Erastin-like anti-Warburg compounds X1 and X4 are GLS2-selective covalent glutaminase inhibitors
Clea Crane,
Morgan Miele,
Ranjini Iyengar
et al.
Abstract:The Warburg effect is a metabolic alteration in cancer cells characterized by aerobic glycolysis and lactate production. A recent phenotypic screen for compounds that reverse Warburg metabolism identified two compounds, X1 and X4, that restore the mitochondrial membrane potential, decrease lactate production, and increase the level of reactive oxygen species in cancer cells. Here we show that X1 and X4 are GLS2-selective covalent glutaminase inhibitors. Glutaminase enzymes hydrolyze glutamine to glutamate, whi… Show more
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