1h1d
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CATECHOL O-METHYLTRANSFERASE
OverviewOverview
Catechol-O-methyltransferase (COMT; E.C. 2.1.1.6) is a ubiquitous enzyme, in nature that plays an important role in the metabolism of catechol, neurotransmitters and xenobiotics. In particular, inactivation of drugs, such as L-3,4-dihydroxyphenylalanine (L-DOPA) via O-methylation is of, relevant pharmacological importance, because L-DOPA is currently the most, effective drug used in the treatment of Parkinson's disease. This, justified the interest in developing COMT inhibitors as potential adjuncts, to L-DOPA therapy. The kinetics of inhibition by BIA 3-335, (1-[3,4-dihydroxy-5-nitrophenyl]-3-(N-3'-trifluormethylphenyl)-piperazine-, 1-propanone dihydrochloride) were characterized using recombinant rat, soluble COMT. BIA 3-335 was found to act as a potent, reversible, tight-binding ... [(full description)]
About this StructureAbout this Structure
1H1D is a [Single protein] structure of sequence from [Rattus norvegicus] with MG, SAM and BIA as [ligands]. Active as [[1]], with EC number [2.1.1.6]. Full crystallographic information is available from [OCA].
ReferenceReference
Kinetics and crystal structure of catechol-o-methyltransferase complex with co-substrate and a novel inhibitor with potential therapeutic application., Bonifacio MJ, Archer M, Rodrigues ML, Matias PM, Learmonth DA, Carrondo MA, Soares-Da-Silva P, Mol Pharmacol. 2002 Oct;62(4):795-805. PMID:12237326
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