Melanocortin 5 receptor
{{Short description|Protein-coding gene in the species Homo sapiens}}
{{Infobox_gene}}
Melanocortin 5 receptor (MC5R) is a protein that in humans is encoded by the {{gene|MC5R}} gene.{{cite journal | vauthors = Chhajlani V, Muceniece R, Wikberg JE | title = Molecular cloning of a novel human melanocortin receptor | journal = Biochemical and Biophysical Research Communications | volume = 195 | issue = 2 | pages = 866–73 | date = September 1993 | pmid = 8396929 | doi = 10.1006/bbrc.1993.2125 }}{{cite web | title = Entrez Gene: MC5R melanocortin 5 receptor| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4161 }} It is located on the chromosome 18 in the human genome. When the MC5R was disrupted in transgenic mice, it induced disruption of their exocrine glands and resulted in decreased production of sebum.{{cite journal | vauthors = Thiboutot D, Sivarajah A, Gilliland K, Cong Z, Clawson G | title = The melanocortin 5 receptor is expressed in human sebaceous glands and rat preputial cells | journal = The Journal of Investigative Dermatology | volume = 115 | issue = 4 | pages = 614–9 | date = October 2000 | pmid = 10998132 | doi = 10.1046/j.1523-1747.2000.00094.x | doi-access = free }}
Physiology
MC5R is necessary for normal sebum production.{{cite journal | vauthors = Chen W, Kelly MA, Opitz-Araya X, Thomas RE, Low MJ, Cone RD | title = Exocrine gland dysfunction in MC5-R-deficient mice: evidence for coordinated regulation of exocrine gland function by melanocortin peptides | journal = Cell | volume = 91 | issue = 6 | pages = 789–98 | date = December 1997 | pmid = 9413988 | doi = 10.1016/S0092-8674(00)80467-5 | s2cid = 6251691 | doi-access = free }}{{cite journal | vauthors = Zhang L, Li WH, Anthonavage M, Pappas A, Rossetti D, Cavender D, Seiberg M, Eisinger M | title = Melanocortin-5 receptor and sebogenesis. | journal = Eur J Pharmacol | volume = 660 | issue = 1 | pages = 202–206 | date = June 2011 | pmid = 21215742 | doi = 10.1016/j.ejphar.2010.10.100 }} Stimulation of MC5R promotes fatty acid oxidation in skeletal muscle{{cite journal | vauthors = An JJ, Rhee Y, Kim SH, Kim DM, Han DH, Hwang JH, Jin YJ, Cha BS, Baik JH, Lee WT, Lim SK | title = Peripheral effect of alpha-melanocyte-stimulating hormone on fatty acid oxidation in skeletal muscle | journal = The Journal of Biological Chemistry | volume = 282 | issue = 5 | pages = 2862–70 | date = February 2007 | pmid = 17127674 | doi = 10.1074/jbc.M603454200 | doi-access = free }} and lypolysis in adipocytes.{{cite journal | vauthors = Møller CL, Raun K, Jacobsen ML, Pedersen TÅ, Holst B, Conde-Frieboes KW, Wulff BS | title = Characterization of murine melanocortin receptors mediating adipocyte lipolysis and examination of signalling pathways involved. | journal = Mol Cell Endocrinol | volume = 341 | issue = 1–2 | pages = 9–17 | date = July 2011 | pmid = 21616121 | doi = 10.1016/j.mce.2011.03.010 | s2cid = 31837693 | url = https://hal.archives-ouvertes.fr/hal-00719880/file/PEER_stage2_10.1016%252Fj.mce.2011.03.010.pdf }} MC5R is essential for erythrocyte differentiation.{{cite journal | vauthors = Simamura E, Arikawa T, Ikeda T, Shimada H, Shoji H, Masuta H, Nakajima Y, Otani H, Yonekura H, Hatta T | title = Melanocortins contribute to sequential differentiation and enucleation of human erythroblasts via melanocortin receptors 1, 2 and 5. | journal = PLOS ONE | volume = 10 | issue = 4 | pages = e0123232 | date = April 2015 | pmid = 25860801 | doi = 10.1371/journal.pone.0123232 | pmc=4393082| bibcode = 2015PLoSO..1023232S | doi-access = free }} MC5R is involved in inflammation.{{cite journal | vauthors = Lee DJ, Taylor AW | title = Both MC5r and A2Ar are required for protective regulatory immunity in the spleen of post-experimental autoimmune uveitis in mice. | journal = J. Immunol. | volume = 191| issue = 8 | pages = 4103–4111 | date = October 2013 | pmid = 24043903 | doi = 10.4049/jimmunol.1300182 | pmc=3796047}}{{cite journal | vauthors = Jun DJ, Na KY, Kim W, Kwak D, Kwon EJ, Yoon JH, Yea K, Lee H, Kim J, Suh PG, Ryu SH, Kim KT | title = Melanocortins induce interleukin 6 gene expression and secretion through melanocortin receptors 2 and 5 in 3T3-L1 adipocytes. | journal = J Mol Endocrinol | volume = 44 | issue = 4 | pages = 225–236 | date = April 2010 | pmid = 20089716 | doi = 10.1677/JME-09-0161 | pmc=3058511}} MC5R helps maintain thermal homeostasis.