ACSL4 dictates ferroptosis sensitivity by shaping cellular lipid composition

Nat Chem Biol. 2017 Jan;13(1):91-98. doi: 10.1038/nchembio.2239. Epub 2016 Nov 14.

Abstract

Ferroptosis is a form of regulated necrotic cell death controlled by glutathione peroxidase 4 (GPX4). At present, mechanisms that could predict sensitivity and/or resistance and that may be exploited to modulate ferroptosis are needed. We applied two independent approaches-a genome-wide CRISPR-based genetic screen and microarray analysis of ferroptosis-resistant cell lines-to uncover acyl-CoA synthetase long-chain family member 4 (ACSL4) as an essential component for ferroptosis execution. Specifically, Gpx4-Acsl4 double-knockout cells showed marked resistance to ferroptosis. Mechanistically, ACSL4 enriched cellular membranes with long polyunsaturated ω6 fatty acids. Moreover, ACSL4 was preferentially expressed in a panel of basal-like breast cancer cell lines and predicted their sensitivity to ferroptosis. Pharmacological targeting of ACSL4 with thiazolidinediones, a class of antidiabetic compound, ameliorated tissue demise in a mouse model of ferroptosis, suggesting that ACSL4 inhibition is a viable therapeutic approach to preventing ferroptosis-related diseases.

MeSH terms

  • Animals
  • Apoptosis*
  • Cell Death / drug effects
  • Cell Line
  • Cell Survival / drug effects
  • Coenzyme A Ligases / antagonists & inhibitors
  • Coenzyme A Ligases / deficiency
  • Coenzyme A Ligases / metabolism*
  • Female
  • Glutathione Peroxidase / deficiency
  • Glutathione Peroxidase / metabolism*
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Mammary Neoplasms, Experimental / drug therapy
  • Mammary Neoplasms, Experimental / metabolism*
  • Mammary Neoplasms, Experimental / pathology
  • Mice
  • Mice, Knockout
  • Necrosis
  • Phospholipid Hydroperoxide Glutathione Peroxidase
  • Thiazolidinediones / pharmacology

Substances

  • Hypoglycemic Agents
  • Thiazolidinediones
  • Phospholipid Hydroperoxide Glutathione Peroxidase
  • Glutathione Peroxidase
  • glutathione peroxidase 4, mouse
  • Acsl4 protein, mouse
  • Coenzyme A Ligases