Targeting epigenetic regulators for cancer therapy: modulation of bromodomain proteins, methyltransferases, demethylases, and microRNAs

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

(2015) Peter G. K. Clark et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

SWI/SNF Chromatin Remodeling and Human Malignancies

(2015) Julien Masliah-Planchon et al.   Annual Review of Pathology-Mechanisms of Disease

Proceedings of the second international molecular pathological epidemiology (MPE) meeting

(2015) Shuji Ogino et al.   CANCER CAUSES & CONTROL

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC

(2015) Helai P. Mohammad et al.   CANCER CELL

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies

(2015) Bhavatarini Vangamudi et al.   CANCER RESEARCH

The PRMT5 arginine methyltransferase: many roles in development, cancer and beyond

(2015) Nicole Stopa et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs

(2015) M. Boi et al.   CLINICAL CANCER RESEARCH

Advances in the development of histone lysine demethylase inhibitors

(2015) Tamara Maes et al.   CURRENT OPINION IN PHARMACOLOGY

Targeting EZH2 and PRC2 dependence as novel anticancer therapy

(2015) Bowen Xu et al.   EXPERIMENTAL HEMATOLOGY

Histone deacetylation meets miRNA: epigenetics and post-transcriptional regulation in cancer and chronic diseases

(2015) Stefan Swierczynski et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

miRNA-15a/16: as tumor suppressors and more

(2015) Enyu Huang et al.   Future Oncology

Epigenetic Alterations in Colorectal Cancer: Emerging Biomarkers

(2015) Yoshinaga Okugawa et al.   GASTROENTEROLOGY

TRIM24 suppresses development of spontaneous hepatic lipid accumulation and hepatocellular carcinoma in mice

(2015) Shiming Jiang et al.   JOURNAL OF HEPATOLOGY

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors

(2015) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors

(2015) Emmanuel H. Demont et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF

(2015) James Bennett et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

(2015) Natalie H. Theodoulou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

(2015) Wylie S. Palmer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors

(2015) F. Anthony Romero et al.   JOURNAL OF MEDICINAL CHEMISTRY

BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia

(2015) Jae-Seok Roe et al.   MOLECULAR CELL

Histone Variant H2A.Z.2 Mediates Proliferation and Drug Sensitivity of Malignant Melanoma

(2015) Chiara Vardabasso et al.   MOLECULAR CELL

Integrative analysis of 111 reference human epigenomes

(2015) Anshul Kundaje et al.   NATURE

Cell-of-origin chromatin organization shapes the mutational landscape of cancer

(2015) Paz Polak et al.   NATURE

Transcriptional plasticity promotes primary and acquired resistance to BET inhibition

(2015) Philipp Rathert et al.   NATURE

BET inhibitor resistance emerges from leukaemia stem cells

(2015) Chun Yew Fong et al.   NATURE

Discovery of cancer drug targets by CRISPR-Cas9 screening of protein domains

(2015) Junwei Shi et al.   NATURE BIOTECHNOLOGY

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma

(2015) Pawel K Mazur et al.   NATURE MEDICINE

High-throughput screening using patient-derived tumor xenografts to predict clinical trial drug response

(2015) Hui Gao et al.   NATURE MEDICINE

Getting up to speed with transcription elongation by RNA polymerase II

(2015) Iris Jonkers et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Acute Myeloid Leukemia

(2015) Hartmut Döhner et al.   NEW ENGLAND JOURNAL OF MEDICINE

Alternative splicing regulates the expression of G9A and SUV39H2 methyltransferases, and dramatically changes SUV39H2 functions

(2015) Oriane Mauger et al.   NUCLEIC ACIDS RESEARCH

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

(2015) V Gibaja et al.   ONCOGENE

Beating the odds: BETs in disease

(2015) Chen-Yi Wang et al.   TRENDS IN BIOCHEMICAL SCIENCES

Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells

(2015) Yukihiro Itoh et al.   ACS Medicinal Chemistry Letters

Targeting BET bromodomains for cancer treatment

(2015) Marie Jung et al.   Epigenomics

Tumour suppressor TRIM33 targets nuclear β-catenin degradation

(2015) Jianfei Xue et al.   Nature Communications

Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma

(2015) Matthew B. Siegel et al.   Oncotarget

Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery

(2015) Lei-lei Fu et al.   Oncotarget

GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1

(2015) Krishan Kumar et al.   Scientific Reports

MicroRNAs in Cancer: A Historical Perspective on the Path from Discovery to Therapy

