The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)



Gene Review

MC5R  -  melanocortin 5 receptor

Homo sapiens

Synonyms: MC-2, MC5-R, Melanocortin receptor 5
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of MC5R

  • Variation of melanocortin 5 receptor was examined in patients with acne (n = 21), hidradenitis supprativa (n = 4), and sebaceous gland lesions comprising sebaceous nevi, adenomas, and hyperplasia (n = 13) [1].
  • There was expression of MC5r in retinal pigment epithelial cells, in the ganglion cell and neural outer plexiform layers of healthy wild type mice retinas [2].
  • Alpha-MSH through the melanocortin 5 receptor (MC5r) mediates induction of CD4+ regulatory T cells that suppress in an antigen specific manner autoimmune disease [2].
  • However, when this highly attenuated Junin virus strain is compared with the MC2 strain, which is of intermediate virulence, one nucleotide insertion and four nucleotide substitutions are found at positions that do not affect the predicted secondary structure [3].
  • Menogaril significantly retarded the growth of 3 out of 7 stomach cancers, SC-2, SC-9 and 4-1ST, and 3 out of 4 breast cancers, H-31, MC-2 and MX-1, with overall response rates of 43 and 75% for stomach and breast cancers, respectively [4].

Psychiatry related information on MC5R


High impact information on MC5R

  • Taken together, these results suggest that alpha-MSH increases FAO in skeletal muscle, in which MC5R may play a major role [6].
  • Small interference RNA against MC5R suppressed the alpha-MSH-induced FAO effectively. cAMP analogues mimicked the effect of alpha-MSH on FAO, and the effects of both alpha-MSH and cAMP analogue-mediated FAO were antagonized by a protein kinase A inhibitor (H89) and a cAMP antagonist ((R(p))-cAMP) [6].
  • To date, 5 melanocortin receptors (MCR) have been identified and termed MC1R to MC5R, they have been shown to have a wide and varied distribution throughout the body, being found in the central nervous system (CNS), periphery and immune cells [7].
  • The MC2R and MC5R are found in tandem and remarkably contain one and two introns, respectively [8].
  • The anatomical characterization shows that the MC2R is expressed in the brain in addition to the head-kidney, whereas the MC4R and MC5R are found in both brain regions and peripheral tissues [8].

Chemical compound and disease context of MC5R


Biological context of MC5R


Anatomical context of MC5R

  • Since relatively little is known about MC5R expression and function in the human sebaceous gland, we examined expression of MC5R by immunohistochemistry and RT-PCR in human sebaceous cells in vivo and in vitro [15].
  • Melanocortin receptors (MC1R-MC5R) and their ligands (melanocyte-stimulating hormone (MSH) and adrenocorticotrophin hormone (ACTH)) have been shown to influence physiological functions of cells and organs, including exocrine glands [15].
  • MC4R and MC5R mRNAs have been detected in brain, adipose tissue, and skeletal muscle [16].
  • We also used RT-PCR and rat specific MC2R and MC5R oligonucleotides to amplify the correct size DNA fragments for these melanocortin receptors from rat primary osteoblasts [17].
  • When the MC-2 DNA is expressed in COS-7 cells, it binds [125I]-labelled [Nle4, D-Phe7]- alpha melanocyte stimulating hormone (NDP-MSH) which then could be displaced by melanotropic peptides alpha-MSH, beta-MSH, gamma-MSH and adrenocorticotropic hormone, but not by non-melanotropic peptide beta-endorphin [18].

Associations of MC5R with chemical compounds

  • It has been shown by extensive studies that alpha-MSH bioactivity is critically dependent on the core or central tetrapeptide sequence, His-Phe-Arg-Trp, however with poor selectivity for the human MC3R-MC5R [11].
  • A series of phenylguanidine analogues represented by 10, 12, and 21 were synthesized and found to have high binding affinities for the human melanocortin-5 receptor [19].
  • Evidence is provided that mRNA for ACTH (MC-2) receptor and mRNAs for three obligatory enzymes of steroid synthesis including cytochromes P450scc, P450c17 and P450c21 are expressed in normal and pathologic human skin [20].
  • Once challenged with alphaMSH, the MC5 receptor activates the cyclic AMP response, through the coupling protein subunit G(s) [21].
  • Glutamine235 and arginine272 in human melanocortin 5 receptor determines its low affinity to MSH [22].

