EZH2 in Cancer Progression and Potential Application in Cancer Therapy: A Friend or Foe?

Over-expressed long noncoding RNA HOXA11-AS promotes cell cycle progression and metastasis in gastric cancer

(2017) Zhili Liu et al.   Molecular Cancer

Long Noncoding RNA LINC00673 Is Activated by SP1 and Exerts Oncogenic Properties by Interacting with LSD1 and EZH2 in Gastric Cancer

(2017) Mingde Huang et al.   MOLECULAR THERAPY

Integrated genomic characterization of oesophageal carcinoma

(2017)   NATURE

MicroRNA-30d inhibits the migration and invasion of human esophageal squamous cell carcinoma cells via the post-transcriptional regulation of enhancer of zeste homolog 2

(2017) Rui Xie et al.   ONCOLOGY REPORTS

Long noncoding RNA H19 regulates EZH2 expression by interacting with miR-630 and promotes cell invasion in nasopharyngeal carcinoma

(2016) Xudong Li et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

MALAT1 long non-coding RNA in cancer

(2016) Rei Yoshimoto et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

LncRNA HOXA11-AS Promotes Proliferation and Invasion of Gastric Cancer by Scaffolding the Chromatin Modification Factors PRC2, LSD1, and DNMT1

(2016) Ming Sun et al.   CANCER RESEARCH

Molecular Profiling Reveals Biologically Discrete Subsets and Pathways of Progression in Diffuse Glioma

(2016) Michele Ceccarelli et al.   CELL

The degradation of EZH2 mediated by lncRNA ANCR attenuated the invasion and metastasis of breast cancer

(2016) Zhongwei Li et al.   CELL DEATH AND DIFFERENTIATION

miR-340 impedes the progression of laryngeal squamous cell carcinoma by targeting EZH2

(2016) Wenfa Yu et al.   GENE

Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas

(2016) Rishi G. Vaswani et al.   JOURNAL OF MEDICINAL CHEMISTRY

LncRNA MALAT1 promotes development of mantle cell lymphoma by associating with EZH2

(2016) Xin Wang et al.   Journal of Translational Medicine

Divergent clonal selection dominates medulloblastoma at recurrence

(2016) A. Sorana Morrissy et al.   NATURE

Distinct patterns of somatic genome alterations in lung adenocarcinomas and squamous cell carcinomas

(2016) Joshua D Campbell et al.   NATURE GENETICS

Frequent somatic CDH1 loss-of-function mutations in plasmacytoid variant bladder cancer

(2016) Hikmat A Al-Ahmadie et al.   NATURE GENETICS

HIFI-α activation underlies a functional switch in the paradoxical role of Ezh2/PRC2 in breast cancer

(2016) Sylvia Mahara et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Long non-coding RNA IRAIN suppresses apoptosis and promotes proliferation by binding to LSD1 and EZH2 in pancreatic cancer

(2016) Yifan Lian et al.   TUMOR BIOLOGY

MicroRNA-298 inhibits malignant phenotypes of epithelial ovarian cancer by regulating the expression of EZH2

(2016) Fenmei Zhou et al.   Oncology Letters

Long noncoding RNA MALAT1 promotes malignant development of esophageal squamous cell carcinoma by targeting β-catenin via Ezh2

(2016) Wei Wang et al.   Oncotarget

MALAT1 long ncRNA promotes gastric cancer metastasis by suppressing PCDH10

(2016) Ying Qi et al.   Oncotarget

Deletion of the Polycomb-Group Protein EZH2 Leads to Compromised Self-Renewal and Differentiation Defects in Human Embryonic Stem Cells

(2016) Adam Collinson et al.   Cell Reports

Ampullary Cancers Harbor ELF3 Tumor Suppressor Gene Mutations and Exhibit Frequent WNT Dysregulation

