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
PBB GE MCHR1 221354 s at tn.png
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]

Садржај

[уреди] Funkcija

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]

[уреди] Selektivni Ligandi

[уреди] Agonisti

[уреди] Antagonisti

[уреди] Vidi još

[уреди] Literatura

  1. ^ а б Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1.
  2. ^ Luthin DR (July 2007). "Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists". PMID 17655875. Life Sciences 81 (6): 423–40. DOI:10.1016/j.lfs.2007.05.029.
  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". PMID 18393860. Current Medicinal Chemistry 15 (10): 1025–43. DOI:10.2174/092986708784049621.
  4. ^ Hervieu G (August 2003). "Melanin-concentrating hormone functions in the nervous system: food intake and stress". PMID 12885269. Expert Opinion on Therapeutic Targets 7 (4): 495–511. DOI:10.1517/14728222.7.4.495.
  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". PMID 16999451. CNS Drugs 20 (10): 801–11.
  6. ^ Hervieu GJ (April 2006). "Further insights into the neurobiology of melanin-concentrating hormone in energy and mood balances". PMID 16548771. Expert Opinion on Therapeutic Targets 10 (2): 211–29. DOI:10.1517/14728222.10.2.211.
  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". PMID 16205780. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology 31 (6): 1135–45. DOI:10.1038/sj.npp.1300913.
  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". PMID 16934771. Biological Psychiatry 61 (2): 174–80. DOI:10.1016/j.biopsych.2006.03.076.
  9. ^ Saito Y, Nagasaki H (2008). "The melanin-concentrating hormone system and its physiological functions". PMID 18227983. Results and Problems in Cell Differentiation 46: 159–79. DOI:10.1007/400_2007_052.
  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". PMID 11375253. British Journal of Pharmacology 133 (3): 371–8. DOI:10.1038/sj.bjp.0704085.
  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". PMID 19540226. European Journal of Pharmacology 616 (1-3): 101–6. DOI:10.1016/j.ejphar.2009.06.009.
  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". PMID 16614734. CNS Drug Reviews 11 (4): 341–52.
  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". PMID 19182070. The Journal of Pharmacology and Experimental Therapeutics 329 (2): 429–38. DOI:10.1124/jpet.108.143362.
  14. ^ Doggrell SA (June 2003). "Does the melanin-concentrating hormone antagonist SNAP-7941 deserve 3As?". PMID 12783607. Expert Opinion on Investigational Drugs 12 (6): 1035–8. DOI:10.1517/13543784.12.6.1035.
  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". PMID 17237257. The Journal of Pharmacology and Experimental Therapeutics 321 (1): 237–48. DOI:10.1124/jpet.106.109678.
  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". PMID 11909603. European Journal of Pharmacology 438 (3): 129–35. DOI:10.1016/S0014-2999(02)01314-6.

[уреди] Dodatna literatura

  • Kolakowski LF, Jung BP, Nguyen T, et al. (1997). "Characterization of a human gene related to genes encoding somatostatin receptors.". PMID 8977118. FEBS Lett. 398 (2-3): 253–8. DOI:10.1016/S0014-5793(96)01160-X.
  • 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.". PMID 10421367. Nature 400 (6741): 261–5. DOI:10.1038/22313.
  • Saito Y, Nothacker HP, Wang Z, et al. (1999). "Molecular characterization of the melanin-concentrating-hormone receptor.". PMID 10421368. Nature 400 (6741): 265–9. DOI:10.1038/22321.
  • 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.". PMID 10441476. Biochem. Biophys. Res. Commun. 261 (3): 622–6. DOI:10.1006/bbrc.1999.1104.
  • Dunham I, Shimizu N, Roe BA, et al. (1999). "The DNA sequence of human chromosome 22.". PMID 10591208. Nature 402 (6761): 489–95. DOI:10.1038/990031.
  • 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.". PMID 10860944. Mol. Pharmacol. 58 (1): 217–25.
  • An S, Cutler G, Zhao JJ, et al. (2001). "Identification and characterization of a melanin-concentrating hormone receptor.". PMID 11416225. Proc. Natl. Acad. Sci. U.S.A. 98 (13): 7576–81. DOI:10.1073/pnas.131200698.
  • 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.". PMID 11478907. Biochemistry 40 (31): 9379–86. DOI:10.1021/bi010867p.
  • 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.". PMID 11839762. J. Biol. Chem. 277 (16): 13821–6. DOI:10.1074/jbc.M200563200.
  • Audinot V, Lahaye C, Suply T, et al. (2002). "SVK14 cells express an MCH binding site different from the MCH1 or MCH2 receptor.". PMID 12127971. Biochem. Biophys. Res. Commun. 295 (4): 841–8. DOI:10.1016/S0006-291X(02)00763-5.
  • Hoogduijn MJ, Ancans J, Suzuki I, et al. (2002). "Melanin-concentrating hormone and its receptor are expressed and functional in human skin.". PMID 12176038. Biochem. Biophys. Res. Commun. 296 (3): 698–701. DOI:10.1016/S0006-291X(02)00932-4.
  • Bächner D, Kreienkamp HJ, Richter D (2002). "MIZIP, a highly conserved, vertebrate specific melanin-concentrating hormone receptor 1 interacting zinc-finger protein.". PMID 12208518. FEBS Lett. 526 (1-3): 124–8. DOI:10.1016/S0014-5793(02)03115-0.
  • Verlaet M, Adamantidis A, Coumans B, et al. (2002). "Human immune cells express ppMCH mRNA and functional MCHR1 receptor.". PMID 12220661. FEBS Lett. 527 (1-3): 205–10. DOI:10.1016/S0014-5793(02)03232-5.
  • 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.". PMID 12477932. Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. DOI:10.1073/pnas.242603899.
  • Logan DW, Bryson-Richardson RJ, Pagán KE, et al. (2003). "The structure and evolution of the melanocortin and MCH receptors in fish and mammals.". PMID 12620396. Genomics 81 (2): 184–91. DOI:10.1016/S0888-7543(02)00037-X.
  • 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.". PMID 12865333. Endocrinology 144 (8): 3514–23. DOI:10.1210/en.2002-0004.
  • Gottumukkala RV, Waterman EA, Herd LM, et al. (2003). "Autoantibodies in vitiligo patients recognize multiple domains of the melanin-concentrating hormone receptor.". PMID 14632194. J. Invest. Dermatol. 121 (4): 765–70. DOI:10.1046/j.1523-1747.2003.12494.x.
  • Gibson WT, Pissios P, Trombly DJ, et al. (2004). "Melanin-concentrating hormone receptor mutations and human obesity: functional analysis.". PMID 15166293. Obes. Res. 12 (5): 743–9. DOI:10.1038/oby.2004.89.
  • Hawes BE, Green B, O'Neill K, et al. (2004). "Identification and characterization of single-nucleotide polymorphisms in MCH-R1 and MCH-R2.". PMID 15340116. Obes. Res. 12 (8): 1327–34. DOI:10.1038/oby.2004.167.
  • Collins JE, Wright CL, Edwards CA, et al. (2005). "A genome annotation-driven approach to cloning the human ORFeome.". PMID 15461802. Genome Biol. 5 (10): R84. DOI:10.1186/gb-2004-5-10-r84.
  • Melanin-Concentrating Hormone Receptors: MCH1. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.



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