Melanin-concentrating hormone receptor 1
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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]
Contents
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
References
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External links
- "Melanin-Concentrating Hormone Receptors: MCH1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
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): 253–8. 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): 261–5. 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): 265–9. 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): 622–6. 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): 489–95. 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): 7576–81. doi:10.1073/pnas.131200698. PMC 34710 Freely accessible. PMID 11416225.
- 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): 9379–86. 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): 13821–6. 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): 841–8. 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): 124–8. 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): 205–10. 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): 16899–903. doi:10.1073/pnas.242603899. PMC 139241 Freely accessible. PMID 12477932.
- 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): 184–91. 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): 3514–23. 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): 765–70. 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): 743–9. 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): 1327–34. 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 Freely accessible. PMID 15461802.
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.
sr:Melanin-koncentrirajući hormonski receptor 1- ↑ 1.0 1.1 "Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1".
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ 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): 1025–43. doi:10.2174/092986708784049621. PMID 18393860.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ 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.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Saito Y, Nagasaki H (2008). "The melanin-concentrating hormone system and its physiological functions". Results and Problems in Cell Differentiation. 46: 159–79. doi:10.1007/400_2007_052. PMID 18227983.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ 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): 341–52. doi:10.1111/j.1527-3458.2005.tb00052.x. PMID 16614734.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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