Melanin-koncentrirajući hormonski receptor 1
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| Melanin-koncentrirajući hormonski receptor 1 | |||
|---|---|---|---|
| Identifikatori | |||
| Simboli | MCHR1; GPR24; MCH1R; MGC32129; SLC1 | ||
| Vanjski ID | OMIM: 601751 MGI: 2180756 HomoloGene: 21097 IUPHAR: MCH1 GeneCards: MCHR1 Gene | ||
| Pregled RNK izražavanja | |||
 | |||
| podaci | |||
| Ortolozi | |||
| Vrsta | Čovek | Miš | |
| Entrez | 2847 | 207911 | |
| Ensembl | ENSG00000128285 | ENSMUSG00000050164 | |
| UniProt | Q99705 | Q3UY93 | |
| RefSeq (mRNA) | NM_005297 | NM_145132 | |
| RefSeq (protein) | NP_005288 | NP_660114 | |
| Lokacija (UCSC) | Chr 22: 39.41 - 39.41 Mb | Chr 15: 81.06 - 81.07 Mb | |
| PubMed pretraga | [1] | [2] | |
Melanin-koncentrirajući hormonski receptor 1, takođe poznat kao MCH1, je jedan od ljudskih melanin-koncentrirajućih hormonskih receptora.[1]
Protein kodiran ovim genom je član G protein-spregnuti receptor familije 1. On je integralni protein membrane plazme koji vezuje melanin-koncentrirajući hormon. Ovaj receptor može da inhibira cAMP akumulaciju, i da stimuliše intracelularni kalcijum fluks. Smatra se da on učestvuje u neuronalnoj regulaciju konzumacije hrane. Mada je strukturno sličan sa somatostatin receptorima, ovaj protein ne vezuje somatostatin.[1]
Funkcija[uredi | uredi kod]
MCH1 ima brojne funkcije, u koje se ubrajaju regulacija apetita,[2][3] kao i posredovanje stresa, strepnje i depresije.[4][5][6][7][8][9]
Selektivni Ligandi[uredi | uredi kod]
Agonisti[uredi | uredi kod]
- Melanin koncentrirajući hormon (MCH)
- S-36057 - modifikovani MCH 6-13 fragment zamenjen sa 3-jodotirozinom na N-terminusu putem dioksioktanoil linkera. Koristi se kao 125I radioligand za MCH1 mapiranje in vivo.[10][11]
Antagonisti[uredi | uredi kod]
- ATC-0065
- ATC-0175[12]
- GW-803,430[13]
- NGD-4715
- SNAP-7941[14]
- SNAP-94847[15]
- T-226,296[16]
Vidi još[uredi | uredi kod]
Reference[uredi | uredi kod]
- ↑ 1,0 1,1 „Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1”.
- ↑ Luthin DR (July 2007). „Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists”. Life Sciences 81 (6): 423–40. DOI:10.1016/j.lfs.2007.05.029. PMID 17655875.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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): 211–29. DOI:10.1517/14728222.10.2.211. PMID 16548771.
- ↑ 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 : Official Publication of the American College of Neuropsychopharmacology 31 (6): 1135–45. DOI:10.1038/sj.npp.1300913. PMID 16205780.
- ↑ 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): 174–80. DOI:10.1016/j.biopsych.2006.03.076. PMID 16934771.
- ↑ 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.
- ↑ 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): 371–8. DOI:10.1038/sj.bjp.0704085. PMC 1572795. PMID 11375253.
- ↑ 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): 101–6. DOI:10.1016/j.ejphar.2009.06.009. PMID 19540226.
- ↑ 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. PMID 16614734.
- ↑ 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): 429–38. DOI:10.1124/jpet.108.143362. PMID 19182070.
- ↑ Doggrell SA (June 2003). „Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?”. Expert Opinion on Investigational Drugs 12 (6): 1035–8. DOI:10.1517/13543784.12.6.1035. PMID 12783607.
- ↑ 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.
- ↑ 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): 129–35. DOI:10.1016/S0014-2999(02)01314-6. PMID 11909603.
Literatura[uredi | uredi kod]
- 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. 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. 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. PMID 15461802.
- „Melanin-Concentrating Hormone Receptors: MCH1”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.[mrtav link]