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Melanin-koncentrirajući hormonski receptor 1

Uredi veze

Izvor: Wikipedija

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Melanin-koncentrirajući hormonski receptor 1

Identifikatori

Simboli

MCHR1; GPR24; MCH1R; MGC32129; SLC1

Vanjski ID

OMIM: 601751MGI: 2180756HomoloGene: 21097IUPHAR:MCH₁GeneCards: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

Vrsta

Čovek

Miš

RefSeq (mRNA)

RefSeq (protein)

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 kaoMCH₁, je jedan od ljudskihmelanin-koncentrirajućih hormonskih receptora.^[1]

Protein kodiran ovim genom je članG protein-spregnuti receptor familije 1. On je integralni protein membrane plazme koji vezujemelanin-koncentrirajući hormon. Ovaj receptor može da inhibiracAMP akumulaciju, i da stimuliše intracelularni kalcijum fluks. Smatra se da on učestvuje u neuronalnoj regulaciju konzumacije hrane. Mada je strukturno sličan sasomatostatin receptorima, ovaj protein ne vezujesomatostatin.^[1]

Funkcija

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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

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Agonisti

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Melanin koncentrirajući hormon (MCH)
S-36057 - modifikovani MCH 6-13 fragment zamenjen sa 3-jodotirozinom na N-terminusu putem dioksioktanoil linkera. Koristi se kao¹²⁵Iradioligand za MCH₁ mapiranjein vivo.^[10]^[11]

Antagonisti

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Povezano

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Melanin-koncentrirajući hormonski receptor

Reference

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↑^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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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]}

Transmembranski receptor:G protein spregnuti receptori

Klasa A:Rodopsinu slični

Neurotransmiter

Adrenergički	α1 (A,B,D) • α2 (A,B,C) • β1 • β2 • β3
Purinski	Adenozinski (A1,A2A,A2B,A3) • P2Y (1,2,4,5,6,8,9,10,11,12,13,14)
Serotoninski	(svi osim 5-HT3)5-HT1 (A,B,D,E,F) • 5-HT2 (A,B,C) • 5-HT (4,5A,6,7)
Drugi	Acetilholin (M1,M2,M3,M4,M5) • Dopamin (D1,D2,D3,D4,D5) • Histamin (H1,H2,H3,H4) • Melatonin (1A,1B,1C) • TAAR (1,2,3,5,6,8,9)

Metaboliti i
signalni molekuli

Eikozanoidni	CysLT (1,2) • LTB4 (1,2) • FPRL1 • OXE • Prostaglandin (DP (1,2),EP (1,2,3,4),FP) • Prostaciklin • Tromboksan
Drugi	Žučna kiselina • Kanabinoidni (CB1,CB2,GPR (18,55,119)) • EBI2 • Estrogen • Slobodna masna kiselina (1,2,3,4) • Laktat • Lizofosfatidna kiselina (1,2,3,4,5,6) • Lizofosfolipid (1,2,3,4,5,6,7,8) • Niacin (1,2) • Oksoglutarat • PAF • Sfingozin-1-fosfat (1,2,3,4,5) • Sukcinat

Peptid

Neuropeptidni

B/W (1,2) • FF (1,2) • S • Y (1,2,4,5) • Neuromedin (B,U (1,2)) • Neurotenzin (1,2)

Drugi

Anafilatoksin (C3a,C5a) • Angiotenzin (1,2) • Apelin • Bombezin (BRS3,GRPR,NMBR) • Bradikinin (B1,B2) • Hemokin • Holecistokinin (A,B) • Endotelin (A,B) • Formil peptid (1,2,3) • FSH • Galanin (1,2,3) • GHB receptor • Gonadotropin-oslobađajući hormon (1,2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1,1L,D,E,F,G,X1,X2,X3,X4) • Melanokortin (1,2,3,4,5) • MCHR (1,2) • Motilin • Opioidni (δ,κ,μ,Nociceptin &ζ, ali neσ) • Oreksin (1,2) • Oksitocin • Prokineticin (1,2) • Prolaktin-oslobađajući peptid • Relaksin (1,2,3,4) • Somatostatin (1,2,3,4,5) • Tahikinin (1,2,3) • Tirotropin • Tirotropin-oslobađajući hormon • Urotenzin-II • Vazopresin (1A,1B,2)

Razno

Orfan	GPR (1,3,4,6,12,15,17,18,19,20,21,22,23,25,26,27,31,32,33,34,35,37,39,42,44,45,50,52,55,61,62,63,65,68,75,77,78,81,82,83,84,85,87,88,92,101,103,109A,109B,119,120,132,135,137B,139,141,142,146,148,149,150,151,152,153,160,161,162,171,173,174,176,177,182,183)
Drugi	Adrenomedulin • Mirisni • Opsin (3,4,5,1LW,1MW,1SW,RGR,RRH) • Proteazom-aktivirani (1,2,3,4) • SREB (1,2,3)

Klasa B:Sekretinu slični

Orfan

GPR (56,64,97,98,110,111,112,113,114,115,116,123,124,125,126,128,133,143,144,155,157)

Drugi

Moždano specifični angiogenezni inhibitor (1,2,3) • Cadherin (1,2,3) • Kalcitonin • CALCRL • CD97 • Kortikotropin-oslobađajući hormon (1,2) • EMR (1,2,3) • Glukagon (GR,GIPR,GLP1R,GLP2R) • Hormon rasta oslobađajući hormon • PACAPR1 • GPR • Latrofilin (1,2,3,ELTD1) • Metuselah-slični proteini • Paratiroidni hormon (1,2) • Sekretin • Vazoaktivni intestinalni peptid (1,2)

