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Targeting GPX4 in ferroptosis and cancer: chemical strategies and challenges
Trends in Pharmacological Sciences ( IF 13.9 ) Pub Date : 2024-06-11 , DOI: 10.1016/j.tips.2024.05.006
Jiao Liu , Daolin Tang , Rui Kang

Selenoprotein glutathione peroxidase 4 (GPX4) serves as a crucial suppressor of oxidative stress-induced ferroptosis, making it an attractive target for disease therapy. Here, we discuss recent strategies and challenges associated with targeting GPX4 through covalent inhibitors, proteolysis targeting chimera (PROTAC) degraders, and cell-type-specific degraders in the context of cancer.



中文翻译:


针对铁死亡和癌症中的 GPX4:化学策略和挑战



硒蛋白谷胱甘肽过氧化物酶 4 (GPX4) 是氧化应激诱导的铁死亡的重要抑制剂,使其成为疾病治疗的有吸引力的靶点。在这里,我们讨论了在癌症背景下通过共价抑制剂、蛋白水解靶向嵌合体 (PROTAC) 降解剂和细胞类型特异性降解剂靶向 GPX4 的最新策略和挑战。

更新日期:2024-06-11
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