and related bioactive compounds

Y-zeolite supported catalysts were applied to the hydrocracking of coal-derived liquids. By the introduction of two-stage upgrading consisting of hydrotreating and hydrocracking, Wandoan coal-derived middle distillate was hydrocracked over Ni-Mo/Y-zeolite, producing a high gasoline fraction yield. Zeolite supported catalysts gave little hydrocracked compounds in the hydroprocessing of coal-derived heavy oils, even after hydrotreatment. The reaction inhibitors which seriously poison the active sites of zeolites were found to be small nitrogen-containing molecules. In the hydroprocessing of coal-derived heavy oils, zeolite supported catalysts were inferior to alumina supported catalysts. This is due to the high hydrocracking but low hydrogenation activity of zeolite supported catalysts. 22 refs., 5 figs., 11 tabs.

1990-06-01

386

British Library Electronic Table of Contents (United Kingdom)

Banana (Musa acuminata Colla AAA) peel extracts obtained in this work had a high capacity to scavenge 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2prime-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS+) free radicals, and they were also good lipid peroxidation inhibitors. Acetone:water extracts were considerably more effective (compared with methanol, ethanol, acetone, water, methanol:water or ethanol:water) at inhibiting the peroxidation of lipids in the b-carotene/linoleic acid system or scavenging free radicals. However, aqueous extracts had a high capacity to protect lipids from oxidation in the thiobarbituric acid reactive substances (TBARS) test, as well as in the b-carotene bleaching assay. In addition, acetone:water most efficiently extracted all extractable components (54+-...

2010-01-01

387

Amine treatment and activated charcoal

Absorption of carbon dioxide in waste tanks

Alkanol-amine is used for removing hydrogen sulfide and carbon dioxide from the gas stream. Contaminated amine is the amine which is contaminated by hydrocarbon, organic acid or iron sulfide, etc.. In addition, in the case when an antifoaming agent is excessively added to it or when it is decomposed chemically or thermally, it is considered that it is contaminated. When an amine solution becomes contaminated, several problems concerning operation control occur which would influence the effect of the amine treatment in consequence. By using activated charcoal, it is possible to decrease the additional amount of the antifoaming agent or corrosion inhibitor. This is because activated charcoal removes the decomposed product which causes the foaming phenomenon. In order to derive economical profit sufficiently, an activated charcoal system properly designed is necessary. In this article, the CALGON CLEANAMINE SYSTEM of Calgon Co. is introduced which restores the effect ...

1988-10-01

388

A phase II trial of sorafenib in first-line metastatic urothelial cancer: a study of the PMH Phase II Consortium

Air flow rates and carbon dioxide concentrations of air entering and exiting eight H-Area waste tanks were monitored for a period of one year. The average instanteous concentration of carbon dioxide in air is within the range reported offsite, and therefore is not affect by operation of the coal-fired power plant adjacent to the tank farm. Waste solutions in each of the tanks were observed to be continuously absorbing carbon dioxide. The rate of absorption of carbon dioxide decreased linearly with the pH of the solution. Personnel exposure associated with the routine sampling and analysis of radioactive wastes stored at SRP to determine the levels of corrosion inhibitors in solution could be reduced by monitoring the absorption of carbon dioxide and using the relationship between pH and carbon dioxide absorption to determine the free hydroxide concentration in solution.

1987-09-01

389

British Library Electronic Table of Contents (United Kingdom)

Summary Background Sorafenib is an oral multikinase inhibitor that blocks cell proliferation via the ERK pathway and angiogenesis via the VEGF pathway. This phase II trial was conducted to determine the efficacy and tolerability of sorafenib for the treatment of patients with metastatic urothelial cancer (UC) who had not had prior chemotherapy for advanced disease. Patients and Methods Seventeen chemo-na?ve UC patients with adequate performance status and organ function were treated with sorafenib 400?mg twice daily on a continuous basis until progression or unacceptable toxicity. The primary endpoint was objective tumor response rate as measured by RECIST criteria. Secondary endpoints included rate of prolonged stable disease (>3?months), time to progression, median and 1?yr survival and ...

2011-01-01

390

A new approach to fabrication of gradient WC-Co hardmetals

British Library Electronic Table of Contents (United Kingdom)

WC-Co hardmetals with gradient structure comprising neither -phase nor grain growth inhibitors were produced for the first time by regulating the WC re-crystallisation and carbon content in their near-surface layer and core. Hardmetals with low Co contents in the surface region were obtained by selective carburisation of the near-surface zone of green articles with the original low carbon content and their consequent liquid-phase sintering. The surface region of such gradient hardmetals has a hardness of up 150 Vickers units higher and fracture toughness significantly superior than those of the core. Gradient hardmetals with high Co contents in the surface region were obtained by selective decarburisation of the near-surface zone of green articles with the original high carbon content and ...

2010-01-01

391

5,8,11,14-Eicosatetraynoic acid-induced destruction of mitochondria in human prostate cells (PC-3).

The role of the HCR system in the repair of lethal lesions of Bacillus subtilis phages and their transfecting DNA damaged by radiation and alkylating agents

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.

1992-01-01

392

The role of the HCR system in the repair of prelethal lesions induced by UV light, #gamma# radiation and alkylating agents was studied in the Bacillus subtilis SPP1 phage, its heat sensitive mutants (N3, N73 nad ts_1) and corresponding infectious DNA. The survival of phages and their transfecting DNA after treatment with UV light is substantially higher in hcr"+ cells than in hcr cells, the differences being more striking in intact phages than in their transfecting DNA's. Repair inhibitors reduce survival in hcr"+ cells: caffeine lowers the survival of UV-irradiated phage SPP1 in exponentially growing hcr"+ cells but has no effect on its survival in competent hcr"+ cells; acriflavin and ethidium bromide decrease the survival of the UV-irradiated SPP1 phage in both exponentially growing and competent hcr"+ cells to the level of survival observed in hcr cells; moreover, ethidium bromide lowers the number of infective centres in hcr"+ cells of the UV-irradiated DNA of ...

393

Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening.

The IRG protein Irgm3 preserves cell survival during coxsackievirus B3 (CVB3) infection. However, the molecular mechanisms are not clear. Here, we examined the effect of Irgm3 expression on ER stress triggered by pharmacological agents or CVB3 infection. In Tet-On/Irgm3 HeLa cells, Irgm3 expression suppressed either chemical- or CVB3-induced upregulation of glucose-regulated protein78. Further, Irgm3 strongly inhibited the activation of both the PERK and ATF6 pathways of ER stress responses, which further led to the diminished phosphorylation of eIF2?, reduced cleavage/activation of transcription factor SREBP1 and attenuated induction of proapoptotic genes CHOP and GADD34. These data were further supported by experiments using Irgm3 knockout mouse embryonic fibroblasts, in which the ER stress induced by CVB3 was not relieved due to the lack of Irgm3 expression. In addition, the tunicamycin-triggered ER stress promoted the subsequent CVB3 infection. The effect of Irgm3 on ER stress and ...

2011-10-10

394

Modulation of the intestinal response to ionizing radiation by anticoagulant and non-anticoagulant heparins.

The steroidogenic factor 1 (SF-1, also known as NR5A1) is a transcription factor belonging to the nuclear receptor superfamily. Whereas most of the members of this family have been extensively characterized, the therapeutic potential and pharmacology of SF-1 still remains elusive. Described here is the identification and characterization of selective inhibitory chemical probes of SF-1 by a rational ultra-high-throughput screening (uHTS) strategy. A set of 64,908 compounds from the National Institute of Health's Molecular Libraries Small Molecule Repository was screened in a transactivation cell-based assay employing a chimeric SF-1 construct. Two analogous isoquinolinones, ethyl 2-[2-[2-(2,3-dihydro-1,4-benzodioxin-7-ylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate (SID7969543) and ethyl 2-[2-[2-(1,3-benzodioxol-5-ylmethylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate and (SID7970631), were identified as potent submicromolar inhibitors, yielding ...

2008-03-11

395

In vitro comparison of rat and chicken brain neurotoxic esterase

Endothelial dysfunction is involved in radiation responses in many normal tissues, including intestine. Endothelium-directed interventions ameliorate intestinal radiation injury (radiation enteropathy) in animal models, and anecdotal reports also suggest a beneficial effect of heparin. This study assessed low molecular weight heparin as an intestinal radiation response modifier. Rats underwent localized small bowel irradiation. Groups of rats were treated with saline, nadroparin (3 mg/kg/d), or a non-anticoagulant heparin (SR80258, 3 mg/kg/d), from 3 days before to 2 weeks after irradiation. The intestinal radiation response was assessed 2 weeks and 6 weeks after irradiation using quantitative histology; morphometry, and cellular and molecular end-points. Compared to vehicle-treated controls, nadroparin significantly exacerbated structural radiation injury, neutrophil infiltration, and TGFbeta and collagen I immunoreactivity levels 2 weeks after irradiation. SR80258 was associated with ...

2005-11-01

396

Extracellular Protein Disulfide Isomerase Regulates Feedback Activation of Platelet Thrombin Generation Via Modulation of Coagulation Factor Binding.

A systematic comparison was undertaken to characterize neurotoxic esterase (NTE) from rat and chicken brain in terms of inhibitor sensitivities, pH optima, and molecular weights. Paraoxon titration of phenyl valerate (PV)-hydrolyzing carboxylesterases showed that rat esterases were more sensitive than chicken to paraoxon inhibition at concentrations less than or equal to microM and superimposable with chicken esterases at concentrations of 2.5-1000 microM. Mipafox titration of the paraoxon-resistant esterases at a fixed paraoxon concentration of 100 microM (mipafox concentration: 0-1000 microM) resulted in a mipafox I50 of 7.3 microM for chicken brain NTE and 11.6 microM for rat brain NTE. NTE (i.e., paraoxon-resistant, mipafox-sensitive esterase activity) comprised 80% of chicken and 60% of rat brain paraoxon-resistant activity with the specific activity of chicken brain NTE approximately twice that of rat brain NTE. The pH maxima for NTE from both species was ...

1986-04-01

397

Effect of some physical treatments on anti nutritional factors and fatty acids composition of Vicia faba L. seeds

Background: Protein disulfide isomerase (PDI) controls platelet integrin function, tissue-factor (TF) activation, and concentrates at fibrin and thrombus formation sites of vascular injury. Objective: We investigated involvement of surface thiol isomerases and especially PDI, in thrombin-mediated thrombin amplification on human platelets. Methods/Results: Using a new developed thrombin-dependent platelet thrombin generation assay we observed that the feedback activation of thrombin generation on the platelet surface does not depend on TF, as anti-TF antibodies inhibiting TF-induced thrombin formation in platelet-depleted plasma had no effect compared to vehicle-treated controls. Feedback activation of thrombin generation in the presence of platelets was significantly diminished by membrane impermeant thiol blockers or by the thiol isomerase-inhibitors bacitracin and anti-PDI antibody RL90, respectively. Platelet thrombin formation depends on binding of coagulation ...

2011-09-19

398

Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers.

This study was carried out to evaluate the effects of irradiation (gamma irradiation at dose levels of 0.0, 2.5, 5.0, 10.0 or 20.0 kGy, He-Ne and their combination) on nutritive characteristics of Vicia faba L. seeds (Giza 843). Analyses included levels of anti-nutrients (total phenolic compounds, tannins, phytic acid, trypsin inhibitor and vicine), chemical composition (sugars, crude proteins, fat, dry matter and ash) and fatty acids profile. All treatments caused significant (P<0.05) decreases in the antinutrational factors under investigation. The reduction in the content of tannins and phenolic compounds were more pronounced with He-Ne alone or He-Ne in combination with gamma irradiation. At dose levels 10.0 and 20.0 kGy without or with combination of He-Ne were more efficiency in the reduction of phytic acid content by 24.3, 32.8, 34.5 and 45.5 %, respectively. Also, for trypsin inhibitor activity, the maximum inhibition was observed ...

399

Dendroaspis natriuretic peptide and the designer natriuretic peptide, CD-NP, are resistant to proteolytic inactivation.

Vildagliptin is a potent and selective dipeptidyl peptidase IV inhibitor in development for the treatment of type 2 diabetes that improves glycemic control by enhancing alpha- and beta-cell responsiveness to glucose. Two open-label, single-dose, randomized, crossover studies in healthy subjects (ages 18-45 years) investigated the dose proportionality of vildagliptin pharmacokinetics (n = 20) and the effect of food (n = 24) on vildagliptin pharmacokinetics. There was a linear relationship (r(2) = 0.999) between vildagliptin doses of 25, 50, 100, and 200 mg and area under the plasma concentration-time curve from time zero to infinity (AUC(0-infinity)) and maximum plasma concentration (C(max)). Dose proportionality was assessed using a statistical power model [X = alpha x (dose)(beta)]. The 90% confidence intervals of the proportionality coefficient, beta, for AUC(0-infinity) (1.15-1.19) and C(max) (1.04-1.14) indicated that deviations from dose proportionality were ...

