Journal of medicinal chemistry

Catechol O-Methyltransferase. 12. Affinity labeling the active site with the oxidation products of 5, 6-Dihydroxyindole

RT Borchardt, P Bhatia

Index: Borchardt, Ronald T.; Bhatia, Pramila Journal of Medicinal Chemistry, 1982 , vol. 25, # 3 p. 263 - 271

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Citation Number: 23

Abstract

5, 6-Dihydroxyindole (5, 6-DHI) and a series of 4-and/or 7-methylated analogues of 5, 6-DHI have been synthesized and evaluated for their ability to inactivate purified rat liver catechol 0- methyltransferase (COMT). The inactivation of COMT by these agents could be prevented by excluding oxygen from the incubation mixtures, indicating the necessity for their oxidation to the corresponding aminochromes. Substrate protection studies and kinetic studies ...