Target Information

Target General Infomation
Target ID
T76846
Former ID
TTDR00375
Target Name
Melanocortin-3 receptor
Gene Name
MC3R
Synonyms
MC3-R; MC3R
Target Type
Research
Disease Sexual dysfunction; Obesity; Type 2 diabetes [ICD9: 250, 250.00, 250.02, 278, 302.7; ICD10: E08-E13, E11, E66, F52]
Function
Receptor for MSH (alpha, beta and gamma) and ACTH. This receptor is mediated by G proteins which activate adenylate cyclase. Required for expression of anticipatory patterns of activity and wakefulness during periods of limited nutrient availability and for the normal regulation of circadian clock activity in the brain.
BioChemical Class
GPCR rhodopsin
Target Validation
T76846
UniProt ID
P41968
Sequence
MNASCCLPSVQPTLPNGSEHLQAPFFSNQSSSAFCEQVFIKPEVFLSLGIVSLLENILVI
LAVVRNGNLHSPMYFFLCSLAVADMLVSVSNALETIMIAIVHSDYLTFEDQFIQHMDNIF
DSMICISLVASICNLLAIAVDRYVTIFYALRYHSIMTVRKALTLIVAIWVCCGVCGVVFI
VYSESKMVIVCLITMFFAMMLLMGTLYVHMFLFARLHVKRIAALPPADGVAPQQHSCMKG
AVTITILLGVFIFCWAPFFLHLVLIITCPTNPYCICYTAHFNTYLVLIMCNSVIDPLIYA
FRSLELRNTFREILCGCNGMNLG
Drugs and Mode of Action
Drug(s) Melanotetan II Drug Info Preclinical Sexual dysfunction; Obesity; Type 2 diabetes [536122]
Inhibitor Ac-dR[CEHdFRWC]-NH2 Drug Info [527529]
Ac-His-D-Phe-Arg-2-Nal-NHCH3 Drug Info [528247]
Ac-Nle-c[Asp-His-DNal(2')-Pro-Trp-Lys]-NH2 Drug Info [530169]
Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 Drug Info [530169]
Ac-R[CEHdFRWC]-NH2 Drug Info [527529]
Ac-Tyr-D-Phe-Arg-2-Nal-NHCH3 Drug Info [528247]
Ac-YCit[CEHdFRWC]-NH2 Drug Info [527529]
Ac-YK[CEHdFRWC]-NH2 Drug Info [527529]
Ac-YRC(Me)*EHdFRWC(Me)NH2 Drug Info [527529]
Ac-YRMEHdFRWG-NH2 Drug Info [527529]
Ac-YRMEHdFRWGSPPKD-NH2 Drug Info [527529]
Ac-YR[CEH(d-2alpha-Nal)RWC]-NH2 Drug Info [527529]
Ac-YR[CEH(pCl-dF)RWC]-NH2 Drug Info [527529]
Ac-YR[CEH(pF-dF)RWC]-NH2 Drug Info [527529]
Ac-YR[CEHdFRWC]-NH2 Drug Info [527529]
Ac-YR[CEHdFRWC]SPPKD-NH2 Drug Info [527529]
Ac-[CEHdFRWC]-NH2 Drug Info [527529]
AEKKDEGPYRMEHFRWGSPPKD Drug Info [527529]
C[CO-(CH2)2-CO-Nle-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-(CH2)2-CO-Nle-D-Phe-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-(CH2)3-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-(CH2)3-CO-Pro-D-Phe-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-2,3-pyrazine-CO-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-2,3-pyrazine-CO-D-Phe-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[CO-o-C6H4-CO-Pro-D-Nal(2)-Arg-Trp-Lys]-NH2 Drug Info [529226]
C[Nle-Arg-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Asp-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Gln-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Gln-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Glu-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Glu-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-His-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-His-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Nle-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Nle-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Pro-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Pro-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Val-D-Nal(2')-Arg-Trp-Glu]-NH2 Drug Info [528082]
C[Nle-Val-D-Phe-Arg-Trp-Glu]-NH2 Drug Info [528082]
GPYRMEHFRWGSPPKD-NH2 Drug Info [527529]
MK-10 Drug Info [526348]
MK-11 Drug Info [526348]
MK-9 Drug Info [529226]
NDP-SYSMEHFRWGKPVG Drug Info [527529]
Tic-D-Phe-Arg-2-Nal-NHCH3 Drug Info [527941]
Agonist Melanotetan II Drug Info [536122]
MT-II Drug Info [525589]
Antagonist SHU9119 Drug Info [535586]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
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 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 525589Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat. Eur J Pharmacol. 1999 Aug 13;378(3):249-58.
Ref 526348J 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.
Ref 527529J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist.
Ref 527941Bioorg 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 528082J 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 528247Bioorg 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 529226J 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 530169J 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 535586Activation of melanocortin type 3 receptor as a molecular mechanism for adrenocorticotropic hormone efficacy in gouty arthritis. Arthritis Rheum. 2002 Oct;46(10):2765-75.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.

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