Target intelligence / Profile preview

G protein-coupled receptor 119 (GPR119)

Target
GPR119
Molecular classification
G protein-coupled receptor, GPCR, Class A (Rhodopsin-like) GPCR
01

Overview

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.

Other names
GPCR2G protein-coupled receptor 119
02

Mechanism of action

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.

03

Biological functions

Signal transductionGlucose homeostasisInsulin secretionIncretin hormone releaseAppetite regulation
04

Disease associations

Type II diabetes mellitusObesity
05

Safety considerations

Potential for hypoglycemia if not acting in a glucose-dependent fashion (though GPR119 agonists are thought to act in this way).
06

Interacting drugs

Oleoylethanolamide (OEA)

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