The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia von Stein, Eytan M., Garcia-Manero, Guillermo, Rizzieri, David A., Tibes, Raoul, Berdeja, Jesus G., Savona, Michael R., Jongen-Lavrenic, Mojca, Altman, Jessica K., Thomson, Blythe, Blakemore, Stephen J., Daigle, Scott R., Waters, Nigel J., Suttle, A. Benjamin, Clawson, Alicia, Pollock, Roy, Krivtsov, Andrei, Armstrong, Scott A., DiMartino, Jorge, Hedrick, Eric, Löwenberg, Bob, Tallman, Martin S.

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Potent inhibition of DOT1L as treatment of MLL-fusion leukemia von Daigle, Scott R., Olhava, Edward J., Therkelsen, Carly A., Basavapathruni, Aravind, Jin, Lei, Boriack-Sjodin, P. Ann, Allain, Christina J., Klaus, Christine R., Raimondi, Alejandra, Scott, Margaret Porter, Waters, Nigel J., Chesworth, Richard, Moyer, Mikel P., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M.

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Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor von Daigle, Scott R., Olhava, Edward J., Therkelsen, Carly A., Majer, Christina R., Sneeringer, Christopher J., Song, Jeffrey, Johnston, L. Danielle, Scott, Margaret Porter, Smith, Jesse J., Xiao, Yonghong, Jin, Lei, Kuntz, Kevin W., Chesworth, Richard, Moyer, Mikel P., Bernt, Kathrin M., Tseng, Jen-Chieh, Kung, Andrew L., Armstrong, Scott A., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M.

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DOT1L as a therapeutic target for the treatment of DNMT3A-mutant acute myeloid leukemia von Rau, Rachel E., Rodriguez, Benjamin A., Luo, Min, Jeong, Mira, Rosen, Allison, Rogers, Jason H., Campbell, Carly T., Daigle, Scott R., Deng, Lishing, Song, Yongcheng, Sweet, Steve, Chevassut, Timothy, Andreeff, Michael, Kornblau, Steven M., Li, Wei, Goodell, Margaret A.

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Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l von Deshpande, Aniruddha J., Chen, Liying, Fazio, Maurizio, Sinha, Amit U., Bernt, Kathrin M., Banka, Deepti, Dias, Stuart, Chang, Jenny, Olhava, Edward J., Daigle, Scott R., Richon, Victoria M., Pollock, Roy M., Armstrong, Scott A.

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Ivosidenib and Azacitidine in IDH1-Mutated Acute Myeloid Leukemia von Montesinos, Pau, Recher, Christian, Vives, Susana, Zarzycka, Ewa, Wang, Jianxiang, Bertani, Giambattista, Heuser, Michael, Calado, Rodrigo T, Schuh, Andre C, Yeh, Su-Peng, Daigle, Scott R, Hui, Jianan, Pandya, Shuchi S, Gianolio, Diego A, de Botton, Stephane, Döhner, Hartmut

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Identifying and targeting cancer stem cells in leiomyosarcoma: prognostic impact and role to overcome secondary resistance to PI3K/mTOR inhibition von Fourneaux, Benjamin, Bourdon, Aurélien, Dadone, Bérengère, Lucchesi, Carlo, Daigle, Scott R, Richard, Elodie, Laroche-Clary, Audrey, Le Loarer, François, Italiano, Antoine

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Immunologic Correlates of the Abscopal Effect in a SMARCB1/INI1-negative Poorly Differentiated Chordoma after EZH2 Inhibition and Radiotherapy von Gounder, Mrinal M, Zhu, Guo, Roshal, Lev, Lis, Eric, Daigle, Scott R, Blakemore, Steven J, Michaud, Neil R, Hameed, Meera, Hollmann, Travis J

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Expression of Concern to: Identifying and targeting cancer stem cells in leiomyosarcoma: prognostic impact and role to overcome secondary resistance to PI3K/mTOR inhibition von Fourneaux, Benjamin, Bourdon, Aurélien, Dadone, Bérengère, Lucchesi, Carlo, Daigle, Scott R, Richard, Elodie, Laroche-Clary, Audrey, Le Loarer, François, Italiano, Antoine

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MLL partial tandem duplication leukemia cells are sensitive to small molecule DOT1L inhibition von Kühn, Michael W M, Hadler, Michael J, Daigle, Scott R, Koche, Richard P, Krivtsov, Andrei V, Olhava, Edward J, Caligiuri, Michael A, Huang, Gang, Bradner, James E, Pollock, Roy M, Armstrong, Scott A

