EZH2: an emerging role in melanoma biology and strategies for targeted therapy

Genetic and epigenetic loss of microRNA-31 leads to feed-forward expression of EZH2 in melanoma

(2015) Irfan A Asangani et al.   Oncotarget

EZH2: biology, disease and structure-based drug discovery

(2013) Jin-zhi Tan et al.   ACTA PHARMACOLOGICA SINICA

EZH2 mutations are frequent and represent an early event in follicular lymphoma

(2013) C. Bodor et al.   BLOOD

BAP1germline mutation in two first grade family members with uveal melanoma

(2013) David A Maerker et al.   BRITISH JOURNAL OF OPHTHALMOLOGY

EZH2 Is Required for Germinal Center Formation and Somatic EZH2 Mutations Promote Lymphoid Transformation

(2013) Wendy Béguelin et al.   CANCER CELL

Interplay between the Cancer Genome and Epigenome

(2013) Hui Shen et al.   CELL

Concurrent loss of Ezh2 and Tet2 cooperates in the pathogenesis of myelodysplastic disorders

(2013) Tomoya Muto et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Signatures of mutational processes in human cancer

(2013) Ludmil B. Alexandrov et al.   NATURE

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

(2013) Woojin Kim et al.   Nature Chemical Biology

Advances in targeting cell surface signalling molecules for immune modulation

(2013) Sheng Yao et al.   NATURE REVIEWS DRUG DISCOVERY

Poly-combing the genome for RNA

(2013) Loyal A Goff et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Promiscuous RNA binding by Polycomb repressive complex 2

(2013) Chen Davidovich et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

PRC2 binds active promoters and contacts nascent RNAs in embryonic stem cells

(2013) Syuzo Kaneko et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

PRMT5 Is Upregulated in Malignant and Metastatic Melanoma and Regulates Expression of MITF and p27Kip1

(2013) Courtney Nicholas et al.   PLoS One

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

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

Cancer Epigenetics: From Mechanism to Therapy

(2012) Mark A. Dawson et al.   CELL

A Landscape of Driver Mutations in Melanoma

(2012) Eran Hodis et al.   CELL

The BRAFV600E causes widespread alterations in gene methylation in the genome of melanoma cells

(2012) Peng Hou et al.   CELL CYCLE

Epigenetic regulation of skin: focus on the Polycomb complex

(2012) Jisheng Zhang et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Inner workings and regulatory inputs that control Polycomb repressive complex 2

(2012) M. Maggie O’Meara et al.   CHROMOSOMA

Deregulation of protein methylation in melanoma

(2012) Katharina Limm et al.   EUROPEAN JOURNAL OF CANCER

miR-137 Inhibits the Invasion of Melanoma Cells through Downregulation of Multiple Oncogenic Target Genes

(2012) Chonglin Luo et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Novel mutations target distinct subgroups of medulloblastoma

(2012) Giles Robinson et al.   NATURE

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

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 protein families: a new frontier for drug discovery

(2012) Cheryl H. Arrowsmith et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting Epigenetic Readers in Cancer

(2012) Mark A. Dawson et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mining Gene Expression Signature for the Detection of Pre-Malignant Melanocytes and Early Melanomas with Risk for Metastasis

(2012) Camila Ferreira de Souza et al.   PLoS One

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

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

(2012) K. Xu et al.   SCIENCE

Emerging Epigenetic Targets and Therapies in Cancer Medicine

(2012) Relja Popovic et al.   Cancer Discovery

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

(2012) Ethan Cerami et al.   Cancer Discovery

The histone methyltransferase inhibitor, DZNep, up-regulates TXNIP, increases ROS production, and targets leukemia cells in AML

(2011) J. Zhou et al.   BLOOD

EZH1 and EZH2 cogovern histone H3K27 trimethylation and are essential for hair follicle homeostasis and wound repair

(2011) E. Ezhkova et al.   GENES & DEVELOPMENT

Germline BAP1 mutation predisposes to uveal melanoma, lung adenocarcinoma, meningioma, and other cancers

(2011) M. H. Abdel-Rahman et al.   JOURNAL OF MEDICAL GENETICS

EZH2-Dependent Suppression of a Cellular Senescence Phenotype in Melanoma Cells by Inhibition of p21/CDKN1A Expression

(2011) T. Fan et al.   MOLECULAR CANCER RESEARCH

The histone methyltransferase SETDB1 is recurrently amplified in melanoma and accelerates its onset

(2011) Craig J. Ceol et al.   NATURE

Genome-wide association study identifies a new melanoma susceptibility locus at 1q21.3

(2011) Stuart MacGregor et al.   NATURE GENETICS

ChIP-seq analysis reveals distinct H3K27me3 profiles that correlate with transcriptional activity

(2011) Matthew D. Young et al.   NUCLEIC ACIDS RESEARCH

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

Histone H2A deubiquitinase activity of the Polycomb repressive complex PR-DUB

(2010) Johanna C. Scheuermann 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

A method and server for predicting damaging missense mutations

(2010) Ivan A Adzhubei et al.   NATURE METHODS

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

Frequent Mutation of BAP1 in Metastasizing Uveal Melanomas

(2010) J. W. Harbour et al.   SCIENCE

Down-regulation of Rap1GAP via Promoter Hypermethylation Promotes Melanoma Cell Proliferation, Survival, and Migration

(2009) H. Zheng et al.   CANCER RESEARCH

Polycomb protein EZH2 regulates E2F1-dependent apoptosis through epigenetically modulating Bim expression

(2009) Z L Wu et al.   CELL DEATH AND DIFFERENTIATION

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

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

Roles of the EZH2 histone methyltransferase in cancer epigenetics

(2008) Jeffrey A. Simon et al.   MUTATION RESEARCH-FUNDAMENTAL AND MOLECULAR MECHANISMS OF MUTAGENESIS

An embryonic stem cell–like gene expression signature in poorly differentiated aggressive human tumors

(2008) Ittai Ben-Porath et al.   NATURE GENETICS