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br Conclusions Our in vitro and
2022-03-07

Conclusions Our in vitro and in vivo data collectively demonstrate that zifaxaban is effective in preventing thrombus formation via direct and specific inhibition of FXa in a dose-dependent manner. Furthermore, zifaxaban has a potency that is similar to that of rivaroxaban and shows a similar or
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AdipoRon receptor br Factor Xa an enzyme in the coagulation
2022-03-07

Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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A pyrimidine class of compounds
2022-03-07

A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove
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The structures of KDM A
2022-03-07

The structures of KDM4A revealed a Cys-His Zn(II) binding site that is close to the substrate binding spot, which bioinformatic analyses indicated was not present in any other histone demethylase subfamily. Therefore, an alternative method to inhibit the KDM4 family (95) would be to use compounds th
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Sulforaphane The first suggestion that histamine may play a
2022-03-07

The first suggestion that histamine may play a role in memory consolidation was from Almeida and Izquierdo (de Almeida & Izquierdo, 1986) who showed that the immediate posttraining intracerebroventricular (i.c.v.) administration of 1–10ng of the drug were found to enhance the retention of one-trial
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The molecular mechanism of gliotransmitter
2022-03-07

The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular Celastrol of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in glutamate relea
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In our substudy patients carrying the Ile
2022-03-07

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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TMC125 br Disp Cleavage and Membrane Trafficking
2022-03-07

Disp Cleavage and Membrane Trafficking Knowledge of how Disp is regulated in Shh-producing TMC125 to control ligand deployment has, until recently, remained limited. Early studies examining Disp function in Madin–Darby Canine Kidney (MDCK) cells and Drosophila tissue suggested that it is likely
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Cyclopamine synthesis GSTP is a class Glutathione S transfer
2022-03-07

GSTP1 is a π-class Glutathione S-transferase (GST-π) enzyme involved in tumor suppression by protecting Cyclopamine synthesis against genomic damage mediated by various oxidants. Although the loss of GSTP1 function by hypermethylation has been reported as a common epigenetic alteration in prostate c
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The experiments reported herein were designed to test
2022-03-07

The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, wh
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Notably Cu labeled dimeric exendin subunit which
2022-03-07

Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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Previous studies have shown that zinc interacts
2022-03-04

Previous studies have shown that zinc interacts with other allosteric modulators at the glycine receptor (Kirson et al., 2013, McCracken et al., 2010, McCracken et al., 2013). Of note, the chelation of zinc via tricine decreases the effects of alcohol at α1-, α2-, and α3-containing glycine receptors
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br Conclusion These are exciting times in
2022-03-04

Conclusion These are exciting times in EAAT research. The discovery and use of the GltPh and GltTk transporters as model systems for EAATs has provided detailed understanding of structure–function aspects of the transporters. Moreover, recent studies into the physiological functions of the transp
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Although EAAT may not be involved
2022-03-04

Although EAAT3 may not be involved in the induction of morphine-induced CPP, our results suggest that other EAATs may play a role in the behavior because riluzole, an EAAT activator (Frizzo et al., 2004, Fumagalli et al., 2008), abolished morphine-induced CPP. Consistent with this suggestion, a few
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In accordance with its similarity to classical
2022-03-04

In accordance with its similarity to classical NLSs, Importin α3 was recently reported as a nuclear transport receptor for Ci (). We therefore superimposed the Gli1 NLS model with the Importin α2 structure (3EFX), which has a structure similar to Drosophila Importin α3 () (Fig. 4.4B). Gli1 NLS fitte
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