%0 Journal Article %T Glutathione Transferase (GST)-Activated Prodrugs %A Paolo Ruzza %A Andrea Calderan %J Pharmaceutics %D 2013 %I MDPI AG %R 10.3390/pharmaceutics5020220 %X 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. %K glutatione transferase %K glutathione %K anticancer prodrugs %U http://www.mdpi.com/1999-4923/5/2/220