Melanin-concentrating hormone receptor 1

Melanin-concentrating hormone receptor 1
Identifiers
Symbols	MCHR1; GPR24; MCH1R; MGC32129; SLC1
External IDs	OMIM: 601751 MGI: 2180756 HomoloGene: 21097 GeneCards: MCHR1 Gene
Gene Ontology Molecular function • receptor activity • G-protein coupled receptor activity • protein C-terminus binding • neuropeptide receptor activity • melanin-concentrating hormone receptor activity • hormone binding Cellular component • plasma membrane • plasma membrane • integral to plasma membrane • nonmotile primary cilium Biological process • generation of precursor metabolites and energy • G-protein coupled receptor protein signaling pathway • inhibition of adenylate cyclase activity by G-protein signaling pathway • elevation of cytosolic calcium ion concentration • neuropeptide signaling pathway • feeding behavior • positive regulation of calcium ion transport Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	2847	207911
Ensembl	ENSG00000128285	ENSMUSG00000050164
UniProt	Q99705	Q3UY93
RefSeq (mRNA)	NM_005297	NM_145132.2
RefSeq (protein)	NP_005288	NP_660114.1
Location (UCSC)	Chr 22: 41.07 – 41.08 Mb	Chr 15: 81.07 – 81.07 Mb
PubMed search	[1]	[2]

Melanin-concentrating hormone receptor 1, also known as MCH₁, is one of the human melanin-concentrating hormone receptors.^[1]

The protein encoded by this gene, a member of the G protein-coupled receptor family 1, is an integral plasma membrane protein which binds melanin-concentrating hormone. The encoded protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption. Although structurally similar to somatostatin receptors, this protein does not seem to bind somatostatin.^[1]

Function

MCH₁ is thought to have a number of functions including in the regulation of appetite,^[2][3] and in stress, anxiety and depression.^{[4][5][6][7][8][9]}

Selective Ligands

Agonists

• Melanin concentrating hormone (MCH)
• S-36057 - modified MCH 6-13 fragment substituted with 3-iodotyrosine at N-terminus via dioxyoctanoyl linker, used as ¹²⁵I radioligand for mapping MCH₁ in vivo.^[10][11]

Antagonists

• ATC-0065
• ATC-0175^[12]
• GW-803,430^[13]
• NGD-4715
• SNAP-7941^[14]
• SNAP-94847^[15]
• T-226,296^[16]

