EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

Michael T. McCabe, Heidi M. Ott, Gopinath Ganji, +19

Nature

Ezh2 InhibitionLymphoid NeoplasiaHematological MalignancyMedicinePathology +8

EZH2 Is Required for Germinal Center Formation and Somatic EZH2 Mutations Promote Lymphoid Transformation

Wendy Béguelin, Relja Popovic, Matt Teater, +30

Cancer Cell

ChromatinDevelopmental BiologyGerm CellSomatic VariantGerminal Center Formation +7

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

Michael T. McCabe, Alan P. Graves, Gopinath Ganji, +18

Proceedings of the National Academy of Sciences

Histone ModificationsEpigenetic ChangePathologyMolecular BiologyEpigenetics +18

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

Sharad K. Verma, Xinrong Tian, Louis V. LaFrance, +24

ACS Medicinal Chemistry Letters

Histone ModificationsDrug Discovery ProgramEngineeringEpigenetic ChangeCell-active Inhibitors +16

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma

Allison E. Drew, Oscar Moradei, Suzanne L. Jacques, +21

Scientific Reports

JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia

Carl L. Manthey, Dana L. Johnson, Carl R. Illig, +21

Molecular Cancer Therapeutics

Solid TumorsImmunologyCancer BiologyTumor BiologyMyeloid Neoplasia +15

Long Residence Time Inhibition of EZH2 in Activated Polycomb Repressive Complex 2

Glenn S. Van Aller, Melissa B. Pappalardi, Heidi M. Ott, +10

ACS Chemical Biology

Histone ModificationsChromatinTranscriptional RegulationSignal TransductionEpigenetic Change +13

2-Hydroxy-4,6-diamino-[1,3,5]triazines: A Novel Class of VEGF-R2 (KDR) Tyrosine Kinase Inhibitors

Nand Baindur, Naresh K. Chadha, Benjamin Brandt, +10

Journal of Medicinal Chemistry

A687V EZH2 Is a Driver of Histone H3 Lysine 27 (H3K27) Hypertrimethylation

Heidi M. Ott, Alan P. Graves, Melissa B. Pappalardi, +16

Molecular Cancer Therapeutics

Histone ModificationsA687v Ezh2Epigenetic ChangeMolecular BiologyEzh2 Activity +19

Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3

Raymond J. Patch, Christian A. Baumann, Jian Liu, +4

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicinePharmacological AgentPharmacotherapyPotent Inhibitors +4