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

Synthetic Lethal Vulnerabilities of Cancer

(2015) Ferran Fece de la Cruz et al.   Annual Review of Pharmacology and Toxicology

Gene mutations in primary tumors and corresponding patient-derived xenografts derived from non-small cell lung cancer

(2015) Chuncheng Hao et al.   CANCER LETTERS

Snail2/Slug cooperates with Polycomb repressive complex 2 (PRC2) to regulate neural crest development

(2015) C.-L. Tien et al.   DEVELOPMENT

Functional proteomics of the epigenetic regulators ASXL1, ASXL2 and ASXL3: a convergence of proteomics and epigenetics for translational medicine

(2015) Masaru Katoh   Expert Review of Proteomics

The Chromatin-Modifying Enzyme Ezh2 Is Critical for the Maintenance of Regulatory T Cell Identity after Activation

(2015) Michel DuPage et al.   IMMUNITY

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

(2015) Christine M. Fillmore et al.   NATURE

Targeting histone lysine methylation in cancer

(2015) John McGrath et al.   PHARMACOLOGY & THERAPEUTICS

Functional Characterization of D9, a Novel Deazaneplanocin A (DZNep) Analog, in Targeting Acute Myeloid Leukemia (AML)

(2015) Xia Jiang et al.   PLoS One

STAT3-driven transcription depends upon the dimethylation of K49 by EZH2

(2015) Maupali Dasgupta et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

To be or not to be: The host genetic factor and beyond inHelicobacter pylorimediated gastro-duodenal diseases

(2015) Dipanjana Datta De   WORLD JOURNAL OF GASTROENTEROLOGY

The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors

(2015) Daniel Zingg et al.   Nature Communications

Wedelolactone disrupts the interaction of EZH2-EED complex and inhibits PRC2-dependent cancer

(2015) Huiming Chen et al.   Oncotarget

Somatic cancer mutations in the MLL3-SET domain alter the catalytic properties of the enzyme

(2015) Sara Weirich et al.   Clinical Epigenetics

EZH2 Protects Glioma Stem Cells from Radiation-Induced Cell Death in a MELK/FOXM1-Dependent Manner

(2015) Sung-Hak Kim et al.   Stem Cell Reports

Germline mutations in the oncogene EZH2 cause Weaver syndrome and increased human height

(2015) Katrina Tatton-Brown et al.   Oncotarget

Genetic alterations of histone lysine methyltransferases and their significance in breast cancer

(2015) Lanxin Liu et al.   Oncotarget

Reaction Coupling between Wild-Type and Disease-Associated Mutant EZH2

(2014) Brooke M. Swalm et al.   ACS Chemical Biology

Complex karyotype in a polycythemia vera patient with a novel SETD1B/GTF2H3 fusion gene

(2014) Clelia Tiziana Storlazzi et al.   AMERICAN JOURNAL OF HEMATOLOGY

Microdeletion of 12q24.31: Report of a girl with intellectual disability, stereotypies, seizures and facial dysmorphisms

(2014) Orazio Palumbo et al.   AMERICAN JOURNAL OF MEDICAL GENETICS PART A

Examining the impact of gene variants on histone lysine methylation

(2014) Capucine Van Rechem et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia

(2014) B. Xu et al.   BLOOD

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

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

VEGF/VEGFR-2 Upregulates EZH2 Expression in Lung Adenocarcinoma Cells and EZH2 Depletion Enhances the Response to Platinum-Based and VEGFR-2-Targeted Therapy

(2014) E. Riquelme et al.   CLINICAL CANCER RESEARCH

6LBA Phase 1 first-in-human study of the enhancer of zeste-homolog 2 (EZH2) histone methyl transferase inhibitor E7438 as a single agent in patients with advanced solid tumors or B cell lymphoma

(2014) V. Ribrag et al.   EUROPEAN JOURNAL OF CANCER

Identification of anMLL4-GPS2fusion as an oncogenic driver of undifferentiated spindle cell sarcoma in a child

