An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

Relationship between Tumor Biomarkers and Efficacy in EMILIA, a Phase III Study of Trastuzumab Emtansine in HER2-Positive Metastatic Breast Cancer

(2016) J. Baselga et al.   CLINICAL CANCER RESEARCH

Quantitative Profiling of Combinational K27/K36 Modifications on Histone H3 Variants in Mouse Organs

(2016) Yanyan Yu et al.   JOURNAL OF PROTEOME RESEARCH

Structural basis for activity regulation of MLL family methyltransferases

(2016) Yanjing Li et al.   NATURE

Structural basis of oncogenic histone H3K27M inhibition of human polycomb repressive complex 2

(2016) Neil Justin et al.   Nature Communications

Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance

(2016) Alexei Brooun et al.   Nature Communications

Ezh2 loss in hematopoietic stem cells predisposes mice to develop heterogeneous malignancies in an Ezh1-dependent manner

(2015) M. Mochizuki-Kashio et al.   BLOOD

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

(2015) V Gibaja et al.   ONCOGENE

Structural basis of histone H3K27 trimethylation by an active polycomb repressive complex 2

(2015) L. Jiao et al.   SCIENCE

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

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

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

Targeting MLL1 H3K4 Methyltransferase Activity in Mixed-Lineage Leukemia

(2014) Fang Cao et al.   MOLECULAR CELL

Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C

(2014) Katharine L. Sackton et al.   NATURE

Recurrent point mutations in the kinetochore gene KNSTRN in cutaneous squamous cell carcinoma

(2014) Carolyn S Lee et al.   NATURE GENETICS

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

(2014) Christopher G. Nasveschuk et al.   ACS Medicinal Chemistry Letters

An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1

(2013) Kyle D. Konze et al.   ACS Chemical Biology

A liquid chromatography/mass spectrometry-based generic detection method for biochemical assay and hit discovery of histone methyltransferases

(2013) Shu Li et al.   ANALYTICAL BIOCHEMISTRY

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

Structure of the Arginine Methyltransferase PRMT5-MEP50 Reveals a Mechanism for Substrate Specificity

(2013) Meng-Chiao Ho et al.   PLoS One

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

(2012) Guillermo Senisterra et al.   BIOCHEMICAL JOURNAL

On WD40 proteins: Propelling our knowledge of transcriptional control?

(2012) Valentina Migliori et al.   Epigenetics

A687V EZH2 is a gain-of-function mutation found in lymphoma patients

(2012) Christina R. Majer et al.   FEBS LETTERS

Lapatinib with trastuzumab for HER2-positive early breast cancer (NeoALTTO): a randomised, open-label, multicentre, phase 3 trial

(2012) José Baselga et al.   LANCET

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

(2012) Michael T. McCabe et al.   NATURE

Genetic inactivation of the polycomb repressive complex 2 in T cell acute lymphoblastic leukemia

(2012) Panagiotis Ntziachristos et al.   NATURE MEDICINE

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

(2012) M. T. McCabe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Crystal structure of the human PRMT5:MEP50 complex

(2012) S. Antonysamy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

EZH2 Mediates Epigenetic Silencing of Neuroblastoma Suppressor Genes CASZ1, CLU, RUNX3, and NGFR

(2011) C. Wang et al.   CANCER RESEARCH

H3K36 Methylation Antagonizes PRC2-mediated H3K27 Methylation

(2011) Wen Yuan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure and function of WD40 domain proteins

(2011) Chao Xu et al.   Protein & Cell

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

Analysis of the Binding of Mixed Lineage Leukemia 1 (MLL1) and Histone 3 Peptides to WD Repeat Domain 5 (WDR5) for the Design of Inhibitors of the MLL1−WDR5 Interaction

(2010) Hacer Karatas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Somatic mutations of the histone methyltransferase gene EZH2 in myelodysplastic syndromes

(2010) Gorica Nikoloski et al.   NATURE GENETICS

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

Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

(2010) Thomas Ernst et al.   NATURE GENETICS

Binding of different histone marks differentially regulates the activity and specificity of polycomb repressive complex 2 (PRC2)

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

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

WD40 proteins propel cellular networks

(2010) Christian U. Stirnimann et al.   TRENDS IN BIOCHEMICAL SCIENCES

Role of the polycomb protein EED in the propagation of repressive histone marks

(2009) Raphael Margueron et al.   NATURE