Epigenome-based personalized medicine in human cancer

FDA Approval: Belinostat for the Treatment of Patients with Relapsed or Refractory Peripheral T-cell Lymphoma

(2015) H.-Z. Lee et al.   CLINICAL CANCER RESEARCH

Mixed lineage rearranged leukaemia

(2015) Eytan M. Stein et al.   CURRENT OPINION IN HEMATOLOGY

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

(2015) Christine M. Fillmore et al.   NATURE

A New Initiative on Precision Medicine

(2015) Francis S. Collins et al.   NEW ENGLAND JOURNAL OF MEDICINE

HDAC Inhibitors as Novel Anti-Cancer Therapeutics

(2015) Cristabelle Souza et al.   Recent Patents on Anti-Cancer Drug Discovery

NCL1, a highly selective lysine-specific demethylase 1 inhibitor, suppresses prostate cancer without adverse effect

(2015) Toshiki Etani et al.   Oncotarget

Inhibition of histone H3K79 methylation selectively inhibits proliferation, self-renewal and metastatic potential of breast cancer

(2015) Li Zhang et al.   Oncotarget

Targeting epigenetic regulators for cancer therapy

(2014) Susan Wee et al.   Annals of the New York Academy of Sciences

A Cell-Permeable Ester Derivative of the JmjC Histone Demethylase Inhibitor IOX1

(2014) Rachel Schiller et al.   ChemMedChem

microRNAs as Anti-Cancer Therapy

(2014) Michela Garofalo et al.   CURRENT PHARMACEUTICAL DESIGN

New answers to old questions from genome-wide maps of DNA methylation in hematopoietic cells

(2014) Mira Jeong et al.   EXPERIMENTAL HEMATOLOGY

DNA methylome profiling beyond promoters - taking an epigenetic snapshot of the breast tumor microenvironment

(2014) Jana Jeschke et al.   FEBS Journal

Predictive value of CHFR and MLH1 methylation in human gastric cancer

(2014) Yazhuo Li et al.   Gastric Cancer

Targeting histone methyltransferase EZH2 as cancer treatment

(2014) Y. Kondo   JOURNAL OF BIOCHEMISTRY

Harnessing the potential of epigenetic therapy to target solid tumors

(2014) Nita Ahuja et al.   JOURNAL OF CLINICAL INVESTIGATION

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

Contrasting roles of histone 3 lysine 27 demethylases in acute lymphoblastic leukaemia

(2014) Panagiotis Ntziachristos et al.   NATURE

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Bromodomains: pockets with therapeutic potential

(2014) Kostas A. Papavassiliou et al.   TRENDS IN MOLECULAR MEDICINE

Epigenetic drug therapy based on bromodomain inhibition

(2014) Dashzeveg Bayarsaihan et al.   Epigenomics

Targeting the BET family for the treatment of leukemia

(2014) Xavier Lucas et al.   Epigenomics

EZH2: biology, disease and structure-based drug discovery

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

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Bromodomains as therapeutic targets in cancer

(2013) I. Barbieri et al.   Briefings in Functional Genomics

KDM4/JMJD2 Histone Demethylases: Epigenetic Regulators in Cancer Cells

(2013) W. L. Berry et al.   CANCER RESEARCH

Gemtuzumab ozogamicin in combination with vorinostat and azacitidine in older patients with relapsed or refractory acute myeloid leukemia: a phase I/II study

(2013) R. B. Walter et al.   HAEMATOLOGICA

Pharmacokinetics of different formulations of oral azacitidine (CC-486) and the effect of food and modified gastric pH on pharmacokinetics in subjects with hematologic malignancies

(2013) Eric Laille et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Momentum grows to make 'personalized' medicine more 'precise'

(2013) Alla Katsnelson   NATURE MEDICINE

The future of epigenetic therapy in solid tumours—lessons from the past

(2013) Nilofer Azad et al.   Nature Reviews Clinical Oncology

Histone lysine demethylases as targets for anticancer therapy

(2013) Jonas W. Højfeldt et al.   NATURE REVIEWS DRUG DISCOVERY

Cancer Genome Landscapes

(2013) B. Vogelstein et al.   SCIENCE

Mining cancer methylomes: prospects and challenges

(2013) Clare Stirzaker et al.   TRENDS IN GENETICS

Therapeutic Delivery of MicroRNA-29b by Cationic Lipoplexes for Lung Cancer

(2013) Yun Wu et al.   Molecular Therapy-Nucleic Acids

Phase 2 study of the lenalidomide and azacitidine combination in patients with higher-risk myelodysplastic syndromes

(2012) M. A. Sekeres et al.   BLOOD

Cancer Genetics and Epigenetics: Two Sides of the Same Coin?

