title: 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.
authors.affiliation: Institute of Biomolecular Chemistry of CNR, Padova Unit, Via Marzolo 1, Padova 35131, Italy. paolo.ruzza@unipd.it.
authors.forename: Paolo
authors.initials: P
authors.lastname: Ruzza
authors.forename: Andrea
authors.initials: A
authors.lastname: Calderan