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Tyrosine phosphorylation inhibits PKM2 to promote the Warburg effect and tumor growth.
Hitosugi T, Kang S, Vander Heiden MG, Chung TW, Elf S, Lythgoe K, Dong S, Lonial S, Wang X, Chen GZ, Xie J, Gu TL, Polakiewicz RD, Roesel JL, Boggon TJ, Khuri FR, Gilliland DG, Cantley LC, Kaufman J, Chen J. Hitosugi T, et al. Among authors: cantley lc. Sci Signal. 2009 Nov 17;2(97):ra73. doi: 10.1126/scisignal.2000431. Sci Signal. 2009. PMID: 19920251 Free PMC article.
Pyruvate kinase M2 is a phosphotyrosine-binding protein.
Christofk HR, Vander Heiden MG, Wu N, Asara JM, Cantley LC. Christofk HR, et al. Among authors: cantley lc. Nature. 2008 Mar 13;452(7184):181-6. doi: 10.1038/nature06667. Nature. 2008. PMID: 18337815
Cancer's insatiable appetite.
Locasale JW, Cantley LC, Vander Heiden MG. Locasale JW, et al. Among authors: cantley lc. Nat Biotechnol. 2009 Oct;27(10):916-7. doi: 10.1038/nbt1009-916. Nat Biotechnol. 2009. PMID: 19816448 Free PMC article.
Identification of small molecule inhibitors of pyruvate kinase M2.
Vander Heiden MG, Christofk HR, Schuman E, Subtelny AO, Sharfi H, Harlow EE, Xian J, Cantley LC. Vander Heiden MG, et al. Among authors: cantley lc. Biochem Pharmacol. 2010 Apr 15;79(8):1118-24. doi: 10.1016/j.bcp.2009.12.003. Epub 2009 Dec 11. Biochem Pharmacol. 2010. PMID: 20005212 Free PMC article.
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Jiang JK, Boxer MB, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW, Inglese J, Cantley LC, Auld DS, Thomas CJ. Jiang JK, et al. Among authors: cantley lc. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3387-93. doi: 10.1016/j.bmcl.2010.04.015. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20451379 Free PMC article.
673 results