Therapeutic Targets Database
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TTD Target ID: TTDR00057

Target Information
NameMelanocortin receptor    
Type of targetResearch target    
DiseaseObesity
[ICD9: 278   ICD10: E66]
[1]
Related US Patent6,410,548
6,458,790
Target ValidationClick to Find Target Validation Information.    
InhibitorAEKKDEGPYRMEHFRWGSPPKD[2]
Ac-His-DNal (2)-Arg-Trp-NH2[3]
Ac-His-DPhe (3,4-diCl)-Arg-Trp-NH2[3]
Ac-His-DPhe (pBr)-Arg-Trp-NH2[3]
Ac-His-DPhe (pCF3)-Arg-Trp-NH2[3]
Ac-His-DPhe (pI)-Arg-Trp-NH2[3]
Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH2[4]
Ac-Nle-c[Asp-His-DNal (2')-Pro-Trp-Lys]-NH2[5]
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2[5]
Ac-YRC (Me)*EHdFRWC[2]
Ac-YRMEHdFRWG-NH2[2]
Ac-YRMEHdFRWGSPPKD-NH2[2]
Ac-YR[CEH (d-2alpha-Nal)RWC]-NH2[2]
Ac-YR[CEH (pCl-dF)RWC]-NH2[2]
Ac-YR[CEH (pF-dF)RWC]-NH2[2]
Alpha-MSH[6]
GPYRMEHFRWGSPPKD-NH2[2]
MK-10[7]
MK-11[7]
NDP-SYSMEHFRWGKPVG[2]
c[CO- (CH2)2-CO-Nle-D-Nal[4]
c[CO- (CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2[4]
c[CO- (CH2)3-CO-Pro-D-Nal[4]
c[CO- (CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2[4]
c[CO-2,3-pyrazine-CO-D-Nal (2)-Arg-Trp-Lys]-NH2[4]
c[CO-o-C6H4-CO-Pro-D-Nal (2)-Arg-Trp-Lys]-NH2[4]
c[Nle-Arg-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2[8]
c[Nle-Asp-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-Gln-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2[8]
c[Nle-Glu-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2[8]
c[Nle-His-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-His-D-Phe-Arg-Trp-Glu]-NH2[8]
c[Nle-Nle-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2[8]
c[Nle-Pro-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2[8]
c[Nle-Val-D-Nal (2')-Arg-Trp-Glu]-NH2[8]
c[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2[8]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 2J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. To Reference
Ref 3J Med Chem. 2008 Sep 25;51(18):5585-93.Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. To Reference
Ref 4J 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 5J 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 6Bioorg 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 7J 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 8J 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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