Gonadotropin-Releasing Hormone Receptor (GnRHR)

The gonadotropin-releasing hormone receptor (GnRHR) is a G protein-coupled receptor (GPCR) that mediates the action of gonadotropin-releasing hormone (GnRH), a key regulator of reproductive function. It is primarily expressed on pituitary gonadotrope cells, controlling the synthesis and secretion of LH and FSH. Upon binding GnRH, the receptor activates Gq/11 proteins, triggering phospholipase C activation, leading to increased inositol phosphate production, calcium mobilization, and protein kinase C activation, ultimately resulting in LH and FSH release. Mutations can cause congenital hypogonadotropic hypogonadism, and pharmacological modulation is used for infertility treatment and management of sex steroid-dependent diseases such as uterine fibroids, endometriosis, and prostate cancer.

Other names

GnRH receptorLHRHRLHRH receptorGonadoliberin receptor

GnRH agonists stimulate the receptor leading to initial gonadotropin release, but prolonged use causes desensitization/downregulation. GnRH antagonists block the receptor activity, reducing sex steroid production.