| 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 | 881 | 2012 |
| Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 SK Knutson, NM Warholic, TJ Wigle, CR Klaus, CJ Allain, A Raimondi, ... Proceedings of the National Academy of Sciences 110 (19), 7922-7927, 2013 | 806 | 2013 |
| Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma SK Knutson, S Kawano, Y Minoshima, NM Warholic, KC Huang, Y Xiao, ... Molecular cancer therapeutics 13 (4), 842-854, 2014 | 609 | 2014 |
| A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells M Vedadi, D Barsyte-Lovejoy, F Liu, S Rival-Gervier, A Allali-Hassani, ... Nature chemical biology 7 (8), 566-574, 2011 | 547 | 2011 |
| A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models E Chan-Penebre, KG Kuplast, CR Majer, PA Boriack-Sjodin, TJ Wigle, ... Nature chemical biology 11 (6), 432-437, 2015 | 536 | 2015 |
| Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2, 4-diamino-7-aminoalkoxy-quinazolines. F Liu, X Chen, A Allali-Hassani, AM Quinn, TJ Wigle, GA Wasney, A Dong, ... Journal of medicinal chemistry 53 (15), 5844-5857, 2010 | 218 | 2010 |
| A687V EZH2 is a gain-of-function mutation found in lymphoma patients CR Majer, L Jin, MP Scott, SK Knutson, KW Kuntz, H Keilhack, JJ Smith, ... FEBS letters 586 (19), 3448-3451, 2012 | 180 | 2012 |
| Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L A Basavapathruni, L Jin, SR Daigle, CRA Majer, CA Therkelsen, TJ Wigle, ... Chemical biology & drug design 80 (6), 971-980, 2012 | 157 | 2012 |
| 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 | 155 | 2016 |
| Small-molecule ligands of methyl-lysine binding proteins JM Herold, TJ Wigle, JL Norris, R Lam, VK Korboukh, C Gao, ... Journal of medicinal chemistry 54 (7), 2504-2511, 2011 | 136 | 2011 |
| EPZ011989, a potent, orally-available EZH2 inhibitor with robust in vivo activity JE Campbell, KW Kuntz, SK Knutson, NM Warholic, H Keilhack, TJ Wigle, ... ACS medicinal chemistry letters 6 (5), 491-495, 2015 | 132 | 2015 |
| Aryl pyrazoles as potent inhibitors of arginine methyltransferases: identification of the first PRMT6 tool compound LH Mitchell, AE Drew, SA Ribich, N Rioux, KK Swinger, SL Jacques, ... ACS medicinal chemistry letters 6 (6), 655-659, 2015 | 125 | 2015 |
| The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states TJ Wigle, SK Knutson, L Jin, KW Kuntz, RM Pollock, VM Richon, ... FEBS letters 585 (19), 3011-3014, 2011 | 116 | 2011 |
| Screening for Inhibitors of Low-Affinity Epigenetic Peptide-Protein Interactions: An AlphaScreen™-Based Assay for Antagonists of Methyl-Lysine Binding Proteins TJ Wigle, J Martin Herold, GA Senisterra, M Vedadi, DB Kireev, ... Journal of biomolecular screening 15 (1), 62-71, 2010 | 99 | 2010 |
| Synergistic anti-tumor activity of EZH2 inhibitors and glucocorticoid receptor agonists in models of germinal center non-Hodgkin lymphomas SK Knutson, NM Warholic, LD Johnston, CR Klaus, TJ Wigle, ... PloS one 9 (12), e111840, 2014 | 94 | 2014 |
| PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity JM Gozgit, MM Vasbinder, RP Abo, K Kunii, KG Kuplast-Barr, B Gui, AZ Lu, ... Cancer Cell 39 (9), 1214-1226. e10, 2021 | 79 | 2021 |
| Novel oxindole sulfonamides and sulfamides: EPZ031686, the first orally bioavailable small molecule SMYD3 inhibitor LH Mitchell, PA Boriack-Sjodin, S Smith, M Thomenius, N Rioux, ... ACS medicinal chemistry letters 7 (2), 134-138, 2016 | 79 | 2016 |
| Directed molecular screening for RecA ATPase inhibitors TJ Wigle, SF Singleton Bioorganic & medicinal chemistry letters 17 (12), 3249-3253, 2007 | 74 | 2007 |
| Inhibitors of RecA activity discovered by high-throughput screening: cell-permeable small molecules attenuate the SOS response in Escherichia coli TJ Wigle, JZ Sexton, AV Gromova, MB Hadimani, MA Hughes, GR Smith, ... SLAS Discovery 14 (9), 1092-1101, 2009 | 70 | 2009 |
| Novel inhibitors of E. coli RecA ATPase activity JZ Sexton, TJ Wigle, Q He, MA Hughes, GR Smith, SF Singleton, ... Current chemical genomics 4, 34, 2010 | 64 | 2010 |
