Target intelligence / Profile preview

Adhesion G protein-coupled receptor G2 (ADGRG2)

Target
ADGRG2
Molecular classification
G protein-coupled receptor, Adhesion class G protein-coupled receptor, Transmembrane receptor
01

Overview

Adhesion G protein-coupled receptor G2 (ADGRG2), also known as GPR64, is a member of the adhesion family of G protein-coupled receptors predominantly expressed in the male reproductive tract, especially in the epididymis and efferent ducts[2][3][4]. It plays a critical role in regulating fluid reabsorption and maintaining male fertility by mediating signal transduction via G protein pathways (primarily Gs and Gq), affecting the function of downstream effectors such as adenylate cyclase and phospholipase C[2][3]. Mutations in ADGRG2 are implicated in disorders such as congenital bilateral absence of the vas deferens, leading to male infertility[2][3]. Recent structural studies identified steroid hormones, including DHEA, as ligands, providing the basis for ongoing pharmacological research and making ADGRG2 a potential therapeutic target for male reproductive health and related conditions[1].

Other names
G protein-coupled receptor 64GPR64Human epididymis-specific protein 6HE6TM7LN2EDDM6Epididymal protein 6CBAVDX
02

Mechanism of action

Agonist binding (e.g., DHEA) activates G protein signaling via Gs and Gq proteins, leading to stimulation of adenylate cyclase or phospholipase C pathways[1][2][3].

03

Biological functions

Signal transductionRegulation of fluid reabsorption in male reproductive tractMaintenance of male fertility
04

Disease associations

Male infertilityCongenital bilateral absence of the vas deferens (CBAVD)
05

Safety considerations

Potential on-target effects relating to male fertility due to its essential physiologic role[3].Mutations can cause male infertility and CBAVD[2][3].
06

Interacting drugs

Dehydroepiandrosterone (DHEA)

3 more in the full profile.

07

Biomarkers

No validated clinical biomarkers for patient selection or efficacy monitoring

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