(2015) Esteban Orellana et al.   Cancers

The Regulatory Role of MicroRNAs in EMT and Cancer

(2015) Apostolos Zaravinos   Journal of Oncology

Differential CARM1 Isoform Expression in Subcellular Compartments and among Malignant and Benign Breast Tumors

(2015) David Shlensky et al.   PLoS One

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

(2015) William N. Pappano et al.   PLoS One

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

(2015) Li Zhang et al.   Oncotarget

Methylation of miR-129-5p CpG island modulates multi-drug resistance in gastric cancer by targeting ABC transporters

(2015) Qiong Wu et al.   Oncotarget

Targeting histone lysine demethylases — Progress, challenges, and the future

(2014) Cyrille C. Thinnes et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

MicroRNA-155 influences B-cell receptor signaling and associates with aggressive disease in chronic lymphocytic leukemia

(2014) B. Cui et al.   BLOOD

CARM1 Methylates Chromatin Remodeling Factor BAF155 to Enhance Tumor Progression and Metastasis

(2014) Lu Wang et al.   CANCER CELL

Ezh2 is required for neural crest-derived cartilage and bone formation

(2014) D. Schwarz et al.   DEVELOPMENT

Investigational epigenetically targeted drugs in early phase trials for the treatment of haematological malignancies

(2014) Jessica Okosun et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

KDM4 histone demethylase inhibitors for anti-cancer agents: a patent review

(2014) Young-Won Chin et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Affinity Map of Bromodomain Protein 4 (BRD4) Interactions with the Histone H4 Tail and the Small Molecule Inhibitor JQ1

(2014) Marie Jung et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pleiotrophin antagonizes Brd2 during neuronal differentiation

(2014) P. Garcia-Gutierrez et al.   JOURNAL OF CELL SCIENCE

KDM4B as a Target for Prostate Cancer: Structural Analysis and Selective Inhibition by a Novel Inhibitor

(2014) Chia-Han Chu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Inhibitors of Protein Methyltransferases

(2014) H. Ümit Kaniskan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Reversible Inhibitors of LSD1 as Therapeutic Agents in Acute Myeloid Leukemia: Clinical Significance and Progress to Date

(2014) Daniel P. Mould et al.   MEDICINAL RESEARCH REVIEWS

Kinesin Family Deregulation Coordinated by Bromodomain Protein ANCCA and Histone Methyltransferase MLL for Breast Cancer Cell Growth, Survival, and Tamoxifen Resistance

(2014) June X. Zou 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

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

Targeting bromodomains: epigenetic readers of lysine acetylation

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

BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones

(2014) Tomohiko Kanno et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A combinatorial microRNA therapeutics approach to suppressing non-small cell lung cancer

(2014) A L Kasinski et al.   ONCOGENE

c-Myc suppresses microRNA-29b to promote tumor aggressiveness and poor outcomes in non-small cell lung cancer by targeting FHIT

(2014) D-W Wu et al.   ONCOGENE

Knockdown of Tripartite Motif Containing 24 by Lentivirus Suppresses Cell Growth and Induces Apoptosis in Human Colorectal Cancer Cells

(2014) Jianwei Wang et al.   ONCOLOGY RESEARCH

Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells

(2014) Trent Fowler et al.   PLoS One

DOT1L Inhibition Sensitizes MLL-Rearranged AML to Chemotherapy

(2014) Wei Liu et al.   PLoS One

Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas

(2014) Sarah K. Knutson et al.   PLoS One

Chem-seq permits identification of genomic targets of drugs against androgen receptor regulation selected by functional phenotypic screens

