Divergent effects of compounds on the hydrolysis and transpeptidation reactions of γ-glutamyl transpeptidase

S Wickham, N Regan, MB West, VP Kumar…

Index: Wickham, Stephanie; Regan, Nicholas; West, Matthew B.; Kumar, Vidya Prasanna; Thai, Justin; Li, Pui Kai; Cook, Paul F.; Hanigan, Marie H. Journal of Enzyme Inhibition and Medicinal Chemistry, 2012 , vol. 27, # 4 p. 476 - 489

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Citation Number: 6

Abstract

A novel class of inhibitors of the enzyme γ-glutamyl transpeptidase (GGT) were evaluated. The analog OU749 was shown previously to be an uncompetitive inhibitor of the GGT transpeptidation reaction. The data in this study show that it is an equally potent uncompetitive inhibitor of the hydrolysis reaction, the primary reaction catalyzed by GGT in vivo. A series of structural analogs of OU749 were evaluated. For many of the analogs, the ...