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DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs and Hypomethylating Agents in MLL-Rearranged Leukemia Cells von Klaus, Christine R., Iwanowicz, Dorothy, Johnston, Danielle, Campbell, Carly A., Smith, Jesse J., Moyer, Mikel P., Copeland, Robert A., Olhava, Edward J., Scott, Margaret Porter, Pollock, Roy M., Daigle, Scott R., Raimondi, Alejandra

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Mechanisms of Pinometostat (EPZ-5676) Treatment-Emergent Resistance in MLL -Rearranged Leukemia von Campbell, Carly T, Haladyna, Jessica N, Drubin, David A, Thomson, Ty M, Maria, Michael J, Yamauchi, Taylor, Waters, Nigel J, Olhava, Edward J, Pollock, Roy M, Smith, Jesse J, Copeland, Robert A, Blakemore, Stephen J, Bernt, Kathrin M, Daigle, Scott R

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Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L von Basavapathruni, Aravind, Jin, Lei, Daigle, Scott R., Majer, Christina R. A., Therkelsen, Carly A., Wigle, Tim J., Kuntz, Kevin W., Chesworth, Richard, Pollock, Roy M., Scott, Margaret P., Moyer, Mikel P., Richon, Victoria M., Copeland, Robert A., Olhava, Edward J.

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MLL1 and DOT1L cooperate with meningioma-1 to induce acute myeloid leukemia von Riedel, Simone S, Haladyna, Jessica N, Bezzant, Matthew, Stevens, Brett, Pollyea, Daniel A, Sinha, Amit U, Armstrong, Scott A, Wei, Qi, Pollock, Roy M, Daigle, Scott R, Jordan, Craig T, Ernst, Patricia, Neff, Tobias, Bernt, Kathrin M

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Abstract 137: Development and application of a 62-gene panel for assessment of somatic sequence and structural variants in tumor DNA derived from non-Hodgkin lymphoma patients trea... von Daigle, Scott R., Angiuoli, Samuel, Jones, Sian, Ribich, Scott, Keilhack, Heike, Sausen, Mark, Ho, Peter T., Blakemore, Stephen J.

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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 ta... von Waters, Nigel J., Daigle, Scott R., Rehlaender, Bruce N., Basavapathruni, Aravind, Campbell, Carly T., Jensen, Tyler B., Truitt, Brett F., Olhava, Edward J., Pollock, Roy M., Stickland, Kim A., Dovletoglou, Angelos

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Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor von Basavapathruni, Aravind, Olhava, Edward J., Daigle, Scott R., Therkelsen, Carly A., Jin, Lei, Boriack-Sjodin, P. Ann, Allain, Christina J., Klaus, Christine R., Raimondi, Alejandra, Scott, Margaret Porter, Dovletoglou, Angelos, Richon, Victoria M., Pollock, Roy M., Copeland, Robert A., Moyer, Mikel P., Chesworth, Richard, Pearson, Paul G., Waters, Nigel J.

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Abstract 312: Evidence of EZH2 dependent and independent mechanisms of tazemetostat treatment emergent resistance in models of diffuse large B cell lymphoma von Campbell, Carly T., Jasper, Jeff S., Daigle, Scott R., Ribich, Scott A., Keilhack, Heike, Smith, Jesse S., Ho, Peter T., Blakemore, Stephen J.

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Abrogation of MLL–AF10 and CALM–AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l von Chen, L, Deshpande, A J, Banka, D, Bernt, K M, Dias, S, Buske, C, Olhava, E J, Daigle, S R, Richon, V M, Pollock, R M, Armstrong, S A

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AGILE: A Global, Randomized, Double-Blind, Phase 3 Study of Ivosidenib + Azacitidine Versus Placebo + Azacitidine in Patients with Newly Diagnosed Acute Myeloid Leukemia with an ID... von Montesinos, Pau, Recher, Christian, Vives, Susana, Zarzycka, Ewa, Wang, Jianxiang, Bertani, Giambattista, Heuser, Michael, Calado, Rodrigo T., Schuh, Andre C., Yeh, Su-Peng, Daigle, Scott R., Hui, Jianan, Zhang, Vickie, Pandya, Shuchi S., Gianolio, Diego A., de Botton, Stephane, Döhner, Hartmut

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