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Reaction coupling between wild-type and disease-associated mutant EZH2.
Swalm BM, Knutson SK, Warholic NM, Jin L, Kuntz KW, Keilhack H, Smith JJ, Pollock RM, Moyer MP, Scott MP, Copeland RA, Wigle TJ. Swalm BM, et al. Among authors: keilhack h. ACS Chem Biol. 2014 Nov 21;9(11):2459-64. doi: 10.1021/cb500548b. Epub 2014 Aug 28. ACS Chem Biol. 2014. PMID: 25154026
EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.
Campbell JE, Kuntz KW, Knutson SK, Warholic NM, Keilhack H, Wigle TJ, Raimondi A, Klaus CR, Rioux N, Yokoi A, Kawano S, Minoshima Y, Choi HW, Porter Scott M, Waters NJ, Smith JJ, Chesworth R, Moyer MP, Copeland RA. Campbell JE, et al. Among authors: keilhack h. ACS Med Chem Lett. 2015 Mar 4;6(5):491-5. doi: 10.1021/acsmedchemlett.5b00037. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005520 Free PMC article.
A687V EZH2 is a gain-of-function mutation found in lymphoma patients.
Majer CR, Jin L, Scott MP, Knutson SK, Kuntz KW, Keilhack H, Smith JJ, Moyer MP, Richon VM, Copeland RA, Wigle TJ. Majer CR, et al. Among authors: keilhack h. FEBS Lett. 2012 Sep 21;586(19):3448-51. doi: 10.1016/j.febslet.2012.07.066. Epub 2012 Jul 28. FEBS Lett. 2012. PMID: 22850114 Free article.
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.
Knutson SK, Wigle TJ, Warholic NM, Sneeringer CJ, Allain CJ, Klaus CR, Sacks JD, Raimondi A, Majer CR, Song J, Scott MP, Jin L, Smith JJ, Olhava EJ, Chesworth R, Moyer MP, Richon VM, Copeland RA, Keilhack H, Pollock RM, Kuntz KW. Knutson SK, et al. Among authors: keilhack h. Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30. Nat Chem Biol. 2012. PMID: 23023262
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
Knutson SK, Warholic NM, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Porter Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM, Kuntz KW, Keilhack H. Knutson SK, et al. Among authors: keilhack h. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. doi: 10.1073/pnas.1303800110. Epub 2013 Apr 25. Proc Natl Acad Sci U S A. 2013. PMID: 23620515 Free PMC article.
Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.
Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H. Knutson SK, et al. Among authors: keilhack h. Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21. Mol Cancer Ther. 2014. PMID: 24563539
Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas.
Knutson SK, Warholic NM, Johnston LD, Klaus CR, Wigle TJ, Iwanowicz D, Littlefield BA, Porter-Scott M, Smith JJ, Moyer MP, Copeland RA, Pollock RM, Kuntz KW, Raimondi A, Keilhack H. Knutson SK, et al. Among authors: keilhack h. PLoS One. 2014 Dec 10;9(12):e111840. doi: 10.1371/journal.pone.0111840. eCollection 2014. PLoS One. 2014. PMID: 25493630 Free PMC article.
Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma.
Kawano S, Grassian AR, Tsuda M, Knutson SK, Warholic NM, Kuznetsov G, Xu S, Xiao Y, Pollock RM, Smith JS, Kuntz KK, Ribich S, Minoshima Y, Matsui J, Copeland RA, Tanaka S, Keilhack H. Kawano S, et al. Among authors: keilhack h. PLoS One. 2016 Jul 8;11(7):e0158888. doi: 10.1371/journal.pone.0158888. eCollection 2016. PLoS One. 2016. PMID: 27391784 Free PMC article.
43 results