Target intelligence / Profile preview

Glucose-dependent Insulinotropic Receptor (GPR119)

Target
GPR119
Molecular classification
G protein-coupled receptor, GPCR, Orphan GPCR
01

Overview

Glucose-dependent insulinotropic receptor (GPR119) is a G protein-coupled receptor primarily expressed in gastrointestinal secretory cells and pancreatic beta cells. Activation of GPR119 stimulates the secretion of incretin hormones (GLP-1 and GIP) and insulin, thereby regulating glucose metabolism. It is a promising drug target for metabolic diseases like type 2 diabetes, obesity, and fatty liver disease.

02

Mechanism of action

Activation of GPR119 leads to increased intracellular cAMP levels, stimulating the release of GLP-1, GIP, and insulin.

03

Biological functions

Signal transductionRegulation of insulin secretionRegulation of incretin hormone secretionRegulation of glucose homeostasis
04

Disease associations

Type 2 diabetesObesityFatty liver diseaseMetabolic disorders
05

Safety considerations

Potential for off-target effects due to GPCR promiscuityRisk of hypoglycemia in susceptible individuals (though considered low under normoglycemic conditions)
06

Interacting drugs

APD597

1 more in the full profile.

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