Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED

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

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

Towards understanding methyllysine readout

(2014) Catherine A. Musselman et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

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

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

(2014) H. M. Ott et al.   MOLECULAR CANCER THERAPEUTICS

Polycomb Protein EED is Required for Silencing of Pluripotency Genes upon ESC Differentiation

(2014) Nadine Obier et al.   Stem Cell Reviews and Reports

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

Targeted disruption of the EZH2–EED complex inhibits EZH2-dependent cancer

(2013) Woojin Kim et al.   Nature Chemical Biology

Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations

(2013) Hong Wu et al.   PLoS One

Genetic defects in PRC2 components other than EZH2 are not common in myeloid malignancies

(2012) L. I. Kroeze et al.   BLOOD

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

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

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

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

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

(2012) Sharad K. Verma et al.   ACS Medicinal Chemistry Letters

Molecular architecture of human polycomb repressive complex 2

(2012) Claudio Ciferri et al.   eLife

REFMAC5 for the refinement of macromolecular crystal structures

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

The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states

(2011) Tim J. Wigle et al.   FEBS LETTERS

Druggability of methyl-lysine binding sites

(2011) C. Santiago et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Structure and function of WD40 domain proteins

(2011) Chao Xu et al.   Protein & Cell

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

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

Molecular replacement withMOLREP

(2009) Alexei Vagin et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

(2009) Raphael Margueron et al.   NATURE

A homogeneous method for investigation of methylation-dependent protein-protein interactions in epigenetics

(2009) A. M. Quinn et al.   NUCLEIC ACIDS RESEARCH