2007-07-26

400

Chemopreventive effects of Furan-2-yl-3-pyridin-2-yl-propenone against 7,12-dimethylbenz[a]anthracene-inducible genotoxicity

Designer natriuretic peptides (NPs) represent an active area of drug development. In canine and human studies, the designer natriuretic peptide CD-NP demonstrated more desirable therapeutic potential than recombinant B-type NP (BNP), which is known as nesiritide and is approved for treatment of acute decompensated heart failure. However, why CD-NP is more effective than BNP is not known. We previously reported that CD-NP is a poorer activator of human guanylyl cyclase-A (GC-A) and a better activator of human guanylyl cyclase-B than BNP. Here, guanylyl cyclase bioassays were used to compare the susceptibility of CD-NP verses ANP, BNP, CNP and DNP to inactivation by human kidney membranes. The half time (t(1/2)) for CD-NP inactivation was increased by factors of 13, 3 and 4 compared to ANP, BNP and CNP, respectively, when measured in the same assay. Surprisingly, DNP failed to undergo complete inactivation and was the most degradation resistant of the peptides tested. The neutral ...

2011-04-01

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401

Biocide and corrosion inhibition use in the oil and gas industry: Effectiveness and potential environmental impacts

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 and enzymatic ...

2008-05-01

402

B chain is a functional subunit of beta-bungarotoxin for inducing apoptotic death of human neuroblastoma SK-N-SH cells.

Treatment chemicals are used in all facets of the natural gas industry (NGI) from well development through transmission and storage of natural gas. The multitude of chemicals used, combined with the dozens of chemical manufacturers and/or suppliers has lead to the availability of hundreds of possible chemical products. Because of the widespread use of chemical products and their numerous sources, the NGI needs access to consistent data regarding their effectiveness and potential environmental impacts. The objective of this work was to evaluate the effectiveness and potential environmental impacts of, chemical products used in the NGI. This assessment was initially focused on biocides and corrosion inhibitors and their use in the gas production, storage and transmission facilities, The overall approach was obtain the necessary data on chemical use and effectiveness directly from the oil and gas industry, supplemented with data/information obtained from the published ...

1995-03-27

403

A?(1-42) Aggregates into non-Toxic Amyloid Assemblies in the Presence of the Natural Polyphenol Oleuropein Aglycon.

beta-Bungarotoxin (beta-Bgt), a presynaptic phospholipase A(2) (PLA(2)) neurotoxin isolated from the venom of Bungarus multicinctus, consists of A chain and B chain. The goal of the present study is to explore the functional contribution of the two subunits to the toxicity of beta-Bgt. beta-Bgt was found to induce apoptotic death of SK-N-SH cells via elevating intracellular Ca(2+) and intracellular ROS production. Moreover, an activation of p38 MAPK was associated with the cytotoxicity of beta-Bgt. SB202190 (p38 MAPK inhibitor), N-acetylcysteine (antioxidant reagent), 1,2-bis(2-aminophenoxy)ethane-N,N,N,N-tetraacetic acid (BAPTA) (Ca(2+) chelator) and the inhibitors of Ca(2+) release from intracellular depots (ruthenium red and 2-aminoethoxydiphenyl borate) effectively attenuated the cytotoxicity of beta-Bgt. In sharp contrast to the inability of A chain, B chain was able to induce cytotoxic effects on SK-N-SH cells as beta-Bgt did. Abolishment ...

2007-10-13

404

A laboratory and field investigation of naphthenic acid corrosion inhibition

Amyloid aggregation starts with the initial misfolding of peptide/protein precursors, with subsequent structural rearrangement into oligomers and protofibrils; the latter eventually organize into fibrils with shared basic structural features, found deposited in amyloid diseases. Mounting evidence indicates early oligomers as the most toxic amyloid species; accordingly, the search of inhibitors of their growth is considered a promising target to prevent amyloid toxicity. We recently showed that oleuropein aglycon, a polyphenol abundant in the extra virgin olive oil, interferes with the aggregation of amylin (involved in type-2 diabetes), eliminating its cytotoxicity. Here we report that oleuropein aglycon also hinders amyloid aggregation of A?(1-42) and its cytotoxicity, suggesting a general effect of such polyphenol. In particular, by using a wide panel of different spectroscopic, immunologic, cell viability and imaging techniques we provide a more detailed ...

2011-05-18

405

p73 protein regulates DNA damage repair.

This paper presents results of a laboratory and field study of naphthenic acid corrosion and the development of an effective chemical inhibitor for this type of corrosive attack. In the laboratory corrosion test, which involved 20 hour weight loss measurements in high flash solvent with a total acid number (TAN) of 16 mg KOH/gm at a temperature of 600 F (316 C), blank corrosion rates averaged 140 to 150 mpy (3.56 to 3.81 mm/y). Inhibited rates averaged about 10 to 12 mpy (0.254 to 0.305 mm/y). The field test was carried out on a heavy vacuum gas oil (HVGO) stream at 550 F (288 C) . Blanks varied from a high of 425 mpy (10.79 mm/y) for a 24 hour test to a low of about 100 mpy (2.54 mm/y) for a 150 hour test. Both electrical resistance (ER) probes and weight loss coupons showed corrosion rates below 5 mpy (0.127 mm/y) as long as they were adequately passivated. Passivation consisted of exposing the coupons to a high inhibitor dosage for a ...

1995-11-01

406

Tyrosine phosphorylation of a 66KD soluble protein and augmentation of lectin induced mitogenesis by DMSO in human T lymphocytes

Although the p53 tumor suppressor is relatively well characterized, much less is known about the functions of other members of the p53 family, p73 and p63. Here, we present evidence that in specific pathological conditions caused by exposure of normal cells to bile acids in acidic conditions, p73 protein plays the predominant role in the DNA damage response. These pathological conditions frequently occur during gastric reflux in the human esophagus and are associated with progression to esophageal adenocarcinoma. We found that despite strong DNA damage induced by bile acid exposure, only p73 (but not p53 and p63) is selectively activated in a c-Abl kinase-dependent manner. The activated p73 protein induces DNA damage repair. Using a human DNA repair PCR array, we identified multiple DNA repair genes affected by p73. Two glycosylases involved in base excision repair, SMUG1 and MUTYH, were characterized and found to be transcriptionally regulated by p73 in DNA damage ...

2011-09-01

407

The effect of phytic acid on the levels of blood glucose and some enzymes of carbohydrate and lipid metabolism.

The authors have demonstrated that induction of mitogenesis in human T lymphocytes is associated with the tyrosine phosphorylation of a 66KD soluble substrate-TPP 66. Since DMSO has been shown to be a non-specific stimulator of tyrosine protein kinases they have examined the effect of DMSO on both activation and tyrosine phosphorylation in human T cells. Human peripheral blood T lymphocytes were isolated by dextran sedimentation, Ficol/Paque centrifugation and nylon wool filtration. Phosphorylation was performed in cells incubated with ["3"2P] orthophosphate followed by DMSO for 30 min. TPP 66 was identified by 2-D PAGE, autoradiography, and HV electrophoresis of the hydrolyzed protein. Concentrations of DMSO from 1% to 50% induced the tyrosine phosphorylation of TPP 66 with maximal stimulation seen at 20%. DMSO alone did not activate the T cells (measured by ["3H] thymidine incorporation) when tested at high concentrations for 30 sec to 10 min. (longer incubations ...

1986-04-13

408

Natriuretic peptides in vascular physiology and pathology.

In this study, six groups of rats were fed as follows: Groups 1 and 2 were fed formulated diets supplemented with zinc or without zinc respectively. Groups 3 and 4 were fed formulated diets supplemented with zinc plus phytic acid extracted from sweet potato (Ipomea batatas) or commercial phytic acid respectively. Groups 5 and 6 were fed formulated diets supplemented with phytic acid extract from sweet potato or commercial phytic acid respectively. The animals were fed for three weeks and then sacrificed The activities of key enzymes of carbohydrate and lipid metabolism as well as transaminases in the liver were determined. Blood glucose level was also assessed. Phytic acid extract consumption from sweet potato and commercial phytic acid plus zinc supplement lowered blood glucose levels. There was no significant change in the activity of 6-phosphogluconate dehydrogenase among the groups. Similarly, phytic acid supplementation showed no significant decrease in the activity of pyruvate ...

2005-03-01

409

Molecular characterization of the Spirometra mansonoides genome: renaturation kinetics, methylation, and hybridization to human cDNA probes.

Four major natriuretic peptides have been isolated: atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), C-type natriuretic peptide (CNP), and Dendroaspis-type natriuretic peptide (DNP). Natriuretic peptides play an important role in the regulation of cardiovascular homeostasis maintaining blood pressure and extracellular fluid volume. The classical endocrine effects of natriuretic peptides to modulate fluid and electrolyte balance and vascular smooth muscle tone are complemented by autocrine and paracrine actions that include regulation of coronary blood flow and, therefore, myocardial perfusion; modulation of proliferative responses during myocardial and vascular remodeling; and cytoprotective anti-ischemic effects. The actions of natriuretic peptides are mediated by the specific binding of these peptides to three cell surface receptors: type A natriuretic peptide receptor (NPR-A), type B natriuretic peptide receptor (NPR-B), and type C natriuretic peptide receptor ...

2008-01-01

410

Missense mutations in the growth hormone receptor dimerization region in Laron syndrome

High molecular weight DNA from pleroceroid larvae of the tapeworm Spirometra mansonoides was purified from isolated nuclei by conventional techniques. The DNA so isolated has a melting temperature (Tm) of 87 degrees C and a guanine plus cytosine (G/C) content of 44%. 5-Methyl cytosine could not be detected in plerocercoid DNA by HPLC analysis of DNA hydrolysates, by radiolabeling 5'-termini of MspI digests with polynucleotide kinase, or by comparing restriction patterns generated by MspI and HpaII. Renaturation kinetics demonstrated that the genome of S. mansonoides contains repetitive as well as single copy sequences and has a genome size estimated at approx. 1.6 X 10(9) bp. Hybridization was carried out between plerocercoid DNA and cDNAs for human beta-actin, alpha-tubulin and growth hormone (hGH). Rationale for this analysis was based on known homologies among actin and tubulin genes in numerous species and on apparent similarities between hGH and a plerocercoid ...

1990-06-21

411

Genome analysis of F. nucleatum sub spp vincentii and its comparison with the genome of F. nucleatum ATCC 25586.

Laron syndrome (LS) is an autosomal recessively inherited condition characterized by insensitivity to endogenous and exogenous GH. Affected individuals have severe episodes and other characteristic features. GH receptor gene mutations are present in all affected individuals in whom molecular studies have been reported. The GH receptor is a plasma membrane-spanning protein in which the extracellular domain binds circulating GH and the intracellular domain interacts with the JAK-2 kinase and possibly other intracellular signaling molecules. GH receptor dimerization occurs on GH binding and is thought to be required for normal signal transduction. We have studied the GH receptor genes of four unrelated individuals affected with LS from the United States, Italy, Saudi Arabia, and India. We have identified four different missense mutations that alter consecutive amino acids 152 to 155 in or near the dimerization domain of the GH receptor. One of these mutations, D152H, ...

1994-09-01

412

Gene Repressive Activity of RIP140 Through Direct Interaction with CDK8.

We present the draft genome sequence and its analysis for Fusobacterium nucleatum sub spp. vincentii (FNV), and compare that genome with F. nucleatum ATCC 25586 (FN). A total of 441 FNV open reading frames (ORFs) with no orthologs in FN have been identified. Of these, 118 ORFs have no known function and are unique to FNV, whereas 323 ORFs have functional orthologs in other organisms. In addition to the excretion of butyrate, H2S and ammonia-like FN, FNV has the additional capability to excrete lactate and aminobutyrate. Unlike FN, FNV is likely to incorporate galactopyranose, galacturonate, and sialic acid into its O-antigen. It appears to transport ferrous iron by an anaerobic ferrous transporter. Genes for eukaryotic type serine/threonine kinase and phosphatase, transpeptidase E-transglycosylase Pbp1A are found in FNV but not in FN. Unique ABC transporters, cryptic phages, and three types of restriction-modification systems have been identified in FNV. ORFs for ...

2003-06-01

413

Expression and function of fibroblast growth factor (FGF) 9 in hepatic stellate cells and its role in toxic liver injury

Receptor interacting protein 140 (RIP140) is a coregulator for numerous nuclear receptors and transcription factors and primarily exerts gene-repressive activities on various target genes. We previously identified a spectrum of posttranslational modifications on RIP140 that augment its property and biological activity. In T(3)-triggered biphasic regulation of cellular retinoic acid binding protein 1 (Crabp1) gene along the course of fibroblast-adipocyte differentiation, we found TRAP220(MED1) critical for T(3)-activated chromatin remodeling whereas RIP140 essential for T(3)-repressive chromatin remodeling of this gene promoter. In this current study, we aim to examine whether and how RIP140 replaces TRAP220(MED1) on the CrabpI promoter in differentiating adipocyte cultures. We find increasing recruitment of RIP140 to this promoter, with corresponding reduction in TRAP220(MED1) recruitment during the T(3)-repressive phase. We also uncover direct interaction of RIP140 with ...

2011-08-25

414

Effects of low-intensity prolonged exercise on PGC-1 mRNA expression in rat epitrochlearis muscle.