Regulatory relationships of MC5R

  • However, in the mPOA, the action of MCH was blocked only by the MC5-R antagonist [23].

Other interactions of MC5R


Analytical, diagnostic and therapeutic context of MC5R


  1. Expression, candidate gene, and population studies of the melanocortin 5 receptor. Hatta, N., Dixon, C., Ray, A.J., Phillips, S.R., Cunliffe, W.J., Dale, M., Todd, C., Meggit, S., Birch-MacHin, M.A., Rees, J.L. J. Invest. Dermatol. (2001) [Pubmed]
  2. Melanocortin 5 receptor and ocular immunity. Taylor, A.W., Kitaichi, N., Biros, D. Cell. Mol. Biol. (Noisy-le-grand) (2006) [Pubmed]
  3. The glycoprotein precursor gene of the attenuated Junin virus vaccine strain (Candid #1). Ghiringhelli, P.D., Albarino, C.G., Piboul, M., Romanowski, V. Am. J. Trop. Med. Hyg. (1997) [Pubmed]
  4. Anticancer activities of orally administered menogaril against human stomach and breast cancers implanted in nude mice. Inaba, M., Sato, S., Yamori, T., Tashiro, T., Ohnishi, Y., Maruo, K., Ueyama, Y., Tsuruo, T. Anticancer Res. (1992) [Pubmed]
  5. Lack of association between variations in the melanocortin 5 receptor gene and bipolar disorder. Lohoff, F.W., Berrettini, W.H. Psychiatr. Genet. (2005) [Pubmed]
  6. Peripheral Effect of {alpha}-Melanocyte-stimulating Hormone on Fatty Acid Oxidation in Skeletal Muscle. An, J.J., Rhee, Y., Kim, S.H., Kim, D.M., Han, D.H., Hwang, J.H., Jin, Y.J., Cha, B.S., Baik, J.H., Lee, W.T., Lim, S.K. J. Biol. Chem. (2007) [Pubmed]
  7. Targeting melanocortin receptors as potential novel therapeutics. Getting, S.J. Pharmacol. Ther. (2006) [Pubmed]
  8. The melanocortin system in Fugu: determination of POMC/AGRP/MCR gene repertoire and synteny, as well as pharmacology and anatomical distribution of the MCRs. Klovins, J., Haitina, T., Fridmanis, D., Kilianova, Z., Kapa, I., Fredriksson, R., Gallo-Payet, N., Schiöth, H.B. Mol. Biol. Evol. (2004) [Pubmed]
  9. Tissue transglutaminase expression in quail epiphyseal chondrocytes. Gionti, E., Sanchez, M., Arcella, A., Pontarelli, G., Tavassi, S., Gentile, V., Cozzolino, A., Porta, R. Cell Biol. Int. (1999) [Pubmed]
  10. Effects of thymidine analogues on murine and human cells. Smellie, S.G., Parsons, P.G. The Australian journal of experimental biology and medical science. (1979) [Pubmed]
  11. Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R. Balse-Srinivasan, P., Grieco, P., Cai, M., Trivedi, D., Hruby, V.J. J. Med. Chem. (2003) [Pubmed]
  12. Localization of the human melanocortin-5 receptor gene (MC5R) to chromosome band 18p11.2 by fluorescence in situ hybridization. Chowdhary, B.P., Gustavsson, I., Wikberg, J.E., Chhajlani, V. Cytogenet. Cell Genet. (1995) [Pubmed]
  13. Improving electrotransfection efficiency by post-pulse centrifugation. Li, L.H., Ross, P., Hui, S.W. Gene Ther. (1999) [Pubmed]
  14. Molecular cloning, characterization and brain mapping of the melanocortin 5 receptor in the goldfish. Cerdá-Reverter, J.M., Ling, M.K., Schiöth, H.B., Peter, R.E. J. Neurochem. (2003) [Pubmed]
  15. Melanocortin-5 receptor: a marker of human sebocyte differentiation. Zhang, L., Li, W.H., Anthonavage, M., Eisinger, M. Peptides (2006) [Pubmed]