(2016) Marie-Claude Gingras et al.   Cell Reports

Genomic Correlates of Immune-Cell Infiltrates in Colorectal Carcinoma

(2016) Marios Giannakis et al.   Cell Reports

Mutational Profile of Metastatic Breast Cancers: A Retrospective Analysis

(2016) Celine Lefebvre et al.   PLOS MEDICINE

Polycomb repressive complex’s evolutionary conserved function: the role of EZH2 status and cellular background

(2016) Koraljka Gall Trošelj et al.   Clinical Epigenetics

Downregulation of Enhancer of Zeste Homolog 2 (EZH2) is essential for the Induction of Autophagy and Apoptosis in Colorectal Cancer Cells

(2016) Yizhou Yao et al.   Genes

Long Intergenic Noncoding RNA 00511 Acts as an Oncogene in Non–small-cell Lung Cancer by Binding to EZH2 and Suppressing p57

(2016) Cheng-Cao Sun et al.   Molecular Therapy-Nucleic Acids

Long non-coding RNA LINC00628 functions as a gastric cancer suppressor via long-range modulating the expression of cell cycle related genes

(2016) Zi-Zhen Zhang et al.   Scientific Reports

LncRNA-ANCR down-regulation suppresses invasion and migration of colorectal cancer cells by regulating EZH2 expression

(2016) Zhao-Yang Yang et al.   Cancer Biomarkers

SAM/SAH Analogs as Versatile Tools for SAM-Dependent Methyltransferases

(2015) Jing Zhang et al.   ACS Chemical Biology

siRNA Silencing EZH2 Reverses Cisplatin-resistance of Human Non-small Cell Lung and Gastric Cancer Cells

(2015) Wen Zhou et al.   Asian Pacific Journal of Cancer Prevention

Malat1 as an evolutionarily conserved lncRNA, plays a positive role in regulating proliferation and maintaining undifferentiated status of early-stage hematopoietic cells

(2015) Xian-Yong Ma et al.   BMC GENOMICS

Long Noncoding RNA MALAT1 Promotes Aggressive Renal Cell Carcinoma through Ezh2 and Interacts with miR-205

(2015) H. Hirata et al.   CANCER RESEARCH

Comprehensive Molecular Portraits of Invasive Lobular Breast Cancer

(2015) Giovanni Ciriello et al.   CELL

Genomic Analysis of Metastatic Cutaneous Squamous Cell Carcinoma

(2015) Y. Y. Li et al.   CLINICAL CANCER RESEARCH

Genomic Predictors of Survival in Patients with High-grade Urothelial Carcinoma of the Bladder

(2015) Philip H. Kim et al.   EUROPEAN UROLOGY

Phosphorylation-mediated EZH2 inactivation promotes drug resistance in multiple myeloma

(2015) Jiro Kikuchi et al.   JOURNAL OF CLINICAL INVESTIGATION

Comprehensive genomic profiles of small cell lung cancer

(2015) Julie George et al.   NATURE

Comprehensive genomic characterization of head and neck squamous cell carcinomas

(2015)   NATURE

Exome sequencing of desmoplastic melanoma identifies recurrent NFKBIE promoter mutations and diverse activating mutations in the MAPK pathway

(2015) A Hunter Shain et al.   NATURE GENETICS

Exome sequencing of hepatocellular carcinomas identifies new mutational signatures and potential therapeutic targets

(2015) Kornelius Schulze et al.   NATURE GENETICS

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

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

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

(2015) Daniel Zingg et al.   Nature Communications

The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells

(2015) Christian Mayr et al.   Oncotarget

EZH2 in normal hematopoiesis and hematological malignancies

(2015) Laurie Herviou et al.   Oncotarget

EZH2 is crucial for both differentiation of regulatory T cells and T effector cell expansion

(2015) Xiang-Ping Yang et al.   Scientific Reports

Prolonged Ezh2 Depletion in Glioblastoma Causes a Robust Switch in Cell Fate Resulting in Tumor Progression

