Melanin-koncentrirajući hormonski receptor 1

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
Ontologija gena
Molekularna funkcija	• rodopsinu-slična receptorska aktivnost; • receptorska aktivnost; • neuropeptidna receptorska aktivnost; • aktivnost melanin-koncentrirajućeg hormonskog receptora;
Celularna komponenta	• membrana plazme; • integralno sa membranom plazme; • membrana; • integralno sa membranom;
Biološki proces	• generisanje prekursorskih metabolita i energije; • prenos signala; • G-protein signalizacija, inhibirajuči put adenilat ciklaze; • povišenje koncentracije kalcijumovih jona; • neuropeptidni signalni put; • ishrana;
Pregled RNK izražavanja
	podaci
Ortolozi

edit

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

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

Agonisti

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

Povezano

Melanin-koncentrirajući hormonski receptor

Reference

↑ ^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. 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 |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=321 |issue=1 |pages=237–48 |year=2007 |month=April |pmid=17237257 |doi=10.1124/jpet.106.109678 |url=}}
↑ 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

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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.
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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.
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„Melanin-Concentrating Hormone Receptors: MCH₁”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. ^{[mrtav link]}

[entrez-1] 1,0 ^1,1 „Entrez Gene: MCHR1 melanin-concentrating hormone receptor 1”.

[pmid17655875-2] 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.

[pmid18393860-3] 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): 1025–43. DOI:10.2174/092986708784049621. PMID 18393860.

[pmid12885269-4] 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.

[pmid16999451-5] 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.

[pmid16548771-6] 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): 211–29. DOI:10.1517/14728222.10.2.211. PMID 16548771.

[pmid16205780-7] 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 : Official Publication of the American College of Neuropsychopharmacology 31 (6): 1135–45. DOI:10.1038/sj.npp.1300913. PMID 16205780.

[pmid16934771-8] 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): 174–80. DOI:10.1016/j.biopsych.2006.03.076. PMID 16934771.

[pmid18227983-9] 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.

[pmid11375253-10] 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): 371–8. DOI:10.1038/sj.bjp.0704085. PMC 1572795. PMID 11375253.

[pmid19540226-11] 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): 101–6. DOI:10.1016/j.ejphar.2009.06.009. PMID 19540226.

[pmid16614734-12] 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): 341–52. PMID 16614734.

[pmid19182070-13] 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): 429–38. DOI:10.1124/jpet.108.143362. PMID 19182070.

[pmid12783607-14] 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.

[pmid17237257-15] 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. 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 |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=321 |issue=1 |pages=237–48 |year=2007 |month=April |pmid=17237257 |doi=10.1124/jpet.106.109678 |url=}}

[pmid11909603-16] 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): 129–35. DOI:10.1016/S0014-2999(02)01314-6. PMID 11909603.

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