格宁生物相关实验 GLP-1:β-Arrestin/ Internalization Assay/Gs cAMP/Reporter gene检测 参考文献 Pabreja K, Mohd MA, Koole C, Wootten D, Furness SG. Molecular mechanisms underlying physiological and receptor pleiotropic effects mediated by GLP-1R activation. Br J Pharmacol. 2014 Mar;171(5):1114-28...
Understanding into the factors that regulate GLP-1R internalization and recycling may shed light on the insulinotropic properties of these ligands. Disclosure S. M. Gray: None. K. Sloop: Employee; Self; Eli Lilly and Company. P. Ravn: None. J. Campbell: None. D. A. D'alessio: Advisory ...
Intracellular loop and C-terminal tail: The intracellular portion of GLP-1R contains several loops and C-terminal tails that are involved in receptor internalization, signal transduction, and interaction with G proteins.Signal transduction: Certain sequences in the intracellular portion are able to bind...
Post-stimulation, GRK phosphorylates serine and threonine residues on the GLP1R C-terminal tail, which leads to recruitment of beta-arrestin(s), desensitization and endocytosis (internalization) (reviewed in [59], [60]). In the endosomal compartment, GLP1R will then: 1) continue to signal via...
Glucagon Like Peptide-1 Receptor;Glucagon Like Peptide 1 Receptor;GLP-1 receptor;GLP1 Receptor;GLP-1-R Historical Background In the 1960s, it was shown that orally administered glucose induces a much stronger insulin response than that induced by intravenously administered glucose, despite the simi...
2) GLP1R/GIPR are 7 transmembrane proteins present at the cell surface in their unstimulated state, so immunostaining/labeling should be observed primarily in this location (with the caveat that constitutive internalization is theoretically possible); and 3) do not rely on specificity of commercial ...
Glucagon Like Peptide-1 Receptor;Glucagon Like Peptide 1 Receptor;GLP-1 receptor;GLP1 Receptor;GLP-1-R Historical Background In the 1960s, it was shown that orally administered glucose induces a much stronger insulin response than that induced by intravenously administered glucose, despite the simi...
Intriguingly, CHU-128 has a similar signaling and regulatory profile to TT-OAD2, where neither agonist promoted β-arrestin recruitment or internalization and both were also very poor agonists for pERK1/2 and calcium mobilization. Nonetheless, CHU-128 was a more efficient agonist for cAMP productio...
Widmann, C.; Dolci, W.; Thorens, B. Agonist-induced internalization and recycling of the glucagon-like peptide-1 receptor in transfected fibroblasts and in insulinomas.Biochem. J.1995,310, 203–214. [Google Scholar] [CrossRef] [PubMed] ...
基本信息 药物类型 小分子化药 别名 dual GLP-1R/GIPR agonists (Carmot Therapeutics)、CT-859 靶点 GIPR x GLP-1R 作用方式 调节剂 作用机制 GIPR调节剂(肠抑胃肽受体调节剂)、GLP-1R调节剂(胰高血糖素样肽-1调节剂) 治疗领域 肿瘤消化系统疾病其他疾病 ...