Hepatic injury and regeneration of the liver are associated with activation of hepatic stellate cells (HSC). Fibroblast growth factors (FGFs) and their receptors are important regulators of repair in various tissues. HSC express FGFR3IIIc as well as FGFGR4 and different spliced FGFR1IIIc and FGFR2IIIc isoforms which differ in the presence or absence of the acid box and of the first Ig-like domain. Expression of FGF9, known to be capable to activate the HSC FGFR2/3-isoforms, was increased in HSC in liver slice cultures after exposition to carbon tetrachloride, as an acute liver injury model. FGF9 significantly stimulated 3-H thymidine incorporation of hepatocytes, but failed to induce DNA synthesis in HSC despite the fact that FGF9 induced a sustained activation of extracellular signal-related kinases (ERK) 1/2. FGF9 induced an increased phosphorylation of Tyr436 of the fibroblast growth factor receptor substrate (FRS) 2, while phosphorylation of Tyr196 which is ...

2007-09-21

415

A human breast cell model of pre-invasive to invasive transition

We previously reported that the peroxisome proliferator-activated receptor gamma coactivator-1 (PGC-1) mRNA in rat epitrochlearis muscle was increased after swimming exercise training. In the present study, we demonstrated further that PGC-1 mRNA expression in the epitrochlearis muscle of 4-5-week-old male Sprague-Dawley rats was increased after a 6-h acute bout of low-intensity swimming exercise. With this increase, the expression level was approximately 8-fold of control and immersion group rats that stayed for 6-h in warm water, maintained at the identical temperature of the swimming barrel (35 degrees C) (p<0.01). Second, PGC-1 mRNA expression in the muscle was found to have increased 6-h after 30 10-s tetani contractions were induced by in vitro electrical stimulation. Finally, PGC-1 mRNA expression in the muscle incubated for 18-h with 0.5mM 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR: a 5' AMP-activated protein kinase (AMPK) activator) was ...

2002-08-16

416

comparative study of the electrochemical behaviour of iron in alkaline media containing red mud and grey slurries. the effect of Al"3+

A crucial step in human breast cancer progression is the acquisition of invasiveness. There is a distinct lack of human cell culture models to study the transition from pre-invasive to invasive phenotype as it may occur 'spontaneously' in vivo. To delineate molecular alterations important for this transition, we isolated human breast epithelial cell lines that showed partial loss of tissue polarity in three-dimensional reconstituted-basement membrane cultures. These cells remained non-invasive; however, unlike their non-malignant counterparts, they exhibited a high propensity to acquire invasiveness through basement membrane in culture. The genomic aberrations and gene expression profiles of the cells in this model showed a high degree of similarity to primary breast tumor profiles. The xenograft tumors formed by the cell lines in three different microenvironments in nude mice displayed metaplastic phenotypes, including squamous and basal characteristics, with ...

2008-03-10

417

Vitamin C and a-naphthoflavone prevent estrogen-induced mammary tumors and decrease oxidative stress in female ACI rats

Red mud (RM) is the main by-product of the Bayer process for alumina extraction from bauxite, and grey slurries (GS) are generated during the granite rocks transformation processes. the huge volume of those wastes generated every year suppose a serious environmental problem. Recent works by our group demonstrate the efficiency of both types of muds as corrosion inhibitors for iron and steel in alkaline media containing chlorides. The elemental analysis of these slurried shows that Al"3+ is the main common element. Therefore, the aim of this paper is to study the effect of the soluble Al"3+ in the electrochemical behaviour of iron in alkaline media, in presence and absence of chlorides. The electrochemical study using Cyclic Voltammetry (CV) and Electrochemical Impedance Spectroscopy (EIS) together with surface analysis techniques allowed to conclude that Al"3+ blocks the surface of steel in alkaline media chloride increasing the steel resistance to chlorides ...

418

British Library Electronic Table of Contents (United Kingdom)

The mechanisms underlying the pathogenesis of estrogen-induced breast carcinogenesis remain unclear. The present study investigated the roles of estrogen metabolism and oxidative stress in estrogen-mediated mammary carcinogenesis in vivo. Female August Copenhagen Irish (ACI) rats were treated with 17b-estradiol (E2), the antioxidant vitamin C, the estrogen metabolic inhibitor a-naphthoflavone (ANF), or cotreated with E2 + vitamin C or E2 + ANF for up to 8 months. E2 (3 mg) was administered as an subcutaneous implant, ANF was given via diet (0.2%) and vitamin C (1%) was added to drinking water. At necropsy, breast tumor incidence in the E2, E2 + vitamin C and E2 + ANF groups was 82, 29 and 0%, respectively. Vitamin C and ANF attenuated E2-induced alterations in oxidative stress markers in b...

2009-01-01

419

Uptake and utilization of nutrients by developing kernels of Zea mays L

The structure of myostatin:follistatin 288: insights into receptor utilization and heparin binding

The mechanisms involved in amino acid and sugar uptake by developing maize kernels were investigated. In the pedicel region of maize kernel, the site of nutrient unloading from phloem terminals, amino acids are accumulated in considerable amounts and undergo significant interconversion. A wide spectrum of enzymatic activities involved in the metabolism of amino acids is observed in these tissues. Subsequently, amino acids are taken up by the endosperm tissue in processes which require energy and the presence of carrier proteins. Conversely, no evidence was found that energy and carriers are involved in sugar uptake. This process of sugar uptake is not inhibited by metabolic inhibitors and shows nonsaturable kinetics, but the uptake is pH-dependent. L-glucose is taken up at a significantly reduced rate in comparison to D-glucose uptake. Based on analysis of radioactivity distribution among sugar fractions after incubations of kernels with radiolabeled D-glucose, it ...

1987-01-01

420

The crystal structure Escherichia coli Spy.

Myostatin is a member of the transforming growth factor-{beta} (TGF-{beta}) family and a strong negative regulator of muscle growth. Here, we present the crystal structure of myostatin in complex with the antagonist follistatin 288 (Fst288). We find that the prehelix region of myostatin very closely resembles that of TGF-{beta} class members and that this region alone can be swapped into activin A to confer signalling through the non-canonical type I receptor Alk5. Furthermore, the N-terminal domain of Fst288 undergoes conformational rearrangements to bind myostatin and likely acts as a site of specificity for the antagonist. In addition, a unique continuous electropositive surface is created when myostatin binds Fst288, which significantly increases the affinity for heparin. This translates into stronger interactions with the cell surface and enhanced myostatin degradation in the presence of either Fst288 or Fst315. Overall, we have identified several characteristics unique to ...

2009-09-29

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

421

Synthesis of (Bi0.5Na0.5)TiO3 (BNT) and Pr doped BNT using the soft combustion technique and its properties

Escherichia coli spheroplast protein y (EcSpy) is a small periplasmic protein that is homologous with CpxP, an inhibitor of the extracytoplasmic stress response. Stress conditions such as spheroplast formation induce the expression of Spy via the Cpx or the Bae two-component systems in E. coli, though the function of Spy is unknown. Here, we report the crystal structure of EcSpy, which reveals a long kinked hairpin-like structure of four ?-helices that form an antiparallel dimer. The dimer contains a curved oval shape with a highly positively charged concave surface that may function as a ligand binding site. Sequence analysis reveals that Spy is highly conserved over the Enterobacteriaceae family. Notably, three conserved regions that contain identical residues and two LTxxQ motifs are placed at the horizontal end of the dimer structure, stabilizing the overall fold. CpxP also contains the conserved sequence motifs and has a predicted secondary structure similar ...

2010-11-01

422

British Library Electronic Table of Contents (United Kingdom)

In this work, bismuth sodium titanate (Bi0.5Na0.5)TiO3 (BNT) and praseodymium (Pr)-doped BNT were successfully produced using the soft combustion technique. The effects of Pr doping on stoichiometry, microstructure, density and dielectric properties were studied. Pure Pr-doped BNT was obtained in all samples containing 5, 10 and 20mol% Pr after calcination at 800^oC for 3h. The produced powders were then pressed into pellets and sintered at 1100^oC for 3h. The very similar ionic radii of Pr^3^+ with Bi^3^+ and Na^+ made it possible to substitute both Bi and Na. The crystallite size and grain size decreased with increasing Pr amount because Pr acted as grain growth inhibitor, both for calcined powders and for sintered pellets. Maximum density was obtained in 5mol% Pr-doped BNT, beyond which...

2011-01-01

423

Structural and morphology studies of praseodymium-doped bismuth titanate prepared using a wet chemical route

Structural and morphology studies of praseodymium-doped bismuth titanate prepared using a wet chemical route

Praseodymium-doped Bi{sub 4}Ti{sub 3}O{sub 12} (BIT) with various compositions of dopant, Pr (x = 0.5, 0.6, 0.7, 0.8) in Bi{sub 4-x}Pr{sub x}Ti{sub 3}O{sub 12} (BPT) were synthesized using a low temperature wet chemical technique. Powders calcined at 800 deg. C exhibit a single phase polycrystalline perovskite bismuth-layered structure. Randomly oriented plate-like structures were observed under Scanning Electron Microscope (SEM). A small amount of Pr doping (x = 0.5) resulted in dramatically reduced of grain size from 2 {mu}m to less than 50 nm in which Pr plays the role as a grain growth inhibitor. However, by increasing the composition of Pr, bigger grain size of up to 1 {mu}m was observed for x = 0.8 that was caused by diffusion of Pr in the perovskite structure. Dielectric properties showed that dielectric permittivity decreased with the addition of x = 0.50, and increasing with further addition of Pr. Dissipation factor (tan {delta}) followed the same trend ...

2009-05-05

424

Structural and morphology studies of praseodymium-doped bismuth titanate prepared using a wet chemical route

Praseodymium-doped Bi_4Ti_3O_1_2 (BIT) with various compositions of dopant, Pr (x = 0.5, 0.6, 0.7, 0.8) in Bi_4_-_xPr_xTi_3O_1_2 (BPT) were synthesized using a low temperature wet chemical technique. Powders calcined at 800 deg. C exhibit a single phase polycrystalline perovskite bismuth-layered structure. Randomly oriented plate-like structures were observed under Scanning Electron Microscope (SEM). A small amount of Pr doping (x = 0.5) resulted in dramatically reduced of grain size from 2 #mu#m to less than 50 nm in which Pr plays the role as a grain growth inhibitor. However, by increasing the composition of Pr, bigger grain size of up to 1 #mu#m was observed for x = 0.8 that was caused by diffusion of Pr in the perovskite structure. Dielectric properties showed that dielectric permittivity decreased with the addition of x = 0.50, and increasing with further addition of Pr. Dissipation factor (tan #delta#) followed the same trend as dielectric constant that was ...

2009-05-05

425

British Library Electronic Table of Contents (United Kingdom)

Praseodymium-doped Bi4Ti3O12 (BIT) with various compositions of dopant, Pr (x=0.5, 0.6, 0.7, 0.8) in Bi4-xPrxTi3O12 (BPT) were synthesized using a low temperature wet chemical technique. Powders calcined at 800degreeC exhibit a single phase polycrystalline perovskite bismuth-layered structure. Randomly oriented plate-like structures were observed under Scanning Electron Microscope (SEM). A small amount of Pr doping (x=0.5) resulted in dramatically reduced of grain size from 2mm to less than 50nm in which Pr plays the role as a grain growth inhibitor. However, by increasing the composition of Pr, bigger grain size of up to 1mm was observed for x=0.8 that was caused by diffusion of Pr in the perovskite structure. Dielectric properties showed that dielectric permittivity decreased with the ad...

2009-01-01

426

Structural and magnetic properties of barium-gadolinium hexaferrites

Structural and magnetic properties of barium-gadolinium hexaferrites

A series of Gd-substituted M-type barium hexaferrites has been prepared by the ceramic route, according to the formula (Ba{sub 1-x}Gd{sub x})O.5.25Fe{sub 2}O{sub 3} (x=0-0.30). XRD analysis revealed that all the samples present primarily an M-type structure. Samples x=0 and x=0.05 are single-phase. Hematite (Fe{sub 2}O{sub 3}) and GdFeO{sub 3} were detected in the remaining samples. Coercivity (H{sub c}) shows remarkably high values, {approx}293kA/m for x=0.20 and 0.30 with a maximum of 322kA/m for x=0.25. Specific saturation magnetization ({sigma}{sub sat}) of the samples presents a small increase up to x=0.10. The microstructure examination indicates that Gd may act as a grain growth inhibitor.

2007-03-15

427

Steam-generator dilute chemical-cleaning program. Steam-generator chemical-cleaning project. Annual report, program start through 1980

A series of Gd-substituted M-type barium hexaferrites has been prepared by the ceramic route, according to the formula (Ba_1_-_xGd_x)O.5.25Fe_2O_3 (x=0-0.30). XRD analysis revealed that all the samples present primarily an M-type structure. Samples x=0 and x=0.05 are single-phase. Hematite (Fe_2O_3) and GdFeO_3 were detected in the remaining samples. Coercivity (H_c) shows remarkably high values, #approx#293kA/m for x=0.20 and 0.30 with a maximum of 322kA/m for x=0.25. Specific saturation magnetization (#sigma#_s_a_t) of the samples presents a small increase up to x=0.10. The microstructure examination indicates that Gd may act as a grain growth inhibitor.

