Dichloroacetate (DCA) as a potential metabolic-targeting therapy for cancer

作者: E D Michelakis , L Webster , J R Mackey

DOI: 10.1038/SJ.BJC.6604554

关键词: Cancer researchAnaerobic glycolysisEndocrinologyCancerWarburg effectPyruvate dehydrogenase kinaseGlycolysisSodium DichloroacetateCancer cellMedicineMitochondrionInternal medicine

摘要: The unique metabolism of most solid tumours (aerobic glycolysis, i.e., Warburg effect) is not only the basis diagnosing cancer with metabolic imaging but might also be associated resistance to apoptosis that characterises cancer. glycolytic phenotype in appears common denominator diverse molecular abnormalities and may a (potentially reversible) suppression mitochondrial function. generic drug dichloroacetate an orally available small molecule that, by inhibiting pyruvate dehydrogenase kinase, increases flux into mitochondria, promoting glucose oxidation over glycolysis. This reverses suppressed results tumour growth vitro vivo. Here, we review scientific clinical rationale supporting rapid translation this promising modulator early-phase trials.

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