Targeting GPX4 in ferroptosis and cancer: chemical strategies and challenges

descriptionPublicationkeyboard_double_arrow_right Article 01 Aug 2024 English Publisher:Elsevier BVJournal:Trends in Pharmacological Sciences, volume 45, pages 666-670 (issn: 0165-6147,

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Authors: Jiao Liu; Daolin Tang; Rui Kang;

doi: 10.1016/j.tips.2024.05.006

pmid: 38866667

Targeting GPX4 in ferroptosis and cancer: chemical strategies and challenges

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Abstract

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.

Related Organizations

The University of Texas Southwestern Medical Center
United States
Third Affiliated Hospital of Guangzhou Medical University
China (People's Republic of)

Keywords

Oxidative Stress, Neoplasms, Ferroptosis, Humans, Animals, Antineoplastic Agents, Enzyme Inhibitors, Phospholipid Hydroperoxide Glutathione Peroxidase

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