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br Experimental br Results br Discussion The
2022-07-27
Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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Receptors for glucagon Gcgr GLP Glp
2022-07-27
Receptors for glucagon (Gcgr), GLP-1 (Glp1r), and GLP-2 (Glp2r) are G-protein coupled receptors (GPCRs) belonging to class B-1 (secretin receptor-like) family of GPCRs (Harmar, 2001, Fredriksson et al., 2003). The mammalian Gcgr, Glp1r, and Glp2r genes, together with the NVP DPP 728 dihydrochloride
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With the identification of small nonpolar substituents at R
2022-07-27
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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The co crystal structure of GPR complexed with
2022-07-27
The co-crystal structure of GPR40 complexed with TAK-875 provided precise structural information for the rational design of novel GPR40 agonists. The key interactions between the carboxylate with the residues Arg183, Arg258, Tyr91 and Tyr240 of GPR40 were observed. And Trp174ECL2 was oriented nearly
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br Introduction For decades regulated apoptosis and unregula
2022-07-27
Introduction For decades, regulated apoptosis and unregulated, accidental necrosis have been considered as the two sole cell death routes in multicellular organisms. With the beginning of the 21st century a paradigm shift has been witnessed by researchers in the field with the recognition that ma
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br Discussion In response to an
2022-07-27
Discussion In response to an increase in glucose or DHA concentration, FBPase showed nuclear import and recruitment in a peripheral cell compartment. Interestingly, FBPase and GS were co-recruited to the periphery of the cells. This is precisely the site where glycogen is initially synthesized an
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br Introduction Ovarian cancer patients have the highest
2022-07-26
Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is cancer estrogen antagonist with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone methy
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In NAFLD models the first hit
2022-07-26
In NAFLD models, the “first hit” is liver fat accumulation, which causes insulin resistance, whereas the interplay of inflammatory cytokines, which causes inflammation, acts as the representative “second hit” [9]. However, recently, the “multiple hit” hypothesis has taken into consideration that mul
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Sometime ago we have described diamino triazines as histamin
2022-07-26
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by 5-Azacytidine australia and zymosan. In this work we descr
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Biochemical and genetic studies indicate that the
2022-07-26
Biochemical and genetic studies indicate that the endosomal sorting complex required for transport (ESCRT) machinery is crucial for Hh exovesicle packaging and morphogen gradient function 39., 43., 44.. In vertebrates, ESCRT proteins promote the release of Shh exovesicles to maintain progenitor cell
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Priming phosphorylation can also generate a
2022-07-26
Priming CT-99021 can also generate a binding site for some protein-interaction domains and adaptor proteins that recruit kinases to phosphorylate more distal sites [36]. Well-characterized phosphoprotein-interacting domains include pTyr-binding SH2 domains present in many nonreceptor TyrKs and the
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Currently the computational chemical biology has been applie
2022-07-26
Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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On the basis of the foregoing set
2022-07-26
On the basis of the foregoing set of considerations, L1 could exert three possible actions on sGC determining its deactivation, schematically depicted in Fig. 6: i) oxidation of Fe2+ to Fe3+; ii) coordination to sGC, conjecturably, via the pyridyl nitrogen of the canthin-6-one; iii) coordinating and
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spleen tyrosine kinase br Materials and methods br Results b
2022-07-26
Materials and methods Results Discussion Directly modulating specific target proteins and signaling pathways with small-molecule drugs or agonistic spleen tyrosine kinase is widely used for cancer metastasis therapies [[39], [40], [41]]. ANXA7 acts as a metastasis suppressor in prostate ca
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One of pathogenesis of COPD is oxidant antioxidant imbalance
2022-07-26
One of pathogenesis of COPD is oxidant/antioxidant imbalance. Indeed, it is well known that chronic tobacco smoking is a major risk factor for the development of COPD, and a defect in the detoxification of reactive species produced by cigarette smoke may predispose smokers to airflow obstruction and
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