(2015) Nienke A. de Vries et al.   Cell Reports

miR-101 is down-regulated in glioblastoma resulting in EZH2-induced proliferation, migration, and angiogenesis

(2015)   Oncotarget

EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation

(2014) William D. Bradley et al.   CHEMISTRY & BIOLOGY

EZH2 promotes tumor progression by increasing VEGF expression in clear cell renal cell carcinoma

(2014) Z. Q. Xu et al.   Clinical & Translational Oncology

The role of polycomb repressive complexes in biliary tract cancer

(2014) Christian Mayr et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Role of EZH2 in oral squamous cell carcinoma carcinogenesis

(2014) Lingbo Zhao et al.   GENE

Genomic portrait of resectable hepatocellular carcinomas: Implications ofRB1andFGF19aberrations for patient stratification

(2014) Sung-Min Ahn et al.   HEPATOLOGY

microRNA-124 inhibits proliferation and induces apoptosis by directly repressing EZH2 in gastric cancer

(2014) Liming Xie et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

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

Comprehensive molecular characterization of gastric adenocarcinoma

(2014) Adam J. Bass et al.   NATURE

Comprehensive molecular profiling of lung adenocarcinoma

(2014) Eric A. Collisson et al.   NATURE

Identification of genomic alterations in oesophageal squamous cell cancer

(2014) Yongmei Song et al.   NATURE

Comprehensive molecular characterization of urothelial bladder carcinoma

(2014)   NATURE

Downregulation of microRNA-26a is associated with metastatic potential and the poor prognosis of osteosarcoma patients

(2014) QI-CHUN SONG et al.   ONCOLOGY REPORTS

MicroRNA-101 inhibits the metastasis of osteosarcoma cells by downregulation of EZH2 expression

(2014) KAILIANG ZHANG et al.   ONCOLOGY REPORTS

MiR-138 Induces Renal Carcinoma Cell Senescence by Targeting EZH2 and Is Downregulated in Human Clear Cell Renal Cell Carcinoma

(2014) Jiaqian Liang et al.   ONCOLOGY RESEARCH

MicroRNA-124 inhibits cellular proliferation and invasion by targeting Ets-1 in breast cancer

(2014) Wentao Li et al.   TUMOR BIOLOGY

Genomic analyses of gynaecologic carcinosarcomas reveal frequent mutations in chromatin remodelling genes

(2014) Siân Jones et al.   Nature Communications

The Genomic Landscape of Pediatric Ewing Sarcoma

(2014) B. D. Crompton et al.   Cancer Discovery

Somatic ERCC2 Mutations Correlate with Cisplatin Sensitivity in Muscle-Invasive Urothelial Carcinoma

(2014) E. M. Van Allen et al.   Cancer Discovery

Genomic Landscape of Ewing Sarcoma Defines an Aggressive Subtype with Co-Association of STAG2 and TP53 Mutations

(2014) F. Tirode et al.   Cancer Discovery

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

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

Enhancer of Zeste Homolog 2 (EZH2) Promotes Progression of Cholangiocarcinoma Cells by Regulating Cell Cycle and Apoptosis

(2013) Shigeki Nakagawa et al.   ANNALS OF SURGICAL ONCOLOGY

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

(2013) Eunhee Kim et al.   CANCER CELL

Long non-coding RNA H19 increases bladder cancer metastasis by associating with EZH2 and inhibiting E-cadherin expression

(2013) Ming Luo et al.   CANCER LETTERS

The Somatic Genomic Landscape of Glioblastoma

(2013) Cameron W. Brennan et al.   CELL

Three-dimensional culture sensitizes epithelial ovarian cancer cells to EZH2 methyltransferase inhibition

(2013) Michael Amatangelo et al.   CELL CYCLE

MiR-138 Inhibits Tumor Growth Through Repression of EZH2 in Non-Small Cell Lung Cancer

