Robert A. Copeland
Active 1988–2025
- 80
- Papers
- 24,623
- Citations
- 69
- h-index
- 78
- i10-index
Citations
Citation sources
Countries
Institutions
Fields
- Biochemistry, Genetics and Molecular Biology55.2%
- Medicine27.7%
- Computer Science5.1%
- Chemistry3.2%
- Immunology and Microbiology2.5%
- Neuroscience2.5%
- Other3.8%
Topics
- Epigenetics and DNA Methylation6.6%
- Cancer-related gene regulation4.4%
- Computational Drug Discovery Methods3.8%
- Protein Degradation and Inhibitors3.1%
- RNA modifications and cancer2.6%
- Histone Deacetylase Inhibitors Research2.4%
- Other77.1%
Coauthors
- Margaret Porter Scott20
- Mikel P. Moyer16
- Richard Chesworth14
- J. Joshua Smith13
- Roy M. Pollock13
- Victoria M. Richon12
- Kevin W. Kuntz11
- Lei Jin11
- Scott Ribich11
- Tim J. Wigle11
- Heike Keilhack10
- P. Ann Boriack‐Sjodin10
- Sarah K. Knutson10
- Alejandra Raimondi9
- Zhihong Lai9
- Christina R. Majer8
- Nigel J. Waters8
- Peter J. Tummino8
- Christine R. Klaus7
- Nathalie Rioux7
- Ronald L. Magolda7
- Carl P. Decicco6
- Christina J. Allain6
- Edward J. Olhava6
All papers
- Drug–target residence time and its implications for lead optimization
Authors: Robert A. Copeland, David L. Pompliano, Thomas D. Meek - Nature Reviews Drug Discovery 2006 cited by 1,446
- The drug–target residence time model: a 10-year retrospective
Authors: Robert A. Copeland - Nature Reviews Drug Discovery 2015 cited by 733
- Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study
Authors: Antoîne Italiano, Jean‐Charles Soria, Maud Toulmonde, Jean‐Marie Michot, Carlo Lucchesi, Andréa Varga, Jean‐Michel Coindre, Stephen J. Blakemore, Alicia Clawson, Benjamin Suttle, Alice McDonald, Mark Woodruff, Scott Ribich, Eric Hedrick, Heike Keilhack, Blythe Thomson, Takashi Owa, Robert A. Copeland, Peter Ho, Vincent Ribrag - The Lancet Oncology 2018 cited by 614
- Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2
Authors: Sarah K. Knutson, Natalie M. Warholic, Tim J. Wigle, Christine R. Klaus, Christina J. Allain, Alejandra Raimondi, Margaret Porter Scott, Richard Chesworth, Mikel P. Moyer, Robert A. Copeland, Victoria M. Richon, Roy M. Pollock, Kevin W. Kuntz, Heike Keilhack - National Academy of Sciences, Proceedings of the National Academy of Sciences 2013 cited by 782
- Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss
Authors: Andrew Fedoriw, Satyajit Rajapurkar, Shane W. O’Brien, Sarah V. Gerhart, Lorna H. Mitchell, Nicholas D. Adams, Nathalie Rioux, Trupti Lingaraj, Scott Ribich, Melissa B. Pappalardi, Niyant Shah, Jenny Laraio, Yan Liu, Michael Butticello, Chris Carpenter, Caretha L. Creasy, Susan Korenchuk, Michael T. McCabe, Charles F. McHugh, Raman P. Nagarajan, Craig D. Wagner, Francesca Zappacosta, Roland S. Annan, N.O. Concha, Roberta Thomas, Timothy K. Hart, J. Joshua Smith, Robert A. Copeland, Mikel P. Moyer, John Campbell, Kim Stickland, James E. Mills, Suzanne Jacques-O’Hagan, Christina J. Allain, Danielle Johnston, Alejandra Raimondi, Margaret Porter Scott, Nigel J. Waters, Kerren K. Swinger, Ann Boriack-Sjodin, Tom Riera, Gideon Shapiro, Richard Chesworth, Rabinder Prinjha, Ryan G. Kruger, Olena Barbash, Helai P. Mohammad - Cancer Cell 2019 cited by 347
- The promise and peril of chemical probes
