Gonadotropin-releasing Hormone Receptor Family

The gonadotropin-releasing hormone (GnRH) receptor, also known as the luteinizing hormone releasing hormone (LHRH) receptor. It is a receptor of G-protein coupled receptor (GPCR) family, which has seven transmembranes. GnRH receptor, with a weight of a 60 kDa, is found primarily in the pituitary and is responsible for triggering the release of GnRH from the hypothalamus. There is evidence of the presence of GnRH and its receptors in extra-pituitary tissues as well as a role in the progression of certain cancers. GnRH receptor is expressed on the surface of pituitary gonadal cells and lymphocytes. It is also expressed on the cells of prostate, breasts and ovaries.

GnRH receptor signaling networks. Fig.1 GnRH receptor signaling networks. (Perrett, 2013)

GnRH regulates reproduction by binding and activating GnRH receptors on pituitary gonadotrope cells, which synthesize and secrete the LH, FSH, and gonadotropins. The gonadotropins act on the gonads to stimulate gametogenesis, gonadal cell proliferation, and gonadal steroids production. GnRH secretion is inhibited during childhood. It increases during puberty when increased production of gonadotropins and gonadal steroids triggers sexual development. Destruction of GnRH receptor function disrupts the replication and mutation of the GnRH receptor gene. GnRHR disrupts or delays pubertal development and leads to congenital hypogonadotropic hypogonadism.

There are two major GnRH receptors in humans, including GNRHR and GNRHR2, which are encoded by GNRHR and GNRHR2, respectively.

Human GnRH Receptor Members

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Gonadotropin-releasing Hormone Receptor Family

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  1. Perrett RM, et al. (2013). Molecular mechanisms of gonadotropin-releasing hormone signaling: integrating cyclic nucleotides into the network. Front Endocrinol (Lausanne). 4: 180.

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