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Pyruvate kinase M2 isozyme (PKM2)

Cell culture and mouse studies suggest PKM2 activators could help treat cancer. In a lung cancer cell line grown under hypoxic conditions, PKM2 activators altered glucose metabolism plus other metabolic pathways and decreased cell proliferation compared with vehicle. In xenograft mice with the lung cancer cell line, the PKM2 activator increased the tumor latency period and decreased tumor size compared with vehicle. Next steps include evaluating PKM2 activators in mice with established tumors.
Agios Pharmaceuticals Inc. has a discovery-stage program targeting PKM2 in cancer.
Dynamix Pharmaceuticals Ltd.'s PKM2 activator, DNX-3000, is in preclinical development for cancer.

SciBX 5(40); doi:10.1038/scibx.2012.1049
Published online Oct. 11, 2012

Composition of matter patented; available for licensing from NIH

Anastasiou, D. et al. Nat. Chem. Biol.; published online Aug. 26, 2012;
Contact: Matthew G. Vander Heiden, Massachusetts Institute of Technology, Cambridge, Mass.