2007-03-01

428

Spark plasma sintered tantalum carbide: Effect of pressure and nano-boron carbide addition on microstructure and mechanical properties

Vertical U-tube steam generators in Pressurized Water Reactors (PWRs) operating an All Volatile Treatment (AVT) secondary chemistry have experienced corrosion problems, particularly denting and sludges. The studies reported evaluate the feasibility of using a low-concentration (0.5 wt%) chemical cleaning process to remove corrosion product deposits from steam generator surfaces and magnetite from tube-to-support plate crevices of PWR steam generators. The process potentially may be applied at schedule intervals, such as during normal refueling outages, to maintain a steam generator in clean operating condition. This report describes the results of testing to evaluate the effectiveness of several chelant acids for dissolving steam generator sludges and crevice magnetite. Corrosion of carbon steel by the chelant acids and the effects of various inhibitors are evaluated. The effectiveness of ion-exchange regeneration of several chelant-based solvents is also ...

429

British Library Electronic Table of Contents (United Kingdom)

TaC and TaC-1wt.% B4C powders were consolidated using spark plasma sintering (SPS) at 1850^oC and varying pressure of 100, 255 and 363MPa. The effect of pressure on the densification and grain size is evaluated. The role of nano-sized B4C as sintering aid and grain growth inhibitor is studied by means of XRD, SEM and high resolution TEM. Fully dense TaC samples were produced at a pressure of 255MPa and higher at 1850^oC. The increasing pressure also resulted in an increase in TaC grain size. Addition of B4C leads to an increase in the density of 100MPa sample from 89% to 97%. B4C nano-powder resists grain growth even at high pressure of 363MPa. The formation of TaB2/Carbon at TaC grain boundaries helps in pinning the grain boundary and inhibiting grain growth. The effect of B4C addition on...

2011-01-01

430

Spark plasma sintered tantalum carbide-carbon nanotube composite: Effect of pressure, carbon nanotube length and dispersion technique on microstructure and mechanical properties

British Library Electronic Table of Contents (United Kingdom)

TaC-4wt.% CNT composites were synthesized using spark plasma sintering. Two kinds of CNTs, having long (10-20mm) and short (1-3mm) length, were dispersed by wet chemistry and spray drying techniques respectively. Spark plasma sintering was carried out at 1850^oC at pressures of 100, 255 and 363MPa. Addition of CNTs leads to an increase in the density of 100MPa sample from 89% to 95%. Short CNTs are more effective in increasing the density of the composites whereas long CNTs are more effective grain growth inhibitors. The longer CNTs are more effective in increasing the fracture toughness and an increase up to 60% was observed for 363MPa sample. Hardness and elastic modulus are found to increase by 22% and 18% respectively for 100MPa samples by addition of long CNTs. Raman spectroscopy, SEM...

2011-01-01

431

Sintering of nano-sized WC-Co powders produced by a gas reduction-carburization process

Sintering of nano-sized WC-Co powders produced by a gas reduction-carburization process

Nanocrystalline cemented tungsten carbide has attracted considerable interests for use in cutting tool because of its superior mechanical properties. In this study, nano-sized powders of mixed WC and Co were prepared from attrition-milled oxides by a gas reduction-carburization process. The effects of compacting pressure, heating schedule, additional ball-milling, and the presence of a grain growth inhibitor on the sintering properties of the nano-sized WC-Co powders were examined. The grain size and phases in WC-Co alloy were clearly affected by compacting pressure. Because of the trapped gases and the lower melting point of the cobalt binder, when a compact of nano-sized WC-Co powder was sintered through a heating schedule with holding steps, the sintered alloy maintained the small size of WC grains without any {eta} phase. In addition, the additional ball-milling improved the microstructure and mechanical properties of the nano-sized WC-Co powder by producing a ...

2006-08-10

432

Selective metabolic stimulation of the subfornical organ and pituitary neural lobe by peripheral angiotensin II

Nanocrystalline cemented tungsten carbide has attracted considerable interests for use in cutting tool because of its superior mechanical properties. In this study, nano-sized powders of mixed WC and Co were prepared from attrition-milled oxides by a gas reduction-carburization process. The effects of compacting pressure, heating schedule, additional ball-milling, and the presence of a grain growth inhibitor on the sintering properties of the nano-sized WC-Co powders were examined. The grain size and phases in WC-Co alloy were clearly affected by compacting pressure. Because of the trapped gases and the lower melting point of the cobalt binder, when a compact of nano-sized WC-Co powder was sintered through a heating schedule with holding steps, the sintered alloy maintained the small size of WC grains without any #eta# phase. In addition, the additional ball-milling improved the microstructure and mechanical properties of the nano-sized WC-Co powder by producing a ...

2006-08-10

433

Role of the triple bond in acid corrosion inhibition

The subfornical organ is a major receptor area for one of the principal stimuli of thirst, the octapeptide, angiotensin II. In conscious water-sated rats, the authors examined the effects of intravenous infusion of angiotensin II on the rate of glucose utilization in the subfornical organ and in structures anatomically and functionally connected with it. Angiotensin II produced pressor and drinking responses and increased glucose utilization selectively in the subfornical organ and pituitary neural lobe and in no other brain structure. Treatment with the angiotensin II antagonist, sar1-leu8-angiotensin II, before intravenous administration of angiotensin II prevented metabolic stimulation of the subfornical organ and neural lobe. Captopril, an inhibitor of angiotensin-converting enzyme, reduced subfornical organ glucose metabolism to a level similar to that found in control animals. These results demonstrate that peripheral angiotensin II stimulates glucose ...

1985-01-01

434

Rapid toxicity testing based on mitochondrial respiratory activity

It is now over 30 yr since the original discovery was made that acetylenic compounds are effective in inhibiting the corrosion of iron in acid media. Since then, the industrial practice of oil-well acidizing has become well-established, with key acetylenic compounds such as propargyl alcohol, hexynol, and ethyl octynol assuming increasingly important roles. New and more stable triple-bonded compounds properly formulated and synergized with nitrogen compounds are expected to be used more extensively as temperature, stability, and performance requirements increase. An evaluation is made of the structural features which enhance or limit the corrosion performance of a given acetylenic. New data involving mixtures of acetylenics, hydrogen-bonded complexes, and the use of new nitrogen synergists are covered also. Tabular data at 200/sup 0/F approximate the more strenuous conditions of an oil-well acidizing job using N-80 tubing. The performance of such inhibitors as ...

1970-01-01

435

Radiation inactivation target size of rat adipocyte glucose transporters in the plasma membrane and intracellular pools

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 ...

1990-05-01

436

Quantification of antibiotic drug potency by a two-compartment radioassay of bacterial growth

The in situ assembly states of the glucose transport carrier protein in the plasma membrane and in the intracellular (microsomal) storage pool of rat adipocytes were assessed by studying radiation-induced inactivation of the D-glucose-sensitive cytochalasin B binding activities. High energy radiation inactivated the glucose-sensitive cytochalasin B binding of each of these membrane preparations by reducing the total number of the binding sites without affecting the dissociation constant. The reduction in total number of binding sites was analyzed as a function of radiation dose based on target theory, from which a radiation-sensitive mass (target size) was calculated. When the plasma membranes of insulin-treated adipocytes were used, a target size of approximately 58,000 daltons was obtained. For adipocyte microsomal membranes, we obtained target sizes of approximately 112,000 and 109,000 daltons prior to and after insulin treatment, respectively. In the case of microsomal membranes, ...

1987-06-15

437

Preparation, characterization and electrical properties of SnO{sub 2} based liquid petroleum gas sensor

The two-compartment radioassay for microbial kinetics based on continuous measurement of the {sup 14}CO{sub 2} released by bacterial metabolism of 14C-labeled substrate offers a valuable approach to testing the potency of antimicrobial drugs. By using a previously validated radioassay with gram-positive and gram-negative bacteria, a group of protein synthesis inhibitors was evaluated for their effect on microbial growth kinetics. All tested drugs induced changes in both the slopes and intercepts of the growth curves. An exponential growth model was applied to quantify the drug effect on the processes of bacterial {sup 14}CO{sub 2} liberation and cell generation. The response was measured in terms of a generation rate constant. A linear dependence of the generation rate constant on the dose of spectinomycin was observed with Escherichia coli. Sigmoidal-shaped curves were found in the assays of chloramphenicol and tetracycline. The implications of dose-response ...

1990-06-01

438

Preparation of a high-J sub c YBCO bulk superconductor by the platinum doped melt growth method

The present investigation deals with the fabrication of liquid petroleum gas (LPG) sensor based on semiconducting oxide SnO{sub 2}. The gas sensor elements have been prepared by conventional solid state route. Addition of noble metal sensitizer, palladium and grain growth inhibitor, aluminum silicate to the base material SnO{sub 2}, not only improved the sensitivity towards LPG but also the selectivity in the presence of CO and CH{sub 4} gases. Out of various sensor compositions, SnO{sub 2}:Al{sub 2}Si{sub 2}O{sub 7} (35 wt.%):Pd (1.5 wt.%) sintered at 800 C for 5 h has shown high sensitivity (0.97) towards LPG at an operating temperature of 350 C. Different characterization techniques have been employed, such as differential thermal analysis (DTA), surface area analyzer, X-ray diffraction (XRD), to study the formation of SnO{sub 2}, surface area and crystallite size, respectively. The results suggested the possibility of utilizing the sensor element for the ...

1999-03-25

439

Preparation and photocatalytic property of pyrochlore Bi{sub 2}Ti{sub 2}O{sub 7} and (Bi, La) {sub 2}Ti{sub 2}O{sub 7} films

Recently we have found a highly effective additive for the melt growth processings attaining high critical currents in YBCO superconductor. It is platinum and it behaves as an effective grain growth inhibitor for the Y{sub 2}BaCuO{sub 5} phase. Even with less than 1 wt.% doping, Y{sub 2}BaCuO{sub 5} particles becomes less than one micron in size and distribute themselves to become homogeneously embedded in the large grown YBa{sub 2}Cu{sub 3}O{sub y} grains. The sample shows large magnetic hysteresis and a typical J{sub c} value estimated by using Bean's model critical state model is 18000 A/cm{sup 2} at 77 K and 1 T. We found that rhodium has a similar remarkable effect. (orig.).

1991-06-15

440

Potential for erosion corrosion of SRS high level waste tanks

Dopant-free Bi{sub 2}Ti{sub 2}O{sub 7} thin films with pyrochlore structure and La-doped bismuth titanate thin films have been fabricated by means of chemical solution decomposition, and characterized by X-ray diffraction, atomic force microscopy, scanning electron microscopy and UV-Vis spectrophotometry in this study. Their photocatalytic activities have been evaluated by photodegrading methyl orange solution, and the optimum processing parameters for the highest photocatalytic activity have been found. Moreover, the effects of La-doping on the phase transformation and the photocalalytic activity have been studied. It has been deduced from the experiment result that substituted La{sup 3+} ions can act as a stabilizer of Aurivillus phase BLT and a grain-growth inhibitor in BLT thin films.

2008-11-28

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

441

Possible preparation of wood-plastic materials based on unsaturated polyester resins and methyl metacrylate, by radiation and chemical methods in combination

SRS high-level radioactive waste tanks will not experience erosion corrosion to any significant degree during slurry pump operations. Erosion corrosion in carbon steel structures at reported pump discharge velocities is dominated by electrochemical (corrosion) processes. Interruption of those processes, as by the addition of corrosion inhibitors, sharply reduces the rate of metal loss from erosion corrosion. The well-inhibited SRS waste tanks have a near-zero general corrosion rate, and therefore will be essentially immune to erosion corrosion. The experimental data on carbon steel erosion corrosion most relevant to SRS operations was obtained at the Hanford Site on simulated Purex waste. A metal loss rate of 2.4 mils per year was measured at a temperature of 102 C and a slurry velocity comparable to calculated SRS slurry velocities on ground specimens of the same carbon steel used in SRS waste tanks. Based on these data and the much lower expected temperatures, ...

1994-01-01

442

Possible preparation of wood-plastic materials based on unsaturated polyester resins and methyl metacrylate, by radiation and chemical methods in combination

The preparation of wood-plastic combinations (WPC) using combined methods for curing intermediate products and final products is described. In the first step, impregnated wood was irradiated using doses of 1 to 10 kGy in the presence of chemical initiators of polymerization. Thereafter, curing of this partly cured impregnating mixture was accomplished in the wood at elevated temperatures with the aid of chemical initiators of polymerization. Impregnation mixtures based on unsaturated polyester resins and methyl methacrylate, and the wood species European Beech (Fagus silvatica) and Black Alder (Alnus glutinosa) were used. The results indicate that this method of preparing WPC allows substantially lower radiation doses to be used, i.e., doses in the range of 1 to 2.5 kGy. These doses gelatinate the impregnation mixture in the wood so that the subsequent curing by chemical polymerization initiators proceeds without the impregnation mixture flowing out of the wood, and without forming ...

1982-04-01

443

Platelet thrombosis in cardiac-valve prostheses

The preparation of wood-plastic combinations (WPC) using combined methods for curing intermediate products and final products is described. In the first step, impregnated wood was irradiated using doses of 1 to 10 kGy in the presence of chemical initiators of polymerization. Thereafter, curing of this partly cured impregnating mixture was accomplished in the wood at elevated temperatures with the aid of chemical initiators of polymerization. Impregnation mixtures based on unsaturated polyester resins and methyl methacrylate, and the wood species European Beech (Fagus silvatica) and Black Alder (Alnus glutinosa) were used. The results indicate that this method of preparing WPC allows substantially lower radiation doses to be used, i.e., doses in the range of 1 to 2.5 kGy. These doses gelatinate the impregnation mixture in the wood so that the subsequent curing by chemical polymerization initiators proceeds without the impregnation mixture flowing out of the wood, and without forming ...

