Sandbox Reserved 1646

It is a member of the seven-transmembrane, G-protein coupled receptor (GPCR) family and is activated by the peptide hormone gonadotropin-releasing hormone (GnRH) or the synthetic agonist. The GnRHR is expressed on the surface of pituitary gonadotrope cells as well as lymphocytes, breast, ovary, and prostate. Its activity is critical for successful reproductive function. Several diseases are associated with a dysfunction of this receptor or the corresponding signaling cascade.

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Biological Function

The gonadotropin releasing hormone 1 receptor is activated by GnRH which acts upon GnRHRs as the key regulator of puberty and reproduction. This peptide hormone is produced in the hypothalamus but gets secreted and acts upon GnRHRs in the anterior pituitary to exert its effects on reproductive maturation. The activation of the receptor, associates with G-proteins, leads to the releasing of gonadotropic luteinizing hormone (LH) and follicle stimulating hormone (FSH) by activating several signaling cascades. These pathways mainly corresponds to the inositol 1,4,5-triphosphate (IP3) and diacylglycerol (DAG), MAPK, and adenyl cyclase pathways. (1)

Disease

A mutation or a dysfonctionnement of the receptor could cause disease like idiopati hypogonadotropic hypogonadism (HH) which corresponds to a hypogonadism.

Relevance

One of the main using of the couple GnRH - GnRHR in the medicine field is for fertility preservation (1). Indeed a mutation of the receptor gene sometimes lead to failure of detectable ligand binding

Structural highlights

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