(2014) Elaine O'Meara et al.   GENES CHROMOSOMES & CANCER

Frameshift mutation of a histone methylation-related gene SETD1B and its regional heterogeneity in gastric and colorectal cancers with high microsatellite instability

(2014) Youn Jin Choi et al.   HUMAN PATHOLOGY

Role of EZH2 Polymorphisms in Esophageal Squamous Cell Carcinoma Risk in Han Chinese Population

(2014) Zhen-Bin Ma et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Mutations inSETD2cause a novel overgrowth condition

(2014) Armelle Luscan et al.   JOURNAL OF MEDICAL GENETICS

Histone Methyltransferase EZH2 Is Transcriptionally Induced by Estradiol as Well as Estrogenic Endocrine Disruptors Bisphenol-A and Diethylstilbestrol

(2014) Arunoday Bhan et al.   JOURNAL OF MOLECULAR BIOLOGY

NFIB-Mediated Repression of the Epigenetic Factor Ezh2 Regulates Cortical Development

(2014) M. Piper et al.   JOURNAL OF NEUROSCIENCE

Ezh2 Regulates Adult Hippocampal Neurogenesis and Memory

(2014) J. Zhang et al.   JOURNAL OF NEUROSCIENCE

EZH2: Not EZHY (Easy) to Deal

(2014) Gauri Deb et al.   MOLECULAR CANCER RESEARCH

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 BRG1 Chromatin Remodeler via Its Bromodomain for Enhanced Tumor Cell Radiosensitivity In Vitro and In Vivo

(2014) S.-J. Kwon et al.   MOLECULAR CANCER THERAPEUTICS

Synaptic, transcriptional and chromatin genes disrupted in autism

(2014) Silvia De Rubeis et al.   NATURE

Identification of genomic alterations in oesophageal squamous cell cancer

(2014) Yongmei Song et al.   NATURE

Exome sequencing identifies rare LDLR and APOA5 alleles conferring risk for myocardial infarction

(2014) Ron Do et al.   NATURE

Most genetic risk for autism resides with common variation

(2014) Trent Gaugler et al.   NATURE GENETICS

Identification of functional cooperative mutations of SETD2 in human acute leukemia

(2014) Xiaofan Zhu et al.   NATURE GENETICS

Inflammation-induced repression of chromatin bound by the transcription factor Foxp3 in regulatory T cells

(2014) Aaron Arvey et al.   NATURE IMMUNOLOGY

Impact of EZH2 Polymorphisms on Urothelial Cell Carcinoma Susceptibility and Clinicopathologic Features

(2014) Yung-Luen Yu et al.   PLoS One

Exome Sequencing Identifies Three Novel Candidate Genes Implicated in Intellectual Disability

(2014) Zehra Agha et al.   PLoS One

O-GlcNAcylation regulates EZH2 protein stability and function

(2014) C.-S. Chu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

EZH2 expands breast stem cells through activation of NOTCH1 signaling

(2014) M. E. Gonzalez et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Integrated analysis of germline and somatic variants in ovarian cancer

(2014) Krishna L. Kanchi et al.   Nature Communications

Ezh2 loss promotes development of myelodysplastic syndrome but attenuates its predisposition to leukaemic transformation

(2014) Goro Sashida et al.   Nature Communications

EZH2-Mediated Inactivation of IFN-γ-JAK-STAT1 Signaling Is an Effective Therapeutic Target in MYC-Driven Prostate Cancer

(2014) Zhen Ning Wee et al.   Cell Reports

De Novo Insertions and Deletions of Predominantly Paternal Origin Are Associated with Autism Spectrum Disorder

(2014) Shan Dong et al.   Cell Reports

Regulation of p53 and Rb Links the Alternative NF-κB Pathway to EZH2 Expression and Cell Senescence

(2014) Alessio Iannetti et al.   PLoS Genetics

Epigenetic therapy of acute myeloid leukemia using 5-aza-2'-deoxycytidine (decitabine) in combination with inhibitors of histone methylation and deacetylation

