Structure??Based Design, Synthesis, and in vitro Evaluation of Bisubstrate Inhibitors for Catechol O??Methyltransferase (COMT)

…, R Jakob??Roetne, F Diederich

Index: Masjost, Birgit; Ballmer, Patrick; Borroni, Edilio; Zuercher, Gerhard; Winkler, Fritz K.; Jakob-Roetne, Roland; Diederich, Francois Chemistry - A European Journal, 2000 , vol. 6, # 6 p. 971 - 982

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Citation Number: 53

Abstract

Abstract The enzyme catechol O-methyltransferase (COMT) catalyzes the Me group transfer from the cofactor S-adenosylmethionine (SAM) to the hydroxy group of catechol substrates. Potential bisubstrate inhibitors of COMT were developed by structure-based design and synthesized. The compounds were tested for in vitro inhibitory activity against COMT obtained from rat liver, and the inhibition kinetics were examined with regard to the ...