2022
DOI: 10.1101/2022.08.17.504231
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An examination of the divergent spatiotemporal signaling of GLP-1R versus GIPR in pancreatic beta cells

Abstract: The incretin receptors, glucagon-like peptide-1 receptor (GLP-1R) and glucose-dependent insulinotropic polypeptide receptor (GIPR), are class B GPCRs and prime therapeutic targets for the treatment of type 2 diabetes (T2D) and obesity. They are expressed in pancreatic beta cells where they potentiate insulin release in response to food intake. Despite GIP being the main incretin in healthy individuals, GLP-1R has been favoured versus GIPR as a therapeutic target due to GIPR responses being blunted in T2D patie… Show more

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“…Both GLP-1 and GIP stimulate insulin secretion from pancreatic beta cells, with GIP also stimulating alpha cells to secrete glucagon (Manchanda et al, 2022). These functions occur via binding and activation of their cognate secretin-like (class B) G protein-coupled receptors (GPCRs).…”
Section: Incretin Signalling and Biased Agonism: Basic Conceptsmentioning
confidence: 99%
“…Both GLP-1 and GIP stimulate insulin secretion from pancreatic beta cells, with GIP also stimulating alpha cells to secrete glucagon (Manchanda et al, 2022). These functions occur via binding and activation of their cognate secretin-like (class B) G protein-coupled receptors (GPCRs).…”
Section: Incretin Signalling and Biased Agonism: Basic Conceptsmentioning
confidence: 99%