Mitochondrial acetyl-coenzyme A (CoA) acetyltransferase 1 (ACAT1) plays a pivotal role in ketogenesis and branched chain amino acid metabolism. Research studies have demonstrated that ACAT1 also plays a key role in carbohydrate metabolism of tumor cells by directly acetylating and inhibiting the activity of the pyruvate dehydrogenase complex (PDH) and PDH phosphatase, which leads to decreased carbon flux through PDH and increased glycolysis. Mechanistically, it has been shown that numerous oncogenic tyrosine kinases directly phosphorylate ACAT1 at Y407, which promotes tetramerization and stabilization of the active enzyme in order to drive glycolysis and tumor growth.