Inactivation of the ferroptosis regulator Gpx4 triggers acute renal failure in mice

JP Friedmann Angeli, M Schneider, B Proneth…�- Nature cell�…, 2014 - nature.com
JP Friedmann Angeli, M Schneider, B Proneth, YY Tyurina, VA Tyurin, VJ Hammond…
Nature cell biology, 2014nature.com
Ferroptosis is a non-apoptotic form of cell death induced by small molecules in specific
tumour types, and in engineered cells overexpressing oncogenic RAS. Yet, its relevance in
non-transformed cells and tissues is unexplored and remains enigmatic. Here, we provide
direct genetic evidence that the knockout of glutathione peroxidase 4 (Gpx4) causes cell
death in a pathologically relevant form of ferroptosis. Using inducible Gpx4−/− mice, we
elucidate an essential role for the glutathione/Gpx4 axis in preventing lipid-oxidation�…
Abstract
Ferroptosis is a non-apoptotic form of cell death induced by small molecules in specific tumour types, and in engineered cells overexpressing oncogenic RAS. Yet, its relevance in non-transformed cells and tissues is unexplored and remains enigmatic. Here, we provide direct genetic evidence that the knockout of glutathione peroxidase 4 (Gpx4) causes cell death in a pathologically relevant form of ferroptosis. Using inducible Gpx4−/− mice, we elucidate an essential role for the glutathione/Gpx4 axis in preventing lipid-oxidation-induced acute renal failure and associated death. We furthermore systematically evaluated a library of small molecules for possible ferroptosis inhibitors, leading to the discovery of a potent spiroquinoxalinamine derivative called Liproxstatin-1, which is able to suppress ferroptosis in cells, in Gpx4−/− mice, and in a pre-clinical model of ischaemia/reperfusion-induced hepatic damage. In sum, we demonstrate that ferroptosis is a pervasive and dynamic form of cell death, which, when impeded, promises substantial cytoprotection.
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