{{cite journal | vauthors = Lute B, Jou W, Lateef DM, Goldgof M, Xiao C, Piñol RA, Kravitz AV, Miller NR, Huang YG, Girardet C, Butler AA, Gavrilova O, Reitman ML | title = Biphasic effect of melanocortin agonists on metabolic rate and body temperature. | journal = Cell Metab. | volume = 20 | issue = 2 | pages = 333–345 | date = August 2014 | pmid = 24981835 | doi = 10.1016/j.cmet.2014.05.021 | pmc=4126889}}
MC5R is expressed in the brain at different levels depending on physical activity.{{cite journal | vauthors = Shukla C, Britton SL, Koch LG, Novak CM | title = Region-specific differences in brain melanocortin receptors in rats of the lean phenotype. | journal = NeuroReport | volume = 23 | issue = 10 | pages = 596–600 | date = July 2012 | pmid = 22643233 | doi = 10.1097/WNR.0b013e328354f5c1 | pmc=3831884}}
= Pheromones =
MC5R is heavily expressed in the preputial gland in mice (a modified sebaceous gland involved in pheromone production). MC5R deficiency in male mice decreases aggressive behavior, promotes defensive behavior and encourages other male mice to attack MC5R-deficient males through pheromonal signals.{{cite journal | vauthors = Morgan C, Thomas RE, Cone RD | title = Melanocortin-5 receptor deficiency promotes defensive behavior in male mice. | journal = Horm. Behav. | volume = 45 | issue = 1 | pages = 56–63 | date = January 2004 | pmid = 14733892 | doi = 10.1016/j.yhbeh.2003.08.004 | s2cid = 32531156 }}{{cite journal | vauthors = Morgan C, Thomas RE, Ma W, Novotny MV, Cone RD | title = Melanocortin-5 receptor deficiency reduces a pheromonal signal for aggression in male mice. | journal = Chem Senses | volume = 29 | issue = 2 | pages = 111–115 | date = February 2004 | pmid = 14977807 | doi=10.1093/chemse/bjh011| doi-access = free }}{{cite journal | vauthors = Morgan C, Cone RD | title = Melanocortin-5 receptor deficiency in mice blocks a novel pathway influencing pheromone-induced aggression. | journal = Behav. Genet. | volume = 36 | issue = 2 | pages = 291–300 | date = January 2006 | pmid = 16408249 | doi=10.1007/s10519-005-9024-9| s2cid = 9659300 }}
=MRAP=
Melanocortin 2 receptor accessory protein (MRAP) traps MC5R protein inside cells.{{cite journal | vauthors = Sebag JA, Hinkle PM | title = Opposite effects of the melanocortin-2 (MC2) receptor accessory protein MRAP on MC2 and MC5 receptor dimerization and trafficking. | journal = J Biol Chem | volume = 284 | issue = 34 | pages = 22641–22648 | date = August 2009 | pmid = 19535343 | doi = 10.1074/jbc.M109.022400 | pmc=2755671| doi-access = free }}
Evolution
= [[Sequence homology|Paralogues]] =
See also
References
{{reflist|33em}}
Further reading
{{refbegin|33em}}
- {{cite journal | vauthors = Fathi Z, Iben LG, Parker EM | title = Cloning, expression, and tissue distribution of a fifth melanocortin receptor subtype | journal = Neurochemical Research | volume = 20 | issue = 1 | pages = 107–13 | date = January 1995 | pmid = 7739752 | doi = 10.1007/BF00995160 | s2cid = 20792213 }}
- {{cite journal | vauthors = Chowdhary BP, Gustavsson I, Wikberg JE, Chhajlani V | title = Localization of the human melanocortin-5 receptor gene (MC5R) to chromosome band 18p11.2 by fluorescence in situ hybridization | journal = Cytogenetics and Cell Genetics | volume = 68 | issue = 1–2 | pages = 79–81 | year = 1994 | pmid = 7956366 | doi = 10.1159/000133895 }}
- {{cite journal | vauthors = Griffon N, Mignon V, Facchinetti P, Diaz J, Schwartz JC, Sokoloff P | title = Molecular cloning and characterization of the rat fifth melanocortin receptor | journal = Biochemical and Biophysical Research Communications | volume = 200 | issue = 2 | pages = 1007–14 | date = April 1994 | pmid = 8179577 | doi = 10.1006/bbrc.1994.1550 }}
