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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: pollock rm. 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.
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: pollock rm. 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.
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: pollock rm. 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: pollock rm. 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
Exploring drug delivery for the DOT1L inhibitor pinometostat (EPZ-5676): Subcutaneous administration as an alternative to continuous IV infusion, in the pursuit of an epigenetic target.
Waters NJ, Daigle SR, Rehlaender BN, Basavapathruni A, Campbell CT, Jensen TB, Truitt BF, Olhava EJ, Pollock RM, Stickland KA, Dovletoglou A. Waters NJ, et al. Among authors: pollock rm. J Control Release. 2015 Dec 28;220(Pt B):758-65. doi: 10.1016/j.jconrel.2015.09.023. Epub 2015 Sep 15. J Control Release. 2015. PMID: 26385168
The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia.
Stein EM, Garcia-Manero G, Rizzieri DA, Tibes R, Berdeja JG, Savona MR, Jongen-Lavrenic M, Altman JK, Thomson B, Blakemore SJ, Daigle SR, Waters NJ, Suttle AB, Clawson A, Pollock R, Krivtsov A, Armstrong SA, DiMartino J, Hedrick E, Löwenberg B, Tallman MS. Stein EM, et al. Blood. 2018 Jun 14;131(24):2661-2669. doi: 10.1182/blood-2017-12-818948. Epub 2018 May 3. Blood. 2018. PMID: 29724899 Free PMC article. Clinical Trial.
MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L.
Bernt KM, Zhu N, Sinha AU, Vempati S, Faber J, Krivtsov AV, Feng Z, Punt N, Daigle A, Bullinger L, Pollock RM, Richon VM, Kung AL, Armstrong SA. Bernt KM, et al. Among authors: pollock rm. Cancer Cell. 2011 Jul 12;20(1):66-78. doi: 10.1016/j.ccr.2011.06.010. Cancer Cell. 2011. PMID: 21741597 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: pollock rm. 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
38 results