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The active site of PS is
2022-01-15

The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed
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The objective of this study is
2022-01-14

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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The other possibility for the lack
2022-01-14

The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,
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2881 synthesis br Materials and methods br Results br Discus
2022-01-14

Materials and methods Results Discussion Numerous studies have identified important roles for HIF-1α in cellular function and dysfunction through its transcriptional activity [4]. A few studies have reported that HIF-1α is translocated to the mitochondria in human and mouse cancer cell line
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Our previous study provided some evidence that the
2022-01-14

Our previous study provided some evidence that the pre-treatment of livers with rapamycin induces the expression of HO-1 and Prx-1 (Kist et al., 2012). The present results define the dose-response curve for the induction of HO-1 and Prx-1 expression by rapamycin in normal hepatocytes. While, in the
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W 54011 receptor br Acknowledgements This work has been supp
2022-01-14

Acknowledgements This work has been supported by TSTAR USDA and Florida Citrus Advanced Technology Program Grants to D.B., C.P and R.S. One of us (D.B.) is an established scientist fellow at the Oak Ridge Institute for Science and Education (ORISE). This research was supported in part by an appoi
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The biological function of NPRA is demonstrated primarily th
2022-01-14

The biological function of NPRA is demonstrated primarily through the ANP/BNP-dependent GC catalytic activity of the receptor and the production of cGMP, which is regulated by several factors, including hormones, growth factors, physiological milieu, and the ligand itself [26,34,[36], [37], [38], [3
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Toxoplasma gondii is an exceptionally tractable apicomplexan
2022-01-14

Toxoplasma gondii is an exceptionally tractable apicomplexan parasite that expresses a limited yet representative subset of apicomplexan cyclase orthologs, making it an ideal model for investigating cyclic nucleotide signaling in Apicomplexa. Of the five putative nucleotide cyclases, only TgACα1 and
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Several studies have found that GPR possesses a distinct
2022-01-14

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected BCATc Inhibitor 2 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR1417
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The synthesis of is shown
2022-01-14

The synthesis of is shown in . The ---Boc--diaminopropanoic acid--butyl ester () fragment was synthesized in four steps from Boc--asparagine (). The key step in this synthesis was a Hofmann rearrangement of the terminal carboxamide, which was performed according to the elegant protocol of Zhang that
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Additionally increased GLO gene expression protein expressio
2022-01-14

Additionally, increased GLO1 gene expression, protein expression, and activity have been reported in a variety of cancers, including breast,22, 23, 24 pancreatic, melanoma, and prostate.27, 28, 29 Vince and Daluge proposed that inhibitors of GLO1 could serve as anti-tumor agents, by increasing conce
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br Materials animals and methods br Results br
2022-01-14

Materials, animals and methods Results Discussion This study presents mice with a missense point mutation in R258 of FFAR1 that has functional consequences. Firstly, in islets of Ffar1R258W/R258W mice, both the physiological agonist palmitate and the synthetic agonist TUG-469 were unable to
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Proteinase K receptor In contrast to short term
2022-01-14

In contrast to short-term effects, long-term exposure of beta cells to FFAs impairs insulin secretion and triggers apoptosis [13]. The deleterious effects of FFAs have been linked to altered glucose/fatty Proteinase K receptor oxidation cycle [13], decreased NADPH content [14], endoplasmic reticulu
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tie2 br Materials and methods br Results Analysis of the
2022-01-14

Materials and methods Results Analysis of the post-mortem human prefrontal cortex by western blotting indicated that GLAST expression was increased 1.6-fold in the extracts of alcoholic brains relative to controls (Fig. 1A and B). To resolve the distinct sub-pools of GLAST within our samples w
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br Materials and methods br
2022-01-14

Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast DPP4 Activity Fluorometric Assay Kit mg by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of
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