(2013) Huijun Zhang et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

EZH2 Promotes E2F-Driven SCLC Tumorigenesis through Modulation of Apoptosis and Cell-Cycle Regulation

(2013) Roland Hubaux et al.   Journal of Thoracic Oncology

PAF and EZH2 Induce Wnt/β-Catenin Signaling Hyperactivation

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

Comprehensive molecular characterization of clear cell renal cell carcinoma

(2013)   NATURE

Integrated genomic characterization of endometrial carcinoma

(2013) Gad Getz et al.   NATURE

Exome and whole-genome sequencing of esophageal adenocarcinoma identifies recurrent driver events and mutational complexity

(2013) Austin M Dulak et al.   NATURE GENETICS

The genomic landscape of hypodiploid acute lymphoblastic leukemia

(2013) Linda Holmfeldt et al.   NATURE GENETICS

Genomic and Epigenomic Landscapes of Adult De Novo Acute Myeloid Leukemia

(2013)   NEW ENGLAND JOURNAL OF MEDICINE

Mutational Analysis Reveals the Origin and Therapy-Driven Evolution of Recurrent Glioma

(2013) B. E. Johnson et al.   SCIENCE

Integrative Analysis of Complex Cancer Genomics and Clinical Profiles Using the cBioPortal

(2013) J. Gao et al.   Science Signaling

EZH2 inhibition: targeting the crossroad of tumor invasion and angiogenesis

(2012) Francesco Crea et al.   CANCER AND METASTASIS REVIEWS

CellMiner: A Web-Based Suite of Genomic and Pharmacologic Tools to Explore Transcript and Drug Patterns in the NCI-60 Cell Line Set

(2012) W. C. Reinhold et al.   CANCER RESEARCH

A Landscape of Driver Mutations in Melanoma

(2012) Eran Hodis et al.   CELL

Mapping the Hallmarks of Lung Adenocarcinoma with Massively Parallel Sequencing

(2012) Marcin Imielinski et al.   CELL

PRC2 directly methylates GATA4 and represses its transcriptional activity

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

EZH2 couples pancreatic regeneration to neoplastic progression

(2012) J. Mallen-St. Clair et al.   GENES & DEVELOPMENT

Non-coding RNAs and EZH2 interactions in cancer: Long and short tales from the transcriptome

(2012) Leonidas Benetatos et al.   INTERNATIONAL JOURNAL OF CANCER

MicroRNA-98 and microRNA-214 post-transcriptionally regulate enhancer of zeste homolog 2 and inhibit migration and invasion in human esophageal squamous cell carcinoma

(2012) Sheng-Dong Huang et al.   Molecular Cancer

EZH2 Generates a Methyl Degron that Is Recognized by the DCAF1/DDB1/CUL4 E3 Ubiquitin Ligase Complex

(2012) Ji Min Lee et al.   MOLECULAR CELL

Recurrent R-spondin fusions in colon cancer

(2012) Somasekar Seshagiri et al.   NATURE

Comprehensive molecular characterization of human colon and rectal cancer

(2012)   NATURE

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

Comprehensive genomic characterization of squamous cell lung cancers

(2012)   NATURE

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

(2012) Sarah K Knutson et al.   Nature Chemical Biology

Comprehensive genomic analysis identifies SOX2 as a frequently amplified gene in small-cell lung cancer

(2012) Charles M Rudin et al.   NATURE GENETICS

Exome sequencing identifies recurrent somatic RAC1 mutations in melanoma

(2012) Michael Krauthammer et al.   NATURE GENETICS

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

(2012) Panagiotis Ntziachristos et al.   NATURE MEDICINE

Epigenetic expansion of VHL-HIF signal output drives multiorgan metastasis in renal cancer

(2012) Sakari Vanharanta et al.   NATURE MEDICINE

Hypoxia Induced Aggressiveness of Prostate Cancer Cells Is Linked with Deregulated Expression of VEGF, IL-6 and miRNAs That Are Attenuated by CDF

(2012) Bin Bao et al.   PLoS One

Hypoxia-Induced Aggressiveness of Pancreatic Cancer Cells Is Due to Increased Expression of VEGF, IL-6 and miR-21, Which Can Be Attenuated by CDF Treatment

(2012) Bin Bao 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

Discovery and prioritization of somatic mutations in diffuse large B-cell lymphoma (DLBCL) by whole-exome sequencing

(2012) J. G. Lohr 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

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

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

The cBio Cancer Genomics Portal: An Open Platform for Exploring Multidimensional Cancer Genomics Data: Figure 1.

