The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

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

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

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EZH2 Inhibition Blocks Multiple Myeloma Cell Growth through Upregulation of Epithelial Tumor Suppressor Genes

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

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The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia

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Acquired mutations in BCL2 family proteins conferring resistance to the BH3 mimetic ABT-199 in lymphoma

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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

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

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

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The histone H3.3K27M mutation in pediatric glioma reprograms H3K27 methylation and gene expression

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A new world of Polycombs: unexpected partnerships and emerging functions

(2013) Yuri B. Schwartz et al.   NATURE REVIEWS GENETICS

Transcriptional regulation by Polycomb group proteins

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

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Inhibition of PRC2 Activity by a Gain-of-Function H3 Mutation Found in Pediatric Glioblastoma

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The structure–activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface

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EED mutants impair polycomb repressive complex 2 in myelodysplastic syndrome and related neoplasms

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

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Epigenetic protein families: a new frontier for drug discovery

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

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Data processing and analysis with theautoPROCtoolbox

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Thermal Denaturation Assays in Chemical Biology

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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

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Analysis of the coding genome of diffuse large B-cell lymphoma

(2011) Laura Pasqualucci et al.   NATURE GENETICS

EZH2 Codon 641 Mutations are Common in BCL2-Rearranged Germinal Center B Cell Lymphomas

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Recognition and Specificity Determinants of the Human Cbx Chromodomains

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Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

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

In Brief

(2009)   NATURE REVIEWS NEUROSCIENCE

Cause and Consequences of Genetic and Epigenetic Alterations in Human Cancer

(2008) B. Sadikovic et al.   CURRENT GENOMICS

Ezh1 and Ezh2 Maintain Repressive Chromatin through Different Mechanisms

(2008) Raphael Margueron et al.   MOLECULAR CELL

EZH1 Mediates Methylation on Histone H3 Lysine 27 and Complements EZH2 in Maintaining Stem Cell Identity and Executing Pluripotency

(2008) Xiaohua Shen et al.   MOLECULAR CELL

A model for transmission of the H3K27me3 epigenetic mark

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