In vitro inhibition of rat and human glutathione S-transferase isoenzymes by disulfiram and diethyldithiocarbamate.

J.P.H.T.M. Ploemen, M. van Iersel, L.W. Wormhoudt, J.N.M. Commandeur, N.P.E. Vermeulen, P.J. van Bladeren

    Research output: Contribution to JournalArticleAcademicpeer-review

    Abstract

    The drug disulfiram (DSF, Antabuse®) has been used in the therapy of alcohol abuse. It is a potent inhibitor of aldehyde dehydrogenase. Its reduced form, diethyldithiocarbamate (DDTC), and further metabolites show similar activities. DSF and DDTC have also been widely used to inhibit mixed-function oxidases. In this study, the reversible inhibition and time-dependent inactivation of the major rat and human glutathione S-transferase (GST) isoenzymes by DSF and DDTC was investigated. Reversible inhibition, using 1-chloro-2,4-dinitrobenzene as substrate for the GST alpha-, mu-, and pi-class, expressed as I
    Original languageEnglish
    Pages (from-to)197-204
    JournalBiochemical Pharmacology
    Volume52
    DOIs
    Publication statusPublished - 1996

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