GNRHR

Synonyms

GNRHR, Gonadotropin Releasing Hormone Receptor, GnRH-R, GRHR, Gonadotropin-Releasing Hormone (Type 1) Receptor 1, Leutinizing-Releasing Hormone Receptor, Type I GnRH Receptor, Luliberin Receptor, GNRHR1, LHRHR, LRHR, HH7, Receptors, LHRH, GnRH receptor, Gonadotropin-Releasing Hormone Receptor, Leutinizing Hormone Releasing Horomone Receptor

Description

Gonadotropin-releasing hormone receptor(GNRHR)is a protein that in humans is encoded by the GNRHR gene. This gene encodes the receptor for type 1 gonadotropin-releasing hormone. This receptor is a member of the seven-transmembrane, G-protein coupled receptor (GPCR) family. It is expressed on the surface of pituitary gonadotrope cells as well as lymphocytes, breast, ovary, and prostate. Following binding of gonadotropin-releasing hormone, the receptor associates with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Activation of the receptor ultimately causes the release of gonadotropic luteinizing hormone (LH) and follicle stimulating hormone (FSH). Defects in this gene are a cause of hypogonadotropic hypogonadism (HH). Alternative splicing results in multiple transcript variants encoding different isoforms. More than 18 transcription initiation sites in the 5' region and multiple polyA signals in the 3' region have been identified for this gene.

KO Status

F0

Drug Information

Launched drugs: 10
Drugs in clinical trials: 5
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Alarelin Acetate

Approved

Maanshan Fengyuan Pharmaceutical Co Ltd

Endometriosis

Relugolix/Estradiol/Norethindrone Acetate

Approved

Myovant Sciences

Leiomyoma, Menorrhagia

Degarelix Acetate

ASP-3550, FE-200486, Uglypeptide-1

Approved

Ferring Bv

Prostatic Hyperplasia, Prostatic Neoplasms, Lower Urinary Tract Symptoms, Infertility, Female

Cetrorelix Acetate

SB-75, NS 75B, SB-075, D-20761, NS-75A (acetate), NS-75B (pamoate salt), D-20453 (trifluoroacetate)

Approved

Merck Serono

Prostatic Hyperplasia, Polycystic Ovary Syndrome, Endometriosis, Endocrine System Diseases, Infertility, Female

Elagolix Sodium

ABT-620, NBI-56418

Approved

Neurocrine Biosciences

Pain, Polycystic Ovary Syndrome, Endometriosis, Leiomyoma, Menorrhagia, Uterine Hemorrhage

Triptorelin Pamoate

Debio-8206 (pamoate salt), D-Trp6-LHRH, Debio 8206 SC, (D-Trp6)-LH-RH, Debio 8206 CPP, AY-25650, BN-52014, Wy-42422, Wy-42462, BIM-21003, CL-118532

Approved

Actavis A/S

Endometriosis, Prostatic Neoplasms, Puberty, Precocious

Relugolix

P76B05O5V6 (UNII code), TAK-385, RVT-601

Approved

Takeda Pharmaceutical Co Ltd

Pain, Contraception, Endometriosis, Prostatic Neoplasms, Leiomyoma, Menorrhagia

Ganirelix Acetate

D-24598, RS-26306, ORG 37462, Org-37462

Approved

Organon

Endocrine System Diseases, Infertility, Female

Triptorelin Acetate

LY-01007

Approved

HIV Infections, Endometriosis, Prostatic Neoplasms, Leiomyoma, Myoma, Puberty, Precocious

Gonadorelin acetate

Abbott-41070

Approved

Mitsubishi Tanabe Pharma Corp

Prostatic Hyperplasia, Polycystic Ovary Syndrome, Endometriosis

References


Title

Authors

Source

Inhibition of gonadotropin-releasing hormone receptor signaling by expression of a splice variant of the human receptor

Grosse R., Schoneberg T., Schultz G., Gudermann T.,

Mol. Endocrinol. 11:1305-1318(1997)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Tissue-specific pattern of variant transcripts of the human gonadotropin-releasing hormone receptor gene

Kottler M.L., Bergametti F., Carre M.C., Morice S., Decoret E., Lagarde J.P., Starzec A., Counis R.,

Eur. J. Endocrinol. 140:561-569(1999)

A family with hypogonadotropic hypogonadism and mutations in the gonadotropin-releasing hormone receptor

de Roux N., Young J., Misrahi M., Genet R., Chanson P., Schaison G., Milgrom E.,

N. Engl. J. Med. 337:1597-1602(1997)

Mutations in gonadotropin-releasing hormone receptor gene cause hypogonadotropic hypogonadism

Layman L.C., Cohen D.P., Jin M., Xie J., Li Z., Reindollar R.H., Bolbolan S., Bick D.P., Sherins R.R., Duck L.W., Musgrove L.C., Sellers J.C., Neill J.D.,

Nat. Genet. 18:14-15(1998)

The same molecular defects of the gonadotropin-releasing hormone receptor determine a variable degree of hypogonadism in affected kindred

de Roux N., Young J., Brailly-Tabard S., Misrahi M., Milgrom E., Schaison G.,

J. Clin. Endocrinol. Metab. 84:567-572(1999)

Resistance of hypogonadic patients with mutated GnRH receptor genes to pulsatile GnRH administration

Caron P., Chauvin S., Christin-Maitre S., Bennet A., Lahlou N., Counis R., Bouchard P., Kottler M.-L.,

J. Clin. Endocrinol. Metab. 84:990-996(1999)

Cloning, sequencing, and expression of human gonadotropin releasing hormone (GnRH) receptor

Kakar S.S., Musgrove L.C., Devor D.C., Sellers J.C., Neill J.D.,

Biochem. Biophys. Res. Commun. 189:289-295(1992)

Cloning and characterization of the human GnRH receptor

Chi L., Zhou W., Prikhozhan A., Flanagan C.A., Davidson J.S., Golembo M., Illing N., Millar R.P., Sealfon S.C.,

Mol. Cell. Endocrinol. 91:R1-R6(1993)

The nucleotide sequences of human GnRH receptors in breast and ovarian tumors are identical with that found in pituitary

Kakar S.S., Grizzle W.E., Neill J.D.,

Mol. Cell. Endocrinol. 106:145-149(1994)