(2012) Ethan Cerami et al.   Cancer Discovery

MicroRNA-26a regulates tumorigenic properties of EZH2 in human lung carcinoma cells

(2012) Xiaomin Dang et al.   Cancer Genetics

MicroRNA-138 suppresses epithelial–mesenchymal transition in squamous cell carcinoma cell lines

(2011) Xiqiang Liu et al.   BIOCHEMICAL JOURNAL

Dependency on the polycomb gene Ezh2 distinguishes fetal from adult hematopoietic stem cells

(2011) M. Mochizuki-Kashio et al.   BLOOD

The putative tumour suppressor microRNA-124 modulates hepatocellular carcinoma cell aggressiveness by repressing ROCK2 and EZH2

(2011) Fang Zheng et al.   GUT

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

(2011) Shuet Theng Lee et al.   MOLECULAR CELL

Frequent pathway mutations of splicing machinery in myelodysplasia

(2011) Kenichi Yoshida et al.   NATURE

Predicting the functional impact of protein mutations: application to cancer genomics

(2011) Boris Reva et al.   NUCLEIC ACIDS RESEARCH

The Mutational Landscape of Head and Neck Squamous Cell Carcinoma

(2011) N. Stransky et al.   SCIENCE

MicroRNAs: Synthesis, mechanism, function, and recent clinical trials

(2010) Fazli Wahid et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

The H19 locus: Role of an imprinted non-coding RNA in growth and development

(2010) Anne Gabory et al.   BIOESSAYS

MicroRNA-101 is down-regulated in gastric cancer and involved in cell migration and invasion

(2010) Hui-Ju Wang et al.   EUROPEAN JOURNAL OF CANCER

The Nuclear-Retained Noncoding RNA MALAT1 Regulates Alternative Splicing by Modulating SR Splicing Factor Phosphorylation

(2010) Vidisha Tripathi et al.   MOLECULAR CELL

Long non-coding RNA HOTAIR reprograms chromatin state to promote cancer metastasis

(2010) Rajnish A. Gupta et al.   NATURE

Recruitment of Polycomb group complexes and their role in the dynamic regulation of cell fate choice

(2009) B. Schuettengruber et al.   DEVELOPMENT

Long non-coding RNAs: insights into functions

(2009) Tim R. Mercer et al.   NATURE REVIEWS GENETICS

Mechanisms of Polycomb gene silencing: knowns and unknowns

(2009) Jeffrey A. Simon et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Regulation of Pancreatic Tumor Cell Proliferation and Chemoresistance by the Histone Methyltransferase Enhancer of Zeste Homologue 2

(2008) A. V. Ougolkov et al.   CLINICAL CANCER RESEARCH

Polycomb Group Protein-associated Chromatin Is Reproduced in Post-mitotic G1Phase and Is Required for S Phase Progression

(2008) Takahiro Aoto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dominant Alleles Identify SET Domain Residues Required for Histone Methyltransferase of Polycomb Repressive Complex 2

(2008) Preeti Joshi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ezh1 and Ezh2 Maintain Repressive Chromatin through Different Mechanisms

(2008) Raphael Margueron et al.   MOLECULAR CELL

Genomic Loss of microRNA-101 Leads to Overexpression of Histone Methyltransferase EZH2 in Cancer

(2008) S. Varambally et al.   SCIENCE