1982-01-01

444

Pattern of anti-HIV dipyranocoumarin expression in callus cultures of Calophyllum inophyllum Linn.

The contribution of platelets and clotting factors in thrombosis on cardiovascular prostheses had been quantified with several tracers. Thrombus formation in vivo could be measured semiquantitatively in animal models and patients with indium-111, Technetium-99m labeled platelets, iodine-123, iodine-131 labeled fibrinogen, and In-111 and Tc-99m labeled antibody to the fibrinogen-receptor on the platelet- membrane, or fibrin. The early studies demonstrated that certain platelet-inhibitors, e.g. sulfinpyrazone, aspirin or aspirin- persantine increased platelet survival time with mechanical valves implanted in the baboon model and patients. Thrombus localization by imaging is possible for large thrombus on thrombogenic surface of prosthesis in the acute phase. The majority of thrombus was found in the sewing ring (Dacron) in the acute phase in both the mechanical and tissue valves. The amount of retained thrombus in both mechanical and tissue valves in our one-day ...

1989-06-08

445

British Library Electronic Table of Contents (United Kingdom)

Callus cultures of Calophyllum inophyllum were established using seed, nodal/ internodal and leaf explants on WPM basal medium supplemented with indole-3-butyric acid (IBA), a-naphthalene acetic acid (NAA), picloram (4-amino-3,5,6-trichloropicolinic acid), and 6-benzylaminopurine (BAP) in different combinations and concentrations with the view to study the influence of hormones on callus induction and the pattern of expression of dipyranocoumarins including anti-HIV, non-nucleoside reverse transcriptase inhibitors inophyllum B and P in callus cultures. 96.01% seed explants, 87.50% nodal/internodal explants and 86.66% leaf explants were converted into calluses when inoculated on WPM supplemented with IBA 4.0mgl-1 along with BAP 1.0mgl-1, IBA 4.0mgl-1, and picloram 6.0mgl-1 along with BAP 2....

2007-01-01

446

One-year follow-up of the effects of sildenafil on pulmonary arterial hypertension and veno-occlusive disease

Scientific Electronic Library Online (English)

Abstract in english We hypothesized that chronic oral administration of the phosphodiesterase-5 inhibitor sildenafil could improve the exercise capacity and pulmonary hemodynamics in patients with pulmonary arterial hypertension (PAH) on the basis of previous short-term studies. We tested this hypothesis in 14 subjects with PAH, including seven patients with the idiopathic form and seven patients with atrial septal defects, but no other congenital heart abnormalities. Patients were subjected (more) to a 6-min walk test and dyspnea was graded according to the Borg scale. Pulmonary flow and pressures were measured by Doppler echocardiography. Patients were given sildenafil, 75 mg orally three times a day, and followed up for 1 year. Sildenafil therapy resulted in the following changes: increase in the 6-min walk distance from a median value of 387 m (range 0 to 484 m) to 462 m (range 408 to 588 m; P

2005-02-01

447

Nuclear factor of activated T cell (NFAT) transcription proteins regulate genes involved in adipocyte metabolism and lipolysis

Novel high-throughput screening system for identifying STAT3-SH2 antagonists

NFAT involvement in adipocyte physiological processes was examined by treatment with CsA and/or GSK3{beta} inhibitors (Li{sup +} or TZDZ-8), which prevent or increase NFAT nuclear translocation, respectively. CsA treatment reduced basal and TNF{alpha}-induced rates of lipolysis by 50%. Adipocytes preincubated with Li{sup +} or TZDZ-8 prior to CsA and/or TNF{alpha}, exhibited enhanced basal rates of lipolysis and complete inhibition of CsA-mediated decreased rates of lipolysis. CsA treatment dramatically reduced the mRNA levels of adipocyte-specific genes (aP2, HSL, PPAR{gamma}, ACS and Adn), compared with control or TNF{alpha}-treatment, whereas Li{sup +} pretreatment blocked the inhibitory effects of CsA, and mRNA levels of aP2, HSL, PPAR{gamma}, and ACS were found at or above control levels. NFAT nuclear localization, assessed by EMSA, confirmed that CsA or Li{sup +} treatments inhibited or increased NFAT nuclear translocation, respectively. These results show ...

2007-09-21

448

Morusin induces apoptosis and suppresses NF-#kappa#B activity in human colorectal cancer HT-29 cells

Constitutive activation of the oncogenic transcription factor STAT3 frequently occurs in various human malignancies. STAT3 activation involves dimerization via intermolecular pTyr-SH2 interaction. Thus, antagonizing this interaction is a feasible approach to inhibit STAT3 activation for cancer therapy. In order to identify selective STAT3 inhibitors, we developed a biochemical HTS system based on AlphaScreen technology, which measures the abilities of test compounds to antagonize pTyr-SH2 interactions. We screened our chemical libraries using this system and identified 5,15-diphenylporphyrin (5,15-DPP) as a selective STAT3-SH2 antagonist. Selective inhibition of STAT3 nuclear translocation and DNA biding activity was observed in cells treated with 5,15-DPP. IL-6-dependent dimerization of STAT3, c-myc promoter binding and c-myc protein expression were all suppressed by 5,15-DPP, whereas no decrement in either expression or phosphorylation level of STAT3 was ...

2009-03-13

449

Modulation of gene expression in differentiating 3T3 - L1 preadipocytes

Morusin is a pure compound isolated from root bark of Morusaustralis (Moraceae). In this study, we demonstrated that morusin significantly inhibited the growth and clonogenicity of human colorectal cancer HT-29 cells. Apoptosis induced by morusin was characterized by accumulation of cells at the sub-G_1 phase, fragmentation of DNA, and condensation of chromatin. Morusin also inhibited the phosphorylation of IKK-#alpha#, IKK-#beta# and I#kappa#B-#alpha#, increased expression of I#kappa#B-#alpha#, and suppressed nuclear translocation of NF-#kappa#B and its DNA binding activity. Dephosphorylation of NF-#kappa#B upstream regulators PI3K, Akt and PDK1 was also displayed. In addition, activation of caspase-8, change of mitochondrial membrane potential, release of cytochrome c and Smac/DIABLO, and activation of caspase-9 and -3 were observed at the early time point. Downregulation in the expression of Ku70 and XIAP was exhibited afterward. Caspase-8 or wide-ranging caspase ...

2008-07-18

450

Microstructural evolution of WC-Co alloys

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 OMA.

1997-12-31

451

Microstructural evolution of WC-Co alloys

The microstructural development and grain-coarsening behavior of WC-Co alloys, with and without a VC additive, were investigated. The primary goal was to determine the mechanism through which VC acts as a grain-growth inhibitor. The study involved long-time sintering experiments (1 to 100 hours) on fully dense material, nascent stage sintering (90 to 1,320 seconds) starting with the green compact, and surrogate liquid phase experiments to characterize the WC powder prior to sintering. Quantitative microstructural analysis using intercept length distributions was performed for the long-term sintering. The nascent stage experiments involved the measurement of the specific surface area (S{sub v}) of each type of interface separately allowing the determination of the contribution of each developing entity to the overall microstructural evolution. The VC addition has been found to enhance the breakup of multigrained particles in the earliest stages of sintering, ...

1991-01-01

452

Microstructural and mechanical characterization of high energy ball milled and sintered WC-10wt%Co-xTaC nano powders

The microstructural development and grain-coarsening behavior of WC-Co alloys, with and without a VC additive, were investigated. The primary goal was to determine the mechanism through which VC acts as a grain-growth inhibitor. The study involved long-time sintering experiments (1 to 100 hours) on fully dense material, nascent stage sintering (90 to 1,320 seconds) starting with the green compact, and surrogate liquid phase experiments to characterize the WC powder prior to sintering. Quantitative microstructural analysis using intercept length distributions was performed for the long-term sintering. The nascent stage experiments involved the measurement of the specific surface area (S_v) of each type of interface separately allowing the determination of the contribution of each developing entity to the overall microstructural evolution. The VC addition has been found to enhance the breakup of multigrained particles in the earliest stages of sintering, producing a ...

453

British Library Electronic Table of Contents (United Kingdom)

Ultra fine tungsten carbide and cobalt powders were milled by high energy planetary ball mill at different ball to powder weight ratios (BPR) to produce particles of WC-10wt%Co hard metal in nanometer scale size. Microstructural characterizations by TEM show that the particle size of tungsten carbide was achieved to 32nm after milling at 15 BPR during 10h. In order to reduce the WC grain growth during the sintering process, tantalum carbide was added to the hard metal as a WC grain growth inhibitor. The nano hard metal powders were compacted at 200MPa pressure and sintered at 1370-1450degreeC temperatures in a high purity hydrogen atmosphere. The results show that the addition of 0.6wt% of TaC improves the hardness and fracture toughness from 1493 HV30 and 11.8MPam (for TaC free sample) to...

2009-01-01

454

Local therapies to heal the penis: fact or fiction?

Kinetics of nucleotide transport in rat heart mitochondria studied by a rapid filtration technique

Penile rehabilitation has been an area of intense study and debate over the last decade. Interest in this topic was stimulated by the observation that erectile dysfunction remained a significant problem after radical prostatectomy despite meticulous nerve-sparing technique. Smooth muscle alterations and fibrotic changes in the penis were identified as the underlying causes of penile atrophy, veno-occlusive dysfunction, and Peyronie's-like changes that were observed after surgery. 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 oral type V phosphodiesterase inhibitors is now commonly used by urologists after radical prostatectomy despite a lack of convincing evidence from randomized, placebo-controlled clinical trials. Use of local therapies to heal the penis may have ...

2008-11-20

455

Involvement of the NF-?B pathway in multidrug resistance induced by HBx in a hepatoma cell line.

A rapid filtration technique has been used to measure at room temperature the kinetics of ADP and ATP transport in rat heart mitochondria in the millisecond time range. Transport was stopped by cessation of the nucleotide supply, without the use of a transport inhibitor, thus avoiding any quenching delay. The kinetics of ({sup 14}C)ADP transport in energized mitochondria were apparently monophasic. The rate of transport of ({sup 14}C)ATP in energized mitochondria was 5-10 times lower than that of ({sup 14}C)ADP. Upon uncoupling, the rate of ({sup 14}C)ATP uptake was enhanced, and that of ({sup 14}C)ADP uptake was decreased. However, the two rates did not equalize, indicating that transport was not exclusively electrogenic. Transport of ({sup 14}C)ADP and ({sup 14}C)ATP by resting mitochondria followed biphasic kinetics. Depletion of nucleotides in resting mitochondria resulted in a greater decrease in the extent of the slow phase than of the rapid one. In addition, ...

1990-10-01

456

Interactions between organic anions on multiple transporters in Caco-2 cells.

Summary.? It is widely believed that hepatocellular cancer (HCC), especially HBV associated HCC, is highly resistant to chemotherapy. To investigate the molecular influence of HBx protein on multidrug resistance (MDR) in HCC and the potential role of the NF-?B pathway in this process. We established HBx-expressing cells by liposome-mediated transfection of the HBx into the HepG2 cell line. We found that HBx expression in HCC cells induces drug resistance against multiple drugs, a significantly lower apoptosis ratio in HepG2-HBx and HepG2.2.15 cells, compared with HepG2 and HepG2-3.1 cells (P?HCC cells were downregulated by IMD-0354 treatment, which is the NF-?B pathway inhibitor. Taken together, these results suggest that HBx protein might be one of the causes for the occurrence of MDR in HCC, and the NF-?B pathway might be involved in this change. PMID:21914061

2011-05-27

457

Influence of suspended solids on pitting corrosion of carbon steel in cooling water. Tansoko no koshoku ni oyobosu reikyaku suichu no kendaku busshitsu no eikyo

In drug development, Caco-2 cells are often employed to study the influence of membrane transporters on drug permeability. The aim of the current study was to characterize permeability and kinetic parameters of selected organic anionic compounds in Caco-2 cells, and to investigate whether the Caco-2 cell line may be used as an overall model to predict interactions on multiple membrane transporters in the intestine. Taurocholic acid (TCA) and estrone-3-sulfate (E(1) S) were used as model substrates. Possible inhibitors studied were TCA, E(1) S, taurolithocholic acid, fluvastatin, and glipizide. The effects of these compounds on initial uptake, apparent permeability, and intracellular end-point accumulations of the probe substrates were studied. Both interactions on apical and basolateral influx transporters were observed. These interactions were proposed to be mediated mainly by the apical sodium-dependent bile acid transporter and the organic solute transporter ...

2011-05-23

458

Influence of substrates on nitrogen removal performance and microbiology of anaerobic ammonium oxidation by operating two UASB reactors fed with different substrate levels.

