Publications by authors named "Roy Pollock"

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Discovery of CFT8634, a Potent, Selective, and Orally Bioavailable Heterobifunctional Degrader of BRD9.
Katrina L Jackson, Ning Yin, Roman V Agafonov, Prasoon Chaturvedi, Kyle Cole, Roy M Pollock

J Med Chem· December 2025

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CFT1946 is an Orally Available Brain-Penetrant BRAFV600-Mutant Degrader that Overcomes BRAF Inhibitor Resistance.
Bridget T Kreger, Yanke Liang, Nicole M Reilly, Meghan E Spears, William A Scott, Roy M Pollock

Cancer Res· October 2025

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High-Throughput Quantitative Assay Technologies for Accelerating the Discovery and Optimization of Targeted Protein Degradation Therapeutics.
Jeffrey R Simard, Linda Lee, Ellen Vieux, Reina Improgo, Trang Tieu, Roy M Pollock

SLAS Discov· April 2021

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Genomic discovery of an evolutionarily programmed modality for small-molecule targeting of an intractable protein surface.
Uddhav K Shigdel, Seung-Joo Lee, Mathew E Sowa, Brian R Bowman, Keith Robison, Roy M Pollock

Proc Natl Acad Sci U S A· July 2020

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The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia.
Eytan M Stein, Guillermo Garcia-Manero, David A Rizzieri, Raoul Tibes, Jesus G Berdeja, Roy Pollock

Blood· June 2018

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Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas.
Sarah K Knutson, Natalie M Warholic, L Danielle Johnston, Christine R Klaus, Tim J Wigle, Roy M Pollock

PLoS One· October 2017

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Mechanisms of Pinometostat (EPZ-5676) Treatment-Emergent Resistance in -Rearranged Leukemia.
Carly T Campbell, Jessica N Haladyna, David A Drubin, Ty M Thomson, Michael J Maria, Roy M Pollock

Mol Cancer Ther· August 2017

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Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma.
Satoshi Kawano, Alexandra R Grassian, Masumi Tsuda, Sarah K Knutson, Natalie M Warholic, Roy M Pollock

PLoS One· July 2017

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Correction: Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma.
Satoshi Kawano, Alexandra R Grassian, Masumi Tsuda, Sarah K Knutson, Natalie M Warholic, Roy M Pollock

PLoS One· January 2017

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MLL1 and DOT1L cooperate with meningioma-1 to induce acute myeloid leukemia.
Simone S Riedel, Jessica N Haladyna, Matthew Bezzant, Brett Stevens, Daniel A Pollyea, Roy M Pollock

J Clin Invest· April 2016

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The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.
Kevin W Kuntz, John E Campbell, Heike Keilhack, Roy M Pollock, Sarah K Knutson

J Med Chem· February 2016

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Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.
Kenneth W Duncan, Nathalie Rioux, P Ann Boriack-Sjodin, Michael J Munchhof, Lawrence A Reiter, Roy M Pollock

ACS Med Chem Lett· February 2016

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Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human.
Nigel J Waters, Sherri A Smith, Edward J Olhava, Kenneth W Duncan, Richard D Burton, Roy M Pollock

Cancer Chemother Pharmacol· January 2016

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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 target.
Nigel J Waters, Scott R Daigle, Bruce N Rehlaender, Aravind Basavapathruni, Carly T Campbell, Roy M Pollock

J Control Release· December 2015

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A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Elayne Chan-Penebre, Kristy G Kuplast, Christina R Majer, P Ann Boriack-Sjodin, Tim J Wigle, Roy M Pollock

Nat Chem Biol· June 2015

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MLL partial tandem duplication leukemia cells are sensitive to small molecule DOT1L inhibition.
Michael W M Kühn, Michael J Hadler, Scott R Daigle, Richard P Koche, Andrei V Krivtsov, Roy M Pollock

Haematologica· May 2015

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Reaction coupling between wild-type and disease-associated mutant EZH2.
Brooke M Swalm, Sarah K Knutson, Natalie M Warholic, Lei Jin, Kevin W Kuntz, Roy M Pollock

ACS Chem Biol· November 2014

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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.
Christine R Klaus, Dorothy Iwanowicz, Danielle Johnston, Carly A Campbell, Jesse J Smith, Roy M Pollock

J Pharmacol Exp Ther· September 2014

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Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.
Aravind Basavapathruni, Edward J Olhava, Scott R Daigle, Carly A Therkelsen, Lei Jin, Roy M Pollock

Biopharm Drug Dispos· May 2014

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Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.
Sarah K Knutson, Satoshi Kawano, Yukinori Minoshima, Natalie M Warholic, Kuan-Chun Huang, Roy M Pollock

Mol Cancer Ther· April 2014

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Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.
Scott R Daigle, Edward J Olhava, Carly A Therkelsen, Aravind Basavapathruni, Lei Jin, Roy M Pollock

Blood· August 2013

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Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
Sarah K Knutson, Natalie M Warholic, Tim J Wigle, Christine R Klaus, Christina J Allain, Roy M Pollock

Proc Natl Acad Sci U S A· May 2013

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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, Roy M Pollock

Blood· March 2013

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Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L.
Aravind Basavapathruni, Lei Jin, Scott R Daigle, Christina R A Majer, Carly A Therkelsen, Roy M Pollock

Chem Biol Drug Des· December 2012

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A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.
Sarah K Knutson, Tim J Wigle, Natalie M Warholic, Christopher J Sneeringer, Christina J Allain, Roy M Pollock

Nat Chem Biol· November 2012

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