Li Xiaona, Lü Zirui, Wang Cong, Li Kebin, Xu Fengrong, Xu Ping, Niu Yan
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, P.R. China.
ACS Med Chem Lett. 2021 May 3;12(5):720-725. doi: 10.1021/acsmedchemlett.0c00627. eCollection 2021 May 13.
The abnormally high expression of glutathione transferases is closely associated with cancer incidence and drug resistance. By introducing a hydrophobic moiety to the inhibitor structure, we organized a series of degraders of glutathione transferases and demonstrated them potently inducing apoptosis in cancer cells, presenting their pharmacological potential in cancer therapy.
谷胱甘肽转移酶的异常高表达与癌症发病率和耐药性密切相关。通过在抑制剂结构中引入疏水部分，我们构建了一系列谷胱甘肽转移酶降解剂，并证明它们能有效诱导癌细胞凋亡，展现出其在癌症治疗中的药理学潜力。