(2012) Jueng Soo You et al.   CANCER CELL

Transient Low Doses of DNA-Demethylating Agents Exert Durable Antitumor Effects on Hematological and Epithelial Tumor Cells

(2012) Hsing-Chen Tsai et al.   CANCER CELL

Anti-miR-155 oligonucleotide enhances chemosensitivity of U251 cell to taxol by inducing apoptosis

(2012) Wei Meng et al.   CELL BIOLOGY INTERNATIONAL

Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L

(2012) Aravind Basavapathruni et al.   Chemical Biology & Drug Design

Whole-genome methylation analysis of benign and malignant colorectal tumours

(2012) Andrew D Beggs et al.   JOURNAL OF PATHOLOGY

The long non-coding RNAs, a new cancer diagnostic and therapeutic gold mine

(2012) Peng Qi et al.   MODERN PATHOLOGY

Histone Lysine Methylation Dynamics: Establishment, Regulation, and Biological Impact

(2012) Joshua C. Black et al.   MOLECULAR CELL

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

(2012) Michael T. McCabe et al.   NATURE

Inhibition of natural antisense transcripts in vivo results in gene-specific transcriptional upregulation

(2012) Farzaneh Modarresi et al.   NATURE BIOTECHNOLOGY

DNA methylation profiling in the clinic: applications and challenges

(2012) Holger Heyn et al.   NATURE REVIEWS GENETICS

TFAP2E–DKK4and Chemoresistance in Colorectal Cancer

(2012) Matthias P.A. Ebert et al.   NEW ENGLAND JOURNAL OF MEDICINE

Preparing for Precision Medicine

(2012) Reza Mirnezami et al.   NEW ENGLAND JOURNAL OF MEDICINE

Epigenetic mechanisms in gastric cancer

(2012) Carolina Oliveira Gigek et al.   Epigenomics

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

Targeting Histone Lysine Demethylases by Truncating the Histone 3 Tail to Obtain Selective Substrate-Based Inhibitors

(2011) Brian Lohse et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis

(2011) A. T. Nguyen et al.   BLOOD

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

(2011) Scott R. Daigle et al.   CANCER CELL

Validation of the histone methyltransferase EZH2 as a therapeutic target for various types of human cancer and as a prognostic marker

(2011) Masashi Takawa et al.   CANCER SCIENCE

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Cancer epigenetics: linking basic biology to clinical medicine

(2011) Hsing-Chen Tsai et al.   CELL RESEARCH

DNA hypermethylation as a chemotherapy target

(2011) Juan Ren et al.   CELLULAR SIGNALLING

Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds

(2011) Kai-Hsuan Chang et al.   ChemMedChem

Epigenetic Alteration of PRKCDBP in Colorectal Cancers and Its Implication in Tumor Cell Resistance to TNF -Induced Apoptosis

(2011) J.-H. Lee et al.   CLINICAL CANCER RESEARCH

Association of CHFR Promoter Methylation with Disease Recurrence in Locally Advanced Colon Cancer

(2011) M. Tanaka et al.   CLINICAL CANCER RESEARCH

Developing therapeutic microRNAs for cancer

(2011) A G Bader et al.   GENE THERAPY

The diverse functions of Dot1 and H3K79 methylation

(2011) A. T. Nguyen et al.   GENES & DEVELOPMENT

Deficiency of H3K79 Histone Methyltransferase Dot1-like Protein (DOT1L) Inhibits Cell Proliferation

(2011) Wootae Kim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Role of androgen receptor and associated lysine-demethylase coregulators, LSD1 and JMJD2A, in localized and advanced human bladder cancer

(2011) Eric C. Kauffman et al.   MOLECULAR CARCINOGENESIS

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

Function of leukemogenic mixed lineage leukemia 1 (MLL) fusion proteins through distinct partner protein complexes

(2011) D. Biswas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Combination Epigenetic Therapy Has Efficacy in Patients with Refractory Advanced Non-Small Cell Lung Cancer

(2011) R. A. Juergens et al.   Cancer Discovery

RNA Targeting Therapeutics: Molecular Mechanisms of Antisense Oligonucleotides as a Therapeutic Platform

(2010) C. Frank Bennett et al.   Annual Review of Pharmacology and Toxicology

A Higher-Order Complex Containing AF4 and ENL Family Proteins with P-TEFb Facilitates Oncogenic and Physiologic MLL-Dependent Transcription

(2010) Akihiko Yokoyama et al.   CANCER CELL

Structural insights into histone lysine demethylation

(2010) Haifeng Hou et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Promoter methylation ofHIN-1in the progression to esophageal squamous cancer

(2010) MingZhou Guo et al.   Epigenetics

MLL-AF9 and MLL-ENL alter the dynamic association of transcriptional regulators with genes critical for leukemia

