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
Journal of Medicinal Chemistry 59 ( 4) 1556 -1564
111
2016
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
PLoS ONE 9 ( 12) e111840
59
2014
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
Molecular Cancer Therapeutics 13 ( 4) 842 -854
327
2014
Identification of a First-in-Class PRMT5 Inhibitor with Potent in Vitro and in Vivo Activity in Preclinical Models of Mantle Cell Lymphoma
Elayne Penebre , Kristy G Kuplast , Christina R Majer , L. Danielle Johnston
Blood 124 ( 21) 438 -438
3
2014
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.
Lorna H. Mitchell , Allison E. Drew , Scott A. Ribich , Nathalie Rioux
ACS Medicinal Chemistry Letters 6 ( 6) 655 -659
74
2015
EZH2 inhibitor EPZ-6438 (E7438) in non-hodgkin lymphoma: Pre-clinical models and early clinical observations
Robert A Copeland , Heike Keilhack , Antoine Italiano , Sarah K Knutson
annual American Society of Hematology (ASH) meeting 12
6
2014
277 The discovery and pre-clinical development of the first clinical stage EZH2-inhibitor, EPZ-6438 (E7438)
H. Keilhack , R. Pollock , S. Knutson , N. Warholic
European Journal of Cancer 50 92
1
2014
Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor
Scott R. Daigle , Edward J. Olhava , Carly A. Therkelsen , Christina R. Majer
Cancer Cell 20 ( 1) 53 -65
937
2011
Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys27 methylation by human polycomb repressive complex 2 and vSET
Brooke M. Swalm , Kenneth K. Hallenbeck , Christina R. Majer , Lei Jin
Biochemical Journal 453 ( 2) 241 -247
4
2013
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2
S. K. Knutson , N. M. Warholic , T. J. Wigle , C. R. Klaus
Proceedings of the National Academy of Sciences of the United States of America 110 ( 19) 7922 -7927
718
2013
DOT1L inhibitor EPZ-5676 synergizes with cytarabine and azacitidine in preclinical models of MLL-rearranged leukemia
Christine R Klaus , Scott R Daigle , Vivek Chopra , Jeffrey A Keats
Cancer Research 75 ( 15_Supplement) 5383 -5383
2015
Kinetic mechanism of the p38-α MAP kinase: phosphoryl transfer to synthetic peptides
Guanjing Chen , Margaret D Porter , John R Bristol , Matthew J Fitzgibbon
Biochemistry 39 ( 8) 2079 -2087
78
2000
Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis.
Robert A. Copeland , Aravind Basavapathruni , Mikel Moyer , Margaret Porter Scott
Analytical Biochemistry 416 ( 2) 206 -210
49
2011
Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.
Scott R. Daigle , Edward J. Olhava , Carly A. Therkelsen , Aravind Basavapathruni
Blood 122 ( 6) 1017 -1025
475
2013
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Matthew O. Duffey , Tricia J. Vos , Ruth Adams , Jennifer Alley
Journal of Medicinal Chemistry 55 ( 1) 197 -208
29
2012
A peptide model system for processive phosphorylation by Src family kinases.
Margaret Porter Scott , W. Todd Miller
Biochemistry 39 ( 47) 14531 -14537
45
2000
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
Journal of Pharmacology and Experimental Therapeutics 350 ( 3) 646 -656
84
2014
Chemogenetic analysis of human protein methyltransferases.
Victoria M. Richon , Danielle Johnston , Christopher J. Sneeringer , Lei Jin
Chemical Biology & Drug Design 78 ( 2) 199 -210
140
2011
The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states
Tim J. Wigle , Sarah K. Knutson , Lei Jin , Kevin W. Kuntz
FEBS Letters 585 ( 19) 3011 -3014
83
2011
Characterization of the Enzymatic Activity of SETDB1 and Its 1:1 Complex with ATF7IP
Aravind Basavapathruni , Jodi Gureasko , Margaret Porter Scott , William Hermans
Biochemistry 55 ( 11) 1645 -1651
12
2016