Oxidized arachidonic and adrenic PEs navigate cells to ferroptosis

Nat Chem Biol. 2017 Jan;13(1):81-90. doi: 10.1038/nchembio.2238. Epub 2016 Nov 14.

Abstract

Enigmatic lipid peroxidation products have been claimed as the proximate executioners of ferroptosis-a specialized death program triggered by insufficiency of glutathione peroxidase 4 (GPX4). Using quantitative redox lipidomics, reverse genetics, bioinformatics and systems biology, we discovered that ferroptosis involves a highly organized oxygenation center, wherein oxidation in endoplasmic-reticulum-associated compartments occurs on only one class of phospholipids (phosphatidylethanolamines (PEs)) and is specific toward two fatty acyls-arachidonoyl (AA) and adrenoyl (AdA). Suppression of AA or AdA esterification into PE by genetic or pharmacological inhibition of acyl-CoA synthase 4 (ACSL4) acts as a specific antiferroptotic rescue pathway. Lipoxygenase (LOX) generates doubly and triply-oxygenated (15-hydroperoxy)-diacylated PE species, which act as death signals, and tocopherols and tocotrienols (vitamin E) suppress LOX and protect against ferroptosis, suggesting a homeostatic physiological role for vitamin E. This oxidative PE death pathway may also represent a target for drug discovery.

MeSH terms

  • Animals
  • Arachidonic Acid / antagonists & inhibitors
  • Arachidonic Acid / metabolism*
  • Cell Death / drug effects
  • Cell Line
  • Coenzyme A Ligases / antagonists & inhibitors
  • Coenzyme A Ligases / deficiency
  • Coenzyme A Ligases / metabolism
  • Fatty Acids, Unsaturated / antagonists & inhibitors
  • Fatty Acids, Unsaturated / metabolism*
  • Female
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Phospholipids / metabolism*

Substances

  • Fatty Acids, Unsaturated
  • Phospholipids
  • adrenic acid
  • Arachidonic Acid
  • Acsl4 protein, mouse
  • Coenzyme A Ligases