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Journal Articles

CFT8634, a Clinical Stage BRD9 Bi DAC™ Degrader, Is Active in a Subset of Multiple Myeloma Cell Line Models and Synergistic When Combined with Pomalidomide

Laura L Poling, David Cocozziello, Minsheng He, Eunju Hurh, Riadh Lobbardi, Katrina L Jackson, Stewart L Fisher, Roy M Pollock

Blood (2023) 142 (Supplement 1): 6594.

https://doi.org/10.1182/blood-2023-174555

Published: 2023

Journal Articles

Identification of a First-in-Class PRMT5 Inhibitor with Potent in Vitro and in Vivo Activity in Preclinical Models of Mantle Cell Lymphoma

Blood (2014) 124 (21): 438.

https://doi.org/10.1182/blood.V124.21.438.438

Published: 2014

Journal Articles

Pediatric Dose Determinations for the Phase I Study of the DOT1L Inhibitor, EPZ-5676, in MLL-r Acute Leukemia: Leveraging Early Clinical Data in Adults through Physiologically-Based Pharmacokinetic Modeling

Nigel J Waters, PhD, Blythe Thomson, MD, Iain Gardner, PhD, Trevor N Johnson, PhD, Edward J Olhava, PhD, Roy M Pollock, PhD, Michelle Legler, MSHS, Robert A Copeland, PhD, Eric E Hedrick, MD

Blood (2014) 124 (21): 3619.

https://doi.org/10.1182/blood.V124.21.3619.3619

Published: 2014

Journal Articles

The DOT1L Inhibitor EPZ-5676: Safety and Activity in Relapsed/Refractory Patients with MLL-Rearranged Leukemia

Blood (2014) 124 (21): 387.

https://doi.org/10.1182/blood.V124.21.387.387

Published: 2014

Journal Articles

EZH2 Inhibitor EPZ-6438 Synergizes With Anti-Lymphoma Therapies In Preclinical Models

L. Danielle Johnston, Sarah Knutson, PhD, Natalie Warholic, Christine R Klaus, Tim J. Wigle, PhD, Dorothy Iwanowicz, Bruce A. Littlefield, PhD, Margaret Porter Scott, PhD, Jesse J Smith, PhD, Mikel P Moyer, PhD, Robert A. Copeland, PhD, Roy M. Pollock, PhD, Kevin W Kuntz, PhD, Heike Keilhack, PhD, Alejandra Raimondi

Blood (2013) 122 (21): 4416.

https://doi.org/10.1182/blood.V122.21.4416.4416

Published: 2013

Journal Articles

DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs or DNA Hypomethylating Agents in MLL -Rearranged Leukemia Cells

Christine R Klaus, Scott R. Daigle, PhD, Dorothy Iwanowics, L. Danielle Johnston, Carly A Therkelsen, Jesse J Smith, PhD, Mikel P Moyer, PhD, Robert A. Copeland, PhD, Edward J Olhava, PhD, Margaret Porter Scott, PhD, Roy M. Pollock, PhD, Alejandra Raimondi

Blood (2013) 122 (21): 3930.

https://doi.org/10.1182/blood.V122.21.3930.3930

Published: 2013

Journal Articles

Myeloid Leukemia Cells With MLL partial Tandem Duplication Are Sensitive To Pharmacological Inhibition Of The H3K79 Methyltransferase DOT1L

Michael W.M. Kühn, MD, Michael Hadler, MSc, Scott R. Daigle, PhD, Chun-Wei Chen, PhD, Amit U. Sinha, PhD, Andrei V. Krivtsov, PhD, Edward J. Olhava, PhD, Michael A. Caligiuri, MD, James E Bradner, MD, Roy M. Pollock, PhD, Scott A. Armstrong, MD, PhD

Blood (2013) 122 (21): 1256.

https://doi.org/10.1182/blood.V122.21.1256.1256

Published: 2013

Journal Articles

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

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

Blood (2013) 122 (6): 1017–1025.

https://doi.org/10.1182/blood-2013-04-497644

Published: 2013

Includes: Supplemental data

Journal Articles

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

Aniruddha J. Deshpande, Liying Chen, Maurizio Fazio, Amit U. Sinha, Kathrin M. Bernt, Deepti Banka, Stuart Dias, Jenny Chang, Edward J. Olhava, Scott R. Daigle, Victoria M. Richon, Roy M. Pollock, Scott A. Armstrong

Blood (2013) 121 (13): 2533–2541.

https://doi.org/10.1182/blood-2012-11-465120

Published: 2013

Includes: Supplemental data

Journal Articles

MLL-AF6 Mediated Transformation Is Dependent On the H3K79 Methyl-transferase Dot1l

Aniruddha J Deshpande, Liying Chen, Maurizio Fazio, Amit U. Sinha, Kathrin M Bernt, MD, Deepti Banka, Stuart Dias, Edward J Olhava, PhD, Scott R Daigle, Victoria M Richon, PhD, Roy M Pollock, PhD, Scott A. Armstrong, MD, PhD

Blood (2012) 120 (21): 3502.

https://doi.org/10.1182/blood.V120.21.3502.3502

Published: 2012

Journal Articles

Preclinical Characterization of E7438, a Potent, Selective Inhibitor of Protein Methyltransferase EZH2 with Robust Antitumor Activity Against EZH2 Mutated Non-Hodgkin Lymphoma Xenografts in Mice

Blood (2012) 120 (21): 3712.

https://doi.org/10.1182/blood.V120.21.3712.3712

Published: 2012

Journal Articles

Preclinical Characterization of a Potent, Selective Inhibitor of the Protein Methyltransferase DOT1L for Use in the Treatment of MLL -Rearranged Leukemia.

