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br Materials and methods br Results br Discussion Enolase
2019-09-30
Materials and methods Results Discussion Enolase (2-phospho-D-glycerate hydrolase) is a glycolytic enzyme that is also involved with various important roles in the intracellular and extracellular space (Copley, 2003; S. Zhang et al., 2015) such as transcriptional regulation, apoptosis, grow
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purinergic receptor Although high concentrations of SCR G an
2019-09-30
Although high concentrations of SCR7-G and SCR7-R inhibited LigIV as reported [11], the SCR7 derivatives were more effective inhibitors of LigIIIα and, in particular, LigI. Although it is possible that differences in the DNA substrate underlie this discrepancy, it appears more likely that this refle
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In our current work we have undertaken liquid phase
2019-09-30
In our current work, we have undertaken liquid phase combinatorial synthesis methods for the synthesis of 1,2,5-trisubstituted benzimidazole derivatives as hDHODH inhibitors. Synthesised GDC-0994 were also screened by molecular docking studies over the reported hDHODH structure. The synthesised mol
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MTX and MTXPGs block the activity of
2019-09-30
MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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Steady state mRNA levels of
2019-09-30
Steady-state mRNA levels of CYP3A isoforms were not changed during liver insufficiency. Suppression of these isoforms was observed only at the protein and activity levels, suggesting a nongenomic mechanism of CYP3A isoform downregulation during liver insufficiency. Nonetheless, transcriptional activ
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AMD is equally active against a broad range
2019-09-30
AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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To the best of our knowledge this study
2019-09-30
To the best of our knowledge, this study was the first to demonstrate in vitro and in vivo that the lipolytic effect of kinsenoside results from coordination between PKA and AMPK pathways. We validated the lipolytic effect of kinsenoside in vivo and the effect of PKA activation on the modulating AMP
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In addition PK studies on indicate that
2019-09-29
In addition, PK studies on indicate that it displays excellent bioavailability, pharmacological and toxicological parameters., A concern was initially raised about compound that it may cause EPAC denaturing properties and false positives. To address this issue, Cheng and co-workers have conducted a
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br Substrate characterization of candidate peptide reporters
2019-09-29
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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Our finding that activating DDR variants are a cause of
2019-09-29
Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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Recent results from our group found that SPMs not
2019-09-29
Recent results from our group found that SPMs, not only play a part in terminating inflammation, but also have a physiological role in conjunctival goblet PRT-060318 to maintain ocular surface health in the absence of disease. Amongst the SPMs that are effective in the conjunctiva are resolvin D1 (
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Altogether these data suggested that GlmU
2019-09-29
Altogether these data suggested that GlmU might be involved in the M. smegmatis biofilm mediated defence mechanisms. GlmU belongs to a metabolic pathway leading to UDP-GlcNAc from fructose-1-phosphate involved in the biosynthesis of peptidoglycan and lipopolysaccharide (Fig. 8). Recently, we demonst
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br Authors contributions br Acknowledgements br Introduction
2019-09-29
Authors’ contributions Acknowledgements Introduction Retinoic Sulfo-NHS-LC-Biotin is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic acid is made by oxidat
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Kinase Inhibitor Library pathway The binding of collagen X t
2019-09-29
The binding of collagen X to DDR2 differs from the binding of collagen X to α2β1 integrin in that the triple helical conformation is essential for DDR2 binding. We previously reported that heat denatured pepsinised collagen X supported cell adhesion via α2β1, indicating that the triple-helical confo
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CA-074 Me Introduction Tumor necrosis factor TNF
2019-09-29
Introduction Tumor necrosis factor (TNF) is a pro-inflammatory mediator with the capacity to induce apoptosis (Benderska et al., 2012). Recent reports have shown that TNF might trigger cell death, at least in part, by directly affecting the reorganization of the CA-074 Me cytoskeleton (Campos et a
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