Klasa C:Metabotropni
glutamat /feromon

Ukus	TAS1R (1,2,3) • TAS2R (1,3,4,5,8,9,10,12,13,14,16,19,20,30,31,38,39,40,41,42,43,45,46,50)
Drugi	Kalcijum-detektujući receptor • GABA B (1,2) • Glutamatni receptor (Metabotropni glutamat (1,2,3,4,5,6,7,8)) • GPRC6A • GPR (156,158,179) • RAIG (1,2,3,4)

Klasa F:
Frizzled /Zaglađeni

Uvojiti	Frizzled (1,2,3,4,5,6,7,8,9,10)
Zaglađeni	Zaglađeni

B trdu:peptidi (nrpl/grfl/cytl/horl),receptori (lgic,enzr,gprc,igsr,intg,nrpr/grfr/cytr),itra (adap,gbpr,mapk),calc,lipd, signalni putevi (hedp,wntp,tgfp+mapp,notp,jakp,fsap,hipp,tlrp)

Neuropeptidni ligandi

Holecistokinin

CCK_A	Agonisti:Holecistokinin •CCK-4 Antagonisti:Asperlicin •Proglumid •Lorglumid •Devazepid •Deksloksiglumid
CCK_B	Agonisti:Holecistokinin •CCK-4 •Gastrin Antagonisti:Proglumid •CI-988

CRH

CRF₁	Agonisti:Kortikotropin-oslobađajući hormon Antagonisti:Antalarmin •CP-154,526 •Peksacerfont
CRF₂	Agonisti:Kortikotropin-oslobađajući hormon

Galanin

GAL₁	Agonisti:Galanin •Galaninu-sličan peptid •Galmic •Galnon
GAL₂	Agonisti:Galanin •Galaninu-sličan peptid •Galmic •Galnon
GAL₃	Agonisti:Galanin •Galmic •Galnon

Grelin

Agonisti:Grelin •Kapromorelin •MK-677 •Sermorelin •SM-130,686 •Tabimorelin

MCH

MCH₁	Agonisti:Melanin-koncentrirajući hormon Antagonisti:ATC-0175 •GW-803,430 •NGD-4715 •SNAP-7941 •SNAP-94847
MCH₂	Agonisti:Melanin-koncentrirajući hormon

Melanokortin

MC₁	Agonisti:alfa-MSH •Afamelanotid •Bremelanotid •Melanotan II Antagonisti:Aguti signalni peptid
MC₂	Agonisti:ACTH •Kosintropin •Tetrakosaktid
MC₃	Agonisti:alfa-MSH •Bremelanotid •Melanotan II
MC₄	Agonisti:alfa-MSH •Bremelanotid •Melanotan II •THIQ Antagonisti:Agutiju srodni peptid
MC₅	Agonisti:alfa-MSH •Melanotan II

Neuropeptid S

Agonisti:Neuropeptid S
Antagonisti:SHA-68

Neuropeptid Y

Y₁	Agonisti:Neuropeptid Y •Peptid YY Antagonisti:BIBP-3226
Y₂	Agonisti:Neuropeptid Y •Peptid YY Antagonisti:BIIE-0246
Y₄	Agonisti:Neuropeptid Y •Pankreasni polipeptid •Peptid YY Antagonisti:UR-AK49
Y₅	Agonisti:Neuropeptid Y •Peptid YY Antagonisti:Lu AA-33810

Neurotenzin

NTS₁	Agonisti:Neurotenzin •Neuromedin N Antagonisti:SR-48692 •SR-142,948
NTS₂	Agonisti:Neurotenzin Antagonisti:Levokabastin •SR-142,948

Opioid

vidiOpioidi

Oreksin

OX₁	Agonisti:Oreksin-A Antagonisti:Almoreksant •SB-334,867 •SB-408,124 •SB-649,868
OX₂	Agonisti:Oreksin-A Antagonisti:Almoreksant •SB-649,868 •TCS-OX2-29

Oksitocin

Agonisti:Karbetocin •Demoksitocin •Oksitocin •WAY-267,464
Antagonisti:Atosiban •L-371,257 •L-368,899

Tahikinin

NK₁	Agonisti:Supstanca P Antagonisti:Aprepitant •Befetupitant •Kasopitant •CI-1021 •CP-96,345 •CP-99,994 •CP-122,721 •Dapitant •Ezlopitant •FK-888 •Fosaprepitant •GR-203,040 •GW-597,599 •HSP-117 •L-733,060 •L-741,671 •L-743,310 •L-758,298 •Lanepitant •LY-306,740 •Maropitant •Netupitant •NKP-608 •Nolpitantium •Orvepitant •RP-67,580 •SDZ NKT 343 •Vestipitant •Vofopitant
NK₂	Agonisti:Neurokinin A Antagonisti:GR-159897 •Ibodutant •Saredutant
NK₃	Agonisti:Neurokinin B Antagonisti:Osanetant •Talnetant

Vazopresin

V_1A	Agonisti:Dezmopresin •Felipresin •Ornipresin •Terlipresin •Vazopresin Antagonisti:Konivaptan •Demeklociklin •Relkovaptan
V_1B	Agonisti:Felipresin •Ornipresin •Terlipresin •Vazopresin Antagonisti:Demeklociklin •Nelivaptan
V₂	Agonisti:Dezmopresin •Ornipresin •Vazopresin Antagonisti:Konivaptan •Demeklociklin •Liksivaptan •Mozavaptan •Satavaptan •Tolvaptan

Izvor:https://sh.wikipedia.org/w/index.php?title=Melanin-koncentrirajući_hormonski_receptor_1&oldid=42508172

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