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. © 2013 by the authors; licensee MDPI, Basel, Switzerland.
Ruzza, P., & Calderan, A. (2013, April 2). Glutathione transferase (GST)-activated prodrugs. Pharmaceutics. https://doi.org/10.3390/pharmaceutics5020220