Glutathione S-transferase π: a potential role in antitumor therapy.
Glutathione S-transferase π: a potential role in antitumor therapy.
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谷胱甘肽 S-转移酶 Ï：在抗肿瘤治疗中的潜在作用
DOI：
10.2147/dddt.s169833
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发表时间：
2018
期刊：
影响因子：
--
通讯作者：
Feng J
中科院分区：
文献类型：
--
作者：
Dong SC;Sha HH;Xu XY;Hu TM;Lou R;Li H;Wu JZ;Dan C;Feng J
谷胱甘肽S-转移酶π（GSTπ）是一种II相代谢酶，是细胞解毒的重要促进剂。传统的教条认为GSTπ的功能是催化谷胱甘肽（GSH）-底物结合，以在暴露于氧化应激时保护大分子，从而保护细胞免受各种有毒化合物的侵害。在过去的20年中，GSTπ的异常表达与肿瘤对化疗药物的耐药性的发生有关，表明这种酶具有代谢以外的功能。这一发现揭示了药物发现领域令人兴奋的可能性，因为GSTπ抑制剂及其前药为设计以逆转肿瘤耐药性为主要目的的抗癌药物提供了可行的策略。本文结合作者的研究现状，对GSTπ的生物学功能、GSTπ靶向药物的研究进展进行了综述，并对未来的研究策略进行了展望。
Glutathione S-transferase π (GSTπ) is a Phase II metabolic enzyme that is an important facilitator of cellular detoxification. Traditional dogma asserts that GSTπ functions to catalyze glutathione (GSH)-substrate conjunction to preserve the macromolecule upon exposure to oxidative stress, thus defending cells against various toxic compounds. Over the past 20 years, abnormal GSTπ expression has been linked to the occurrence of tumor resistance to chemotherapy drugs, demonstrating that this enzyme possesses functions beyond metabolism. This revelation reveals exciting possibilities in the realm of drug discovery, as GSTπ inhibitors and its prodrugs offer a feasible strategy in designing anticancer drugs with the primary purpose of reversing tumor resistance. In connection with the authors’ current research, we provide a review on the biological function of GSTπ and current developments in GSTπ-targeting drugs, as well as the prospects of future strategies.
影响因子：
28.5
作者：
Raza A;Galili N;Mulford D;Smith SE;Brown GL;Steensma DP;Lyons RM;Boccia R;Sekeres MA;Garcia-Manero G;Mesa RA
通讯作者：
Mesa RA