  16. Linkage and association studies between the melanocortin receptors 4 and 5 genes and obesity-related phenotypes in the Québec Family Study. Chagnon, Y.C., Chen, W.J., Pérusse, L., Chagnon, M., Nadeau, A., Wilkison, W.O., Bouchard, C. Mol. Med. (1997) [Pubmed]
  17. Evidence for direct actions of melanocortin peptides on bone metabolism. Dumont, L.M., Wu, C.S., Tatnell, M.A., Cornish, J., Mountjoy, K.G. Peptides (2005) [Pubmed]
  18. Molecular cloning of a novel human melanocortin receptor. Chhajlani, V., Muceniece, R., Wikberg, J.E. Biochem. Biophys. Res. Commun. (1993) [Pubmed]
  19. Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists. Chen, C., Yu, J., Fleck, B.A., Hoare, S.R., Saunders, J., Foster, A.C. J. Med. Chem. (2004) [Pubmed]
  20. ACTH receptor, CYP11A1, CYP17 and CYP21A2 genes are expressed in skin. Slominski, A., Ermak, G., Mihm, M. J. Clin. Endocrinol. Metab. (1996) [Pubmed]
  21. Functional characterization of human neuropeptide Y receptor subtype five specific antagonists using a luciferase reporter gene assay. Beauverger, P., Rodriguez, M., Nicolas, J.P., Audinot, V., Lamamy, V., Dromaint, S., Nagel, N., Macia, C., Léopold, O., Galizzi, J.P., Caignard, D.H., Aldana, I., Monge, A., Chomarat, P., Boutin, J.A. Cell. Signal. (2005) [Pubmed]
  22. Glutamine235 and arginine272 in human melanocortin 5 receptor determines its low affinity to MSH. Frändberg, P.A., Xu, X., Chhajlani, V. Biochem. Biophys. Res. Commun. (1997) [Pubmed]
  23. Evidence for a stimulatory action of melanin-concentrating hormone on luteinising hormone release involving MCH1 and melanocortin-5 receptors. Murray, J.F., Hahn, J.D., Kennedy, A.R., Small, C.J., Bloom, S.R., Haskell-Luevano, C., Coen, C.W., Wilson, C.A. J. Neuroendocrinol. (2006) [Pubmed]
  24. Biological and conformational study of beta-substituted prolines in MT-II template: steric effects leading to human MC5 receptor selectivity. Cai, M., Cai, C., Mayorov, A.V., Xiong, C., Cabello, C.M., Soloshonok, V.A., Swift, J.R., Trivedi, D., Hruby, V.J. J. Pept. Res. (2004) [Pubmed]
  25. CRF and stress in fish. Flik, G., Klaren, P.H., Van den Burg, E.H., Metz, J.R., Huising, M.O. Gen. Comp. Endocrinol. (2006) [Pubmed]
  26. Species-dependent pharmacological properties of the melanocortin-5 receptor. Huang, R.R., Singh, G., Van der Ploeg, L.H., Fong, T.M. J. Recept. Signal Transduct. Res. (2000) [Pubmed]
  27. Thyrotropin releasing hormone (TRH) selectively binds and activates the melanocortin 1 receptor. Schiöth, H.B., Prusis, P., Muceniece, R., Mutulis, F., Mutule, I., Wikberg, J.E. Peptides (1999) [Pubmed]
  28. Stimulation of intracellular free calcium in GH3 cells by gamma3-melanocyte-stimulating hormone. Involvement of a novel melanocortin receptor? Langouche, L., Roudbaraki, M., Pals, K., Denef, C. Endocrinology (2001) [Pubmed]
  29. Characterization of the porcine melanocortin 2 receptor gene (MC2R ). Jacobs, K., Van Poucke, M., Mattheeuws, M., Chardon, P., Yerle, M., Rohrer, G., Van Zeveren, A., Peelman, L.J. Anim. Genet. (2002) [Pubmed]
  30. The melanocortin 5 receptor is expressed in human sebaceous glands and rat preputial cells. Thiboutot, D., Sivarajah, A., Gilliland, K., Cong, Z., Clawson, G. J. Invest. Dermatol. (2000) [Pubmed]
WikiGenes - Universities