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

Mutation spectra of histone methyltransferases with canonical SET domains and EZH2-targeted therapy

(2016) Masaru Katoh   Epigenomics

Gain-of-function mutation of chromatin regulators as a tumorigenic mechanism and an opportunity for therapeutic intervention

(2015) Chen Shen et al.   CURRENT OPINION IN ONCOLOGY

302 A phase 1 study of EPZ-6438 (E7438), an Enhancer of Zeste-Homolog 2 (EZH2) inhibitor: Preliminary activity in INI1-negative tumors

(2015) A. Italiano et al.   EUROPEAN JOURNAL OF CANCER

Targeting of cancer stem cells by inhibitors of DNA and histone methylation

(2015) Richard L Momparler et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors

(2015) Ping Zhang et al.   INTERNATIONAL JOURNAL OF CANCER

EZH2 inhibition sensitizes BRG1 and EGFR mutant lung tumours to TopoII inhibitors

(2015) Christine M. Fillmore et al.   NATURE

Loss of BAP1 function leads to EZH2-dependent transformation

(2015) Lindsay M LaFave et al.   NATURE MEDICINE

Development of secondary mutations in wild-type and mutant EZH2 alleles cooperates to confer resistance to EZH2 inhibitors

(2015) V Gibaja et al.   ONCOGENE

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

(2015) John E. Campbell et al.   ACS Medicinal Chemistry Letters

Small molecule inhibitors of EZH2: the emerging translational landscape

(2015) Heike Keilhack et al.   Epigenomics

Mutation of chromatin modifiers; an emerging hallmark of germinal center B-cell lymphomas

(2015) M A Lunning et al.   Blood Cancer Journal

EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells

(2014) Bryson W Katona et al.   CANCER BIOLOGY & THERAPY

Inhibition enhancer of zeste homologue 2 promotes senescence and apoptosis induced by doxorubicin inp53mutant gastric cancer cells

(2014) J. Bai et al.   CELL PROLIFERATION

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

(2014) S. K. Knutson et al.   MOLECULAR CANCER THERAPEUTICS

Metronomic Docetaxel in PRINT Nanoparticles and EZH2 Silencing Have Synergistic Antitumor Effect in Ovarian Cancer

(2014) K. M. Gharpure et al.   MOLECULAR CANCER THERAPEUTICS

Epigenomic alterations define lethal CIMP-positive ependymomas of infancy

(2014) S. C. Mack et al.   NATURE

Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas

(2014) Sarah K. Knutson et al.   PLoS One

Histone H3.3 Mutations: A Variant Path to Cancer

(2013) Benjamin T.K. Yuen et al.   CANCER CELL

Identification of EZH2 and EZH1 Small Molecule Inhibitors with Selective Impact on Diffuse Large B Cell Lymphoma Cell Growth

(2013) Shivani Garapaty-Rao et al.   CHEMISTRY & BIOLOGY

The Polycomb group (PcG) protein EZH2 supports the survival of PAX3-FOXO1 alveolar rhabdomyosarcoma by repressing FBXO32 (Atrogin1/MAFbx)

(2013) R Ciarapica et al.   ONCOGENE

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

(2013) S. K. Knutson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

K27M mutation in histone H3.3 defines clinically and biologically distinct subgroups of pediatric diffuse intrinsic pontine gliomas

(2012) Dong-Anh Khuong-Quang et al.   ACTA NEUROPATHOLOGICA

The ablation of EZH2 uncovers its crucial role in rhabdomyosarcoma formation

(2012) Irene Marchesi et al.   CELL CYCLE

Driver mutations in histone H3.3 and chromatin remodelling genes in paediatric glioblastoma

(2012) Jeremy Schwartzentruber et al.   NATURE

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

(2012) Michael T. McCabe et al.   NATURE

Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

(2012) W. Qi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery and prioritization of somatic mutations in diffuse large B-cell lymphoma (DLBCL) by whole-exome sequencing

(2012) J. G. Lohr et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2011) Scott R. Daigle et al.   CANCER CELL

Aberrations of EZH2 in Cancer

(2011) A. Chase et al.   CLINICAL CANCER RESEARCH

EZH2 Y641 mutations in follicular lymphoma

(2011) C Bödör et al.   LEUKEMIA

Frequent mutation of histone-modifying genes in non-Hodgkin lymphoma

(2011) Ryan D. Morin et al.   NATURE

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation

(2010) D. B. Yap et al.   BLOOD

Epigenetic Antagonism between Polycomb and SWI/SNF Complexes during Oncogenic Transformation

(2010) Boris G. Wilson et al.   CANCER CELL

Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin

(2010) Ryan D Morin et al.   NATURE GENETICS

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

(2010) C. J. Sneeringer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA