Target Information
Target General Infomation | |||||
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Target ID |
T76846
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Former ID |
TTDR00375
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Target Name |
Melanocortin-3 receptor
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Gene Name |
MC3R
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Synonyms |
MC3-R; MC3R
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Target Type |
Research
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T76846
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UniProt ID | |||||
Sequence |
MNASCCLPSVQPTLPNGSEHLQAPFFSNQSSSAFCEQVFIKPEVFLSLGIVSLLENILVI
LAVVRNGNLHSPMYFFLCSLAVADMLVSVSNALETIMIAIVHSDYLTFEDQFIQHMDNIF DSMICISLVASICNLLAIAVDRYVTIFYALRYHSIMTVRKALTLIVAIWVCCGVCGVVFI VYSESKMVIVCLITMFFAMMLLMGTLYVHMFLFARLHVKRIAALPPADGVAPQQHSCMKG AVTITILLGVFIFCWAPFFLHLVLIITCPTNPYCICYTAHFNTYLVLIMCNSVIDPLIYA FRSLELRNTFREILCGCNGMNLG |
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Drugs and Mode of Action | |||||
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 | |||||
References | |||||
Ref 525589 | Characterization 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 526348 | J 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 527529 | J Med Chem. 2005 May 5;48(9):3095-8.Discovery of a beta-MSH-derived MC-4R selective agonist. | ||||
Ref 527941 | Bioorg 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 528082 | J 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 528247 | Bioorg 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 529226 | J 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 530169 | J 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. |
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