- {{cite journal | vauthors = Gantz I, Shimoto Y, Konda Y, Miwa H, Dickinson CJ, Yamada T | title = Molecular cloning, expression, and characterization of a fifth melanocortin receptor | journal = Biochemical and Biophysical Research Communications | volume = 200 | issue = 3 | pages = 1214–20 | date = May 1994 | pmid = 8185570 | doi = 10.1006/bbrc.1994.1580 | url = https://deepblue.lib.umich.edu/bitstream/2027.42/31580/1/0000508.pdf | hdl = 2027.42/31580 | hdl-access = free }}
- {{cite journal | vauthors = Chhajlani V | title = Distribution of cDNA for melanocortin receptor subtypes in human tissues | journal = Biochemistry and Molecular Biology International | volume = 38 | issue = 1 | pages = 73–80 | date = February 1996 | pmid = 8932521 }}
- {{cite journal | vauthors = Yang YK, Ollmann MM, Wilson BD, Dickinson C, Yamada T, Barsh GS, Gantz I | title = Effects of recombinant agouti-signaling protein on melanocortin action | journal = Molecular Endocrinology | volume = 11 | issue = 3 | pages = 274–80 | date = March 1997 | pmid = 9058374 | doi = 10.1210/mend.11.3.9898 | doi-access = free }}
- {{cite journal | vauthors = Frändberg PA, Xu X, Chhajlani V | title = Glutamine235 and arginine272 in human melanocortin 5 receptor determines its low affinity to MSH | journal = Biochemical and Biophysical Research Communications | volume = 236 | issue = 2 | pages = 489–92 | date = July 1997 | pmid = 9240466 | doi = 10.1006/bbrc.1997.6994 }}
- {{cite journal | vauthors = Yang YK, Thompson DA, Dickinson CJ, Wilken J, Barsh GS, Kent SB, Gantz I | title = Characterization of Agouti-related protein binding to melanocortin receptors | journal = Molecular Endocrinology | volume = 13 | issue = 1 | pages = 148–55 | date = January 1999 | pmid = 9892020 | doi = 10.1210/me.13.1.148 | doi-access = }}
- {{cite journal | vauthors = Hatta N, Dixon C, Ray AJ, Phillips SR, Cunliffe WJ, Dale M, Todd C, Meggit S, Birch-MacHin MA, Rees JL | title = Expression, candidate gene, and population studies of the melanocortin 5 receptor | journal = The Journal of Investigative Dermatology | volume = 116 | issue = 4 | pages = 564–70 | date = April 2001 | pmid = 11286624 | doi = 10.1046/j.0022-202x.2001.01286.x | doi-access = free }}
- {{cite journal | vauthors = Bednarek MA, MacNeil T, Kalyani RN, Tang R, Van der Ploeg LH, Weinberg DH | title = Selective, high affinity peptide antagonists of alpha-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro | journal = Journal of Medicinal Chemistry | volume = 44 | issue = 22 | pages = 3665–72 | date = October 2001 | pmid = 11606131 | doi = 10.1021/jm010165y }}
- {{cite journal | vauthors = Lapinsh M, Veiksina S, Uhlén S, Petrovska R, Mutule I, Mutulis F, Yahorava S, Prusis P, Wikberg JE | title = Proteochemometric mapping of the interaction of organic compounds with melanocortin receptor subtypes | journal = Molecular Pharmacology | volume = 67 | issue = 1 | pages = 50–9 | date = January 2005 | pmid = 15470082 | doi = 10.1124/mol.104.002857 | s2cid = 13536417 }}
- {{cite journal | vauthors = Lohoff FW, Berrettini WH | title = Lack of association between variations in the melanocortin 5 receptor gene and bipolar disorder | journal = Psychiatric Genetics | volume = 15 | issue = 4 | pages = 255–8 | date = December 2005 | pmid = 16314755 | doi = 10.1097/00041444-200512000-00007 | s2cid = 21170090 }}
- {{cite journal | vauthors = Grieco P, Cai M, Han G, Trivedi D, Campiglia P, Novellino E, Hruby VJ | title = Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5 | journal = Peptides | volume = 28 | issue = 6 | pages = 1191–6 | date = June 2007 | pmid = 17482720 | pmc = 1955225 | doi = 10.1016/j.peptides.2007.02.012 }}
{{refend}}
External links
- {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2356 | title = Melanocortin Receptors: MC5 | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | access-date = 2008-12-05 | archive-date = 2014-07-14 | archive-url = https://web.archive.org/web/20140714111153/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2356 | url-status = dead }}
{{NLM content}}
{{G protein-coupled receptors}}
{{Melanocortin receptor modulators}}