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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Advance in Antitumor Agents Targeting Glutathione-S-Transferase

Author(s): Guisen Zhao and Xiaobing Wang

Volume 13 , Issue 12 , 2006

Page: [1461 - 1471] Pages: 11

DOI: 10.2174/092986706776872934

Price: $65

Abstract

Glutathione-S-transferases (GSTs; EC 2.5.1.18), 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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