Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00530

Target Information
NameMelanocyte stimulating hormone receptor    
Type of targetResearch target    
SynonymsMC1-R    
MSH-R    
Melanocortin-1 receptor    
Melanotropin receptor    
DiseaseMelanoma
[ICD9: 172   ICD10: C43]
[1]
Obesity
[ICD9: 278   ICD10: E66]
[2]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayMelanogenesis
Neuroactive ligand-receptor interaction
UniProt IDQ01726
FunctionReceptor for msh (alpha, beta and gamma) and acth. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.    
SequenceMAVQGSQRRLLGSLNSTPTAIPQLGLAANQTGARCLEVSISDGLFLSLGLVSLVENALVV ATIAKNRNLHSPMYCFICCLALSDLLVSGSNVLETAVILLLEAGALVARAAVLQQLDNVI DVITCSSMLSSLCFLGAIAVDRYISIFYALRYHSIVTLPRARRAVAAIWVASVVFSTLFI AYYDHVAVLLCLVVFFLAMLVLMAVLYVHMLARACQHAQGIARLHKRQRPVHQGFGLKGA VTLTILLGIFFLCWGPFFLHLTLIVLCPEHPTCGCIFKNFNLFLALIICNAIIDPLIYAF HSQELRRTLKEVLTCSW
Target ValidationClick to Find Target Validation Information.    
InhibitorAEKKDEGPYRMEHFRWGSPPKD[3]
Ac-His-D-Phe-Arg-2-Nal-NHCH3[4]
Ac-His-DPhe-Arg-Trp-NH2[5]
Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH2[6]
Ac-Nle-c[Asp-His-DNaI (2')-Pro-Trp-Lys]-NH2[7]
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[3]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3[4]
Ac-YCit[CEHdFRWC]-NH2[3]
Ac-YK[CEHdFRWC]-NH2[3]
Ac-YRC (Me)*EHdFRWC[3]
Ac-YRMEHdFRWG-NH2[3]
Ac-YRMEHdFRWGSPPKD-NH2[3]
Ac-YR[CEH (d-2alpha-Nal)RWC]-NH2[3]
Ac-YR[CEH (pCl-dF)RWC]-NH2[3]
Ac-YR[CEH (pF-dF)RWC]-NH2[3]
Ac-YR[CEHFRWC]-NH2[3]
Ac-YR[CEHdFRWC]-NH2[3]
Ac-YR[CEHdFRWC]SPPKD-NH2[3]
Ac-[CEHdFRWC]-NH2[3]
Ac-dR[CEHdFRWC]-NH2[3]
D-Phe-Arg-2-Nal-NHCH3[8]
D-Phe-Arg-2-Nal-NHCH3[4]
GPYRMEHFRWGSPPKD-NH2[3]
NDP-SYSMEHFRWGKPVG[3]
Tic-D-Phe-Arg-2-Nal-NHCH3[9]
c[CO- (CH2)2-CO-Nle-D-Nal[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[10]
c[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2[10]
c[Nle-Gln-D-Nal (2')-Arg-Trp-Glu]-NH2[10]
c[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2[10]
c[Nle-Nle-D-Nal (2')-Arg-Trp-Glu]-NH2[10]
c[Nle-Val-D-Nal (2')-Arg-Trp-Glu]-NH2[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Evaluation of the human melanoma targeting properties of radiolabeled alpha-melanocyte stimulating hormone peptide analogues. Bioconjug Chem. 2003 Nov-Dec;14(6):1177-84. To Reference
Ref 2Promising new approaches to the management of obesity. Drugs. 2000 Jul;60(1):1-9. To Reference
Ref 3J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. To Reference
Ref 4Bioorg 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 5J Med Chem. 1997 Jul 4;40(14):2133-9.Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. 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 8J Med Chem. 2006 Jul 27;49(15):4745-61.Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach. To Reference
Ref 9Bioorg 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 10J 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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