The Role of Erastin in Ferroptosis and Its Prospects in Cancer Therapy

Yuechen Zhao; Yanqing Li; Ruifeng Zhang; Feng Wang; Tiejun Wang; Yan Jiao

doi:10.2147/OTT.S254995

The Role of Erastin in Ferroptosis and Its Prospects in Cancer Therapy

Onco Targets Ther. 2020 Jun 11:13:5429-5441. doi: 10.2147/OTT.S254995. eCollection 2020.

Authors

Yuechen Zhao¹, Yanqing Li², Ruifeng Zhang¹, Feng Wang³, Tiejun Wang^#¹, Yan Jiao^#⁴

Affiliations

¹ Department of Radiation Oncology, The Second Hospital of Jilin University, Changchun, People's Republic of China.
² Department of Pathophysiology, College of Basic Medical Sciences, Jilin University, Changchun, People's Republic of China.
³ Department of Oral and Maxillofacial Surgery, Hospital of Stomatology, Jilin University, Changchun, People's Republic of China.
⁴ Department of Hepatobiliary and Pancreatic Surgery, The First Hospital of Jilin University, Changchun, People's Republic of China.

^# Contributed equally.

Abstract

Erastin was initially discovered as a small molecule compound that selectively kills tumor cells expressing ST and RAS^V12 and was later widely investigated as an inducer of ferroptosis. Ferroptosis is a recently discovered form of cell death caused by peroxidation induced by the accumulation of intracellular lipid reactive oxygen species (L-ROS) in an iron-dependent manner. Erastin can mediate ferroptosis through a variety of molecules including the cystine-glutamate transport receptor (system X_C ^-), the voltage-dependent anion channel (VDAC), and p53. Erastin is able to enhance the sensitivity of chemotherapy and radiotherapy, suggesting a promising future in cancer therapy. We hope that this review will help to better understand the role of erastin in ferroptosis and lay the foundation for further research and the development of erastin-based cancer therapies in the future.

Keywords: VDAC; cancer; erastin; ferroptosis; p53; system XC−.

Publication types

Review

Grants and funding

This study was funded by Special Project of Medical and Health Professionals of Jilin Province, China (NO.3D5197457429), Department of Science and Technology of Jilin Province, China (20160101119JC) and Department of Finance of Jilin Province, China (Construction Project of Difficulty Gynecologic Oncology Hierarchical Diagnosis and Treatment Medical Association and Precision Radiotherapy Training Base). The funders had no role in study design, decision to publish, or preparation of the manuscript.