Inhibitor of mitochondrial pyruvate
dehydrogenase kinase (PDK). Shifts pyruvate metabolism from glycolysis and
lactate production to glucose oxidation in the mitochondria. Induces
mitochondrial-dependent apoptosis and reverses the inhibition/downregulation of
KV1.5 channels in cancer but not normal cells. Decreases tumour
growth in vitro and in vivo.
Stacpoole (1989) The
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et al (1998) Evidence for existence of tissue-specific regulation of the
mammalian pyruvate dehydrogenase complex. Biochem.J. 329 191. Bonnet
et al (2007) A mitochondria-K+ channel axis is suppressed
in cancer and its normalization promotes apoptosis and inhibits cancer growth.
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