Authors: C.H. Arrowsmith, James E. Audia, Christopher P. Austin, Jonathan B. Baell, Jonathan P. Bennett, Julian Blagg, C. Bountra, Paul E. Brennan, Peter J. Brown, Mark E. Bunnage, Carolyn Buser‐Doepner, Robert M Campbell, Adrian J. Carter, Philip Cohen, Robert A. Copeland, Ben Cravatt, Jayme L. Dahlin, Dashyant Dhanak, A.M. Edwards, Mathias Frederiksen, Stephen V. Frye, Nathanael S. Gray, Charles E. Grimshaw, David Hepworth, Trevor Howe, K. Huber, Jian Jin, Stefan Knapp, Joanne Kotz, Ryan G. Kruger, Derek Lowe, Mary M. Mader, Brian D. Marsden, Anke Mueller‐Fahrnow, Susanne Müller, Rónán C. O’Hagan, John P. Overington, Dafydd R. Owen, Saul H. Rosenberg, Ruth A. Ross, Bryan L. Roth, Matthieu Schapira, Stuart L. Schreiber, Brian K. Shoichet, M. Sundström, Giulio Superti-Furga, Jack Taunton, Leticia Toledo‐Sherman, Chris Walpole, Michael A. Walters, Timothy M. Willson, Paul Workman, Robert N. Young, William J. Zuercher - Nature Chemical Biology 2015 cited by 850
- Potent inhibition of DOT1L as treatment of MLL-fusion leukemia
Authors: 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 cited by 725
- A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
Authors: Elayne Chan-Penebre, Kristy G. Kuplast, Christina R. Majer, P. Ann Boriack‐Sjodin, Tim J. Wigle, L. Danielle Johnston, Nathalie Rioux, Michael J. Munchhof, Lei Jin, Suzanne L. Jacques, Kip A. West, Trupti Lingaraj, Kimberly Stickland, Scott Ribich, Alejandra Raimondi, Margaret Porter Scott, Nigel J. Waters, Roy M. Pollock, J. Joshua Smith, Olena Barbash, Melissa B. Pappalardi, Thau Ho, Kelvin Nurse, Khyati Oza, Kathleen T. Gallagher, Ryan G. Kruger, Mikel P. Moyer, Robert A. Copeland, Richard Chesworth, Kenneth W. Duncan - Nature Chemical Biology 2015 cited by 546
- Evaluation of Enzyme Inhibitors in Drug Discovery
Authors: Robert A. Copeland - 2013 cited by 673
- Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists.
Authors: Robert A. Copeland - 2005 cited by 1,061
- Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor
Authors: Scott R. Daigle, Edward J. Olhava, Carly A. Therkelsen, Christina R. Majer, Christopher J. Sneeringer, Jeffrey Song, L. Danielle Johnston, Margaret Porter Scott, J. Joshua Smith, Yonghong Xiao, Lei Jin, Kevin W. Kuntz, Richard Chesworth, Mikel P. Moyer, Kathrin M. Bernt, Jen‐Chieh Tseng, Andrew L. Kung, Scott A. Armstrong, Robert A. Copeland, Victoria M. Richon, Roy M. Pollock - Cancer Cell 2011 cited by 934
- Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas
Authors: Christopher J. Sneeringer, Margaret Porter Scott, Kevin W. Kuntz, Sarah K. Knutson, Roy M. Pollock, Victoria M. Richon, Robert A. Copeland - National Academy of Sciences, Proceedings of the National Academy of Sciences 2010 cited by 680
- Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2 -Mutant Non-Hodgkin Lymphoma
Authors: Sarah K. Knutson, Satoshi Kawano, Yukinori Minoshima, Natalie M. Warholic, Kuan‐Chun Huang, Yonghong Xiao, Tadashi Kadowaki, Mai Uesugi, Galina Kuznetsov, Namita Kumar, Tim J. Wigle, Christine R. Klaus, Christina J. Allain, Alejandra Raimondi, Nigel J. Waters, J. Joshua Smith, Margaret Porter-Scott, Richard Chesworth, Mikel P. Moyer, Robert A. Copeland, Victoria M. Richon, Toshimitsu Uenaka, Roy M. Pollock, Kevin W. Kuntz, Akira Yokoi, Heike Keilhack - Molecular Cancer Therapeutics 2014 cited by 522
- A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
Authors: Sarah K. Knutson, Tim J. Wigle, Natalie M. Warholic, Christopher J. Sneeringer, Christina J. Allain, Christine R. Klaus, Joelle D. Sacks, Alejandra Raimondi, Christina R. Majer, Jeffrey Song, Margaret Porter Scott, Lei Jin, J. Joshua Smith, Edward J. Olhava, Richard Chesworth, Mikel P. Moyer, Victoria M. Richon, Robert A. Copeland, Heike Keilhack, Roy M. Pollock, Kevin W. Kuntz - Nature Chemical Biology 2012 cited by 761
