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Glutathione Transferase (GST)-Activated Prodrugs.

ABSTRACT: Glutathione transferase (formerly GST) catalyzes the inactivation of various electrophile-producing anticancer agents via conjugation to the tripeptide glutathione. Moreover, several data link the overexpression of some GSTs, in particular GSTP1-1, to both natural and acquired resistance to various structurally unrelated anticancer drugs. Tumor overexpression of these proteins has provided a rationale for the search of GST inhibitors and GST activated cytotoxic prodrugs. In the present review we discuss the current structural and pharmacological knowledge of GST-activated cytotoxic compounds.

SUBMITTER: Ruzza P 

PROVIDER: S-EPMC3834953 | biostudies-literature | 2013 Apr

REPOSITORIES: biostudies-literature

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Glutathione Transferase (GST)-Activated Prodrugs.

Ruzza Paolo P   Calderan Andrea A  

Pharmaceutics 20130402 2

Glutathione transferase (formerly GST) catalyzes the inactivation of various electrophile-producing anticancer agents via conjugation to the tripeptide glutathione. Moreover, several data link the overexpression of some GSTs, in particular GSTP1-1, to both natural and acquired resistance to various structurally unrelated anticancer drugs. Tumor overexpression of these proteins has provided a rationale for the search of GST inhibitors and GST activated cytotoxic prodrugs. In the present review we  ...[more]