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GPR119 is a Class A (Rhodopsin-like) G protein-coupled receptor highly expressed in pancreatic β-cells and enteroendocrine cells. It plays a crucial role in glucose homeostasis by potentiating glucose-stimulated insulin secretion and stimulating the release of incretin hormones such as GLP-1. Activation of GPR119 leads to increased cAMP production. It is considered a therapeutic target for type II diabetes mellitus and obesity due to its ability to enhance insulin secretion, improve glucose tolerance, and reduce food intake.
Agonist binding stimulates the Gαs subunit, activating adenylate cyclase and increasing intracellular cAMP levels, leading to potentiation of glucose-stimulated insulin secretion (GSIS) from pancreatic β-cells and stimulation of incretin hormone release from enteroendocrine cells.
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