Target Information

Target General Infomation
Target ID
T35842
Former ID
TTDR00530
Target Name
Melanocyte stimulating hormone receptor
Gene Name
MC1R
Synonyms
MC1-R; MSH-R; Melanocortin-1 receptor; Melanotropin receptor; MC1R
Target Type
Clinical Trial
Disease Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Function
Receptor for msh (alpha, beta and gamma) and acth. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
BioChemical Class
GPCR rhodopsin
Target Validation
T35842
UniProt ID
Q01726
Sequence
MAVQGSQRRLLGSLNSTPTAIPQLGLAANQTGARCLEVSISDGLFLSLGLVSLVENALVV
ATIAKNRNLHSPMYCFICCLALSDLLVSGSNVLETAVILLLEAGALVARAAVLQQLDNVI
DVITCSSMLSSLCFLGAIAVDRYISIFYALRYHSIVTLPRARRAVAAIWVASVVFSTLFI
AYYDHVAVLLCLVVFFLAMLVLMAVLYVHMLARACQHAQGIARLHKRQRPVHQGFGLKGA
VTLTILLGIFFLCWGPFFLHLTLIVLCPEHPTCGCIFKNFNLFLALIICNAIIDPLIYAF
HSQELRRTLKEVLTCSW
Drugs and Mode of Action
Drug(s) AP-1030 Drug Info Phase 1/2 Metabolic disorders [1], [2]
Inhibitor Ac-dR[CEHdFRWC]-NH2 Drug Info [3]
Ac-His-D-Phe-Arg-2-Nal-NHCH3 Drug Info [4]
Ac-His-DPhe-Arg-Trp-NH2 Drug Info [5]
Ac-Nle-c[Asp-His-DNaI(2')-Pro-Trp-Lys]-NH2 Drug Info [6]
Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 Drug Info [6]
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 Drug Info [6]
Ac-R[CEHdFRWC]-NH2 Drug Info [3]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3 Drug Info [4]
Ac-YCit[CEHdFRWC]-NH2 Drug Info [3]
Ac-YK[CEHdFRWC]-NH2 Drug Info [3]
Ac-YRC(Me)*EHdFRWC(Me)NH2 Drug Info [3]
Ac-YRMEHdFRWG-NH2 Drug Info [3]
Ac-YRMEHdFRWGSPPKD-NH2 Drug Info [3]
Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 Drug Info [3]
Ac-YR[CEH(pCl-dF)RWC]-NH2 Drug Info [3]
Ac-YR[CEH(pF-dF)RWC]-NH2 Drug Info [3]
Ac-YR[CEHdFRWC]-NH2 Drug Info [3]
Ac-YR[CEHdFRWC]SPPKD-NH2 Drug Info [3]
Ac-YR[CEHFRWC]-NH2 Drug Info [3]
Ac-[CEHdFRWC]-NH2 Drug Info [3]
AEKKDEGPYRMEHFRWGSPPKD Drug Info [3]
C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [7]
C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [7]
C[CO-2,3-pyrazine-CO-D-Phe-Arg-Trp-Lys]-NH2 Drug Info [7]
C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [7]
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [8]
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [8]
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [8]
C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [8]
C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [8]
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [8]
D-Phe-Arg-2-Nal-NHCH3 Drug Info [9]
GPYRMEHFRWGSPPKD-NH2 Drug Info [3]
NDP-SYSMEHFRWGKPVG Drug Info [3]
Tic-D-Phe-Arg-2-Nal-NHCH3 Drug Info [10]
Modulator afamelanotide Drug Info [11]
AP-1030 Drug Info [12]
AP-1189 Drug Info [13]
Agonist MT-II Drug Info [14]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Melanogenesis
Reactome Peptide ligand-binding receptors
G alpha (s) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
REF 1ClinicalTrials.gov (NCT00464958) One Year Extension Study To Protocol C2/5/TZ:MS-05. U.S. National Institutes of Health.
REF 2(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1322).
REF 3J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
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.
REF 5J Med Chem. 1997 Jul 4;40(14):2133-9.Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
REF 6J 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.
REF 7J 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.
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.
REF 9J 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.
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.
REF 11The ChEMBL database in 2017.
REF 12Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 13(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 282).
REF 14Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10. J Med Chem. 1989 Jan;32(1):174-9.

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