Transition-state analogues as inhibitors for GABA-aminotransferase

…, PR Andrews, DA Winkler, RI Brinkworth…

Index: Iskander, MN; Andrews, PR; Winkler, DA; Brinkworth, RI; Paola, C Di; et al. European Journal of Medicinal Chemistry, 1991 , vol. 26, # 2 p. 129 - 136

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Citation Number: 5

Abstract

Abstract Our previous calculations on the reaction catalysed by GABA-aminotransferase (GABA-T) have been utilized in this work in order to synthesize a series of reversible inhibitors of this enzyme. The synthesized transition-state analogues and their precursors inhibited GABA-T competitively in both the holoenzyme and apoenzyme at 10− 3 and 10− 5 M, respectively. In the case of the holoenzyme, the transition-state analogue series (the ...