| Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor SR Daigle, EJ Olhava, CA Therkelsen, CR Majer, CJ Sneeringer, J Song, ... Cancer cell 20 (1), 53-65, 2011 | 1038 | 2011 |
| A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells SK Knutson, TJ Wigle, NM Warholic, CJ Sneeringer, CJ Allain, CR Klaus, ... Nature chemical biology 8 (11), 890-896, 2012 | 908 | 2012 |
| Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas CJ Sneeringer, MP Scott, KW Kuntz, SK Knutson, RM Pollock, VM Richon, ... Proceedings of the National Academy of Sciences 107 (49), 20980-20985, 2010 | 810 | 2010 |
| Chemogenetic analysis of human protein methyltransferases VM Richon, D Johnston, CJ Sneeringer, L Jin, CR Majer, K Elliston, ... Chemical biology & drug design 78 (2), 199-210, 2011 | 225 | 2011 |
| The importance of being me: magic methyls, methyltransferase inhibitors, and the discovery of tazemetostat KW Kuntz, JE Campbell, H Keilhack, RM Pollock, SK Knutson, ... Journal of medicinal chemistry 59 (4), 1556-1564, 2016 | 170 | 2016 |
| Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma AE Drew, O Moradei, SL Jacques, N Rioux, AP Boriack-Sjodin, C Allain, ... Scientific reports 7 (1), 17993, 2017 | 117 | 2017 |
| Inhibitors of human EZH2 and methods of use thereof RA Copeland, VM Richon, MD Scott, CJ Sneeringer, KW Kuntz, ... US Patent 8,895,245, 2014 | 102 | 2014 |
| Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma SM Bronner, KA Merrick, J Murray, L Salphati, JG Moffat, J Pang, ... Bioorganic & Medicinal Chemistry Letters 29 (16), 2294-2301, 2019 | 57 | 2019 |
| Inhibitors of human Ezh2 and methods of use thereof RA Copeland, VM Richon, MD Scott, CJ Sneeringer, KW Kuntz, ... US Patent 8,691,507, 2014 | 48 | 2014 |
| Structural insights into ternary complex formation of human CARM1 with various substrates PA Boriack-Sjodin, L Jin, SL Jacques, A Drew, C Sneeringer, MP Scott, ... ACS chemical biology 11 (3), 763-771, 2016 | 46 | 2016 |
| Hematopoietic progenitor kinase-1 structure in a domain-swapped dimer P Wu, CJ Sneeringer, KE Pitts, ES Day, BK Chan, B Wei, I Lehoux, ... Structure 27 (1), 125-133. e4, 2019 | 39 | 2019 |
| Discovery of spiro-azaindoline inhibitors of hematopoietic progenitor kinase 1 (HPK1) BK Chan, E Seward, M Lainchbury, TF Brewer, L An, T Blench, ... ACS Medicinal Chemistry Letters 13 (1), 84-91, 2021 | 34 | 2021 |
| Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor MP Huestis, D Dela Cruz, AG DiPasquale, MR Durk, C Eigenbrot, ... Journal of Medicinal Chemistry 64 (7), 3940-3955, 2021 | 21 | 2021 |
| Structure-based design of potent, selective, and orally bioavailable VPS34 kinase inhibitors DX Hu, S Patel, H Chen, S Wang, ST Staben, YN Dimitrova, ... Journal of Medicinal Chemistry 65 (17), 11500-11512, 2021 | 17 | 2021 |
| Inhibitors of human EZH2, and methods of use thereof RA Copeland, VM Richon, MD Scott, CJ Sneeringer, KW Kuntz, ... US Patent 9,949,999, 2018 | 16 | 2018 |
| Inhibitors of human ezh2, and methods of use thereof KW Kuntz, SK Knutson, TJN Wigle, RA Copeland, VM Richon, MD Scott, ... US Patent App. 15/132,610, 2017 | 14 | 2017 |
| Lymphoma-Associated Mutations of EZH2 Result in a Change-of-function VM Richon, CJ Sneeringer, MP Scott, KW Kuntz, SK Knutson, RM Pollock, ... Blood 116 (21), 707, 2010 | 9 | 2010 |
| Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor RM Pollock, SR Daigle, EJ Olhava, CA Therkelsen, CR Majer, J Song, ... Blood 116 (21), 780, 2010 | 8 | 2010 |
| From protein to candidate: discovery of EPZ-5676, a potent and selective inhibitor of the histone methyltransferase DOT1L R Chesworth, EJ Olhava, KW Kuntz, A Basavapathruni, CRA Majer, ... ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY 246, 2013 | 4 | 2013 |
| Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor MP Huestis, MR Durk, C Eigenbrot, P Gibbons, TL Hunsaker, H La, ... ACS Medicinal Chemistry Letters 12 (5), 791-797, 2021 | 3 | 2021 |