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cudc 907 GKRP binds to the inactive super open conformation
2022-07-13

GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t
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br Experimental br Results br Discussion The use of
2022-07-13

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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br Conclusions We have shown that despite the development of
2022-07-13

Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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The in vivo biological activity
2022-07-13

The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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I-BET 151 hydrochloride Moreover the ubiquitous expression o
2022-07-13

Moreover, the ubiquitous I-BET 151 hydrochloride of the OTR and GHSR was also observed in hippocampal and hypothalamic primary culture, indicating that this expression pattern is likely due to basal activity of these receptors. GPCR trafficking under control conditions has been linked to biased sig
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In the present study we also found
2022-07-12

In the present study, we also found that specificity concerns persist for antibody-based tools, like ELISAs. Measuring the same human plasma sample with four different commercial galanin ELISA kits produced four widely different galanin concentrations. No recovery of synthetic galanin peptide added
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In total strains with relatively rapid acid
2022-07-12

In total, 5 strains with relatively rapid acid-producing ability (MA14, 15M2, DQHXNQ38–12, 5G2, and 6G5) were selected for further analysis. Compared with the strains ATCC19435, ZN8, and D-XJ4–12, which were used as controls, these 5 strains exhibited significantly different growth and titratable ac
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GPR which is also known as FFA receptor
2022-07-12

GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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br Ethics statements br Introduction Hepatocellular carcinom
2022-07-12

Ethics statements Introduction Hepatocellular carcinoma (HCC) is the fifth most common malignant tumor and the third leading cause of cancer-related mortality worldwide, with rapidly-increasing incidence in recent years [1,2]. Mounting evidence shows that viral hepatitis, toxin exposure, non-a
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Bay 65-1942 HCl salt br Results and discussion Computer
2022-07-12

Results and discussion Computer modelling studies suggested that the endocyclic oxygens in furocoumarin derivatives, such as Bay 65-1942 HCl salt 3a (Fig. 1), could also coordinate metal ions in the HIV-1 IN enzyme active site and inhibit the integration of viral DNA. The coumarin moiety is found
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In this study we evaluated and compared the
2022-07-12

In this study we evaluated and compared the kinetics and duration of the oral and systemic HPV-16 and HPV-18 specific antibody response to three doses of the qHPV vaccine in mid-adult aged HIV+ men from the AIDS Malignancy Cohort (AMC) 052 trial and mid-adult aged HIV− men from the Mid-Adult Male [M
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The newest histamine receptor to be discovered
2022-07-12

The newest histamine receptor to be discovered is the H4 receptor, which was identified in humans and cloned in 2000 (Thurmond, 2010). Genetically, the H4 receptor is closely related to the H3 receptor, but is restricted to jsh within the spleen, intestines and thymus, and to immune cells such as T
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In various models histamine has been shown to
2022-07-12

In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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Type IIIa b the ligand
2022-07-12

Type IIIa/b – the ligand dependent oncogenic Hh pathway (paracrine or reverse paracrine mode) is mediated by paracrine activation and is usually encountered in embryonic development, but also in installation and progression of cancer [58]. Specifically, Hh ligands secreted by malignant WDR5 0103 ac
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br Discussion br Conflict of
2022-07-12

Discussion Conflict of interest Acknowledgements We thank Rosetta Barkley for expert technical assistance. We thank Robin Maser, James Calvet, Darren Wallace, and Jovanka Koo for many helpful discussions and expert technical advice. This work was supported by National Institutes of Health,
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