Roy M Pollock, PhD, Scott R Daigle, Carly A Therkelsen, Aravind Basavapathruni, PhD, Lei Jin, PhD, Christina J Allain, Christine R Klaus, Alejandra Raimondi, PhD, Margaret Porter Scott, PhD, Richard Chesworth, DPhil, Mikel P Moyer, PhD, Robert A Copeland, PhD, Victoria M Richon, PhD, Edward J Olhava, PhD

Blood (2012) 120 (21): 2379.

https://doi.org/10.1182/blood.V120.21.2379.2379

Published: 2012

Journal Articles

Abrogation of MLL-AF10 and CALM-AF10 Mediated Transformation Through Genetic Inactivation or Pharmacological Inhibition of the H3K79 Methyltransferase DOT1L.

Liying Chen, Aniruddha J Deshpande, Deepti Banka, Bernt Kathrin, Stuart Dias, Christian Buske, MD, Edward J Olhava, PhD, Scott R Daigle, Victoria M Richon, PhD, Roy M Pollock, PhD, Scott A. Armstrong, MD, PhD

Blood (2012) 120 (21): 2384.

https://doi.org/10.1182/blood.V120.21.2384.2384

Published: 2012

Journal Articles

Lymphoma-Associated Mutations of EZH2 Result In a Change-of-Function

Victoria M Richon, PhD, Christopher J Sneeringer, MSc, Margaret Porter Scott, PhD, Kevin W Kuntz, PhD, Sarah K Knutson, PhD, Roy M Pollock, PhD, Robert A Copeland, PhD

Blood (2010) 116 (21): 707.

https://doi.org/10.1182/blood.V116.21.707.707

Published: 2010

Journal Articles

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

Roy M Pollock, PhD, Scott R Daigle, Edward J Olhava, PhD, Carly A Therkelsen, Christina R Majer, Jeffrey Song, Christina J Allain, Christopher J Sneeringer, L. Danielle Johnston, Margaret Porter Scott, PhD, Lei Jin, PhD, Kevin W Kuntz, PhD, Richard Chesworth, DPhil, Mikel P Moyer, PhD, Kathrin M Bernt, MD, Scott Armstrong, MD, PhD, Robert A Copeland, PhD, Victoria M Richon, PhD

Blood (2010) 116 (21): 780.

https://doi.org/10.1182/blood.V116.21.780.780

Published: 2010

Journal Articles

Demonstration of a Role for Dot1l In MLL -Rearranged Leukemia Using a Conditional Loss of Function Model

Kathrin M Bernt, MD, Nan Zhu, PhD, Joerg Faber, M.D., Natalie Punt, Roy M Pollock, PhD, Victoria M Richon, PhD, Andrew L. Kung, MD, PhD, Scott Armstrong, MD, PhD

Blood (2010) 116 (21): 62.

https://doi.org/10.1182/blood.V116.21.62.62

Published: 2010

NARROW

CFT8634, a Clinical Stage BRD9 Bi DAC™ Degrader, Is Active in a Subset of Multiple Myeloma Cell Line Models and Synergistic When Combined with Pomalidomide

Identification of a First-in-Class PRMT5 Inhibitor with Potent in Vitro and in Vivo Activity in Preclinical Models of Mantle Cell Lymphoma

Pediatric Dose Determinations for the Phase I Study of the DOT1L Inhibitor, EPZ-5676, in MLL-r Acute Leukemia: Leveraging Early Clinical Data in Adults through Physiologically-Based Pharmacokinetic Modeling

The DOT1L Inhibitor EPZ-5676: Safety and Activity in Relapsed/Refractory Patients with MLL-Rearranged Leukemia

EZH2 Inhibitor EPZ-6438 Synergizes With Anti-Lymphoma Therapies In Preclinical Models

DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs or DNA Hypomethylating Agents in MLL -Rearranged Leukemia Cells

Myeloid Leukemia Cells With MLL partial Tandem Duplication Are Sensitive To Pharmacological Inhibition Of The H3K79 Methyltransferase DOT1L

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

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

MLL-AF6 Mediated Transformation Is Dependent On the H3K79 Methyl-transferase Dot1l

Preclinical Characterization of E7438, a Potent, Selective Inhibitor of Protein Methyltransferase EZH2 with Robust Antitumor Activity Against EZH2 Mutated Non-Hodgkin Lymphoma Xenografts in Mice

Preclinical Characterization of a Potent, Selective Inhibitor of the Protein Methyltransferase DOT1L for Use in the Treatment of MLL -Rearranged Leukemia.

Abrogation of MLL-AF10 and CALM-AF10 Mediated Transformation Through Genetic Inactivation or Pharmacological Inhibition of the H3K79 Methyltransferase DOT1L.

Lymphoma-Associated Mutations of EZH2 Result In a Change-of-Function

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

Demonstration of a Role for Dot1l In MLL -Rearranged Leukemia Using a Conditional Loss of Function Model

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American Society of Hematology

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ASH Publications

American Society of Hematology

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