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In this study our result
2021-10-08
In this study, our result suggests that exogenous GR agonist DEX and GR inhibitor RU486 can affect dopaminergic neurotransmitters in the brain. Pituitary adenylate cyclase-activating polypeptide (PACAP), an endogenous neuropeptide, can regulate the synthesis and release of catecholamine. McArthur et
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AP1903 Ketamine has recently been found to
2021-10-08
Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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br General features of FGFRs and inhibitors
2021-10-07
General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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ADAM has two alternative splicing forms a membrane
2021-10-07
ADAM12 has two alternative splicing forms, a membrane-anchored long form (ADAM12-L) and a secreted short form (ADAM12-S). Both the long and short forms have metalloproteinase, disintegrin, cysteine-rich, and epidermal growth factor-like domains and can shed pro-heparin binding-epidermal growth facto
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Interestingly evidence has emerged recently that suggests no
2021-10-07
Interestingly, evidence has emerged recently that suggests noncanonical roles of EZH2 in various cancers. For example, in addition to histone H3, EZH2 has been shown to methylate non-histone substrates, such as Jarid2 and STAT3, to regulate their transcriptional activities (He et al., 2012, Sanulli
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To understand the structural basis for the
2021-10-07
To understand the structural basis for the mode of action of indole-based compounds the crystal structures of bound to both the wild type and A128T IN CCDs have been solved. The X-ray crystallography studies have revealed that binds at the IN dimer interface in the principal LEDGF/p75 binding pock
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Taken together the four HRs couple
2021-10-07
Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc
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br sGC cGMP PKG pathway in regulation of platelet small
2021-10-07
sGC/cGMP/PKG pathway in regulation of platelet small GTPases All classical Rho family members of small GTPases including RhoA, Rac, Cdc42, some atypical Rho GTPases like RhoB, RhoF and RhoG, and also Ras family members N-Ras, K-Ras, Rap1A, Rap1B, Rap2A and Rap2B, and the Ras-related GTPases of th
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In summary we have successfully identified a series of poten
2021-10-07
In summary, we have successfully identified a series of potent and selective GSNOR inhibitors having imidazole and tetrazole functional groups in both end of the core structure and many compounds have been identified with IC: the subject of future publication. Acknowledgements We would like to th
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Waldeck Weiermair et al demonstrated that in endothelial cel
2021-10-07
Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp
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2-Methoxyestradiol synthesis In this study we describe the r
2021-10-07
In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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New follicular wave emergence is associated closely with
2021-10-07
New follicular wave emergence is associated closely with the stage of the estrous AI-10-49 (Sirois and Fortune, 1988). As indicated by results from the present experiment, cows that had regression of the largest follicle on Day 0 of treatment onset had follicle wave characteristics that were consis
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C steroids and their glycosylation products distribute widel
2021-10-06
C21 steroids and their glycosylation products distribute widely in Asclepiadaceae plants. Their anticancer activities have been shown in different human cell lines and in vivo animal experiments [[27], [28], [29], [30], [31], [32]]. However, the mechanisms of their anticancer activities are still un
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To ensure the induction of CYP enzymes by several
2021-10-06
To ensure the induction of CYP enzymes by several inducers, specific monooxygenase activities of variously induced, uninduced and pooled liver microsomes were compared (Fig. 3). Although 3-MC, phenobarbital, acetone, and dexamethasone could induce CYP1A-, CYP2B-, CYP2E1-, and CYP3A-selective enzyme
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br Conclusions br Introduction Bioinformatics analysis shows
2021-10-06
Conclusions Introduction Bioinformatics analysis shows that there are about 300,000 G-rich sequences in human genome if searching with the consensus sequence (G3+N1-7G3+N1-7G3+N1-7G3+) [1], and their localizations are non-random. These G-rich sequences always localize in functional regions, su
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