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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: copeland ra. 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.
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: copeland ra. PLoS One. 2016 Jul 8;11(7):e0158888. doi: 10.1371/journal.pone.0158888. eCollection 2016. PLoS One. 2016. PMID: 27391784 Free PMC article.
EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL.
Brach D, Johnston-Blackwell D, Drew A, Lingaraj T, Motwani V, Warholic NM, Feldman I, Plescia C, Smith JJ, Copeland RA, Keilhack H, Chan-Penebre E, Knutson SK, Ribich SA, Raimondi A, Thomenius MJ. Brach D, et al. Among authors: copeland ra. Mol Cancer Ther. 2017 Nov;16(11):2586-2597. doi: 10.1158/1535-7163.MCT-16-0840. Epub 2017 Aug 23. Mol Cancer Ther. 2017. PMID: 28835384
Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas.
Sneeringer CJ, Scott MP, Kuntz KW, Knutson SK, Pollock RM, Richon VM, Copeland RA. Sneeringer CJ, et al. Among authors: copeland ra. Proc Natl Acad Sci U S A. 2010 Dec 7;107(49):20980-5. doi: 10.1073/pnas.1012525107. Epub 2010 Nov 15. Proc Natl Acad Sci U S A. 2010. PMID: 21078963 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: copeland ra. 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.
Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L.
Basavapathruni A, Jin L, Daigle SR, Majer CR, Therkelsen CA, Wigle TJ, Kuntz KW, Chesworth R, Pollock RM, Scott MP, Moyer MP, Richon VM, Copeland RA, Olhava EJ. Basavapathruni A, et al. Among authors: copeland ra. Chem Biol Drug Des. 2012 Dec;80(6):971-80. doi: 10.1111/cbdd.12050. Epub 2012 Oct 9. Chem Biol Drug Des. 2012. PMID: 22978415
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: copeland ra. Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30. Nat Chem Biol. 2012. PMID: 23023262
Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.
Daigle SR, Olhava EJ, Therkelsen CA, Basavapathruni A, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Waters NJ, Chesworth R, Moyer MP, Copeland RA, Richon VM, Pollock RM. Daigle SR, et al. Among authors: copeland ra. Blood. 2013 Aug 8;122(6):1017-25. doi: 10.1182/blood-2013-04-497644. Epub 2013 Jun 25. Blood. 2013. PMID: 23801631 Free PMC article.
221 results