IACS-010759, a potent inhibitor of glycolysis-deficient hypoxic tumor cells, inhibits mitochondrial respiratory complex I through a unique mechanism

The small molecule IACS-010759 has been reported to potently inhibit the proliferation of glycolysis-deficient hypoxic tumor cells by interfering with the functions of mitochondrial NADH-ubiquinone oxidoreductase (complex I) without exhibiting cytotoxicity at tolerated doses in normal cells. Conside...

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Veröffentlicht in:	The Journal of biological chemistry 2020-05, Vol.295 (21), p.7481-7491
Hauptverfasser:	Tsuji, Atsuhito, Akao, Takumi, Masuya, Takahiro, Murai, Masatoshi, Miyoshi, Hideto
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Bioenergetics cancer Cattle Cell Hypoxia - drug effects chemical biology complex I Electron Transport Complex I - antagonists & inhibitors Electron Transport Complex I - metabolism enzyme inhibitor Glycolysis - drug effects Humans hypoxia IACS-010759 mitochondria Mitochondria, Heart - enzymology Mitochondria, Heart - pathology Neoplasm Proteins - antagonists & inhibitors Neoplasm Proteins - metabolism Neoplasms - metabolism Neoplasms - pathology Oxadiazoles - pharmacology photoaffinity labeling Piperidines - pharmacology ubiquinone
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