Targeting epigenetic regulations in cancer

HDAC inhibitors still need a home run, despite recent approval

(2015) Malini Guha   NATURE REVIEWS DRUG DISCOVERY

The Bromodomain protein BRD4 controls HOTAIR, a long noncoding RNA essential for glioblastoma proliferation

(2015) Chiara Pastori et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

The SUV39H1 inhibitor chaetocin induces differentiation and shows synergistic cytotoxicity with other epigenetic drugs in acute myeloid leukemia cells

(2015) Y-S Lai et al.   Blood Cancer Journal

Epigenetic Modulation with HDAC Inhibitor CG200745 Induces Anti-Proliferation in Non-Small Cell Lung Cancer Cells

(2015) Sung-Min Chun et al.   PLoS One

Cancer epigenetics drug discovery and development: the challenge of hitting the mark

(2014) Robert M. Campbell et al.   JOURNAL OF CLINICAL INVESTIGATION

Comprehensive molecular characterization of urothelial bladder carcinoma

(2014)   NATURE

Inhibition of demethylases by GSK-J1/J4

(2014) Bo Heinemann et al.   NATURE

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

(2014) Irfan A. Asangani et al.   NATURE

Pharmacologic inhibition of histone demethylation as a therapy for pediatric brainstem glioma

(2014) Rintaro Hashizume et al.   NATURE MEDICINE

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

Driver mutations of cancer epigenomes

(2014) David M. Roy et al.   Protein & Cell

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

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

Histone-lysine methyltransferase EHMT2 is involved in proliferation, apoptosis, cell invasion, and DNA methylation of human neuroblastoma cells

(2013) Ziyan Lu et al.   ANTI-CANCER DRUGS

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

(2013) A. Chaidos et al.   BLOOD

Dynamic Readers for 5-(Hydroxy)Methylcytosine and Its Oxidized Derivatives

(2013) Cornelia G. Spruijt et al.   CELL

Jmjd3 Inhibits Reprogramming by Upregulating Expression of INK4a/Arf and Targeting PHF20 for Ubiquitination

(2013) Wei Zhao et al.   CELL

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

(2013) Michael Amatangelo et al.   CELL CYCLE

A Small Molecule Inhibitor of Polycomb Repressive Complex 1 Inhibits Ubiquitin Signaling at DNA Double-strand Breaks

(2013) Ismail Hassan Ismail et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Small-Molecule Ligands of Methyl-Lysine Binding Proteins: Optimization of Selectivity for L3MBTL3

(2013) Lindsey I. James et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chromatin proteins and modifications as drug targets

(2013) Kristian Helin et al.   NATURE

Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

(2013) Lindsey I James et al.   Nature Chemical Biology

Gene amplification of the histone methyltransferase SETDB1 contributes to human lung tumorigenesis

(2013) M Rodriguez-Paredes et al.   ONCOGENE

Rare insights into cancer biology

(2013) J Adam et al.   ONCOGENE

ERG Induces Epigenetic Activation of Tudor Domain-Containing Protein 1 (TDRD1) in ERG Rearrangement-Positive Prostate Cancer

(2013) Lukasz A. Kacprzyk 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

Inhibition of PRC2 Activity by a Gain-of-Function H3 Mutation Found in Pediatric Glioblastoma

(2013) P. W. Lewis et al.   SCIENCE

Targeting the JMJD2 Histone Demethylases to Epigenetically Control Herpesvirus Infection and Reactivation from Latency

(2013) Y. Liang et al.   Science Translational Medicine

Tudor: a versatile family of histone methylation ‘readers’

(2013) Rui Lu et al.   TRENDS IN BIOCHEMICAL SCIENCES

Thrombocytopenia induced by the histone deacetylase inhibitor abexinostat involves p53-dependent and -independent mechanisms

(2013) A Ali et al.   Cell Death & Disease

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

(2012) Yuan Yuan et al.   ACS Chemical Biology

The Histone Demethylase KDM1A Sustains the Oncogenic Potential of MLL-AF9 Leukemia Stem Cells

(2012) William J. Harris et al.   CANCER CELL

Driver mutations in histone H3.3 and chromatin remodelling genes in paediatric glioblastoma

