Glutathione Transferase (GST)-Activated Prodrugs

Glutathione Transferase (GST)-Activated Prodrugs

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...

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Bibliographic Details
Main Authors: Andrea Calderan, Paolo Ruzza
Format: Article
Language:English
Published: MDPI AG 2013-04-01
Series:Pharmaceutics
Subjects:
glutatione transferase
glutathione
anticancer prodrugs
Online Access:http://www.mdpi.com/1999-4923/5/2/220
Description
Summary: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.
ISSN:1999-4923

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