Advance in antitumor agents targeting glutathione-S-transferase.
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.
Zhao
Guisen
G
Department of Medicinal Chemistry, College of Pharmacy, Shandong University, Jinan, Shandong 250012, PR China. guisenzhao@sdu.edu.cn
Wang
Xiaobing
X
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D017209:Apoptosis / Q000502:physiology; D002384:Catalysis; D004791:Enzyme Inhibitors / Q000008:administration & dosage*; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008658:Inactivation, Metabolic; D048670:MAP Kinase Kinase 4 / Q000378:metabolism; D048848:MAP Kinase Kinase Kinase 5 / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D011355:Prodrugs / Q000494:pharmacology / Q000627:therapeutic use
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011355:Prodrugs; D005982:Glutathione Transferase; D048848:MAP Kinase Kinase Kinase 5; D048670:MAP Kinase Kinase 4