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Many investigators participated in the
2020-10-26

Many investigators participated in the studies on the regulation of the peptide yy and experiments indicated that the process was conserved across many eukaryotic species including humans [127]. Because cancer cells exhibit dysregulated cell division along with the presence of abnormal chromosome nu
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Previously we have shown that
2020-10-26

Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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The oxidation of the lipid fraction of
2020-10-26

The oxidation of the lipid fraction of meat is an extremely complex process because of the high sensitivity of oxidation products to decomposition, their reactions with other components, the complex effect of catalysts and the presence of antioxidants. These changes are the main cause of limited she
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Glycolysis is important to maintain the vital functions of
2020-10-23

Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its growth hormone secretagogue metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egr
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br Acknowledgments br Multicellular organisms respond rapidl
2020-10-23

Acknowledgments Multicellular organisms respond rapidly, and adapt to cellular stress to maximize cell survival. The cellular stress response, also called (ISR), is universally conserved and independent of the stressor. ISR induces rapid, transient reprogramming of cellular protein translation
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br Transparency document br Main Text The centrosome is
2020-10-23

Transparency document Main Text The centrosome is a non-membrane-bound organelle found in most animal cells. It has several important functions, including control of cilia formation, microtubule organization and nucleation, spindle assembly and transport of organelles and vesicles. Centrosomes
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Several highly potent CysLT receptor antagonists with large
2020-10-23

Several highly potent CysLT1 receptor antagonists with large structural PKI-402 have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and thiazoles.
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A cocktail approach can detect the activities of multiple
2020-10-23

A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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The in vitro enantioselective metabolism
2020-10-23

The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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br Results and discussion Compounds
2020-10-23

Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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The molecular mechanism by which CRM regulates
2020-10-23

The molecular mechanism by which CRM1 regulates IEC apoptosis in CD remains to be explored. As an inhibitor of cyclin E-Cdk2, p27kip1 plays a pivotal role in controlling cell proliferation, S phase entry, and G1 phase exit during development and tumorigenesis [38]. As previously reported, p27kip1 is
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2870 australia Acidic substituents showed moderate biochemic
2020-10-23

Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic 2870 australia were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemi
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In the preclinical evaluation of CRF receptor
2020-10-23

In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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br Allosteric inhibitors In general candidate drugs that
2020-10-22

Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Determination of relative potency EC by
2020-10-22

Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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