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Two classes of histones demethylases have
2022-02-15

Two classes of histones demethylases have thus far been identified: the Jumonji C (JmjC) domain-containing proteins and the amine oxidase domain (AOD)-containing proteins. They have distinct enzymatic mechanisms and substrate specificity. The JmjC domain is conserved through evolution and belongs to
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All of the designed compounds was synth http www apexbt
2022-02-15

All of the designed compounds – was synthesized from -cyclopropane aldehyde , which was prepared following a procedure we reported previously. Treatment of with 4-chlorobenzene-1,2-diamine in pyridine constructed benzimidazole structure of , which was subjected to deprotection and subsequent oxidat
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The finding of histamine action on
2022-02-15

The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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In this study there is a limitation in
2022-02-15

In this study, there is a limitation in the study of sex differences. Only female rats were used in our study. This is because the rats cannot urinate autonomously after SCI. Manual Linsitinib emptying was needed until reflex bladder emptying was established (Lu et al., 2008, Ma et al., 2015). Beca
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In our substudy patients carrying the Ile
2022-02-15

In our substudy, patients carrying the Ile/Val or Val/Val genotypes had significantly worse DFS compared to patients carrying the Ile/Ile genotype, after adjustment for potential confounders. Two previous studies examining the association between HER2 Ile655Val polymorphism and trastuzumab response
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pitavastatin The replacement of the P butyl urea
2022-02-15

The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P
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Tubastatin A HCl Since its development the HCV replicon syst
2022-02-15

Since its development, the HCV replicon system (Lohmann et al., 1999) has been a critical tool in the HCV antiviral discovery process (Gottwein et al., 2009, Imhof and Simmonds, 2010, Lohmann et al., 1999, Pietschmann et al., 2001, Imhof and Simmonds, 2010, Gottwein et al., 2009). The replicon assay
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A number of in vivo studies have investigated the antitumor
2022-02-14

A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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Migratory properties of Treg are extremely important for
2022-02-14

Migratory properties of Treg are extremely important for the potential in vivo application. Therefore, the observed expression of CXCR3 on almost all obtained insulin-specific Treg is crucial for directing SB 203580 hydrochloride into the inflamed tissue (in this case pancreatic islets). CXCR3 respo
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GSK2118436 br Acknowledgements Support provided by projects
2022-02-14

Acknowledgements Support provided by projects PTDC/SAU-MIC/115178/2009 and PEst-OE/QUI/UI0612/2011 from the Fundação para a Ciência e a Tecnologia, Portugal. Diabetes Mellitus Diabetes mellitus is a chronic, multisystem metabolic disorder caused by a combination of environmental and genetic f
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The kinetic data obtained from
2022-02-14

The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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Through the analysis of various
2022-02-14

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic TWS119 mg motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK
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Ning et al showed that LPC
2022-02-14

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Caffeine decreased EAAT and EAAT
2022-02-14

Caffeine decreased EAAT1 and EAAT2 BIBR 1532 levels in P2 fraction, as well as [3H]d-aspartate uptake; however, as soon as caffeine is removed from incubation, [3H]-d-Aspartate uptake is recovered to control levels, eliminating the possibility of caffeine as a cell death inducer. In resume, our dat
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In this study we investigated the contribution of GCK G
2022-02-14

In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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