Therapeutic Targets Database
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TTD Target ID: TTDS00362

Target Information
NameCatechol-O-methyl-transferase    
Type of targetSuccessful target    
SynonymsCOMT    
Catechol-O-methyltransferase    
MB-COMT    
S-COMT    
DiseaseParkinson's disease    [1][2]
Drug(s)EntacaponeApprovedParkinson's disease[2][3]
TolcaponeApprovedParkinson's disease[3][4]
Entacapone+levodopa+carbidopaPhase IIIParkinsoní»s disease; Restless legs syndrome[5]
BioChemical ClassTransferases transferring one-carbon groups    
EC NumberEC 2.1.1.6
PathwayMetabolic pathways
Tyrosine metabolism
UniProt IDP21964
PDB Structure3BWM; 3BWY.    
FunctionCatalyzes the o-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like l-dopa, alpha-methyl dopa and isoproterenol.    
SequenceMPEAPPLLLAAVLLGLVLLVVLLLLLRHWGWGLCLIGWNEFILQPIHNLLMGDTKEQRIL NHVLQHAEPGNAQSVLEAIDTYCEQKEWAMNVGDKKGKIVDAVIQEHQPSVLLELGAYCG YSAVRMARLLSPGARLITIEINPDCAAITQRMVDFAGVKDKVTLVVGASQDIIPQLKKKY DVDTLDMVFLDHWKDRYLPDTLLLEECGLLRKGTVLLADNVICPGAPDFLAHVRGSSCFE CTHYQSFLEYREVVDGLEKAIYKGPGSEAGP
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3,4-DIHYDROXY-2-NITROPHENYL)[6]
1- (3,4-dihydroxy-2-nitrophenyl)-2-phenylethanone[7]
1- (3,4-dihydroxy-5-nitrophenyl)-2-phenoxyethanone[8]
3,5-Dinitrocatechol[9]
5,6-dihydroxy-7-nitro-2,3-dihydroinden-1-one[7]
6,7-dihydroxy-8-nitro-1-tetralone[7]
7,8-dihydroxy-4-phenyl-2H-chromen-2-one[6]
BIA[6]
BIA 3-202[10]
Entacapone[2][3]
Entacapone+levodopa+carbidopa[5]
NEBICAPONE[7]
Tolcapone[3][4]
MultitargetEntacapone+levodopa+carbidopa[5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1New medical and surgical treatments for Parkinson's disease. Curr Opin Neurol. 1994 Aug;7(4):346-52. To Reference
Ref 2Entacapone: a catechol-O-methyltransferase inhibitor for the adjunctive treatment of Parkinson's disease. Clin Ther. 2001 Jun;23(6):802-32; discussion 771. To Reference
Ref 3Catechol-O-methyltransferase inhibitors in the management of Parkinson's disease. Semin Neurol. 2001;21(1):15-22. To Reference
Ref 4Tolcapone: a novel approach to Parkinson's disease. Am J Health Syst Pharm. 1999 Nov 1;56(21):2195-205. To Reference
Ref 5Emerging drugs for restless legs syndrome. Expert Opin Emerg Drugs. 2005 Aug;10(3):537-52. To Reference
Ref 6Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 7J Med Chem. 2005 Dec 15;48(25):8070-8.Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase. To Reference
Ref 8J Med Chem. 2004 Dec 2;47(25):6207-17.Synthesis, biological evaluation, and molecular modeling studies of a novel, peripherally selective inhibitor of catechol-O-methyltransferase. To Reference
Ref 9Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 10Chemical synthesis and characterization of conjugates of a novel catechol-O-methyltransferase inhibitor. Bioconjug Chem. 2002 Sep-Oct;13(5):1112-8. To Reference



 

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