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474 results

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Page 1
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: raimondi a. 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.
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: raimondi a. 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: raimondi a. 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: raimondi a. 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: raimondi a. 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
DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells.
Klaus CR, Iwanowicz D, Johnston D, Campbell CA, Smith JJ, Moyer MP, Copeland RA, Olhava EJ, Scott MP, Pollock RM, Daigle SR, Raimondi A. Klaus CR, et al. Among authors: raimondi a. J Pharmacol Exp Ther. 2014 Sep;350(3):646-56. doi: 10.1124/jpet.114.214577. Epub 2014 Jul 3. J Pharmacol Exp Ther. 2014. PMID: 24993360
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: raimondi a. PLoS One. 2014 Dec 10;9(12):e111840. doi: 10.1371/journal.pone.0111840. eCollection 2014. PLoS One. 2014. PMID: 25493630 Free PMC article.
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: raimondi a. Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27. Nat Chem Biol. 2015. PMID: 25915199
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: raimondi a. 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.
Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.
Mitchell LH, Boriack-Sjodin PA, Smith S, Thomenius M, Rioux N, Munchhof M, Mills JE, Klaus C, Totman J, Riera TV, Raimondi A, Jacques SL, West K, Foley M, Waters NJ, Kuntz KW, Wigle TJ, Scott MP, Copeland RA, Smith JJ, Chesworth R. Mitchell LH, et al. Among authors: raimondi a. ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. doi: 10.1021/acsmedchemlett.5b00272. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985287 Free PMC article.
474 results