Characterization of Non-Nitrocatechol Pan and Isoform Specific Catechol-O-methyltransferase Inhibitors and Substrates
نویسندگان
چکیده
منابع مشابه
Nitrocatechol derivatives as inhibitors of catechol-O-methyltransferase.
Catechol-0-methyltransferase (EC 2.1.1.6; COMT) catalyses Sadenosylmethionine-dependent methylation of a variety of catechols and plays a role in terminating the activities of the catecholamine neurotransmitters dopamine and noradrenaline. Two isoenzymes, the soluble and membrane-bound forms (S-COMT and MB-COMT) are present in most tissues and although the former is more abundant, their differe...
متن کاملCatechol O-Methyltransferase: Glucuronidation of Inhibitors and Methylation of Substrates
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متن کاملPurification and characterization of Streptomyces griseus catechol O-methyltransferase.
A soluble (100,000 x g supernatant) methyltransferase catalyzing the transfer of the methyl group of S-adenosyl-L-methionine to catechols was present in cell extracts of Streptomyces griseus. A simple, general, and rapid catechol-based assay method was devised for enzyme purification and characterization. The enzyme was purified 141-fold by precipitation with ammonium sulfate and successive chr...
متن کاملMolecular modeling and metabolic studies of the interaction of catechol-O-methyltransferase and a new nitrocatechol inhibitor.
Catechol-O-methyltransferase (COMT, EC 2.1.1.6) plays a central role in the metabolic inactivation of neurotransmitters and neuroactive xenobiotics possessing a catechol motif. 1-(3,4-Dihydroxy-5-nitrophenyl)-2-phenyl-ethanone (BIA 3-202) is a novel nitrocatechol-type inhibitor of COMT, the potential clinical benefit of which is currently being evaluated in the treatment of Parkinson's disease....
متن کاملCharacterization of NF-kB-mediated inhibition of catechol-O-methyltransferase
BACKGROUND Catechol-O-methyltransferase (COMT), an enzyme that metabolizes catecholamines, has recently been implicated in the modulation of pain. Specifically, low COMT activity is associated with heightened pain perception and development of musculoskeletal pain in humans as well as increased experimental pain sensitivity in rodents. RESULTS We report that the proinflammatory cytokine tumor...
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ژورنال
عنوان ژورنال: ACS Chemical Neuroscience
سال: 2011
ISSN: 1948-7193,1948-7193
DOI: 10.1021/cn200109w