Glyoxalase inhibitors as potential anticancer agents

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Abstract

A study of a series of S-alkylglutathiones as inhibitors of the enzyme, glyoxalase I, revealed that a non-polar region exists on the enzyme which plays an important role in the formation of an enzyme-inhibitor complex. The amount of inhibition of glyoxalase increases as the alkyl chain is lengthened from methyl to n-octyl. By taking advantage of the non-polar region of the enzyme, compounds have been prepared which are 435 times more active than the previously reported S-methylglutathione.

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Supported by Grant CA-10979-01 from the National Cancer Institute and a grant from the Minnesota Division of the American Cancer Society.

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