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Robert A. Copeland
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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
Journal: Blood
Blood (2014) 124 (21): 3619.
https://doi.org/10.1182/blood.V124.21.3619.3619
Published: 2014
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

Elayne Penebre, PhD, Kristy G Kuplast, Christina R Majer, L. Danielle Johnston, MS, Nathalie Rioux, PhD, Michael Munchhof, PhD, Lei Jin, PhD, P. Ann Boriak-Sjodin, PhD, Tim J Wigle, PhD, Suzanne L Jacques, PhD, Kip A West, PhD, Trupti Lingaraj, Kimberly Stickland, PhD, Scott A Ribich, PhD, Alejandra Raimondi, MS, Margaret Porter-Scott, PhD, Nigel J Waters, PhD, Roy M Pollock, PhD, Jesse J Smith, PhD, Olena Barbash, PhD, Ryan G. Kruger, PhD, Robert A Copeland, PhD, Mikel P Moyer, PhD, Richard Chesworth, DPhil, Kenneth W Duncan, PhD
Journal: Blood
Blood (2014) 124 (21): 438.
https://doi.org/10.1182/blood.V124.21.438.438
Published: 2014
Journal Articles

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

Eytan M. Stein, Guillermo Garcia-Manero, MD, David A. Rizzieri, MD, Michael Savona, MD, Raoul Tibes, MD, Jessica K Altman, Mojca Jongen-Lavrencic, MD PhD, Hartmut Döhner, Prof., Scott Armstrong, MD PhD, Roy M Pollock, PhD, Nigel J Waters, PhD, Michelle Legler, MSHS, Blythe Thomson, MD, Scott Daigle, Alice McDonald, Carly Campbell, Ed Olhava, Eric E Hedrick, MD, Bob Lowenberg, MDPhD, Robert A Copeland, PhD, Martin S. Tallman, MD
Journal: Blood
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
Journal: Blood
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
Journal: Blood
Blood (2013) 122 (21): 3930.
https://doi.org/10.1182/blood.V122.21.3930.3930
Published: 2013
Journal Articles

Protein Methyltransferase Inhibitors as Personalized Cancer Therapeutics

Robert A. Copeland, PhD
Journal: Blood
Blood (2013) 122 (21): SCI-21.
https://doi.org/10.1182/blood.V122.21.SCI-21.SCI-21
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
Journal: Blood
Blood (2013) 122 (6): 1017–1025.
https://doi.org/10.1182/blood-2013-04-497644
Published: 2013
Includes: Supplemental data
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
Journal: Blood
Blood (2012) 120 (21): 2379.
https://doi.org/10.1182/blood.V120.21.2379.2379
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

Heike Keilhack, PhD, Akira Yokoi, PhD, Sarah K Knutson, PhD, Tim Wigle, PhD, Natalie Warholic, Satoshi Kawano, PhD, Yukinori Minoshima, PhD, Kuan-Chun Huang, PhD, Galina Kuznetsov, PhD, Namita Kumar, Christine R Klaus, Christina J Allain, Alejandra Raimondi, PhD, Margaret Porter Scott, PhD, Richard Chesworth, DPhil, Mikel P Moyer, PhD, Toshimitsu Uenaka, PhD, Robert A Copeland, PhD, Victoria M Richon, PhD, Roy M Pollock, PhD, Kevin W Kuntz, PhD
Journal: Blood
Blood (2012) 120 (21): 3712.
https://doi.org/10.1182/blood.V120.21.3712.3712
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
Journal: Blood
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
Journal: Blood
Blood (2010) 116 (21): 780.
https://doi.org/10.1182/blood.V116.21.780.780
Published: 2010