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

Epigenetics and pancreatic cancer: Pathophysiology and novel treatment aspects

(2014) Daniel Neureiter   WORLD JOURNAL OF GASTROENTEROLOGY

The KDM5 family of histone demethylases as targets in oncology drug discovery

(2014) Peter Birk Rasmussen et al.   Epigenomics

Cavity-free plasmonic nanolasing enabled by dispersionless stopped light

(2014) Tim Pickering et al.   Nature Communications

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

Prognostic Role of MicroRNA-21 in Gastric Cancer: a Meta-Analysis

(2014) Chen Li   MEDICAL SCIENCE MONITOR

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

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

EZH2: biology, disease and structure-based drug discovery

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

High expression of lysine-specific demethylase 1 correlates with poor prognosis of patients with esophageal squamous cell carcinoma

(2013) Yanyan Yu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Malignant genome reprogramming by ATAD2

(2013) Fayçal Boussouar et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

CARM1 and PRMT1 are dysregulated in lung cancer without hierarchical features

(2013) Rania Elakoum et al.   BIOCHIMIE

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l

(2013) A. J. Deshpande et al.   BLOOD

The oestrogen receptor coactivator CARM1 has an oncogenic effect and is associated with poor prognosis in breast cancer

(2013) Hany Onsy Habashy et al.   BREAST CANCER RESEARCH AND TREATMENT

Runx3 Inactivation Is a Crucial Early Event in the Development of Lung Adenocarcinoma

(2013) You-Soub Lee et al.   CANCER CELL

Histone Demethylase RBP2 Promotes Lung Tumorigenesis and Cancer Metastasis

(2013) Y.-C. Teng et al.   CANCER RESEARCH

Cellular localization of protein arginine methyltransferase-5 correlates with grade of lung tumors

(2013) Konstantin Shilo et al.   Diagnostic Pathology

Crosstalk between epigenetic readers regulates the MOZ/MORF HAT complexes

(2013) Brianna J Klein et al.   Epigenetics

MicroRNA-195 and microRNA-378 mediate tumor growth suppression by epigenetical regulation in gastric cancer

(2013) Hongxia Deng et al.   GENE

Bromodomain-PHD finger protein 1 is critical for leukemogenesis associated with MOZ–TIF2 fusion

(2013) Haruko Shima et al.   INTERNATIONAL JOURNAL OF HEMATOLOGY

Identification of Small Molecule Inhibitors of Jumonji AT-rich Interactive Domain 1B (JARID1B) Histone Demethylase by a Sensitive High Throughput Screen

(2013) Joyce Sayegh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Clinical Role of microRNAs in Cytogenetically Normal Acute Myeloid Leukemia:miR-155Upregulation Independently Identifies High-Risk Patients

(2013) Guido Marcucci et al.   JOURNAL OF CLINICAL ONCOLOGY

The inhibitory role of Mir-29 in growth of breast cancer cells

(2013) Zhenglong Wu et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

The double bromodomain protein Brd2 promotes B cell expansion and mitogenesis

(2013) Anna C. Belkina et al.   JOURNAL OF LEUKOCYTE BIOLOGY

On the Histone Lysine Methyltransferase Activity of Fungal Metabolite Chaetocin

(2013) Fanny L. Cherblanc et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Medicinal Chemistry Perspective for Targeting Histone H3 Lysine-79 Methyltransferase DOT1L

(2013) Justin L. Anglin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP

(2013) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular pathological epidemiology of epigenetics: emerging integrative science to analyze environment, host and disease

(2013) Shuji Ogino et al.   MODERN PATHOLOGY

Histone deacetylases inhibitor trichostatin A increases the expression of Dleu2/miR-15a/16-1 via HDAC3 in non-small cell lung cancer

(2013) Chi-qi Chen et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

Expression and sub-cellular localization of an epigenetic regulator, co-activator arginine methyltransferase 1 (CARM1), is associated with specific breast cancer subtypes and ethnicity

(2013) Melissa B Davis et al.   Molecular Cancer

The lysine specific demethylase-1 (LSD1/KDM1A) regulates VEGF-A expression in prostate cancer

(2013) Vasundhra Kashyap et al.   Molecular Oncology

Histone lysine demethylases as targets for anticancer therapy

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

MYCN and HDAC2 cooperate to repress miR-183 signaling in neuroblastoma

(2013) Marco Lodrini et al.   NUCLEIC ACIDS RESEARCH

Elevated expression of coactivator-associated arginine methyltransferase 1 is associated with early hepatocarcinogenesis

