S-(N-aryl-N-hydroxycarbamoyl) glutathione derivatives are tight-binding inhibitors of glyoxalase I and slow substrates for glyoxalase II

…, T Bakeris, MJ Kavarana, DS Hamilton…

Index: Murthy; Bakeris; Kavarana; Hamilton; Lan; Creighton Journal of Medicinal Chemistry, 1994 , vol. 37, # 14 p. 2161 - 2166

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Citation Number: 62

Abstract

S-(N-Aryl-N-hydroxycarbamoy1) glutathione derivatives are powerful competitive inhibitors of the anticancer target enzyme glyoxalase I. Indeed, the Np-bromophenyl derivative is the strongest inhibitor of the enzyme from human erythrocytes yet reported (Ki= 1.4 X 10-8 M). Structureactivity correlations indicate that the high affinities of the derivatives for both human and yeast glyoxalase I are due to the fact that the derivatives are hydrophobic analogs of ...