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br GPR a G protein coupled receptor GPCR was
2022-05-17
GPR35, a G protein-coupled receptor (GPCR), was discovered and classified as an orphan GPCR in 1998 and deorphanized in 2006 by the discovery of kynurenic Azidobutyric acid NHS ester mg as the endogenous agonist. Since its discovery, limited references on the GPR35 receptor have appeared, due in
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As disclosed in our preceding paper medicinal chemistry
2022-05-17
As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Disuflo Cy5 azide mg
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The biological activity at GPR a of
2022-05-17
The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu
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GW was also the starting point for a study
2022-05-17
GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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Lamina II SG spinal cord neurons play an
2022-05-16
Lamina II (SG) spinal cord neurons play an important role in regulating nociceptive input from the periphery [20,21]. Moreover, lamina II neurons are concentrated with glycinergic or GABAergic inhibitory interneurons. Therefore, it is possible that β-alanine might modulate nociceptive transmission i
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It is known that hypercapnia as well
2022-05-16
It is known that hypercapnia, as well as hypoxia, can result in a decrease in body temperature, but the mechanisms involved are not very well known (Barros and Branco, 1998; Saiki and Mortola, 1996). One N1-Methyl-ATP is that when there is an acute hypercapnic exposure, acidosis plays an inhibitory
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Spermine NONOate br Materials and methods br Acknowledgments
2022-05-16
Materials and methods Acknowledgments Introduction Gentiooligosaccharides are novel functional oligosaccharides composed of glucose units linked through β-1,6 glycosidic bonds, examples of which include gentiobiose, gentiotriose and gentiotetraose (Barreteau et al., 2006, Kim et al., 2003,
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76 2 Type diabetes mellitus is characterised by two major
2022-05-16
Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta 76 2 [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insulin resistance in periphe
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Phylogenetic trees of receptors for
2022-05-16
Phylogenetic trees of receptors for peptides similar to glucagon from diverse vertebrate species typically are similar to the tree presented in Fig. 3 (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et al., 2005, Cardoso et al., 2006, Ng et al., 2010, Park et al., 2013, Hwa
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In Solloway and colleagues reported that mice
2022-05-16
In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino factor xa inhibitors dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of ra
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angiotensin 1 mg Neither GIP nor GIPR SNPs were
2022-05-16
Neither GIP nor GIPR SNPs were associated with occurrence of fractures in the OPRA cohort (Table 4). Discussion The basis for this study lies in the role of glucose-insulinotropic peptide (GIP) hormone in the regulation of insulin secretion as well as its anabolic effect on osteoblasts and inhib
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Analysis of the GHSR screening data for inactive library mem
2022-05-16
Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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br A small conductance chloride channel
2022-05-16
A small conductance chloride channel (SCC) In addition to the above-described channels, a 5pS SCC has been encountered in electrophysiological recordings. This channel, exhibiting long periods of opening separated by long intervals of closing, showed the same characteristics as the SCC described
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orthopoxvirus variola Cx is a phosphoprotein that is
2022-05-16
Cx43 is a phosphoprotein that is predominantly phosphorylated in the control state. Cx43 can be phosphorylated by a number of kinases and dephosphorylated by protein phosphatases such as PP1 and PP2A [6], [10]. Posttranslational phosphorylation of Cx43 is thought to influence intercellular coupling
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The role of GJs in liver fibrogenesis was
2022-05-16
The role of GJs in liver fibrogenesis was studied recently. Studies showed a significant decrease in liver fibrosis in Cx32 knockout mice compared to wild-type mice. Although the mechanism underlying this protective effect of Cx32 deletion is not clear, reduced oxidative stress was suggested as a po
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