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Items: 1 to 20 of 165

1.

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.

Blood. 2013 Aug 8;122(6):1017-25. doi: 10.1182/blood-2013-04-497644. Epub 2013 Jun 25.

2.

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.

J Pharmacol Exp Ther. 2014 Sep;350(3):646-56. doi: 10.1124/jpet.114.214577. Epub 2014 Jul 3.

3.

Pharmacological inhibition of LSD1 for the treatment of MLL-rearranged leukemia.

Feng Z, Yao Y, Zhou C, Chen F, Wu F, Wei L, Liu W, Dong S, Redell M, Mo Q, Song Y.

J Hematol Oncol. 2016 Mar 12;9:24. doi: 10.1186/s13045-016-0252-7.

4.

DOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia.

Chen CW, Koche RP, Sinha AU, Deshpande AJ, Zhu N, Eng R, Doench JG, Xu H, Chu SH, Qi J, Wang X, Delaney C, Bernt KM, Root DE, Hahn WC, Bradner JE, Armstrong SA.

Nat Med. 2015 Apr;21(4):335-43. doi: 10.1038/nm.3832. Epub 2015 Mar 30.

5.

Complementary activities of DOT1L and Menin inhibitors in MLL-rearranged leukemia.

Dafflon C, Craig VJ, Méreau H, Gräsel J, Schacher Engstler B, Hoffman G, Nigsch F, Gaulis S, Barys L, Ito M, Aguadé-Gorgorió J, Bornhauser B, Bourquin JP, Proske A, Stork-Fux C, Murakami M, Sellers WR, Hofmann F, Schwaller J, Tiedt R.

Leukemia. 2017 Jun;31(6):1269-1277. doi: 10.1038/leu.2016.327. Epub 2016 Nov 14.

PMID:
27840424
6.

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.

J Control Release. 2015 Dec 28;220(Pt B):758-65. doi: 10.1016/j.jconrel.2015.09.023. Epub 2015 Sep 15.

PMID:
26385168
7.

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.

Cancer Cell. 2011 Jul 12;20(1):53-65. doi: 10.1016/j.ccr.2011.06.009.

8.

DOT1L inhibition sensitizes MLL-rearranged AML to chemotherapy.

Liu W, Deng L, Song Y, Redell M.

PLoS One. 2014 May 23;9(5):e98270. doi: 10.1371/journal.pone.0098270. eCollection 2014.

9.

Histone H2B ubiquitin ligase RNF20 is required for MLL-rearranged leukemia.

Wang E, Kawaoka S, Yu M, Shi J, Ni T, Yang W, Zhu J, Roeder RG, Vakoc CR.

Proc Natl Acad Sci U S A. 2013 Mar 5;110(10):3901-6. doi: 10.1073/pnas.1301045110. Epub 2013 Feb 14.

10.

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.

Biopharm Drug Dispos. 2014 May;35(4):237-52. doi: 10.1002/bdd.1889. Epub 2014 Feb 14.

PMID:
24415392
11.

Mixed lineage rearranged leukaemia: pathogenesis and targeting DOT1L.

Stein EM, Tallman MS.

Curr Opin Hematol. 2015 Mar;22(2):92-6. doi: 10.1097/MOH.0000000000000123. Review.

PMID:
25635757
12.

Targeting DOT1L and HOX gene expression in MLL-rearranged leukemia and beyond.

Chen CW, Armstrong SA.

Exp Hematol. 2015 Aug;43(8):673-84. doi: 10.1016/j.exphem.2015.05.012. Epub 2015 Jun 25. Review.

13.

H3K79 methylation profiles define murine and human MLL-AF4 leukemias.

Krivtsov AV, Feng Z, Lemieux ME, Faber J, Vempati S, Sinha AU, Xia X, Jesneck J, Bracken AP, Silverman LB, Kutok JL, Kung AL, Armstrong SA.

Cancer Cell. 2008 Nov 4;14(5):355-68. doi: 10.1016/j.ccr.2008.10.001.

14.

Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l.

Deshpande AJ, Chen L, Fazio M, Sinha AU, Bernt KM, Banka D, Dias S, Chang J, Olhava EJ, Daigle SR, Richon VM, Pollock RM, Armstrong SA.

Blood. 2013 Mar 28;121(13):2533-41. doi: 10.1182/blood-2012-11-465120. Epub 2013 Jan 29.

15.

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.

Cancer Cell. 2011 Jul 12;20(1):66-78. doi: 10.1016/j.ccr.2011.06.010.

16.

Hypomethylation and expression of BEX2, IGSF4 and TIMP3 indicative of MLL translocations in acute myeloid leukemia.

Röhrs S, Dirks WG, Meyer C, Marschalek R, Scherr M, Slany R, Wallace A, Drexler HG, Quentmeier H.

Mol Cancer. 2009 Oct 16;8:86. doi: 10.1186/1476-4598-8-86.

17.

DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis.

Nguyen AT, Taranova O, He J, Zhang Y.

Blood. 2011 Jun 23;117(25):6912-22. doi: 10.1182/blood-2011-02-334359. Epub 2011 Apr 26.

18.

The CDK9 Inhibitor Dinaciclib Exerts Potent Apoptotic and Antitumor Effects in Preclinical Models of MLL-Rearranged Acute Myeloid Leukemia.

Baker A, Gregory GP, Verbrugge I, Kats L, Hilton JJ, Vidacs E, Lee EM, Lock RB, Zuber J, Shortt J, Johnstone RW.

Cancer Res. 2016 Mar 1;76(5):1158-69. doi: 10.1158/0008-5472.CAN-15-1070. Epub 2015 Dec 1.

19.

MLL-AF4 Spreading Identifies Binding Sites that Are Distinct from Super-Enhancers and that Govern Sensitivity to DOT1L Inhibition in Leukemia.

Kerry J, Godfrey L, Repapi E, Tapia M, Blackledge NP, Ma H, Ballabio E, O'Byrne S, Ponthan F, Heidenreich O, Roy A, Roberts I, Konopleva M, Klose RJ, Geng H, Milne TA.

Cell Rep. 2017 Jan 10;18(2):482-495. doi: 10.1016/j.celrep.2016.12.054.

20.

MLL partial tandem duplication leukemia cells are sensitive to small molecule DOT1L inhibition.

Kühn MW, Hadler MJ, Daigle SR, Koche RP, Krivtsov AV, Olhava EJ, Caligiuri MA, Huang G, Bradner JE, Pollock RM, Armstrong SA.

Haematologica. 2015 May;100(5):e190-3. doi: 10.3324/haematol.2014.115337. Epub 2015 Jan 16. No abstract available.

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