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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: chesworth r. PLoS One. 2018 Jun 1;13(6):e0197372. doi: 10.1371/journal.pone.0197372. eCollection 2018. PLoS One. 2018. PMID: 29856759 Free PMC article.
Identification of a peptide inhibitor for the histone methyltransferase WHSC1.
Morrison MJ, Boriack-Sjodin PA, Swinger KK, Wigle TJ, Sadalge D, Kuntz KW, Scott MP, Janzen WP, Chesworth R, Duncan KW, Harvey DM, Lampe JW, Mitchell LH, Copeland RA. Morrison MJ, et al. Among authors: chesworth r. PLoS One. 2018 May 9;13(5):e0197082. doi: 10.1371/journal.pone.0197082. eCollection 2018. PLoS One. 2018. PMID: 29742153 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. Among authors: chesworth r. 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.
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: chesworth r. 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: chesworth r. 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: chesworth r. 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.
Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.
Basavapathruni A, Olhava EJ, Daigle SR, Therkelsen CA, Jin L, Boriack-Sjodin PA, Allain CJ, Klaus CR, Raimondi A, Scott MP, Dovletoglou A, Richon VM, Pollock RM, Copeland RA, Moyer MP, Chesworth R, Pearson PG, Waters NJ. Basavapathruni A, et al. Among authors: chesworth r. Biopharm Drug Dispos. 2014 May;35(4):237-52. doi: 10.1002/bdd.1889. Epub 2014 Feb 14. Biopharm Drug Dispos. 2014. PMID: 24415392
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: chesworth r. 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
A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening.
Wigle TJ, Swinger KK, Campbell JE, Scholle MD, Sherrill J, Admirand EA, Boriack-Sjodin PA, Kuntz KW, Chesworth R, Moyer MP, Scott MP, Copeland RA. Wigle TJ, et al. Among authors: chesworth r. J Biomol Screen. 2015 Jul;20(6):810-20. doi: 10.1177/1087057115575689. Epub 2015 Mar 9. J Biomol Screen. 2015. PMID: 25755264
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. Among authors: chesworth r. Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27. Nat Chem Biol. 2015. PMID: 25915199
63 results