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Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis
- Anastasiou, Dimitrios;
- Yu, Yimin;
- Israelsen, William J;
- Jiang, Jian-Kang;
- Boxer, Matthew B;
- Hong, Bum Soo;
- Tempel, Wolfram;
- Dimov, Svetoslav;
- Shen, Min;
- Jha, Abhishek;
- Yang, Hua;
- Mattaini, Katherine R;
- Metallo, Christian M;
- Fiske, Brian P;
- Courtney, Kevin D;
- Malstrom, Scott;
- Khan, Tahsin M;
- Kung, Charles;
- Skoumbourdis, Amanda P;
- Veith, Henrike;
- Southall, Noel;
- Walsh, Martin J;
- Brimacombe, Kyle R;
- Leister, William;
- Lunt, Sophia Y;
- Johnson, Zachary R;
- Yen, Katharine E;
- Kunii, Kaiko;
- Davidson, Shawn M;
- Christofk, Heather R;
- Austin, Christopher P;
- Inglese, James;
- Harris, Marian H;
- Asara, John M;
- Stephanopoulos, Gregory;
- Salituro, Francesco G;
- Jin, Shengfang;
- Dang, Lenny;
- Auld, Douglas S;
- Park, Hee-Won;
- Cantley, Lewis C;
- Thomas, Craig J;
- Vander Heiden, Matthew G
Published Web Location
https://doi.org/10.1038/nchembio.1060Abstract
A small-molecule activator specific for PKM2 binds to a site distinct from the endogenous activator fructose-1,6-bisphosphate, promoting tetramerization and constitutive activation of PKM2, to inhibit xenograft tumor growth in mice.
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