See also

• Melanin-concentrating hormone receptor

References

1. ^ ^{a b} "Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=2847. 
2. ^ Luthin DR (July 2007). "Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists". Life Sciences 81 (6): 423–440. doi:10.1016/j.lfs.2007.05.029. PMID 17655875. 
3. ^ Rivera G, Bocanegra-García V, Galiano S, Cirauqui N, Ceras J, Pérez S, Aldana I, Monge A (2008). "Melanin-concentrating hormone receptor 1 antagonists: a new perspective for the pharmacologic treatment of obesity". Current Medicinal Chemistry 15 (10): 1025–1043. doi:10.2174/092986708784049621. PMID 18393860. 
4. ^ Hervieu G (August 2003). "Melanin-concentrating hormone functions in the nervous system: food intake and stress". Expert Opinion on Therapeutic Targets 7 (4): 495–511. doi:10.1517/14728222.7.4.495. PMID 12885269. 
5. ^ Shimazaki T, Yoshimizu T, Chaki S (2006). "Melanin-concentrating hormone MCH1 receptor antagonists: a potential new approach to the treatment of depression and anxiety disorders". CNS Drugs 20 (10): 801–11. PMID 16999451. 
6. ^ Hervieu GJ (April 2006). "Further insights into the neurobiology of melanin-concentrating hormone in energy and mood balances". Expert Opinion on Therapeutic Targets 10 (2): 211–229. doi:10.1517/14728222.10.2.211. PMID 16548771. 
7. ^ Smith DG, Davis RJ, Rorick-Kehn L, Morin M, Witkin JM, McKinzie DL, Nomikos GG, Gehlert DR (June 2006). "Melanin-concentrating hormone-1 receptor modulates neuroendocrine, behavioral, and corticolimbic neurochemical stress responses in mice". Neuropsychopharmacology 31 (6): 1135–45. doi:10.1038/sj.npp.1300913. PMID 16205780. 
8. ^ Roy M, David N, Cueva M, Giorgetti M (January 2007). "A study of the involvement of melanin-concentrating hormone receptor 1 (MCHR1) in murine models of depression". Biological Psychiatry 61 (2): 174–180. doi:10.1016/j.biopsych.2006.03.076. PMID 16934771. 
9. ^ Saito Y, Nagasaki H (2008). "The melanin-concentrating hormone system and its physiological functions". Results and Problems in Cell Differentiation. Results and Problems in Cell Differentiation 46: 159–179. doi:10.1007/400_2007_052. ISBN 978-3-540-78350-3. PMID 18227983. 
10. ^ Audinot V, Lahaye C, Suply T, Beauverger P, Rodriguez M, Galizzi JP, Fauchère JL, Boutin JA (June 2001). "[125I-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor"]. British Journal of Pharmacology 133 (3): 371–378. doi:10.1038/sj.bjp.0704085. PMC 1572795. PMID 11375253. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1572795. 
11. ^ Able SL, Ivarsson M, Fish RL, Clarke TL, McCourt C, Duckworth JM, Napier C, Katugampola SD (June 2009). "Localisation of melanin-concentrating hormone receptor 1 in rat brain and evidence that sleep parameters are not altered despite high central receptor occupancy". European Journal of Pharmacology 616 (1–3): 101–106. doi:10.1016/j.ejphar.2009.06.009. PMID 19540226. 
12. ^ Chaki S, Yamaguchi J, Yamada H, Thomsen W, Tran TA, Semple G, Sekiguchi Y (2005). "ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety". CNS Drug Reviews 11 (4): 341–352. doi:10.1111/j.1527-3458.2005.tb00052.x. PMID 16614734. 
13. ^ Gehlert DR, Rasmussen K, Shaw J, Li X, Ardayfio P, Craft L, Coskun T, Zhang HY, Chen Y, Witkin JM (May 2009). "Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression". The Journal of Pharmacology and Experimental Therapeutics 329 (2): 429–438. doi:10.1124/jpet.108.143362. PMID 19182070. 
14. ^ Doggrell SA (June 2003). "Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?". Expert Opinion on Investigational Drugs 12 (6): 1035–1038. doi:10.1517/13543784.12.6.1035. PMID 12783607. 
15. ^ David DJ, Klemenhagen KC, Holick KA, Saxe MD, Mendez I, Santarelli L, Craig DA, Zhong H, Swanson CJ, Hegde LG, Ping XI, Dong D, Marzabadi MR, Gerald CP, Hen R (April 2007). "Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocampal neurogenesis". The Journal of Pharmacology and Experimental Therapeutics 321 (1): 237–48. doi:10.1124/jpet.106.109678. PMID 17237257. 
16. ^ Takekawa S, Asami A, Ishihara Y, Terauchi J, Kato K, Shimomura Y, Mori M, Murakoshi H, Kato K, Suzuki N, Nishimura O, Fujino M (March 2002). "T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist". European Journal of Pharmacology 438 (3): 129–135. doi:10.1016/S0014-2999(02)01314-6. PMID 11909603. 

External links

• "Melanin-Concentrating Hormone Receptors: MCH₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2998. 

