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 GST-activated cytotoxic prodrugs. In the present review we discuss the current structural and pharmacological knowledge of both types of GST-targeting compounds.
Original language | English |
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Pages (from-to) | 763-777 |
Number of pages | 15 |
Journal | Anti-Cancer Agents in Medicinal Chemistry |
Volume | 9 |
Issue number | 7 |
DOIs | |
Publication status | Published - 2009 |
Keywords
- Anticancer drug resistance
- Cancer chemotherapy
- GST inhibitors
- GST-activated prodrugs
ASJC Scopus subject areas
- Cancer Research
- Molecular Medicine
- Pharmacology