(2014) Richard L Momparler et al.   Clinical Epigenetics

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

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

Deletion of 3p25.3 in a patient with intellectual disability and dysmorphic features with further definition of a critical region

(2013) Gregory Kellogg et al.   AMERICAN JOURNAL OF MEDICAL GENETICS PART A

PPAPDC1B and WHSC1L1 Are Common Drivers of the 8p11-12 Amplicon, Not Only in Breast Tumors But Also in Pancreatic Adenocarcinomas and Lung Tumors

(2013) Sardar F. Mahmood et al.   AMERICAN JOURNAL OF PATHOLOGY

Phosphorylation of EZH2 Activates STAT3 Signaling via STAT3 Methylation and Promotes Tumorigenicity of Glioblastoma Stem-like Cells

(2013) Eunhee Kim et al.   CANCER CELL

Growth of Triple-Negative Breast Cancer Cells Relies upon Coordinate Autocrine Expression of the Proinflammatory Cytokines IL-6 and IL-8

(2013) Z. C. Hartman et al.   CANCER RESEARCH

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

Smurf2-mediated degradation of EZH2 enhances neuron differentiation and improves functional recovery after ischaemic stroke

(2013) Yung-Luen Yu et al.   EMBO Molecular Medicine

The histone methyltransferase EZH2, an oncogene common to benign and malignant parathyroid tumors

(2013) Jessica Svedlund et al.   ENDOCRINE-RELATED CANCER

A double take on bivalent promoters

(2013) P. Voigt et al.   GENES & DEVELOPMENT

Disruption of the MYC-miRNA-EZH2 loop to suppress aggressive B-cell lymphoma survival and clonogenicity

(2013) X Zhao et al.   LEUKEMIA

FGF Receptors: Cancer Biology and Therapeutics

(2013) Masaru Katoh et al.   MEDICINAL RESEARCH REVIEWS

Quantitative Dissection and Stoichiometry Determination of the Human SET1/MLL Histone Methyltransferase Complexes

(2013) R. van Nuland et al.   MOLECULAR AND CELLULAR BIOLOGY

PAF and EZH2 Induce Wnt/β-Catenin Signaling Hyperactivation

(2013) Hae-Yun Jung et al.   MOLECULAR CELL

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

(2013) Woojin Kim et al.   Nature Chemical Biology

Global chromatin profiling reveals NSD2 mutations in pediatric acute lymphoblastic leukemia

(2013) Jacob D Jaffe et al.   NATURE GENETICS

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

SET for life: biochemical activities and biological functions of SET domain-containing proteins

(2013) Hans-Martin Herz et al.   TRENDS IN BIOCHEMICAL SCIENCES

ASXL1 Mutations Promote Myeloid Transformation through Loss of PRC2-Mediated Gene Repression

(2012) Omar Abdel-Wahab et al.   CANCER CELL

Cancer genetics and genomics of human FOX family genes

(2012) Masuko Katoh et al.   CANCER LETTERS

Cancer Epigenetics: From Mechanism to Therapy

(2012) Mark A. Dawson et al.   CELL

TP53 Genomic Status Regulates Sensitivity of Gastric Cancer Cells to the Histone Methylation Inhibitor 3-Deazaneplanocin A (DZNep)

(2012) L. L. Cheng et al.   CLINICAL CANCER RESEARCH

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

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

PRC2 directly methylates GATA4 and represses its transcriptional activity

(2012) A. He et al.   GENES & DEVELOPMENT

CagA mediates epigenetic regulation to attenuate let-7 expression inHelicobacter pylori-related carcinogenesis

(2012) Yoshito Hayashi et al.   GUT

Human subtelomeric copy number gains suggest a DNA replication mechanism for formation: beyond breakage–fusion–bridge for telomere stabilization

(2012) Svetlana A. Yatsenko et al.   HUMAN GENETICS

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

(2012) Michael T. McCabe et al.   NATURE

The mutational landscape of lethal castration-resistant prostate cancer

(2012) Catherine S. Grasso et al.   NATURE

Epigenetic repression of cardiac progenitor gene expression by Ezh2 is required for postnatal cardiac homeostasis

