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Glutathione Transferase (GST)-Activated Prodrugs
Institute of Biomolecular Chemistry of CNR, Padova Unit, Via Marzolo 1, Padova 35131, Italy
* Author to whom correspondence should be addressed.
Received: 28 February 2013; in revised form: 21 March 2013 / Accepted: 22 March 2013 / Published: 2 April 2013
(This article belongs to the Special Issue 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.
Keywords: glutatione transferase; glutathione; anticancer prodrugs
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Ruzza, P.; Calderan, A. Glutathione Transferase (GST)-Activated Prodrugs. Pharmaceutics 2013, 5, 220-231.
Ruzza P, Calderan A. Glutathione Transferase (GST)-Activated Prodrugs. Pharmaceutics. 2013; 5(2):220-231.
Ruzza, Paolo; Calderan, Andrea. 2013. "Glutathione Transferase (GST)-Activated Prodrugs." Pharmaceutics 5, no. 2: 220-231.