Further reading

• Kolakowski LF, Jung BP, Nguyen T et al. (1997). "Characterization of a human gene related to genes encoding somatostatin receptors". FEBS Lett. 398 (2–3): 253–258. doi:10.1016/S0014-5793(96)01160-X. PMID 8977118. 
• Chambers J, Ames RS, Bergsma D et al. (1999). "Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1". Nature 400 (6741): 261–265. doi:10.1038/22313. PMID 10421367. 
• Saito Y, Nothacker HP, Wang Z et al. (1999). "Molecular characterization of the melanin-concentrating-hormone receptor". Nature 400 (6741): 265–269. doi:10.1038/22321. PMID 10421368. 
• Shimomura Y, Mori M, Sugo T et al. (1999). "Isolation and identification of melanin-concentrating hormone as the endogenous ligand of the SLC-1 receptor". Biochem. Biophys. Res. Commun. 261 (3): 622–626. doi:10.1006/bbrc.1999.1104. PMID 10441476. 
• Dunham I, Shimizu N, Roe BA et al. (1999). "The DNA sequence of human chromosome 22". Nature 402 (6761): 489–495. doi:10.1038/990031. PMID 10591208. 
• Macdonald D, Murgolo N, Zhang R et al. (2000). "Molecular characterization of the melanin-concentrating hormone/receptor complex: identification of critical residues involved in binding and activation". Mol. Pharmacol. 58 (1): 217–25. PMID 10860944. 
• An S, Cutler G, Zhao JJ et al. (2001). "Identification and characterization of a melanin-concentrating hormone receptor". Proc. Natl. Acad. Sci. U.S.A. 98 (13): 7576–7581. doi:10.1073/pnas.131200698. PMC 34710. PMID 11416225. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=34710. 
• Bednarek MA, Feighner SD, Hreniuk DL et al. (2001). "Short segment of human melanin-concentrating hormone that is sufficient for full activation of human melanin-concentrating hormone receptors 1 and 2". Biochemistry 40 (31): 9379–9386. doi:10.1021/bi010867p. PMID 11478907. 
• Bednarek MA, Tan C, Hreniuk DL et al. (2002). "Synthesis and biological evaluation in vitro of a selective, high potency peptide agonist of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1". J. Biol. Chem. 277 (16): 13821–13826. doi:10.1074/jbc.M200563200. PMID 11839762. 
• Audinot V, Lahaye C, Suply T et al. (2002). "SVK14 cells express an MCH binding site different from the MCH1 or MCH2 receptor". Biochem. Biophys. Res. Commun. 295 (4): 841–848. doi:10.1016/S0006-291X(02)00763-5. PMID 12127971. 
• Hoogduijn MJ, Ancans J, Suzuki I et al. (2002). "Melanin-concentrating hormone and its receptor are expressed and functional in human skin". Biochem. Biophys. Res. Commun. 296 (3): 698–701. doi:10.1016/S0006-291X(02)00932-4. PMID 12176038. 
• Bächner D, Kreienkamp HJ, Richter D (2002). "MIZIP, a highly conserved, vertebrate specific melanin-concentrating hormone receptor 1 interacting zinc-finger protein". FEBS Lett. 526 (1–3): 124–128. doi:10.1016/S0014-5793(02)03115-0. PMID 12208518. 
• Verlaet M, Adamantidis A, Coumans B et al. (2002). "Human immune cells express ppMCH mRNA and functional MCHR1 receptor". FEBS Lett. 527 (1–3): 205–210. doi:10.1016/S0014-5793(02)03232-5. PMID 12220661. 
• Strausberg RL, Feingold EA, Grouse LH et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–16903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=139241. 
• Logan DW, Bryson-Richardson RJ, Pagán KE et al. (2003). "The structure and evolution of the melanocortin and MCH receptors in fish and mammals". Genomics 81 (2): 184–191. doi:10.1016/S0888-7543(02)00037-X. PMID 12620396. 
• Pissios P, Trombly DJ, Tzameli I, Maratos-Flier E (2003). "Melanin-concentrating hormone receptor 1 activates extracellular signal-regulated kinase and synergizes with G(s)-coupled pathways". Endocrinology 144 (8): 3514–3523. doi:10.1210/en.2002-0004. PMID 12865333. 
• Gottumukkala RV, Waterman EA, Herd LM et al. (2003). "Autoantibodies in vitiligo patients recognize multiple domains of the melanin-concentrating hormone receptor". J. Invest. Dermatol. 121 (4): 765–770. doi:10.1046/j.1523-1747.2003.12494.x. PMID 14632194. 
• Gibson WT, Pissios P, Trombly DJ et al. (2004). "Melanin-concentrating hormone receptor mutations and human obesity: functional analysis". Obes. Res. 12 (5): 743–749. doi:10.1038/oby.2004.89. PMID 15166293. 
• Hawes BE, Green B, O'Neill K et al. (2004). "Identification and characterization of single-nucleotide polymorphisms in MCH-R1 and MCH-R2". Obes. Res. 12 (8): 1327–1334. doi:10.1038/oby.2004.167. PMID 15340116. 
• Collins JE, Wright CL, Edwards CA et al. (2005). "A genome annotation-driven approach to cloning the human ORFeome". Genome Biol. 5 (10): R84. doi:10.1186/gb-2004-5-10-r84. PMC 545604. PMID 15461802. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=545604. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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