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Page 1
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: majer c. PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018. PLoS One. 2018. PMID: 29856759 Free PMC article.
Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.
Daigle SR, Olhava EJ, Therkelsen CA, Majer CR, Sneeringer CJ, Song J, Johnston LD, Scott MP, Smith JJ, Xiao Y, Jin L, Kuntz KW, Chesworth R, Moyer MP, Bernt KM, Tseng JC, Kung AL, Armstrong SA, Copeland RA, Richon VM, Pollock RM. Daigle SR, et al. Cancer Cell. 2011 Jul 12;20(1):53-65. doi: 10.1016/j.ccr.2011.06.009. Cancer Cell. 2011. PMID: 21741596 Free PMC 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. Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30. Nat Chem Biol. 2012. PMID: 23023262
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K, Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O, Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland RA, Chesworth R, Duncan KW. Chan-Penebre E, et al. Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27. Nat Chem Biol. 2015. PMID: 25915199
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.
Duncan KW, Rioux N, Boriack-Sjodin PA, Munchhof MJ, Reiter LA, Majer CR, Jin L, Johnston LD, Chan-Penebre E, Kuplast KG, Porter Scott M, Pollock RM, Waters NJ, Smith JJ, Moyer MP, Copeland RA, Chesworth R. Duncan KW, et al. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6. doi: 10.1021/acsmedchemlett.5b00380. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985292 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. 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.
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. 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
35 results