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
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
Drugging the human methylome: an emerging modality for reversible control of aberrant gene transcription
Tim J Wigle , Robert A Copeland
Current Opinion in Chemical Biology 17 ( 3) 369 -378
19
2013
Novel Inhibitors of E. coli RecA ATPase Activity
Jonathan Z Sexton , Tim J Wigle , Qingping He , Mark A Hughes
Current Chemical Genomics 4 ( 1) 34 -42
44
2010
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
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
Elayne Chan-Penebre , Kristy G Kuplast , Christina R Majer , P Ann Boriack-Sjodin
Nature Chemical Biology 11 ( 6) 432 -437
457
2015
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
Sarah K Knutson , Tim J Wigle , Natalie M Warholic , Christopher J Sneeringer
Nature Chemical Biology 8 ( 11) 890 -896
587
2012
Directed molecular screening for RecA ATPase inhibitors pp 3249--3253
Tim J Wigle , Scott F Singleton , Gang Zhao , Rajesh R Iyengar
Bioorganic \& Medicinal Chemistry Letters 17 ( 12)
2007
PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity
Joseph M Gozgit , Melissa M Vasbinder , Ryan P Abo , Kaiko Kunii
Cancer Cell 39 ( 9) 1214 -1226
41
2021
Chemical biology of chromatin regulation: The first small molecule antagonists of MBT domains
J Martin Herold , Tim J Wigle , Cen Gao , Dmitri B Kireev
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY 240
2010
Development of small molecule protein lysine methyltransferase G9a inhibitors
Julianne M Yost , Feng Liu , Xin Chen , Abdellah Allali-Hassani
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY 240
2010
Potent, Selective, and Cell-active Chemical Probe of Protein Lysine Methyltransferases G9a and GLP: Cell-Based Assays
Dalia Baryste-Lovejoy , Sylvie Rival-Gervier , Feng Liu , Abdellah Allali-Hassani
2010
RBN-2397: a potent and selective small molecule inhibitor of PARP7 that induces tumor-derived antitumor immunity dependent on CD8 T cells
Joseph M Gozgit , Melissa M Vasbinder , Ryan P Abo , Kaiko Kunii
Cancer Res 81 48 -48
2
2021
Small molecule inhibitor of CD38 modulates its intra-and extracellular functions leading to antitumor activity
Prashant Shambharkar , Danielle J Blackwell , Melissa M Vasbinder , Laurie B Schenkel
Cancer Research 81 ( 13_Supplement) 1344 -1344
2
2021
PARP7 inhibitor RBN-2397 increases tumoral IFN signaling leading to various tumor cell intrinsic effects and tumor regressions in mouse models
Jennifer R Molina , Joseph M Gozgit , Melissa M Vasbinder , Ryan P Abo
Cancer Research 82 ( 12_Supplement) 2154 -2154
1
2022
A bespoke screening platform to study mono (ADP-ribosylation)
Tim J Wigle , Danielle J Blackwell , Laurie B Schenkel , Yue Ren
Cancer Research 80 ( 16_Supplement) 506 -506
2020
PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition leads to tumor regression
Joe Gozgit , Melissa M Vasbinder , Ryan P Abo , Kaiko Kunii
Cancer Research 80 ( 16)
2020
Screening for inhibitors of low-affinity epigenetic peptide-protein interactions: an AlphaScreen™-based assay for antagonists of methyl-lysine binding proteins
Tim J Wigle , J Martin Herold , Guillermo A Senisterra , Masoud Vedadi
SLAS Discovery 15 ( 1) 62 -71
101
2010
Histone methyltransferases: opportunities in cancer drug discovery
Richard Chesworth , Tim J Wigle , Kevin W Kuntz , Jesse J Smith
Springer Berlin Heidelberg 189 -226
3
2013