Cytochrome P450 oxidoreductase contributes to phospholipid peroxidation in ferroptosis

Nat Chem Biol. 2020 Mar;16(3):302-309. doi: 10.1038/s41589-020-0472-6. Epub 2020 Feb 17.

Abstract

Ferroptosis is widely involved in degenerative diseases in various tissues including kidney, liver and brain, and is a targetable vulnerability in multiple primary and therapy-resistant cancers. Accumulation of phospholipid hydroperoxides in cellular membranes is the hallmark and rate-limiting step of ferroptosis; however, the enzymes contributing to lipid peroxidation remain poorly characterized. Using genome-wide, CRISPR-Cas9-mediated suppressor screens, we identify cytochrome P450 oxidoreductase (POR) as necessary for ferroptotic cell death in cancer cells exhibiting inherent and induced susceptibility to ferroptosis. By genetic depletion of POR in cancer cells, we reveal that POR contributes to ferroptosis across a wide range of lineages and cell states, and in response to distinct mechanisms of ferroptosis induction. Using systematic lipidomic profiling, we further map POR's activity to the lipid peroxidation step in ferroptosis. Hence, our work suggests that POR is a key mediator of ferroptosis and potential druggable target for developing antiferroptosis therapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Death
  • Cell Line, Tumor
  • Clustered Regularly Interspaced Short Palindromic Repeats
  • Cytochrome P-450 Enzyme System / genetics*
  • Cytochrome P-450 Enzyme System / metabolism*
  • Ferroptosis / physiology*
  • Glutathione Peroxidase / metabolism
  • Humans
  • Iron / metabolism
  • Lipid Peroxidation / genetics
  • Lipid Peroxidation / physiology
  • Phospholipids
  • Reactive Oxygen Species / metabolism
  • Signal Transduction

Substances

  • POR protein, human
  • Phospholipids
  • Reactive Oxygen Species
  • Cytochrome P-450 Enzyme System
  • Iron
  • Glutathione Peroxidase