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GPR A a G protein coupled receptor
2021-10-08
GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic flt3 [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-mediated inhi
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In vitro studies have shown that some antidepressant drugs b
2021-10-08
In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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The eradication of agonist activity in compound was also con
2021-10-08
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary INO-1001 as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize th
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The overall very satisfactory potency
2021-10-07
The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Senegenin core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sens
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Amphotericin B Conclusions br Author information The obtaine
2021-10-07
Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu
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PK profiles of were evaluated and found to
2021-10-07
PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 cell
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EHop-016 In Kdm c germline and forebrain conditional
2021-10-07
In Kdm5c germline and forebrain conditional knockout mice, RNA sequencing showed the upregulation of a large set of genes, suggesting that Kdm5c functions primarily as a transcriptional repressor [,]. While no changes in global H3K4me3 levels were observed in the knockout neurons, there were thousan
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Pharmacologic approaches of inhibiting GSNOR
2021-10-07
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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Evaluating the plausibility of this selective
2021-10-07
Evaluating the plausibility of this selective scenario is challenging because of the uncertainties concerning the biological role of calpain-10 and the significance of its variants with regard to gene function and disease susceptibility. However, from a strictly evolutionary standpoint, our findings
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In addition to the role of TGR
2021-10-07
In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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br A selective inhibitor of mammalian histone
2021-10-07
A selective inhibitor of mammalian histone deacetylase, trichostatin A, reduces GnRH mRNA expression Epigenetic mechanisms controlling GnRH expression have been reported, and these mechanisms may be involved in the development and maturation of GnRH neurons in the brain (Gan et al., 2012, Kurian
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At this point it needs however
2021-10-04
At this point it needs, however, to be mentioned that most in vivo studies regarding the herein discussed nuclear receptors were performed in rodents, especially in mice. Due to the significant differences in metabolism in mice and humans, not all results are translatable between these species and h
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Brain derived neurotrophic factor BDNF is the most abundant
2021-10-04
Brain-derived neurotrophic factor (BDNF) is the most abundant growth factor in the brain and is critical for neuronal development and synaptic plasticity (Bekinschtein et al., 2008; Lu et al., 2014). Besides playing an important role in mood and cognition, BDNF is also involved in the regulation of
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2768 receptor br Background To treat chronic
2021-10-03
Background To treat chronic HCV genotype (GT) 1-infected patients, telaprevir (TLP) or boceprevir (BOC), first generation protease inhibitors (PIs), were used in combination with pegylated-interferon (PEG-IFN) and ribavirin (RBV) triple therapy [1], [2]. The main weaknesses of the first-generatio
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In this study three potential Otx binding sites were found
2021-10-02
In this study, three potential Otx-2 Leupeptin australia were found in the promoter region of the sheep GnRH gene: −1786 bp to −1770 bp, −825 bp to −819 bp, and − 529 bp to −523 bp. Combined with the results of the double-luciferase assay, it could be inferred that the binding site of Otx-2 in the c
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