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Review
. 2020 Jun 11:13:5429-5441.
doi: 10.2147/OTT.S254995. eCollection 2020.

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

Yuechen Zhao  1 , Yanqing Li  2 , Ruifeng Zhang  1 , Feng Wang  3 , Tiejun Wang #  1 , Yan Jiao #  4
Affiliations
Review

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

Yuechen Zhao et al. Onco Targets Ther. .

Abstract

Erastin was initially discovered as a small molecule compound that selectively kills tumor cells expressing ST and RASV12 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 XC -), 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−.

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Conflict of interest statement

The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
The chemical structure of erastin.
Figure 2
Figure 2
Erastin induces ferroptosis by altering the permeability of VDAC.
Figure 3
Figure 3
The relevant pathways of ferroptosis induced by erastin.
See this image and copyright information in PMC

References

    1. Dixon SJ, Lemberg KM, Lamprecht MR, et al. Ferroptosis: an iron-dependent form of nonapoptotic cell death. Cell. 2012;149(5):1060–1072. doi: 10.1016/j.cell.2012.03.042 - DOI - PMC - PubMed
    1. Yu H, Guo P, Xie X, Wang Y, Chen G. Ferroptosis, a new form of cell death, and its relationships with tumourous diseases. J Cell Mol Med. 2017;21(4):648–657. doi: 10.1111/jcmm.13008 - DOI - PMC - PubMed
    1. Toyokuni S. Iron addiction with ferroptosis-resistance in asbestos-induced mesothelial carcinogenesis: toward the era of mesothelioma prevention. Free Radic Biol Med. 2019;133:206–215. doi: 10.1016/j.freeradbiomed.2018.10.401 - DOI - PubMed
    1. Weiland A, Wang Y, Wu W, et al. Ferroptosis and its role in diverse brain diseases. Mol Neurobiol. 2019;56(7):4880–4893. doi: 10.1007/s12035-018-1403-3 - DOI - PMC - PubMed
    1. Hu Z, Zhang H, Yang SK, et al. Emerging role of ferroptosis in acute kidney injury. Oxid Med Cell Longev. 2019;2019:8010614. doi: 10.1155/2019/8010614 - DOI - PMC - PubMed