Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

Scott R. Daigle, Edward J. Olhava, Carly A. Therkelsen, +18

Cancer Cell

Hematological MalignancyTumor BiologySelective KillingMedicineMixed-phenotype Acute Leukemia +6

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

Sarah K. Knutson, Natalie M. Warholic, Tim J. Wigle, +11

Proceedings of the National Academy of Sciences

EngineeringChemoprevention StrategySmarcb1-deleted Mrt CellsPathologyCancer Biology +22

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

Sarah K. Knutson, Tim J. Wigle, Natalie M. Warholic, +18

Nature Chemical Biology

Lymphoid NeoplasiaMedicineSelective InhibitorAnti-cancer AgentTumor Suppressor +6

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

Scott R. Daigle, Edward J. Olhava, Carly A. Therkelsen, +13

Blood

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

Elayne Chan-Penebre, Kristy G. Kuplast, Christina R. Majer, +27

Nature Chemical Biology

Vitro PotencySignal TransductionMedicineMcl ModelsSelective Inhibitor +8

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in <i>EZH2</i> -Mutant Non-Hodgkin Lymphoma

Sarah K. Knutson, Satoshi Kawano, Yukinori Minoshima, +23

Molecular Cancer Therapeutics

Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss

Andrew Fedoriw, Satyajit Rajapurkar, Shane W. O’Brien, +43

Cancer Cell

Cancer ResearchMtap LossMedicinePharmacologyCell Death +8

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

Kevin W. Kuntz, John E. Campbell, Heike Keilhack, +11

Journal of Medicinal Chemistry

Histone ModificationsEpigenetic ChangePharmacotherapyEpigeneticsTumor Biology +20

Intramolecular nitrogen-hydrogen, oxygen-hydrogen and sulfur-hydrogen insertion reactions. Synthesis of heterocycles from .alpha.-diazo .beta.-keto esters

Mikel P. Moyer, Paul L. Feldman, Henry Rapoport

The Journal of Organic Chemistry

Intramolecular Nitrogen-hydrogenEngineeringHeterocyclicBiochemistrySulfur-hydrogen Insertion Reactions +11

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666

Kenneth W. Duncan, Nathalie Rioux, P. Ann Boriack‐Sjodin, +14

ACS Medicinal Chemistry Letters

Materials ScienceMedicinal ChemistryDrug TargetEngineeringBiochemistry +12