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

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

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity

John E. Campbell, Kevin W. Kuntz, Sarah K. Knutson, +16

ACS Medicinal Chemistry Letters

PharmacotherapyA PotentEzh2 ActivityTumor BiologyMedicinal Chemistry +15

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, +9

Journal of Pharmacology and Experimental Therapeutics

Initial testing (stage 1) of tazemetostat (EPZ‐6438), a novel EZH2 inhibitor, by the Pediatric Preclinical Testing Program

Raushan T. Kurmasheva, Melissa Sammons, Edward Favours, +7

Pediatric Blood & Cancer

IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial

Lindsay Ackerman, Gerard Acloque, Sandro Bacchelli, +28

Nature Medicine

TREM2 triggers microglial density and age‐related neuronal loss

Bettina Linnartz‐Gerlach, Liviu‐Gabriel Bodea, Christine R. Klaus, +6

Glia

ImmunologySocial SciencesNeuroinflammationInflammationDegenerative Pathology +16

Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor

Lorna H. Mitchell, P. Ann Boriack‐Sjodin, Sherri Smith, +18

ACS Medicinal Chemistry Letters

Pharmaceutical ScienceChemoprevention StrategyCancer BiologySmyd3 InhibitorsPharmaceutical Chemistry +16