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Page 1
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
Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA. Thomenius MJ, et al. Among authors: copeland ra. PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018. PLoS One. 2018. PMID: 29856759 Free PMC article.
Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss.
Fedoriw A, Rajapurkar SR, O'Brien S, Gerhart SV, Mitchell LH, Adams ND, Rioux N, Lingaraj T, Ribich SA, Pappalardi MB, Shah N, Laraio J, Liu Y, Butticello M, Carpenter CL, Creasy C, Korenchuk S, McCabe MT, McHugh CF, Nagarajan R, Wagner C, Zappacosta F, Annan R, Concha NO, Thomas RA, Hart TK, Smith JJ, Copeland RA, Moyer MP, Campbell J, Stickland K, Mills J, Jacques-O'Hagan S, Allain C, Johnston D, Raimondi A, Porter Scott M, Waters N, Swinger K, Boriack-Sjodin A, Riera T, Shapiro G, Chesworth R, Prinjha RK, Kruger RG, Barbash O, Mohammad HP. Fedoriw A, et al. Among authors: copeland ra. Cancer Cell. 2019 Jul 8;36(1):100-114.e25. doi: 10.1016/j.ccell.2019.05.014. Epub 2019 Jun 27. Cancer Cell. 2019. PMID: 31257072 Free article.
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.
Chemogenetic analysis of human protein methyltransferases.
Richon VM, Johnston D, Sneeringer CJ, Jin L, Majer CR, Elliston K, Jerva LF, Scott MP, Copeland RA. Richon VM, et al. Among authors: copeland ra. Chem Biol Drug Des. 2011 Aug;78(2):199-210. doi: 10.1111/j.1747-0285.2011.01135.x. Epub 2011 Jun 16. Chem Biol Drug Des. 2011. PMID: 21564555
222 results