A large amount of industrial water is used for cooling the various process fluids in the petroleum purification factories as well as petroleum chemistry factories. Consequently, a lot of heat exchangers as the necessary constitutional instruments are made of carbon steel. Due to the most of the corrosions of the carbon steel occurring in such cooling water systems are pitting corrosions, the inhibition thereof is extremely important for the elongation of the life of the plants and the stable operation. In this paper, the influences of water quality fractions on pitting corrosion of carbon steel in cooling water circumstance are examined aiming at the fouling in the cooling water. The fouling in the cooling water does not only increase the amount of occurrence of pitting corrosion but also accelerates the progress of pitting corrosion enlarging the rust due to its deposition near the anode. Since only the inhibitor is not sufficient to inhibit the pitting corrosion ...

1993-08-15

459

Influence of Ce0.9Gd0.1O2-d particles on microstructure and oxygen permeability of Ba0.5Sr0.5Co0.8Fe0.2O3-d composite membrane

Both ammonium and nitrite act as substrates as well as potential inhibitors of anoxic ammonium-oxidizing (Anammox) bacteria. To satisfy demand of substrates for Anammox bacteria and to prevent substrate inhibition simultaneously; two strategies, namely high or low substrate concentration, were carefully compared in the operation of two Anammox upflow anaerobic sludge blanket (UASB) reactors fed with different substrate concentrations. The reactor working at relatively low influent substrate concentration (NO(2)(-)-N, 240 mg-NL(-1)) was shown to avoid the inhibition caused by nitrite and free ammonia. Using the strategy of low substrate concentration, a record super high volumetric nitrogen removal rate of 45.24 kg-Nm(-3) day(-1) was noted after the operation of 230 days. To our knowledge, such a high value has not been reported previously. The evidence from transmission electron microscopy (TEM) showed that the morphology and ultrastructure of the Anammox cells in ...

2010-04-13

460

British Library Electronic Table of Contents (United Kingdom)

This study examined the oxygen permeation behavior of Ce0.9Gd0.1O2-d (Gadolinium-Doped Ceria, GDC)/Ba0.5Sr0.5Co0.8Fe0.2O3-d (BSCF) composite membranes fabricated using a conventional sintering technique. GDC/BSCF composite membranes with a relative density >95% could be obtained when a green compact of BSCF and GDC was sintered at 1150^oC for 5h. It appears that GDC serves as a grain growth inhibitor because the average grain size of the composite decreased with increasing GDC content. The oxygen permeability of the BSCF and GDC/BSCF composite membranes strongly depends on the grain size and membrane thickness. The addition of GDC to BSCF resulted in a small grain size, low thermal expansion coefficient and high hardness. However, it is believed that oxygen permeation was blocked by GDC, a...

2010-01-01

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

461

Identification of sucrose binding, membrane proteins using a photolyzable sucrose analog. [P. saccharophila

HSP70, the earliest-induced gene in the zebrafish retina during optic nerve regeneration: Its role in cell survival

The sucrose derivative 6'-deoxy-6'-(2-hydroxy-4-azido)benzamidosucrose (6'-HABS) was prepared from sucrose (via 6'-deoxy-6'-aminosucrose) and 4-amino-salicylic acid. 6'-HABS is a competitive inhibitor of sucrose influx into protoplasts from developing soybean cotyledons and of sucrose binding to membranes from the bacteria P. saccharophila. The Ki for inhibition in the soybean protoplasts was 75..mu..M. 6'-Deoxy-6'-(2-hydroxy-3-/sup 125/Iodo-4-azido)benzamidosucrose was prepared by lactoperoxidase iodination of 6'-HABS. Upon photolysis in the presence of membranes from P saccharophila, label from the photoprobe is incorporated into a sucrose inducible polypeptide of mass 84 KD in SDS-PAGE. The polypeptide is protected from labeling by the inclusion of sucrose in the photolysis mixture. Photolysis conditions which lead to specific labeling of the sucrose protectable polypeptide in ...

1986-04-01

462

British Library Electronic Table of Contents (United Kingdom)

Fish retinal ganglion cells (RGCs) can survive and regrow their axons after optic nerve injury. Injured RGCs express anti-apoptotic proteins, such as Bcl-2, after nerve injury; however, upstream effectors of this anti-apoptotic protein are not yet fully understood. Heat shock proteins (HSPs) play a crucial role in cell survival against various stress conditions. In this study, we focused on HSP70 expression in the zebrafish retina after optic nerve injury. HSP70 mRNA and protein levels increased rapidly 2.3-fold in RGCs by 1-6 h after injury and returned to control levels by 1-3 days. HSP70 transcription is regulated by heat shock factor 1 (HSF1). HSF1 mRNA and phosphorylated-HSF1 protein rapidly increased by 2.2-fold in RGCs 0.5-6 h after injury. Intraocular injection of HSP inhibitor I s...

2011-01-01

463

Grain boundary mobility in Y{sub 2}O{sub 3}: defect mechanism and dopant effects

Grain boundary mobility in Y_2O_3: defect mechanism and dopant effects

The effects of the dopants, Mg{sup 2+}, Sr{sup 2+}, Sc{sup 3+}, Yb{sup 3+}, Gd{sup 3+}, La{sup 3+}, Ti{sup 4+}, Zr{sup 4+}, Ce{sup 4+}, and Nb{sup 5+}, on the grain boundary mobility of dense Y{sub 2}O{sub 3} have been investigated from 1,500 to 1,650 C. Parabolic grain growth has been observed in all cases over a grain size from 0.31 to 12.5 {micro}m. Together with atmospheric effects, the results suggest that interstitial transport is the rate-limiting step for diffusive processes in Y{sub 2}O{sub 3}, which is also the case in CeO{sub 2}. The effect of solute drag cannot be ascertained but the anomalous effect of undersized dopants (Ti and Nb) on diffusion enhancement, previously reported in CeO{sub 2}, is again confirmed. Indications of very large binding energies between aliovalent dopants and oxygen defects are also observed. Overall, the most effective grain growth inhibitor is Zr{sup 4+}, while the most potent grain growth promoter is Sr{sup 2+}, both at ...

1996-07-01

464

Four small puzzles that Rosetta doesn't solve

The effects of the dopants, Mg"2"+, Sr"2"+, Sc"3"+, Yb"3"+, Gd"3"+, La"3"+, Ti"4"+, Zr"4"+, Ce"4"+, and Nb"5"+, on the grain boundary mobility of dense Y_2O_3 have been investigated from 1,500 to 1,650 C. Parabolic grain growth has been observed in all cases over a grain size from 0.31 to 12.5 microm. Together with atmospheric effects, the results suggest that interstitial transport is the rate-limiting step for diffusive processes in Y_2O_3, which is also the case in CeO_2. The effect of solute drag cannot be ascertained but the anomalous effect of undersized dopants (Ti and Nb) on diffusion enhancement, previously reported in CeO_2, is again confirmed. Indications of very large binding energies between aliovalent dopants and oxygen defects are also observed. Overall, the most effective grain growth inhibitor is Zr"4"+, while the most potent grain growth promoter is Sr"2"+, both at 1.0% concentration.

465

CERN Document Server

A complete macromolecule modeling package must be able to solve the simplest structure prediction problems. Despite recent successes in high resolution structure modeling and design, the Rosetta software suite fares poorly on deceptively small protein and RNA puzzles, some as small as four residues. To illustrate these problems, this manuscript presents extensive Rosetta results for four well-defined test cases: the 20-residue mini-protein Trp cage, an even smaller disulfide-stabilized conotoxin, the reactive loop of a serine protease inhibitor, and a UUCG RNA tetraloop. In contrast to previous Rosetta studies, several lines of evidence indicate that conformational sampling is not the major bottleneck in modeling these small systems. Instead, approximations and omissions in the Rosetta all-atom energy function currently preclude discriminating experimentally observed conformations from de novo models at atomic resolution. These molecular "puzzles" should serve as ...

2011-01-01

466

Extrusion as a thermo-mechanical pre-treatment for lignocellulosic ethanol

Effects of biomass-generated producer gas constituents on cell growth, product distribution and hydrogenase activity of Clostridium carboxidivorans P7{sup T}

Two physical pre-treatment methods, particle size reduction by grinding and thermo-mechanical extrusion, were evaluated as alternatives to traditional biomass pretreatments for lignocellulosic ethanol. Commonly available agricultural co-products wheat bran and soybean hull were the model substrates. Extrusion led to higher reducing sugar yields as compared to grinding for wheat bran, but not in the case of soybean hulls. The best combination of extrusion screw speed and maximum barrel temperature were 7 Hz/150 C and 3.7 Hz/110 C. The use of a solvent mixture (sodium hydroxide, urea, and thiourea) and calcium chloride solution in combination with extrusion treatment did not lead to improvement in reducing sugar yield. However, extensive washing to get rid of solvents and enzymatic inhibitors improved the conversion efficiency substantially, resulting in total reducing sugar yields of 60-73% and 25-36%, respectively, for wheat bran and soybean hull. (author)

2010-12-15

467

Effect of iron and boron carbide on the densification and mechanical properties of titanium diboride ceramics

In our previous work, we demonstrated that biomass-generated producer gas can be converted to ethanol and acetic acid using a microbial catalyst Clostridium carboxidivorans P7{sup T}. Results showed that the producer gas (1) induced cell dormancy, (2) inhibited H{sub 2} consumption, and (3) affected the acetic acid/ethanol product distribution. Results of this work showed that tars were the likely cause of cell dormancy and product redistribution and that the addition of a 0.025{mu}m filter in the gas cleanup negated the effects of tars. C. carboxidivorans P7{sup T} can adapt to the tars (i.e. grow) only after prolonged exposure. Nitric oxide, present in the producer gas at 150ppm, is an inhibitor of the hydrogenase enzyme involved in H{sub 2} consumption. We conclude that significant conditioning of the producer gas will be required for the successful coupling of biomass-generated producer gas with fermentation to produce ethanol and acetic acid. (author)

2006-07-15

468

Effect of iron and boron carbide on the densification and mechanical properties of titanium diboride ceramics

The effects of Fe and B{sub 4}C on the sintering behavior and mechanical properties of TiB{sub 2} ceramics have been studied. Sintering was performed in an Ar atmosphere at 2000{degrees}C using attrition-milled TiB{sub 2} powder. When a small amount of Fe (0.5 wt%) was added, abnormal grain growth occurred and the sintered density was low. In the case of B{sub 4}C added along with 0.5 wt% Fe, however, abnormal grain growth was remarkably suppressed, and the sintered density was increased up to 95% of theoretical. But with excess Fe addition (5 wt%), B{sub 4}C grains did not act as a grain growth inhibitor, and B{sub 4}C grains were frequently trapped in large TiB{sub 2} grains. The best mechanical properties were obtained for the TiB{sub 2}-10 wt% B{sub 4}C-0.5 wt% Fe ceramics, which exhibited a three-point bending strength of 400 MPa and a fracture toughness of 5.5 MPa {center dot} m{sup 1/2}.

1989-10-01

469

Effect of external pH on the cytoplasmic and vacuolar pHs in Mung bean root-tip cells. A T P nuclear magnetic resonance study

The effects of Fe and B_4C on the sintering behavior and mechanical properties of TiB_2 ceramics have been studied. Sintering was performed in an Ar atmosphere at 2000 degrees C using attrition-milled TiB_2 powder. When a small amount of Fe (0.5 wt%) was added, abnormal grain growth occurred and the sintered density was low. In the case of B_4C added along with 0.5 wt% Fe, however, abnormal grain growth was remarkably suppressed, and the sintered density was increased up to 95% of theoretical. But with excess Fe addition (5 wt%), B_4C grains did not act as a grain growth inhibitor, and B_4C grains were frequently trapped in large TiB_2 grains. The best mechanical properties were obtained for the TiB_2-10 wt% B_4C-0.5 wt% Fe ceramics, which exhibited a three-point bending strength of 400 MPa and a fracture toughness of 5.5 MPa #centre dot# m"1"/"2.

470

Effect of external pH on the cytoplasmic and vacuolar pHs in Mung bean root-tip cells

The effect of the external pH on the intracellular pH in mung bean (Vigna mungo (L.) Hepper) root-tip cells was investigated with the T P nuclear magnetic resonance (NMR) method. The T P NMR spectra showed three peaks caused by cytoplasmic G-6-P, cytoplasmic Psub(i) and vacuolar Psub(i). The cytoplasmic and vacuolar pHs could be determined by comparing the Psub(i) chemical shifts with the titration curve. When the external pH was changed over a range from pH 3 to 10, the cytoplasmic pH showed smaller changes than the vacuolar pH, suggesting that the former is regulated more strictly than the latter. The H -ATPase inhibitor, DCCD, caused the breakdown of the mechanism that regulates the intracellular pH. H -ATPase appears to have an important part in the regulation of the intracellular pH.

1984-12-01

471

Effect of VC and NbC additions on microstructure and properties of ultrafine WC-10Co cemented carbides

The effect of the external pH on the intracellular pH in mung bean (Vigna mungo (L.) Hepper) root-tip cells was investigated with the "3"1P nuclear magnetic resonance (NMR) method. The "3"1P NMR spectra showed three peaks caused by cytoplasmic G-6-P, cytoplasmic Psub(i) and vacuolar Psub(i). The cytoplasmic and vacuolar pHs could be determined by comparing the Psub(i) chemical shifts with the titration curve. When the external pH was changed over a range from pH 3 to 10, the cytoplasmic pH showed smaller changes than the vacuolar pH, suggesting that the former is regulated more strictly than the latter. The H"+-ATPase inhibitor, DCCD, caused the breakdown of the mechanism that regulates the intracellular pH. H"+-ATPase appears to have an important part in the regulation of the intracellular pH. (author).

472

British Library Electronic Table of Contents (United Kingdom)

The nanocomposite WC-Co powders were prepared through planetary ball milling method. Effects of grain growth inhibitor addition and the vacuum sintering parameters on the microstructure and properties of ultrafine WC-10Co cemented carbides were investigated using X-ray diffractometer, scanning electron microscope and mechanical property tester. The results show that VC and NbC additions can refine the WC grains, decrease the volume fraction of Co3W3C phase in ultrafine WC-10Co cemented carbides, and increase the hardness and fracture toughness of the base alloys. After sintering for 60 min at 1400 degreeC, the average grain size and hardness of ultrafine-grained WC-10Co-1VC cemented carbide are 470 nm and HRA 91.5, respectively. The fracture toughness of cemented carbide WC-10Co-1NbC alloy...

2009-01-01

473

Effect of Ho^3^+ substitutions on the structural and magnetic properties of BaFe12O19 hexaferrites

British Library Electronic Table of Contents (United Kingdom)

Holmium doped barium based hexaferrites BaFe12-2xHo2xO19 with (x=0.0-1.0) were synthesized by solid state reaction method. Structural and magnetic characterization of these ferrites provide significant information about their reactive physical properties. X-ray analysis reveals that in all samples M-type structure exist with few secondary phases. Scanning electron microscope revealed the grain size of the specimen. The results show that grain size decreases with the substitution degree of Holmium. Thus rare earth element Holmium Ho^3^+ acts as a grain growth inhibitor. The magnetic hysteresis loops show the variation in the values of magnetic parameters like saturation magnetization (Ms), remanent magnetization (Mr) and coercivity (Hc) were observed by changing Ho^3^+ content in BaFe12-2xH...

2010-01-01

474

Effect of Ho"3"+ substitutions on the structural and magnetic properties of BaFe_1_2O_1_9 hexaferrites

Ectopic expression of wild-type or a dominant-negative mutant of transcription factor NTF-1 disrupts normal Drosophila development.

Holmium doped barium based hexaferrites BaFe_1_2_-_2_xHo_2_xO_1_9 with (x = 0.0-1.0) were synthesized by solid state reaction method. Structural and magnetic characterization of these ferrites provide significant information about their reactive physical properties. X-ray analysis reveals that in all samples M-type structure exist with few secondary phases. Scanning electron microscope revealed the grain size of the specimen. The results show that grain size decreases with the substitution degree of Holmium. Thus rare earth element Holmium Ho"3"+ acts as a grain growth inhibitor. The magnetic hysteresis loops show the variation in the values of magnetic parameters like saturation magnetization (M_s), remanent magnetization (M_r) and coercivity (H_c) were observed by changing Ho"3"+ content in BaFe_1_2_-_2_xHo_2_xO_1_9 ferrites. Coercivity showed a maximum value of 2230 Oe for (x = 0.4) and then decreasing trend were observed in the values of H_c, M_r and M_s with ...

2010-04-09

475

Direct photoaffinity labeling by nucleotides of the apparent catalytic site on the heavy chains of smooth muscle and Acanthamoeba myosins

The Drosophila melanogaster tissue-specific transcription factor NTF-1 was originally identified in vitro as a protein that could bind to and activate transcription from the Dopa decarboxylase (Ddc) gene. A structure-function analysis of NTF-1 led to the identification of a discrete amino-terminal activation domain. Here, we report that an NTF-1 mutant lacking the activation domain acts as a trans-dominant inhibitor of NTF-1 activation in tissue culture cells by forming inactive heterodimers with the full-length protein. Ectopically expressing this dominant-negative protein or the full-length protein in developing Drosophila embryos leads to dire developmental consequences. Overexpressing the trans-dominant NTF-1 leads to lethality, while overexpressing full-length NTF-1 results in both lethality and morphogenetic defects. Our results suggest that both the activity and the regulation of NTF-1 are critical for viability and proper development of the fly.ImagesFig. ...

1993-11-15

476

Diminished osmotic fragility of human erythrocytes following the membrane insertion of oxygenated sterol compounds

The heavy chains of Acanthamoeba myosins, IA, IB and II, turkey gizzard myosin, and rabbit skeletal muscle myosin subfragment-1 were specifically labeled by radioactive ATP, ADP, and UTP, each of which is a substrate or product of myosin ATPase activity, when irradiated with uv light at 0"0C. With UTP, as much as 0.45 mol/mol of Acanthamoeba myosin IA heavy chain and 1 mol/mol of turkey gizzard myosin heavy chain was incorporated. Evidence that the ligands were associated with the catalytic site included the observations that reaction occurred only with nucleotides that are substrates or products of the ATPase activity; that the reaction was blocked by pyrophosphate which is an inhibitor of the ATPase activity; that ATP was bound as ADP; and that label was probably restricted to a single peptide following limited subtilisin proteolysis of labeled Acanthamoeba myosin IA heavy chain and extensive cleavage with CNBr and trypsin of labeled turkey gizzard myosin heavy ...

477

Dielectric properties of fluxed barium titanate ceramics with zirconia additions

Oxygenated sterol compounds (OSC), when incubated for 1 hr with human erythrocytes in lipoprotein-depleted medium at concentrations of 0.625-5 x 10/sup -5/M, are inserted into the cell membrane and remain there despite subsequent washing of the cells. The insertion results in expansion of the surface area of the red cell ghost membrane, an increase in critical hemolytic volume, and as a consequence, in dimished osmotic fragility of the erythrocytes. This effect is seen with echinocyte-forming as well as with non-echinocyte-forming OSC. Erythrocytes treated with OSC do not differ from control cells with respect to their mean cell volume (MCV) in isotonic solution, water content, ion fluxes, and filterability through polycarbonate filters. The shift of the osmotic fragility curve toward lower NaCl concentrations is proportional to the amount of OSC inserted into the red cell membrane. 7BETA-Hydroxycholesterol, 22-ketocholesterol, and 20 ..cap alpha..-hydroxycholesterol are the most ...

1981-08-01

478

Dielectric properties of fluxed barium titanate ceramics with zirconia additions

BaTiO{sub 3} compacts, when fluxed with {lt} 2 vol% of a complex borate glass phase, were sintered to near theoretical density at temperatures {lt} 1175{degrees}C in 2 h. Microstructural analysis showed a uniform grain size {lt} 1.0 {mu}m with 0.75 wt% ZrO{sub 2} added to the flux phase as a grain growth inhibitor. TEM analysis revealed a microcrystalline grain-boundary phase with the ZrO{sub 2} resident along the grain boundaries. These samples displayed an essentially flat dielectric profile, low dissipation factors ({lt} 2%) over the range 25{degrees} to 125{degrees}C, a near linear dependence ({approx} {+-} 15%) between 25{degrees} and {minus} 55{degrees}C, and significantly increased voltage stability. X-ray diffraction analysis of these small-grained materials indicates a suppression of the tetragonal structure toward a more cubic modification.

1990-03-01

479

Corrosion control. 2. ed.

BaTiO_3 compacts, when fluxed with < 2 vol% of a complex borate glass phase, were sintered to near theoretical density at temperatures < 1175 degrees C in 2 h. Microstructural analysis showed a uniform grain size < 1.0 #mu#m with 0.75 wt% ZrO_2 added to the flux phase as a grain growth inhibitor. TEM analysis revealed a microcrystalline grain-boundary phase with the ZrO_2 resident along the grain boundaries. These samples displayed an essentially flat dielectric profile, low dissipation factors (< 2%) over the range 25 degrees to 125 degrees C, a near linear dependence (#approx# #+-# 15%) between 25 degrees and - 55 degrees C, and significantly increased voltage stability. X-ray diffraction analysis of these small-grained materials indicates a suppression of the tetragonal structure toward a more cubic modification.

480

The purpose of this text is to train engineers and technologists not just to understand corrosion but to control it. Materials selection, coatings, chemical inhibitors, cathodic and anodic protection, and equipment design are covered in separate chapters. High-temperature oxidation is discussed in the final two chapters ne on oxidation theory and one on controlling oxidation by alloying and with coatings. This book treats corrosion and high-temperature oxidation separately. Corrosion is divided into three groups: (1) chemical dissolution including uniform attack, (2) electrochemical corrosion from either metallurgical or environmental cells, and (3) stress-assisted corrosion. Corrosion is logically grouped according to mechanisms rather than arbitrarily separated into different types of corrosion as if they were unrelated. For those university students and industry personnel who approach corrosion theory very hesitantly, this text will present the electrochemical ...

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25

481

Corrosion control. 2. ed

Comparative study of the electrochemical behaviour of iron in alkaline media containing red mud and grey slurries. the effect of Al{sup 3}+; Estudio comparativo del comportamiento electroquimico del hierro en medio alcalino en presencia de lodos rojos y lodos grises. Efecto del Al{sup 3}+

The purpose of this text is to train engineers and technologists not just to understand corrosion but to control it. Materials selection, coatings, chemical inhibitors, cathodic and anodic protection, and equipment design are covered in separate chapters. High-temperature oxidation is discussed in the final two chapters ne on oxidation theory and one on controlling oxidation by alloying and with coatings. This book treats corrosion and high-temperature oxidation separately. Corrosion is divided into three groups: (1) chemical dissolution including uniform attack, (2) electrochemical corrosion from either metallurgical or environmental cells, and (3) stress-assisted corrosion. Corrosion is logically grouped according to mechanisms rather than arbitrarily separated into different types of corrosion as if they were unrelated. For those university students and industry personnel who approach corrosion theory very hesitantly, this text will present the electrochemical ...

2001-07-01

482

Common colorectal cancer risk variants in SMAD7 are associated with survival among prediagnostic nonsteroidal anti-inflammatory drug users: A population-based study of postmenopausal women

Red mud (Rm) is the main by-product of the Bayer process for alumina extraction from bauxite, and grey slurries (GS) are generated during the granite rocks transformation processes. the huge volume of those wastes generated every year suppose a serious environmental problem. Recent works by our group demonstrate the efficiency of both types of muds as corrosion inhibitors for iron and steel in alkaline media containing chlorides. The elemental analysis of these slurried shows that Al{sup 3}+ is the main common element. Therefore, the aim of this paper is to study the effect of the soluble Al{sup 3}+ in the electrochemical behaviour of iron in alkaline media, in presence and absence of chlorides. The electrochemical study using Cyclic Voltammetry (CV) and Electrochemical Impedance Spectroscopy (EIS) together with surface analysis techniques allowed to conclude that Al{sup 3}+ blocks the surface of steel in alkaline media chloride increasing the steel resistance to ...

2009-07-01

483

British Library Electronic Table of Contents (United Kingdom)

Abstract Common single nucleotide polymorphisms (SNPs) in SMAD7 (18q21) have been linked to colorectal cancer (CRC) risk in genome-wide association studies, but little is known about their effects on survival. SMAD7 regulates gastrointestinal inflammation by inhibiting transforming growth factor- (TGFB), which can act as both a tumor suppressor and a promoter of metastasis. Regular use of cyclooxygenase-2 (COX2) inhibitors, such as nonsteroidal anti-inflammatory drugs (NSAIDs), reduces the risk of developing CRC. Because COX2 overexpression reduces the growth suppressing effects of TGFB, we hypothesized that survival may depend on both SMAD7 genotype and prediagnostic NSAID use. Postmenopausal women, ages 50-74, diagnosed with incident invasive CRC from 1997 to 2002 were identified using t...

2011-01-01

484

Citrat og nyresten

Characteristics of sugar uptake by immature maize embryos

Citrate is an important naturally occurring inhibitor of calcium stone formation in urine. Urinary citrate excretion was examined in 43 consecutive patients with recurrent idiopathic calcium nephrolithiasis and in 50 normal controls by a specific enzymatic technique. Hypocitraturia (<1.6 mmol/24h) was found in 14 (33%) stone formers compared to 6 (12%) normal controls (p = 0.03). Citrate excretion expressed as citrate-creatinine ratio in 24 hour urine samples was significantly lower in the stone formers than in the healthy controls (p = 0.03), and significantly lower in healthy men, compared to healthy females (p = 0.006). There was a great variability in urinary citrate levels in both groups, and a considerable overlap in the urinary citrate excretion between normal subjects and stone formers. Factors other than urinary citrate excretion must therefore be of importance in the pathophysiology of calcium stone formation. Citrate-calcium ratio in urine proved to ...

1993-01-01

485

Bioscavenger for protection from toxicity of organophosphorus compounds.

Characteristics of sugar uptake by immature maize embryos were determined in vitro utilizing a /sup 14/C-sugar solution incubation method. Hexose uptake rates were greater than those for sucrose, however, all showed biphasic kinetics. Glucose and fructose saturable components were evidence at <50 mM and sucrose at <5 mM. Chemical inhibitors (CCCP, DNP, NaCN, and PCMBS) and low temperature reduced sugar uptake. Sucrose influx was pH dependent while glucose was not. Embryos maintained a high sucrose to hexose ratio throughout development. At 25 days after pollination sucrose levels exceeded 200 mM while hexose levels remained below 5 mM. Glucose was rapidly converted to sucrose upon transport into the embryo. These circumstantial data indicate that sugar uptake by immature maize embryos is metabolically dependent and carrier mediated. Furthermore, sucrose transport appears to occur against its concentration gradient involving a H+/sucrose cotransport mechanism, ...