(2013) SHIGEHIRO OSADA et al.   ONCOLOGY REPORTS

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

(2013) Courtney Nicholas et al.   PLoS One

PRMT5 dimethylates R30 of the p65 subunit to activate NF- B

(2013) H. Wei et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Methylation of miR-124a-1, miR-124a-2, and miR-124a-3 genes correlates with aggressive and advanced breast cancer disease

(2013) Riadh Ben Gacem et al.   TUMOR BIOLOGY

Balancing of Histone H3K4 Methylation States by the Kdm5c/SMCX Histone Demethylase Modulates Promoter and Enhancer Function

(2013) Nikolay S. Outchkourov et al.   Cell Reports

Epigenetic alteration and microRNA dysregulation in cancer

(2013) Hiromu Suzuki et al.   Frontiers in Genetics

A Small-Molecule Probe of the Histone Methyltransferase G9a Induces Cellular Senescence in Pancreatic Adenocarcinoma

(2012) Yuan Yuan et al.   ACS Chemical Biology

Protein arginine methyltransferase 5 is essential for growth of lung cancer cells

(2012) Zhongping Gu et al.   BIOCHEMICAL JOURNAL

Inhibition of DNA methyltransferase activity and expression by treatment with the pan-deacetylase inhibitor panobinostat in hepatocellular carcinoma cell lines

(2012) Steffen Zopf et al.   BMC CANCER

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

(2012) Panagis Filippakopoulos et al.   CELL

MiR-34a inhibits proliferation and migration of breast cancer through down-regulation of Bcl-2 and SIRT1

(2012) Laisheng Li et al.   CLINICAL AND EXPERIMENTAL MEDICINE

High expression of miR-21 and miR-155 predicts recurrence and unfavourable survival in non-small cell lung cancer

(2012) Miaomiao Yang et al.   EUROPEAN JOURNAL OF CANCER

Enhancer of zeste homolog 2 epigenetically silences multiple tumor suppressor microRNAs to promote liver cancer metastasis

(2012) Sandy Leung-Kuen Au et al.   HEPATOLOGY

Impairment of prostate cancer cell growth by a selective and reversible lysine-specific demethylase 1 inhibitor

(2012) Dominica Willmann et al.   INTERNATIONAL JOURNAL OF CANCER

Identification of Small-Molecule Enhancers of Arginine Methylation Catalyzed by Coactivator-Associated Arginine Methyltransferase 1

(2012) Sabrina Castellano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites

(2012) Lewis R. Vidler et al.   JOURNAL OF MEDICINAL CHEMISTRY

The role of histone demethylases in cancer therapy

(2012) Inga Hoffmann et al.   Molecular Oncology

MicroRNA and cancer

(2012) Martin D. Jansson et al.   Molecular Oncology

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

(2012) Michael T. McCabe et al.   NATURE

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

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

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

(2012) Tino Schenk et al.   NATURE MEDICINE

Over-Expression of LSD1 Promotes Proliferation, Migration and Invasion in Non-Small Cell Lung Cancer

(2012) Tangfeng Lv et al.   PLoS One

Protein Arginine Methyltransferase 5 Functions in Opposite Ways in the Cytoplasm and Nucleus of Prostate Cancer Cells

(2012) Zhongping Gu 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

Pathogenesis of NUT Midline Carcinoma

(2011) Christopher A. French   Annual Review of Pathology-Mechanisms of Disease

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

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

MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L

(2011) Kathrin M. Bernt et al.   CANCER CELL

CARM1 Is an Important Determinant of ER -Dependent Breast Cancer Cell Differentiation and Proliferation in Breast Cancer Cells

(2011) M. Al-Dhaheri et al.   CANCER RESEARCH

MicroRNA-145 is regulated by DNA methylation and p53 gene mutation in prostate cancer

(2011) Seong O. Suh et al.   CARCINOGENESIS

Aberrations of EZH2 in Cancer

(2011) A. Chase et al.   CLINICAL CANCER RESEARCH

H3K9 methyltransferase G9a and the related molecule GLP

(2011) Y. Shinkai et al.   GENES & DEVELOPMENT

Regulated recruitment of tumor suppressor BRCA1 to the p21 gene by coactivator methylation

