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Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park HW, Cantley LC, Thomas CJ, Vander Heiden MG. Anastasiou D, et al. Among authors: leister w. Nat Chem Biol. 2012 Oct;8(10):839-47. doi: 10.1038/nchembio.1060. Nat Chem Biol. 2012. PMID: 22922757 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: leister w. 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.
2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M, Auld DS, Thomas CJ, Boxer MB. Walsh MJ, et al. Among authors: leister w. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6322-7. doi: 10.1016/j.bmcl.2011.08.114. Epub 2011 Sep 14. Bioorg Med Chem Lett. 2011. PMID: 21958545 Free PMC article.
Monitoring compound integrity with cytochrome P450 assays and qHTS.
MacArthur R, Leister W, Veith H, Shinn P, Southall N, Austin CP, Inglese J, Auld DS. MacArthur R, et al. Among authors: leister w. J Biomol Screen. 2009 Jun;14(5):538-46. doi: 10.1177/1087057109336954. Epub 2009 May 29. J Biomol Screen. 2009. PMID: 19483146 Free PMC article.
Identification of a potent new chemotype for the selective inhibition of PDE4.
Skoumbourdis AP, Huang R, Southall N, Leister W, Guo V, Cho MH, Inglese J, Nirenberg M, Austin CP, Xia M, Thomas CJ. Skoumbourdis AP, et al. Among authors: leister w. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. doi: 10.1016/j.bmcl.2008.01.028. Epub 2008 Jan 11. Bioorg Med Chem Lett. 2008. PMID: 18243697 Free PMC article.
Structure activity relationships of human galactokinase inhibitors.
Liu L, Tang M, Walsh MJ, Brimacombe KR, Pragani R, Tanega C, Rohde JM, Baker HL, Fernandez E, Blackman B, Bougie JM, Leister WH, Auld DS, Shen M, Lai K, Boxer MB. Liu L, et al. Among authors: leister wh. Bioorg Med Chem Lett. 2015 Feb 1;25(3):721-7. doi: 10.1016/j.bmcl.2014.11.061. Epub 2014 Dec 13. Bioorg Med Chem Lett. 2015. PMID: 25553891
The pilot phase of the NIH Chemical Genomics Center.
Thomas CJ, Auld DS, Huang R, Huang W, Jadhav A, Johnson RL, Leister W, Maloney DJ, Marugan JJ, Michael S, Simeonov A, Southall N, Xia M, Zheng W, Inglese J, Austin CP. Thomas CJ, et al. Among authors: leister w. Curr Top Med Chem. 2009;9(13):1181-93. doi: 10.2174/156802609789753644. Curr Top Med Chem. 2009. PMID: 19807664 Free PMC article. Review.
40 results