Publications by authors named "Patrick Trojer"

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BET inhibitors reduce tumor growth in preclinical models of gastrointestinal gene signature-positive castration-resistant prostate cancer.
Shipra Shukla, Dan Li, Woo Hyun Cho, Dana M Schoeps, Holly M Nguyen, Patrick Trojer

J Clin Invest· August 2025

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Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers.
Patricia J Keller, Elizabeth J Adams, Rentian Wu, Alexandre Côté, Shilpi Arora, Patrick Trojer

Cancer Res· August 2024

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BET inhibitors as a therapeutic intervention in gastrointestinal gene signature-positive castration-resistant prostate cancer.
Shipra Shukla, Dan Li, Holly Nguyen, Jennifer Conner, Gabriella Bayshtok, Patrick Trojer

bioRxiv· March 2024

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A Phase I Study of Pelabresib (CPI-0610), a Small-Molecule Inhibitor of BET Proteins, in Patients with Relapsed or Refractory Lymphoma.
Kristie A Blum, Jeffrey G Supko, Michael B Maris, Ian W Flinn, Andre Goy, Patrick Trojer

Cancer Res Commun· August 2022

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Screening for Small-Molecule Inhibitors of Histone Methyltransferases.
Nico Cantone, Richard T Cummings, Patrick Trojer

Methods Mol Biol· June 2022

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Small molecule targeting of chromatin writers in cancer.
Andrew R Conery, Jennifer L Rocnik, Patrick Trojer

Nat Chem Biol· February 2022

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Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity.
Jacob I Stuckey, Nico R Cantone, Alexandre Côté, Shilpi Arora, Valerie Vivat, Patrick Trojer

J Biol Chem· August 2021

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Author Correction: Merkel cell polyomavirus activates LSD1-mediated blockade of non-canonical BAF to regulate transformation and tumorigenesis.
Donglim Esther Park, Jingwei Cheng, John P McGrath, Matthew Y Lim, Camille Cushman, Patrick Trojer

Nat Cell Biol· June 2020

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Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.
Avinash Khanna, Alexandre Côté, Shilpi Arora, Ludivine Moine, Victor S Gehling, Patrick Trojer

ACS Med Chem Lett· June 2020

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Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
Victor S Gehling, John P McGrath, Martin Duplessis, Avinash Khanna, Francois Brucelle, Patrick Trojer

ACS Med Chem Lett· June 2020

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Merkel cell polyomavirus activates LSD1-mediated blockade of non-canonical BAF to regulate transformation and tumorigenesis.
Donglim Esther Park, Jingwei Cheng, John P McGrath, Matthew Y Lim, Camille Cushman, Patrick Trojer

Nat Cell Biol· May 2020

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Modulation of EZH2 expression in T cells improves efficacy of anti-CTLA-4 therapy.
Sangeeta Goswami, Irina Apostolou, Jan Zhang, Jill Skepner, Swetha Anandhan, Patrick Trojer

J Clin Invest· August 2018

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A KDM5 Inhibitor Increases Global H3K4 Trimethylation Occupancy and Enhances the Biological Efficacy of 5-Aza-2'-Deoxycytidine.
Benjamin R Leadem, Ioannis Kagiampakis, Catherine Wilson, Tommy K Cheung, David Arnott, Patrick Trojer

Cancer Res· March 2018

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From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Jun Liang, Sharada Labadie, Birong Zhang, Daniel F Ortwine, Snahel Patel, Patrick Trojer

Bioorg Med Chem Lett· July 2017

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An Alternative Approach to ChIP-Seq Normalization Enables Detection of Genome-Wide Changes in Histone H3 Lysine 27 Trimethylation upon EZH2 Inhibition.
Brian Egan, Chih-Chi Yuan, Madeleine Lisa Craske, Paul Labhart, Gulfem D Guler, Patrick Trojer

PLoS One· June 2017

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Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Rishi G Vaswani, Victor S Gehling, Les A Dakin, Andrew S Cook, Christopher G Nasveschuk, Patrick Trojer

J Med Chem· November 2016

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Identification of potent, selective KDM5 inhibitors.
Victor S Gehling, Steven F Bellon, Jean-Christophe Harmange, Yves LeBlanc, Florence Poy, Patrick Trojer

Bioorg Med Chem Lett· September 2016

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Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.
Sharada S Labadie, Peter S Dragovich, Richard T Cummings, Gauri Deshmukh, Amy Gustafson, Patrick Trojer

Bioorg Med Chem Lett· September 2016

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Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Jun Liang, Birong Zhang, Sharada Labadie, Daniel F Ortwine, Maia Vinogradova, Patrick Trojer

Bioorg Med Chem Lett· August 2016

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An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.
Maia Vinogradova, Victor S Gehling, Amy Gustafson, Shilpi Arora, Charles A Tindell, Patrick Trojer

Nat Chem Biol· July 2016

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Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes.
John P McGrath, Kaylyn E Williamson, Srividya Balasubramanian, Shobu Odate, Shilpi Arora, Patrick Trojer

Cancer Res· April 2016

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Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Victor S Gehling, Rishi G Vaswani, Christopher G Nasveschuk, Martin Duplessis, Priyadarshini Iyer, Patrick Trojer

Bioorg Med Chem Lett· September 2015

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Epigenetics: Disrupting histone lysine methylation.
Patrick Trojer

Nat Chem Biol· August 2015

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Targeting histone lysine methylation in cancer.
John McGrath, Patrick Trojer

Pharmacol Ther· June 2015

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Mass spectrometric quantification of histone post-translational modifications by a hybrid chemical labeling method.
Tobias M Maile, Anita Izrael-Tomasevic, Tommy Cheung, Gulfem D Guler, Charles Tindell, Patrick Trojer

Mol Cell Proteomics· April 2015

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