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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Glutathione Transferases as Targets for Cancer Therapy

Author(s): Paolo Ruzza, Antonio Rosato, Carlo Riccardo Rossi, Maura Floreani and Luigi Quintieri

Volume 9, Issue 7, 2009

Page: [763 - 777] Pages: 15

DOI: 10.2174/187152009789056895

Price: $65

Abstract

Besides catalyzing the inactivation of various electrophile-producing anticancer agents via conjugation to the tripeptide glutathione, some cytosolic proteins belonging to the glutathione transferase (formerly glutatione-S-transferase; GST) superfamily are emerging as negative modulators of stress/drug-induced cell apoptosis through the interaction with specific signaling kinases. In addition, 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 GSTactivated cytotoxic prodrugs. In the present review we discuss the current structural and pharmacological knowledge of both types of GST-targeting compounds.

Keywords: GST inhibitors, GST-activated prodrugs, cancer chemotherapy, anticancer drug resistance


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