1986-04-01

486

Assessment of epidermal growth factor receptor (EGFR, ErbB1) and HER2 (ErbB2) protein expression levels and response to lapatinib (Tykerb, GW572016) in an expanded panel of human normal and tumour cell lines

Current antidotal regimens for organophosphorus compound (OP) poisoning consist of a combination of pretreatment with a spontaneously reactivating AChE inhibitor such as pyridostigmine bromide, and postexposure therapy with anticholinergic drugs such as atropine sulfate and oximes such as 2-PAM chloride (Gray, 1984). Although these antidotal regimens are effective in preventing lethality of animals from OP poisoning, they do not prevent postexposure incapacitation, convulsions, performance deficits, or, in many cases, permanent brain damage (Dunn and Sidell, 1989). These problems stimulated the development of enzyme bioscavengers as a pretreatment to sequester highly toxic OPs before they reach their physiological targets. Several studies over the last two decades have demonstrated that exogenously administered human serum butyrylcholinesterase (Hu BChE) can be used successfully as a safe, efficacious, and single prophylactic treatment to counteract the toxicity of ...

2006-01-01

487

British Library Electronic Table of Contents (United Kingdom)

Abstract. Objective: Lapatinib (Tykerb, GW572016), a potent inhibitor of the catalytic activities of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) (ErbB2), inhibits population growth of selected EGFR and HER2 overexpressing cell lines. Previous studies with a small number of cell lines suggest a correlation between overexpression of EGFR and/or HER2 and sensitivity to growth inhibition by lapatinib; however, the precise determinants of lapatinib selectivity for tumour and/or other cells remain unclear. Materials and methods: To clarify the determinants of its selectivity in cultured cells, lapatinib-induced cell population growth inhibition and relative EGFR and HER2 protein expression were quantified in 61 different human tumour cell lines fro...

2007-01-01

488

Applications or radiation polymerization hardening to composites

Anti-nuclear antibody positivity and the use of certolizumab in inflammatory bowel disease patients who have had arthralgias or lupus-like reactions from infliximab or adalimumab

Comprehensive investigation has been made into the application of the polymerization hardening by radiation, particularly electron beam, to the composites of polymers and other materials. The report is divided into four parts, namely 1) characteristics and problems of the reaction of curing by radiation polymerization, 2) improvement of the bonding capability of high molecular weight materials, 3) bonding by radiation, and 4) composites made by the impregnation and polymerization hardening of monomers. The first part includes the effects of dose rate, temperature rise during the hardening, the peculiarity of electron beam irradiation at high dose rate, reaction environment and additive effects. Main conclusions are as follows: caution must be taken to the amount of residual double bonds because they affect the quality of hardened polymers; the polymerization hardening reaction at high dose rate cannot be analogized by that at low dose rate; and the presence of the ...

1976-01-01

489

British Library Electronic Table of Contents (United Kingdom)

OBJECTIVE:- Tumor necrosis factor (TNF) inhibitors can be used to treat inflammatory bowel disease (IBD) but may lead to anti-nuclear antibody (ANA) positivity and lupus-like reactions. Because of its unique structure, certolizumab has lower rates of these complications. We sought to investigate whether patients who have had lupus-like reactions to infliximab or adalimumab would be able to tolerate certolizumab. METHODS:- We performed a retrospective analysis on the 23 patients at the Roberts Inflammatory Bowel Disease Center who received certolizumab for the treatment of Crohn's disease from March 2008 to June 2009. We identified 6 patients who were switched to this drug because of lupus-like reactions from prior anti-TNF therapy and had documented ANA after the reaction and prior to cert...

2011-01-01

490

Aliskiren reduces vascular pathology in diabetic retinopathy and oxygen-induced retinopathy in the transgenic (mRen-2)27 rat

British Library Electronic Table of Contents (United Kingdom)

Aim/hypothesis We examined whether the renin inhibitor, aliskiren, provides similar or greater protection than ACE inhibition from non-proliferative diabetic retinopathy and from the proliferative neoangiogenesis of oxygen-induced retinopathy. Methods Transgenic (mRen-2)27 rats, which overexpress mouse renin and angiotensin in extra-renal tissues, were studied. For diabetic studies, non-diabetic, diabetic (streptozotocin, 55?mg/kg), diabetic + aliskiren (10?mg?kg?1?day?1, pump), or diabetic + lisinopril (10?mg?kg?1?day?1, drinking water) rats were evaluated over 16?weeks. For oxygen-induced retinopathy studies, rats were exposed to 80% oxygen (22?h/day) from postnatal days?0 to 11, and then room air from postnatal days?12 to 18. Aliskiren (10 or 30?mg?kg?1?day?1, pump) or lisinopril (10?mg...

2011-01-01

491

Adaptive response of the chicken embryo to low doses of x-irradiation

A human TERT C-terminal polypeptide sensitizes HeLa cells to H2O2-induced senescence without affecting telomerase enzymatic activity.

Chicken embryos were x-irradiated in ovo with 5-30 cGy (=priming dose) at the 13th-15th day of development. After 3-48 h, brain- and liver-cell suspensions were x-irradiated in vitro with (challenge) doses of 4-32 Gy. Significantly less radiation damage was observed when the radiation response was measured by scheduled DNA synthesis, nucleoid sedimentation and viscosity of alkaline cell lysates 12-36 h after the priming exposure. In vivo, pre-irradiation with 10 cGy enhanced regeneration as evidenced by the DNA content of chicken embryo brain and liver 24 h following a challenge dose of 4 Gy. From nucleoid sedimentation analyses in brain and liver cells immediately after irradiation with 16 Gy and after a 30-min repair period in the presence of aphidicolin, dideoxythymidine and 3-aminobenzamide or in the absence of these DNA repair inhibitors, it is concluded that a reduction of the initial radiation damage is the dominant mechanism of the ``radio-adaptive`` ...

1995-08-01

492

Strain differences in the responsiveness between Sprague-Dawley and Fischer rats to nephropathy induced by FYX-051, a xanthine oxidoreductase inhibitor

We have constructed a 27-kDa hTERT C-terminal polypeptide (hTERTC27) devoid of domains required for telomerase activity and demonstrated that it is capable of nuclear translocation/telomere-end targeting. Here we showed that expression of a low level of hTERTC27 renders hTERT positive HeLa cells sensitive to H(2)O(2)-induced oxidative stress and subsequent cell senescence. The senescence-associated gene, the cyclin/cdk inhibitor p21(Waf1), was up-regulated. This occurs without changing the expression of endogenous hTERT, causing significant telomere shortening or inhibiting telomerase activity. Results from this study suggest for the first time that in addition to telomerase activity, the C-terminus of hTERT also plays a role in hTERT-mediated cellular resistance to oxidative stress. PMID:12565825

2003-02-14

493

Topographical distribution of decrements and recovery in muscarinic receptors from rat brains repeatedly exposed to sublethal doses of soman

To determine a rat strain appropriate for carcinogenicity testing of FYX-051, a xanthine oxidoreductase inhibitor, we performed a 4-week oral toxicity study by administering 0.3, 1 and 3 mg/kg, and 1, 3 and 10 mg/kg of FYX-051 to male Sprague-Dawley (SD) and Fischer (F344) rats, respectively. Histopathology revealed that the degree of FYX-051-induced nephropathy was 3-fold stronger in SD rats than in F344 rats. Our previous study demonstrated that the key factor of species differences in FYX-051-induced nephropathy is purine metabolism. This observation led us to examine the involvement of purine metabolism in differences among two strains of rats. However, purine metabolism was proven not to be implicated as an important factor. Subsequently, other factors responsible for the strain differences were examined. FYX-051-induced increases in plasma xanthine concentrations were higher in SD rats than in F344 rats, suggesting more remarkable effects on pharmacodynamics ...

2006-12-15

494

Topographical distribution of decrements and recovery in muscarinic receptors from rat brains repeatedly exposed to sublethal doses of soman

(3H)Quinuclidinyl benzilate binding to rat brain muscarinic receptors decreased after repeated exposure to soman, a potent organophosphorus cholinesterase inhibitor. The topographical distribution of this decrement was analyzed by quantitative receptor autoradiography. After 4 weeks of soman, three times a week, quinuclidinyl benzilate binding decreased to 67 to 80% of control in frontal and parietal cortex, caudate-putamen, lateral septum, hippocampal body, dentate gyrus, superior colliculus, nucleus of the fifth nerve, and central grey. Minor or no decreases were observed in thalamic or hypothalamic nuclei, reticular formation, pontine nuclei, inferior colliculus, nucleus of the seventh nerve, and cerebellum. Scatchard analyses of saturation curves using frontal cortex sections from soman-treated rats revealed a decrease in maximal quinuclidinyl benzilate binding from that in control rats and a return toward control levels by 24 days without any significant ...

1984-08-01

495

Radiation inactivation target size of rat adipocyte glucose transporter

[3H]Quinuclidinyl benzilate binding to rat brain muscarinic receptors decreased after repeated exposure to soman, a potent organophosphorus cholinesterase inhibitor. The topographical distribution of this decrement was analyzed by quantitative receptor autoradiography. After 4 weeks of soman, three times a week, quinuclidinyl benzilate binding decreased to 67 to 80% of control in frontal and parietal cortex, caudate-putamen, lateral septum, hippocampal body, dentate gyrus, superior colliculus, nucleus of the fifth nerve, and central grey. Minor or no decreases were observed in thalamic or hypothalamic nuclei, reticular formation, pontine nuclei, inferior colliculus, nucleus of the seventh nerve, and cerebellum. Scatchard analyses of saturation curves using frontal cortex sections from soman-treated rats revealed a decrease in maximal quinuclidinyl benzilate binding from that in control rats and a return toward control levels by 24 days without any significant ...

1984-01-01

496

Neurite outgrowth effect of 4-O-methylhonokiol by induction of neurotrophic factors through ERK activation.

In situ assembly states of rat adipocyte glucose transport protein in plasma membrane (PM) and in microsomal pool (MM) were assessed by measuring target size (TS) of D glucose-sensitive, cytochalasin B binding activity. High energy radiation inactivated the binding in both PM and MM by reducing the total capacity of the binding (B/sub T/) without affecting the dissociation constant (K/sub D/). The reduction in B/sub T/ as a function of radiation dose was analyzed based on classical target theory, from which TS was calculated. TS in the PM of insulin-treated adipocytes was 58 KDa. TS in the MM of noninsulin-treated and insulin-treated adipocytes were 112 and 109 KDa, respectively. With MM, however, inactivation data showed anomalously low radiation sensitivities at low radiation doses showing a shoulder in the semilog plots, which may be due to an interaction with a radiation sensitive inhibitor. With these results, they propose the following model: Adipocyte ...

1987-05-01

497

Insulin-stimulated conversion of D-[5-"3H] glucose to "3HOH in the perifused isolated rat adipocyte

Compounds isolated from Magnolia officinalis such as magnolol, honokiol and obovatol exhibit several pharmacological effects on CNS including depressant, anxiolytic and anticonvulsant effects, as well as neuroprotective effects against chemical and heat damages. Recently, honokiol was found to have a neurotrophic effect in fetal rat cortical neurons. In the present study, we show that 4-O-methylhonokiol, a novel compound from Magnolia officinalis, promotes neurite outgrowth in a concentration- dependent manner in rat embryonic neuronal cells. In parallel with the neurite outgrowth activity, the expression of neurite outgrowth marker proteins is also increased by treatment with 4-O-methylhonokiol. We also found that 4-O-methylhonokiol promotes the release of NGF and BDNF into cell culture medium. In addition, lower concentration of 4-O-methylhonokiol (1 and 2 lM) further enhanced neurite outgrowth and expression of neurite outgrowth marker proteins in the presence of NGF (50 ng/ml) or ...

2009-12-01

498

Inhibitor of DNA synthesis is present in normal chicken serum

Characteristics of basal and insulin-stimulated glucose utilization by perifused adipocytes have been investigated by measuring the formation of "3HOH from D-(5-"3H) glucose. At a glucose concentration of 0.55 mmol/L, basal glucose utilization ranged from 0.5 to 1.0 nmol/min/10(6) cells. Perifused adipocytes showed a maximal response to insulin of a threefold to fourfold increase in the conversion of (5-"3H) glucose to "3HOH with a half-maximal response at an insulin concentration of 20 microU/mL. The response to insulin was blocked by phlorizin and cytochalasin B, competitive inhibitors of glucose transport, consistent with an effect of insulin on glucose transport. Insulin increased the Vmax for glucose metabolism but had no effect on the apparent affinity for glucose utilization. The characteristics of glucose utilization and the stimulation of glucose metabolism by insulin in the perifused adipocyte are therefore similar to characteristics previously observed ...

499

A newly synthesized glycine derivative to control uniform and pitting corrosion processes of Al induced by SCN"- anions - Chemical, electrochemical and morphological studies

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 actions other than ...

1986-03-05

500