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br GPR is a class A GPCR
2021-11-01

GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine TRAM-34 which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell sig
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Acknowledgments br Introduction The gut derived hormone oxyn
2021-11-01

Acknowledgments Introduction The gut-derived hormone oxyntomodulin (OXM) is a naturally occurring dual agonist of both the glucagon receptor (GCGr) and glucagons-like peptide 1 receptor (GLP-1r). Structurally OXM is the 29 c-src of glucagon with a C-terminal octapeptide tail. Administration of
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Methicillin sodium salt receptor br In vivo actions of GLP G
2021-11-01

In vivo actions of GLP-1/GLP-1R agonists on the vascular endothelium Using contrast-enhanced ultrasound, male Sprague Dawley rats receiving an intravenous infusion of native GLP-1 (30 pmol/kg/min) for 2 h demonstrated significant improvements in both microvascular blood volume and microvascular b
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The biological actions of ghrelin are mainly
2021-11-01

The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept
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br Materials and methods br Results br Discussion Several pe
2021-11-01

Materials and methods Results Discussion Several peripheral hormones that are involved in the central regulation of energy homeostasis, such as leptin, insulin, and amylin [34], [35], [36], [37], [38], cross the BBB by saturable and unsaturable mechanisms. Whether these transport processes
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8711 Emergent studies have recently shown that
2021-11-01

Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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br Presenilins and Wnt catenin signalling
2021-11-01

Presenilins and Wnt/β-catenin signalling Several groups have provided substantial data indicating that PS1 acts as a negative modulator of the transcriptional activity of the β-catenin/Tcf-4 complex (Fig. 4) [120], [121], [122]. β-Catenin is a multifunctional protein that was first described as a
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The first FPR ligand described is the fMLF peptide
2021-11-01

The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o
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Of the cases identified herein three known
2021-11-01

Of the 52 cases identified herein, three known and 11 novel FGFR fusion partners were identified. Notably, an oligomerization domain, including coiled-coil dimerization domains similar to that seen in echinoderm microtubule associated protein like 4 gene (EML4), which is the most common ALK partner
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br Materials and methods br Acknowledgments We are
2021-11-01

Materials and methods Acknowledgments We are grateful for financial support from the National Natural Science Foundation of China (Grants No. 81661148046 and 81773762, China) and the “Personalized Medicines—Molecular Signature-based Drug Discovery and Development”, Strategic Priority Research
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The only approved H R antagonist inverse agonist is
2021-11-01

The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or
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br Materials and methods br Results br Discussion Genetic
2021-11-01

Materials and methods Results Discussion Genetic analyses conducted here were based on specific features of PhyChem indexes for nt dimers extracted to generate a numerical sequence representation, which was used to build models for distinguishing HVR1 variants between CIP and MIP. This data
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The fact that GSK recognition of its
2021-10-29

The fact that GSK-3 recognition of its substrate involves pre-phosphorylation supports the rational for using synthetic phosphorylated peptides as substrate competitive inhibitors [57]. Phosphorylated peptides derived from the N-terminal pseudosubstrate sequence of GSK-3β were very weak inhibitors o
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torin While a role for YAP
2021-10-29

While a role for YAP/TAZ signaling in oligodendrocytes has not been described, these torin are also responsive to mechanical stimuli. OPC proliferation and migration can be altered by plating on substrates of varying stiffness [20], resulting in differentiation in a density-dependent manner. Plating
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The spatial effects of Ebi involve the creation of a
2021-10-29

The spatial effects of Ebi2 involve the creation of a moderate bias in CD4+ T cell distribution toward the LN periphery. Is this modest effect meaningful in an evolutionary sense? In this regard, we think the following considerations are relevant. First, asymmetric CD4+ T cell positioning is highly
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