(2010) Sara C. Monroe et al.   EXPERIMENTAL HEMATOLOGY

Linking H3K79 trimethylation to Wnt signaling through a novel Dot1-containing complex (DotCom)

(2010) M. Mohan et al.   GENES & DEVELOPMENT

Overexpression of LSD1 contributes to human carcinogenesis through chromatin regulation in various cancers

(2010) Shinya Hayami et al.   INTERNATIONAL JOURNAL OF CANCER

DNA methyltransferase 3-like affects promoter methylation of thymine DNA glycosylase independently of DNMT1 and DNMT3B in cancer cells

(2010) Kim   INTERNATIONAL JOURNAL OF ONCOLOGY

BRCA1 CpG Island Hypermethylation Predicts Sensitivity to Poly(Adenosine Diphosphate)- Ribose Polymerase Inhibitors

(2010) Jurgen Veeck et al.   JOURNAL OF CLINICAL ONCOLOGY

DNA methylation profiling in doxorubicin treated primary locally advanced breast tumours identifies novel genes associated with survival and treatment response

(2010) Emelyne Dejeux et al.   Molecular Cancer

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Epigenetic modifications as therapeutic targets

(2010) Theresa K Kelly et al.   NATURE BIOTECHNOLOGY

Targeting microRNAs in cancer: rationale, strategies and challenges

(2010) Ramiro Garzon et al.   NATURE REVIEWS DRUG DISCOVERY

Charting histone modifications and the functional organization of mammalian genomes

(2010) Vicky W. Zhou et al.   NATURE REVIEWS GENETICS

The Path to Personalized Medicine

(2010) Margaret A. Hamburg et al.   NEW ENGLAND JOURNAL OF MEDICINE

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

(2010) Oliver N. F. King et al.   PLoS One

Characterization of the DOT1L Network: Implications of Diverse Roles for DOT1L

(2010) Geunyeong Park et al.   PROTEIN JOURNAL

Regulation of Alternative Splicing by Histone Modifications

(2010) R. F. Luco et al.   SCIENCE

Therapeutic MicroRNA Strategies in Human Cancer

(2009) Chunsheng Li et al.   AAPS Journal

Lysine-Specific Demethylase 1 Is Strongly Expressed in Poorly Differentiated Neuroblastoma: Implications for Therapy

(2009) J. H. Schulte et al.   CANCER RESEARCH

LSD1 Is a Subunit of the NuRD Complex and Targets the Metastasis Programs in Breast Cancer

(2009) Yan Wang et al.   CELL

Methylation and protein expression of DNA repair genes: association with chemotherapy exposure and survival in sporadic ovarian and peritoneal carcinomas

(2009) Elizabeth M Swisher et al.   Molecular Cancer

ChIP-seq accurately predicts tissue-specific activity of enhancers

(2009) Axel Visel et al.   NATURE

Differential methylation of tissue- and cancer-specific CpG island shores distinguishes human induced pluripotent stem cells, embryonic stem cells and fibroblasts

(2009) Akiko Doi et al.   NATURE GENETICS

The human colon cancer methylome shows similar hypo- and hypermethylation at conserved tissue-specific CpG island shores

(2009) Rafael A Irizarry et al.   NATURE GENETICS

Protein methyltransferases as a target class for drug discovery

(2009) Robert A. Copeland et al.   NATURE REVIEWS DRUG DISCOVERY

When chromatin meets splicing

(2009) Alberto R Kornblihtt et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

IGFBP-3 hypermethylation-derived deficiency mediates cisplatin resistance in non-small-cell lung cancer

(2009) I Ibanez de Caceres et al.   ONCOGENE

Misguided Transcriptional Elongation Causes Mixed Lineage Leukemia

(2009) Dorothee Mueller et al.   PLOS BIOLOGY

Restoration of tumor suppressor miR-34 inhibits human p53-mutant gastric cancer tumorspheres

(2008) Qing Ji et al.   BMC CANCER

Identification of CDK10 as an Important Determinant of Resistance to Endocrine Therapy for Breast Cancer

(2008) Elizabeth Iorns et al.   CANCER CELL

The transglutaminase 2 gene ( TGM2 ), a potential molecular marker for chemotherapeutic drug sensitivity, is epigenetically silenced in breast cancer

(2008) Lingbao Ai et al.   CARCINOGENESIS

Phase I Study of Epigenetic Modulation with 5-Azacytidine and Valproic Acid in Patients with Advanced Cancers

(2008) F. Braiteh et al.   CLINICAL CANCER RESEARCH

miR-21: a small multi-faceted RNA

(2008) Anna M. Krichevsky et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas

(2008) S Balasubramanian et al.   LEUKEMIA

Roles of the EZH2 histone methyltransferase in cancer epigenetics

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