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Advance in Antitumor Agents Targeting Glutathione-S-Transferase

[ Vol. 13 , Issue. 12 ]

Author(s):

Guisen Zhao and Xiaobing Wang   Pages 1461 - 1471 ( 11 )

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

Affiliation:

, Department of MedicinalChemistry, College of Pharmacy, Shandong University, Jinan, Shandong250012, PR China.



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