- Antitumor activity of an allosteric inhibitor of centromere-associated protein-E
Authors: Kenneth W. Wood, Latesh Lad, Lusong Luo, Xiangping Qian, Steven D. Knight, Neysa Nevins, Katjuša Brejc, David Sutton, Aidan G. Gilmartin, Penelope Chua, Radhika Desai, Stephen P. Schauer, Dean E. McNulty, Roland S. Annan, Lisa D. Belmont, Carlos Vázquez García, Yan Lee, Melody Diamond, Leo F. Faucette, Michele Giardiniere, ShuYun Zhang, Chiu-Mei Sun, Justin D. Vidal, Serge Lichtsteiner, William D. Cornwell, Joel Greshock, Richard Wooster, Jeffrey T. Finer, Robert A. Copeland, Pearl S. Huang, David J. Morgans, Dashyant Dhanak, Gustave Bergnes, Roman Sakowicz, Jeffrey R. Jackson - National Academy of Sciences, Proceedings of the National Academy of Sciences 2010 cited by 254
- RNA-modifying proteins as anticancer drug targets
Authors: P. Ann Boriack‐Sjodin, Scott Ribich, Robert A. Copeland - Nature Reviews Drug Discovery 2018 cited by 156
- Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma
Authors: Allison E. Drew, Oscar Moradei, Suzanne L. Jacques, Nathalie Rioux, Ann Boriack-Sjodin, Christina J. Allain, Margaret Porter Scott, Lei Jin, Alejandra Raimondi, Jessica L. Handler, Heidi M. Ott, Ryan G. Kruger, Michael T. McCabe, Christopher J. Sneeringer, Thomas V. Riera, Gideon Shapiro, Nigel J. Waters, Lorna H. Mitchell, Kenneth W. Duncan, Mikel P. Moyer, Robert A. Copeland, J. Joshua Smith, Richard Chesworth, Scott Ribich - Scientific Reports 2017 cited by 136
- Residence Time of Receptor−Ligand Complexes and Its Effect on Biological Function
Authors: Peter J. Tummino, Robert A. Copeland - Biochemistry 2008 cited by 546
- Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666
Authors: Kenneth W. Duncan, Nathalie Rioux, P. Ann Boriack‐Sjodin, Michael J. Munchhof, Lawrence A. Reiter, Christina R. Majer, Lei Jin, L. Danielle Johnston, Elayne Chan-Penebre, Kristy G. Kuplast, Margaret Porter Scott, Roy M. Pollock, Nigel J. Waters, J. Joshua Smith, Mikel P. Moyer, Robert A. Copeland, Richard Chesworth - ACS Medicinal Chemistry Letters 2015 cited by 151
- Protein methyltransferases as a target class for drug discovery
Authors: Robert A. Copeland, Michael E. Solomon, Victoria M. Richon - Nature Reviews Drug Discovery 2009 cited by 458
- The importance of binding kinetics and drug–target residence time in pharmacology
Authors: Kevin E. Knockenhauer, Robert A. Copeland - British Journal of Pharmacology 2023 cited by 69
- Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase
Authors: Margaret Favata, Kurumi Y. Horiuchi, Elizabeth J. Manos, Andrea J. Daulerio, Deborah A. Stradley, Wendi S. Feeser, Drew E. Van Dyk, William J. Pitts, Richard A. Earl, Frank W. Hobbs, Robert A. Copeland, Ronald L. Magolda, Peggy Scherle, James M. Trzăskos - Journal of Biological Chemistry 1998 cited by 3,029
- The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat
Authors: Kevin W. Kuntz, John E. Campbell, Heike Keilhack, Roy M. Pollock, Sarah K. Knutson, Margaret Porter-Scott, Victoria M. Richon, Chris Sneeringer, Tim J. Wigle, Christina J. Allain, Christina R. Majer, Mikel P. Moyer, Robert A. Copeland, Richard Chesworth - Journal of Medicinal Chemistry 2016 cited by 171
- Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor
Authors: Glenn S. Van Aller, Jeff D. Carson, Wei Tang, Hao Peng, Lin Zhao, Robert A. Copeland, Peter J. Tummino, Lusong Luo - Biochemical and Biophysical Research Communications 2011 cited by 175
