Therapeutic Targets Database
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TTD Target ID: TTDR00375

Target Information
NameMelanocortin-3 receptor    
Type of targetResearch target    
SynonymsMC3-R    
DiseaseChronic inflammatory diseases[1]
Gouty arthritis
[ICD9: 710-719   ICD10: M00-M25]
[1]
Obesity
[ICD9: 278   ICD10: E66]
[2]
Drug(s)Melanotetan IIPreclinicalSexual dysfunction, Obesity, Type 2 diabetes[3]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP41968
FunctionReceptor for msh (alpha, beta and gamma) and acth. This receptor is mediated by G proteins which activate adenylate cyclase.    
SequenceMSIQKTYLEGDFVFPVSSSSFLRTLLEPQLGSALLTAMNASCCLPSVQPTLPNGSEHLQA PFFSNQSSSAFCEQVFIKPEVFLSLGIVSLLENILVILAVVRNGNLHSPMYFFLCSLAVA DMLVSVSNALETIMIAIVHSDYLTFEDQFIQHMDNIFDSMICISLVASICNLLAIAVDRY VTIFYALRYHSIMTVRKALTLIVAIWVCCGVCGVVFIVYSESKMVIVCLITMFFAMMLLM GTLYVHMFLFARLHVKRIAALPPADGVAPQQHSCMKGAVTITILLGVFIFCWAPFFLHLV LIITCPTNPYCICYTAHFNTYLVLIMCNSVIDPLIYAFRSLELRNTFREILCGCNGMNLG
Target ValidationClick to Find Target Validation Information.    
InhibitorAEKKDEGPYRMEHFRWGSPPKD[4]
Ac-His-D-Phe-Arg-2-Nal-NHCH3[5]
Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH2[6]
Ac-Nle-c[Asp-His-DNal (2')-Pro-Trp-Lys]-NH2[7]
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2[7]
Ac-R[CEHdFRWC]-NH2[4]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3[5]
Ac-YCit[CEHdFRWC]-NH2[4]
Ac-YK[CEHdFRWC]-NH2[4]
Ac-YRC (Me)*EHdFRWC[4]
Ac-YRMEHdFRWG-NH2[4]
Ac-YRMEHdFRWGSPPKD-NH2[4]
Ac-YR[CEH (d-2alpha-Nal)RWC]-NH2[4]
Ac-YR[CEH (pCl-dF)RWC]-NH2[4]
Ac-YR[CEH (pF-dF)RWC]-NH2[4]
Ac-YR[CEHdFRWC]-NH2[4]
Ac-YR[CEHdFRWC]SPPKD-NH2[4]
Ac-[CEHdFRWC]-NH2[4]
Ac-dR[CEHdFRWC]-NH2[4]
Alpha-MSH[8]
GPYRMEHFRWGSPPKD-NH2[4]
MK-10[9]
MK-11[9]
MK-9[6]
NDP-SYSMEHFRWGKPVG[4]
Tic-D-Phe-Arg-2-Nal-NHCH3[10]
c[CO- (CH2)2-CO-Nle-D-Nal[6]
c[CO- (CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2[6]
c[CO- (CH2)3-CO-Pro-D-Nal[6]
c[CO- (CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2[6]
c[CO-2,3-pyrazine-CO-D-Nal (2)-Arg-Trp-Lys]-NH2[6]
c[CO-2,3-pyrazine-CO-D-Phe-Arg-Trp-Lys]-NH2[6]
c[CO-o-C6H4-CO-Pro-D-Nal (2)-Arg-Trp-Lys]-NH2[6]
c[Nle-Arg-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2[11]
c[Nle-Asp-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-Gln-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2[11]
c[Nle-Glu-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2[11]
c[Nle-His-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-His-D-Phe-Arg-Trp-Glu]-NH2[11]
c[Nle-Nle-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2[11]
c[Nle-Pro-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2[11]
c[Nle-Val-D-Nal (2')-Arg-Trp-Glu]-NH2[11]
c[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2[11]
AgonistMelanotetan II[3]
AntagonistSHU9119[1]
MultitargetMelanotetan II[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Activation of melanocortin type 3 receptor as a molecular mechanism for adrenocorticotropic hormone efficacy in gouty arthritis. Arthritis Rheum. 2002 Oct;46(10):2765-75. To Reference
Ref 2The role of melanocortins in body weight regulation: opportunities for the treatment of obesity. Eur J Pharmacol. 2002 Apr 12;440(2-3):141-57. To Reference
Ref 3Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 4J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. To Reference
Ref 5Bioorg Med Chem Lett. 2006 Sep 1;16(17):4668-73.Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists. To Reference
Ref 6J Med Chem. 2008 Jan 24;51(2):187-95. Epub 2007 Dec 19.Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. To Reference
Ref 7J Med Chem. 2009 Jun 25;52(12):3627-35.Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. To Reference
Ref 8Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5.Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist. To Reference
Ref 9J Med Chem. 2002 Jun 6;45(12):2644-50.Novel cyclic templates of alpha-MSH give highly selective and potent antagonists/agonists for human melanocortin-3/4 receptors. To Reference
Ref 10Bioorg Med Chem Lett. 2006 Mar 15;16(6):1721-5. Epub 2005 Dec 20.Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists. To Reference
Ref 11J Med Chem. 2006 Mar 23;49(6):1946-52.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. To Reference



 

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