Research progress on GPX4 targeted compounds

Eur J Med Chem. 2024 Aug 5:274:116548. doi: 10.1016/j.ejmech.2024.116548.

Bingru Li ¹, Keguang Cheng ², Tzumei Wang ¹, Xing Peng ³, Ping Xu ¹, Guoquan Liu ¹, Dong Xue ⁴, Ning Jiao ⁵, Chao Wang ⁶

Affiliations

1 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China.
2 School of Chemistry and Pharmaceutical Sciences, State/Ministry of Education of China Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, Guilin, China.
3 Changping Laboratory, Yard 28, Science Park Road, Changping District, Beijing, China; Academy for Advanced Interdisciplinary Studies, Peking University, Beijing, China.
4 Key Laboratory of Applied Surface and Colloid Chemistry, Ministry of Education and School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an, China.
5 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China; Changping Laboratory, Yard 28, Science Park Road, Changping District, Beijing, China.
6 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China. Electronic address: [email protected].

PMID: 38838547 DOI: 10.1016/j.ejmech.2024.116548

Abstract

Blocking the System X_c^-_ GSH^_GPX4 pathway to induce Ferroptosis in tumor cells is a novel strategy for Cancer treatment. GPX4 serves as the core of the System Xc-/GSH/GPX4 pathway and is a predominant target for inducing Ferroptosis in tumor cells. This article summarizes compounds identified in current research that directly target the GPX4 protein, including inhibitors, activators, small molecule degraders, chimeric degraders, and the application of combination therapies with Other drugs, aiming to promote further research on the target and related diseases.

Name
Email *

	Sorry, but the email address you supplied was invalid.