Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis

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. Cancer cells engage in a metabolic program to enhance biosynthesis...

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Veröffentlicht in:	Nature chemical biology 2012-10, Vol.8 (10), p.839-847
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	631/443/319 631/45/535 631/92/613 692/420/755 Animals BASIC BIOLOGICAL SCIENCES Biochemical Engineering Biochemistry Bioorganic Chemistry Biopolymers - chemistry Biopolymers - metabolism Biosynthesis Blotting, Western Cancer Cell Biology Cell Proliferation Cell Transformation, Neoplastic Cells Chemistry Chemistry and Materials Science Chemistry/Food Science Enzymatic activity Enzyme Activators - pharmacology Genes Humans Metabolites Mice Neoplasms - enzymology Neoplasms - metabolism Neoplasms - pathology Proteins Pyruvate Kinase - chemistry Pyruvate Kinase - metabolism Tumors
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