MC4R

Synonyms

MC4R, MC4-R, Melanocortin 4 Receptor, Melanocortin Receptor 4, Receptor, Melanocortin, Type 4, BMIQ20

Description

Melanocortin receptor 4 (MC4R) is a G-protein-coupled receptor involved in appetite regulation. Mutations in the MC4R gene are the most common cause of monogenic obesity. It acts the receptor specific to the heptapeptide core common to adrenocorticotropic hormone and alpha-, beta-, and gamma-MSH.

KO Status

RenMab: F0

Drug Information

Launched drug: 1
Drug in clinical trials: 1
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Bremelanotide

PT-141

Approved

Amag Pharmaceuticals

Sexual Dysfunctions, Psychological

Setmelanotide Acetate

N7T15V1FUY, CAM-4072, BIM-22493, RM-493

Approved

Ipsen

Renal Insufficiency, Obesity, Morbid, Bardet-Biedl Syndrome, Smith-Magenis Syndrome, Prader-Willi Syndrome, Obesity, Overweight

BIM-22103 (Ipsen)

BIM-22103

Preclinical

Ipsen

Obesity

MK-0493

MK-0493

Pending

Merck Sharp & Dohme Corp

Obesity

Modimelanotide

AP-214, ABT-719, ZP-1480, Ac-(Lys)6-alphaMSH

Discontinued

Zealand Pharma A/S

Aortic Aneurysm, Kidney Diseases, Acute Kidney Injury

AZD-2820

AZD-2820

Discontinued

Astrazeneca Pharmaceutical Co Ltd, Palatin Technologies

Obesity

References


Title

Authors

Source

Molecular cloning, expression, and gene localization of a fourth melanocortin receptor

Gantz I., Miwa H., Konda Y., Shimoto Y., Tashiro T., Waston S.J., Delvalle J.,

J. Biol. Chem. 268:15174-15179(1993)

Localization of the melanocortin-4 receptor (MC4-R) in neuroendocrine and autonomic control circuits in the brain

Mountjoy K.G., Mortrud M.T., Low M.J., Simerly R.B., Cone R.D.,

Mol. Endocrinol. 8:1298-1308(1994)

Complete sequencing and characterization of 21,243 full-length human cDNAs

Ota T., Suzuki Y., Nishikawa T., Otsuki T., Sugiyama T., Irie R., Wakamatsu A., Hayashi K., Sato H., Nagai K., Kimura K., Makita H., Sekine M., Obayashi M., Nishi T., Shibahara T., Tanaka T., Ishii S., Sugano S.,

Nat. Genet. 36:40-45(2004)

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)

Clinical spectrum of obesity and mutations in the melanocortin 4 receptor gene

Farooqi I.S., Keogh J.M., Yeo G.S.H., Lank E.J., Cheetham T., O'Rahilly S.,

N. Engl. J. Med. 348:1085-1095(2003)

Identification and characterization of melanocortin-4 receptor gene mutations in morbidly obese Finnish children and adults

Valli-Jaakola K., Lipsanen-Nyman M., Oksanen L., Hollenberg A.N., Kontula K., Bjoerbaek C., Schalin-Jaentti C.,

J. Clin. Endocrinol. Metab. 89:940-945(2004)

MRAP and MRAP2 are bidirectional regulators of the melanocortin receptor family

Chan L.F., Webb T.R., Chung T.T., Meimaridou E., Cooray S.N., Guasti L., Chapple J.P., Egertova M., Elphick M.R., Cheetham M.E., Metherell L.A., Clark A.J.,

Proc. Natl. Acad. Sci. U.S.A. 106:6146-6151(2009)

Mahogunin ring finger-1 (MGRN1) E3 ubiquitin ligase inhibits signaling from melanocortin receptor by competition with Galphas

Perez-Oliva A.B., Olivares C., Jimenez-Cervantes C., Garcia-Borron J.C.,

J. Biol. Chem. 284:31714-31725(2009)

The melanocortin 4 receptor: oligomer formation, interaction sites and functional significance

Chapman K.L., Findlay J.B.,

Biochim. Biophys. Acta 1828:535-542(2013)

Prevalence of mutations and functional analyses of melanocortin 4 receptor variants identified among 750 men with juvenile-onset obesity

Larsen L.H., Echwald S.M., Soerensen T.I.A., Andersen T., Wulff B.S., Pedersen O.,

J. Clin. Endocrinol. Metab. 90:219-224(2005)