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Glutathione peroxidase 4 (GPX4)

In vitro and mouse studies suggest inhibiting GPX4 could help treat cancer by inducing ferroptosis. Ferroptosis is a form of iron-dependent, nonapoptotic cell death. In cancer cells treated with multiple small molecule inducers of ferroptosis, metabolomic and chemoproteomic profiling identified inhibition of GPX4 as a common mechanism of cell death. In mice with fibrosarcoma or oncogene-expressing fibroblast xenografts, the ferroptosis inducers inhibited tumor growth and decreased size of established tumors compared with vehicle. In a panel of cancer cell lines, renal cell carcinomas and diffuse large B cell lymphomas (DLBCLs) were especially sensitive to GPX4-mediated ferroptotic cell death. Next steps include testing the ferroptotic agents in additional cancer models.

SciBX 7(6); doi:10.1038/scibx.2014.166
Published online Feb. 13, 2014

Patent applications filed covering compounds, their use in treating cancer and methods related to evaluating ferroptosis; unlicensed; availability undisclosed

Yang, W.S. et al. Cell;
published online Jan. 16, 2014;
Contact: Brent R. Stockwell, Columbia University, New York, N.Y.