Anticancer drugs targeting glutathione S-transferase π
10.16438/j.0513-4870.2015-0961
- VernacularTitle:基于GSTπ的抗肿瘤药物研究进展
- Author:
Pian ZOU
1
;
Jiang-hong PEI
1
;
Wei SHI
1
;
Li CHEN
1
Author Information
1. Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China
- Publication Type:REVIEWS
- Keywords:
glutathione S-transferase π;
inhibitor;
anticancer;
prodrug;
drug-resistant
- From:
Acta Pharmaceutica Sinica
2016;51(2):241-
- CountryChina
- Language:Chinese
-
Abstract:
Glutathione S-transferase (GSTπ), one of the phase Ⅱ detoxification enzymes, is usually over-expressed in many human tumors. It displays a key role in protecting cells through catalyzing the conjugation of glutathione (GSH) with a broad range of electrophilic substrates including chemotherapeutic agents. As the above conjugates can be effluxed from cells easily, the efficacy of various chemotherapeutic agents is reduced. Recent studies suggest that GSTπ also plays an important role in inhibiting apoptosis through blocking the JNK signaling pathway. In this way, GSTπ protects cells from apoptosis. Therefore, GSTπ has become an attractive target against cancers, especially for drug-resistant tumors. A great deal of effort has been devoted to the discovery of GSTπ inhibitors and prodrugs over the last decade. In connection with authors' current research, we provide a review on studies on progress of GSTπ inhibitors and prodrugs along with the future strategies.