(2011) Y.-H. Lee et al.   GENES & DEVELOPMENT

The diverse functions of Dot1 and H3K79 methylation

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

Clinical significance of MicoRNA-155 expression in human breast cancer

(2011) Jian Chen et al.   JOURNAL OF SURGICAL ONCOLOGY

Anti-leukemia activity of chaetocin via death receptor-dependent apoptosis and dual modulation of the histone methyl-transferase SUV39H1

(2011) H Chaib et al.   LEUKEMIA

High expression of serum miR-21 and tumor miR-200c associated with poor prognosis in patients with lung cancer

(2011) Xiao-Guang Liu et al.   MEDICAL ONCOLOGY

A Coactivator Role of CARM1 in the Dysregulation of  -Catenin Activity in Colorectal Cancer Cell Growth and Gene Expression

(2011) C.-Y. Ou et al.   MOLECULAR CANCER RESEARCH

Systemic Delivery of Tumor Suppressor microRNA Mimics Using a Neutral Lipid Emulsion Inhibits Lung Tumors in Mice

(2011) Phong Trang et al.   MOLECULAR THERAPY

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

(2011) Masoud Vedadi et al.   Nature Chemical Biology

The microRNA miR-34a inhibits prostate cancer stem cells and metastasis by directly repressing CD44

(2011) Can Liu et al.   NATURE MEDICINE

DNA methylation-associated silencing of tumor-suppressor microRNAs in cancer

(2011) P Lopez-Serra et al.   ONCOGENE

Bromodomain protein Brd3 associates with acetylated GATA1 to promote its chromatin occupancy at erythroid target genes

(2011) J. M. Lamonica et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Epigenetic Regulation by Lysine Demethylase 5 (KDM5) Enzymes in Cancer

(2011) Lauren P. Blair et al.   Cancers

The Brustkrebs-Studien.de website for breast cancer patients: User acceptance of a German internet portal offering information on the disease and treatment options, and a clinical trials matching service

(2010) Markus Wallwiener et al.   BMC CANCER

Regulation of p53: TRIM24 enters the RING

(2010) Abhinav K. Jain et al.   CELL CYCLE

Epigenetics and cancer

(2010) Rajnee Kanwal et al.   JOURNAL OF APPLIED PHYSIOLOGY

G9a and Glp Methylate Lysine 373 in the Tumor Suppressor p53

(2010) Jing Huang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Epigenetic regulation of signaling pathways in cancer: Role of the histone methyltransferase EZH2

(2010) Daisy PF Tsang et al.   JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY

Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches

(2010) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2

(2010) Claudia Binda et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeting microRNAs in cancer: rationale, strategies and challenges

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

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

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

KAP1 Is Associated With Peritoneal Carcinomatosis in Gastric Cancer

(2009) Takeshi Yokoe et al.   ANNALS OF SURGICAL ONCOLOGY

Brd2disruption in mice causes severe obesity without Type 2 diabetes

(2009) Fangnian Wang et al.   BIOCHEMICAL JOURNAL

MicroRNA 29b functions in acute myeloid leukemia

(2009) R. Garzon et al.   BLOOD

Androgen-Induced Coactivator ANCCA Mediates Specific Androgen Receptor Signaling in Prostate Cancer

(2009) J. X. Zou et al.   CANCER RESEARCH

miR-34a as a prognostic marker of relapse in surgically resected non-small-cell lung cancer

(2009) Elena Gallardo et al.   CARCINOGENESIS

Lysine-specific demethylase 1 (LSD1) is highly expressed in ER-negative breast cancers and a biomarker predicting aggressive biology

(2009) Soyoung Lim et al.   CARCINOGENESIS

Therapeutic microRNA Delivery Suppresses Tumorigenesis in a Murine Liver Cancer Model

(2009) Janaiah Kota et al.   CELL

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

(2009) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

(2009) Yanqi Chang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Arginine methylation regulates the p53 response

(2008) Martin Jansson et al.   NATURE CELL BIOLOGY