Glutathione-S-transferases (GSTs; EC 18.104.22.168), a family of phase II detoxification enzymes, catalyze the conjugation of glutathione with broad substrates including chemotherapeutic agents, and are involved in cell protection against apoptotic signals by inhibiting the stress-signaling cascade mediated by ASK1 (Apoptosis signal-regulating kinase)-JNK (c-Jun N-terminal kinase). As GSTs are overexpressed in some malignant tumors, GSTs is a promising therapeutic target. This article reviews the progress in the development of GSTs inhibitors and GSTs activated prodrugs.
Keywords: Glutathione-S-transferases, Antitumor agents, Drug-resistance, GST inhibitors, Prodrugs, Apoptosis
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