(2012) Paul Delgado-Olguín et al.   NATURE GENETICS

Exome sequencing of gastric adenocarcinoma identifies recurrent somatic mutations in cell adhesion and chromatin remodeling genes

(2012) Zhi Jiang Zang et al.   NATURE GENETICS

E2F6 Associates with BRG1 in Transcriptional Regulation

(2012) Janet Y. Leung et al.   PLoS One

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

EZH2 Oncogenic Activity in Castration-Resistant Prostate Cancer Cells Is Polycomb-Independent

(2012) K. Xu et al.   SCIENCE

REST–Mediated Recruitment of Polycomb Repressor Complexes in Mammalian Cells

(2012) Nikolaj Dietrich et al.   PLoS Genetics

An EZH2 polymorphism is associated with clinical outcome in metastatic colorectal cancer patients

(2011) F. Crea et al.   ANNALS OF ONCOLOGY

Polycomb Repressor Complex-2 Is a Novel Target for Mesothelioma Therapy

(2011) C. D. Kemp et al.   CLINICAL CANCER RESEARCH

Polycomb genes and cancer: Time for clinical application?

(2011) Francesco Crea et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

H3K36 Methylation Antagonizes PRC2-mediated H3K27 Methylation

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

Pharmacologic disruption of Polycomb Repressive Complex 2 inhibits tumorigenicity and tumor progression in prostate cancer

(2011) Francesco Crea et al.   Molecular Cancer

Context-Specific Regulation of NF-κB Target Gene Expression by EZH2 in Breast Cancers

(2011) Shuet Theng Lee et al.   MOLECULAR CELL

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

Frequent mutations of chromatin remodeling genes in transitional cell carcinoma of the bladder

(2011) Yaoting Gui et al.   NATURE GENETICS

Inflammation meets cancer, with NF-κB as the matchmaker

(2011) Yinon Ben-Neriah et al.   NATURE IMMUNOLOGY

Cancer epigenetics reaches mainstream oncology

(2011) Manuel Rodríguez-Paredes et al.   NATURE MEDICINE

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

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

Transforming Properties of 8p11-12 Amplified Genes in Human Breast Cancer

(2010) Z.-Q. Yang et al.   CANCER RESEARCH

Oral poly(ADP-ribose) polymerase inhibitor olaparib in patients with BRCA1 or BRCA2 mutations and advanced breast cancer: a proof-of-concept trial

(2010) Andrew Tutt et al.   LANCET

Oral poly(ADP-ribose) polymerase inhibitor olaparib in patients with BRCA1 or BRCA2 mutations and recurrent ovarian cancer: a proof-of-concept trial

(2010) M William Audeh et al.   LANCET

MicroRNA-101 negatively regulates Ezh2 and its expression is modulated by androgen receptor and HIF-1α/HIF-1β

(2010) Paul Cao et al.   Molecular Cancer

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

Exome sequencing identifies MLL2 mutations as a cause of Kabuki syndrome

(2010) Sarah B Ng et al.   NATURE GENETICS

ZEB1 represses E-cadherin and induces an EMT by recruiting the SWI/SNF chromatin-remodeling protein BRG1

(2010) E Sánchez-Tilló et al.   ONCOGENE

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

Mutations of polycomb-associated geneASXL1in myelodysplastic syndromes and chronic myelomonocytic leukaemia

(2009) Véronique Gelsi-Boyer et al.   BRITISH JOURNAL OF HAEMATOLOGY

EZH2 Is Essential for Glioblastoma Cancer Stem Cell Maintenance

(2009) M.-L. Suva et al.   CANCER RESEARCH

An operational definition of epigenetics

(2009) S. L. Berger et al.   GENES & DEVELOPMENT

DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation

(2009) T. B. Miranda et al.   MOLECULAR CANCER THERAPEUTICS

Shared Principles in NF-κB Signaling

(2008) Matthew S. Hayden et al.   CELL