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

Hydrogen deuterium mass spectrometry in drug discovery

(2015) Nino Campobasso et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting EZH2 and PRC2 dependence as novel anticancer therapy

(2015) Bowen Xu et al.   EXPERIMENTAL HEMATOLOGY

Targeting Polycomb systems to regulate gene expression: modifications to a complex story

(2015) Neil P. Blackledge et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

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

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

(2014) Glenn S. Van Aller et al.   ACS Chemical Biology

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

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

Elements of the Polycomb Repressor SU(Z)12 Needed for Histone H3-K27 Methylation, the Interface with E(Z), and In Vivo Function

(2013) A. N. Rai et al.   MOLECULAR AND CELLULAR BIOLOGY

Accurate assessment of mass, models and resolution by small-angle scattering

(2013) Robert P. Rambo et al.   NATURE

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

Structural Context of Disease-Associated Mutations and Putative Mechanism of Autoinhibition Revealed by X-Ray Crystallographic Analysis of the EZH2-SET Domain

(2013) Stephen Antonysamy et al.   PLoS One

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

Oncogenic mutations mimic and enhance dynamic events in the natural activation of phosphoinositide 3-kinase p110  (PIK3CA)

(2012) J. E. Burke 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

Data processing and analysis with theautoPROCtoolbox

(2011) Clemens Vonrhein et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Characterizing flexible and intrinsically unstructured biological macromolecules by SAS using the Porod-Debye law

(2011) Robert P. Rambo et al.   BIOPOLYMERS

Inactivation of polycomb repressive complex 2 components in myeloproliferative and myelodysplastic/myeloproliferative neoplasms

(2011) J. Score et al.   BLOOD

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

Composition, recruitment and regulation of the PRC2 complex

(2011) Vinod Nayak et al.   Nucleus

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

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

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

(2009) Raphael Margueron et al.   NATURE

Robust, high-throughput solution structural analyses by small angle X-ray scattering (SAXS)

(2009) Greg L Hura et al.   NATURE METHODS

A model for transmission of the H3K27me3 epigenetic mark

(2008) Klaus H. Hansen et al.   NATURE CELL BIOLOGY