G protein-coupled receptor class C group 5 member B (GPRC5B) (GPRC5B)

G protein-coupled receptor class C group 5 member B (GPRC5B) is an orphan G protein-coupled receptor (GPCR) belonging to the class C family, characterized by its transcriptional induction by retinoic acid (UniProt P46091). It is widely expressed in the central nervous system, adipose tissue, kidneys, and lymphatic endothelial cells, where it modulates critical physiological processes such as insulin secretion, vascular smooth muscle contractility, and lymphangiogenesis (PMID: 32063046, 24121135). GPRC5B has been identified as a potential therapeutic target for metabolic disorders, including obesity and type 2 diabetes, as well as cardiovascular diseases like hypertension and atherosclerosis (PMID: 31285244). In the brain, it regulates neurogenesis and has been linked to retinoic acid-induced depressive-like behaviors (PMID: 35814944). While no clinical-stage drugs currently target GPRC5B, research has identified small-molecule agonists like 7-fluorotryptamine and explored RNA-targeting strategies, such as siRNA and shRNA, to modulate its expression in disease models. Its role as a mediator of inflammatory responses in podocytes and adipocytes further highlights its significance as a druggable node for inflammatory and fibrotic conditions.

Other names

RAIG2RAIG-2Retinoic acid-induced gene 2 proteinG-protein coupled receptor family C group 5 member BGPRC5B mRNA

Agonism of the GPRC5B receptor or modulation of its mRNA expression via RNA interference.