Pyruvate dehydrogenase (PDH) and α
-ketoglutarate dehydrogenase (KGDH) inhibitor. Disrupts tumor cell mitochondrial metabolism, and increases mitochondrial reactive oxygen species (ROS) production in H460 lung carcinoma cells. Has no effect on KGDH activity in normal bronchial epithelial cells. Induces cell death of multiple tumor cell lines selectively over normal cells in vitro
. Inhibits tumor growth of H460 and BxPC-3 tumor cell xenografts in mice.
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Non-redox-active lipoate derivates disrupt cancer cell mitochondrial metabolism and are potent anticancer agents in vivo.
Zachar et al.
J.Mol.Med. (Berl.), 2011;89:1137
A strategically designed small molecule attacks alpha-ketoglutarate dehydrogenase in tumor cells through a redox process.
Stuart et al.
Cancer Metab., 2014;2:4