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The different NO stimulated and ODQ inhibited cNMP patterns
2021-10-07
The different NO-stimulated and ODQ-inhibited cNMP patterns in terms of absolute and relative magnitude and time course reported herein suggest distinct functional roles of cGMP, cCMP and cUMP. Therefore, it will be necessary to dissect cellular effects of these cNMPs in numerous cell systems. For t
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br Materials and methods br Results br Discussion
2021-10-07
Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin 2478 and functionally characterized the majority of the receptors wh
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Starting from commercially available dioxaspiro decan ol
2021-10-07
Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an BAMB-4 catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was obtain
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lomitapide br Materials and methods br
2021-10-06
Materials and methods Results Discussion Defective regulation and inappropriate activation of the HH signaling pathway is implicated in many cancers. SMO targeting inhibitors were the first to enter clinical trials, however complications with acquired resistance and toxicity, also exemplifi
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Recently a lot of synthetic FFA agonists containing acidic
2021-10-04
Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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Corresponding to the different insulinotropic signaling the
2021-10-04
Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Arecaidine but-2-ynyl ester tosylate on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric b
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Earlier we have showed that tumor associated
2021-10-03
Earlier we have showed that tumor associated sFas mRNA isoform profile and splicing factors expression levels in solid tumors do not correspond to profiles that are observed in cell lines [45]. In the present study, for the first time we show that Fas but not Rac1 pre-mRNA's alternative splicing is
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It is important to mention
2021-10-03
It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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The majority of HCV unaware
2021-10-03
The majority of HCV-unaware individuals, for which HCV RNA was obtainable, had active HCV infection and overall almost one-fifth of them had advanced liver disease according to the FIB-4 score; these persons can be classified as having a late HCV diagnosis and are in immediate need of HCV treatment
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N-Acetylneuraminic acid australia Ras small GTPases are crit
2021-10-03
Ras small GTPases are critical molecular switches that connect extracellular signals to intracellular signaling pathways initiated by membrane receptors, such as growth factor receptors and G protein-coupled receptors (Simanshu et al., 2017). When shifting between active GTP-bound and inactive GDP-b
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br Results and discussion br Conclusion In summary starting
2021-10-02
Results and discussion Conclusion In summary, starting from our previous lead xav 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivatives showed good agonist
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It is well known that the expression
2021-10-02
It is well known that the expression of GPR109A is regulated under physiological and pathological conditions. We previously found that GPR109A expression in islet beta-cells increased with age and was up-regulated by interferon-γ (Li et al., 2011). GPR109A levels in Min6 and INS-1E islet beta-cells
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Na K ATPase adenosine triphosphate ATP and astrocytic glutam
2021-10-02
Na+/K+-ATPase, hiv protease inhibitors and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increased
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Recently multiple receptor agonists have been
2021-10-02
Recently, multiple receptor agonists have been developed to treat type II diabetes (Finan et al., 2013, Finan et al., 2015). We have tested novel dual GLP-1/GIP receptor agonists that showed good neuroprotective effects that are superior to single GLP-1 analogues (Cao et al., 2016, Jalewa et al., 20
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br Results br Discussion secretase mediated proteolysis of i
2021-10-02
Results Discussion γ-secretase-mediated proteolysis of integral membrane proteins is required for diverse biological processes (Lal and Caplan, 2011). One γ-secretase target of particular interest is Notch, as recent work has shown Notch activity to be increased in obesity and associated metab
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