(2012) Jeremy Schwartzentruber et al.   NATURE

The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

(2012) Jordi Barretina et al.   NATURE

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

(2012) Laurens Kruidenier et al.   NATURE

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

Prognostic Relevance of Integrated Genetic Profiling in Acute Myeloid Leukemia

(2012) Jay P. Patel et al.   NEW ENGLAND JOURNAL OF MEDICINE

Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

(2012) Wenyu Yu et al.   Nature Communications

Inhibitors of histone demethylases

(2011) Brian Lohse et al.   BIOORGANIC & MEDICINAL CHEMISTRY

TET2 Inactivation Results in Pleiotropic Hematopoietic Abnormalities in Mouse and Is a Recurrent Event during Human Lymphomagenesis

(2011) Cyril Quivoron et al.   CANCER CELL

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

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

Tet2 Loss Leads to Increased Hematopoietic Stem Cell Self-Renewal and Myeloid Transformation

(2011) Kelly Moran-Crusio et al.   CANCER CELL

TET Family Proteins and Their Role in Stem Cell Differentiation and Transformation

(2011) Luisa Cimmino et al.   Cell Stem Cell

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

(2011) Kai-Hsuan Chang et al.   ChemMedChem

Mechanisms and functions of Tet protein-mediated 5-methylcytosine oxidation

(2011) H. Wu et al.   GENES & DEVELOPMENT

A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-XL

(2011) Jung Jin Hwang et al.   INVESTIGATIONAL NEW DRUGS

5-Aza-2′-deoxycytidine Activates Iron Uptake and Heme Biosynthesis by Increasing c-Myc Nuclear Localization and Binding to the E-boxes of Transferrin Receptor 1 (TfR1) and Ferrochelatase (Fech) Genes

(2011) Bo Ning et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of (2E)-3-{2-Butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an Orally Active Histone Deacetylase Inhibitor with a Superior Preclinical Profile

(2011) Haishan Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

(2011) J. Martin Herold et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery

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

Mocetinostat for relapsed classical Hodgkin's lymphoma: an open-label, single-arm, phase 2 trial

(2011) Anas Younes et al.   LANCET 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

SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies

(2011) S Hart et al.   LEUKEMIA

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

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(2011) Antonio Furlan et al.   MOLECULAR MEDICINE

Inactivating mutations of acetyltransferase genes in B-cell lymphoma

(2011) Laura Pasqualucci et al.   NATURE

The Polycomb complex PRC2 and its mark in life

(2011) Raphaël Margueron et al.   NATURE

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

(2011) Mark A. Dawson et al.   NATURE

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

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Deciphering arginine methylation: Tudor tells the tale

(2011) Chen Chen et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Reversal of Histone Methylation: Biochemical and Molecular Mechanisms of Histone Demethylases

(2010) Nima Mosammaparast et al.   Annual Review of Biochemistry

The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells

(2010) Sonja Mandl-Weber et al.   BRITISH JOURNAL OF HAEMATOLOGY

Siah2-Dependent Concerted Activity of HIF and FoxA2 Regulates Formation of Neuroendocrine Phenotype and Neuroendocrine Prostate Tumors

(2010) Jianfei Qi et al.   CANCER CELL

CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase, Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity

(2010) Cheng-Jung Lai et al.   CANCER RESEARCH

Lestaurtinib, a multitargeted tyrosinse kinase inhibitor: from bench to bedside

(2010) Munira Shabbir et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

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

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

Histone Deacetylase Inhibitors in the Treatment of Hematological Malignancies and Solid Tumors

(2010) Mario Federico et al.   JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY

S110, a novel decitabine dinucleotide, increases fetal hemoglobin levels in baboons (P. anubis)

(2010) Donald Lavelle et al.   Journal of Translational Medicine

SB939, a Novel Potent and Orally Active Histone Deacetylase Inhibitor with High Tumor Exposure and Efficacy in Mouse Models of Colorectal Cancer

(2010) V. Novotny-Diermayr et al.   MOLECULAR CANCER THERAPEUTICS

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Chemical phylogenetics of histone deacetylases

(2010) James E Bradner et al.   Nature Chemical Biology

Somatic mutations of the histone methyltransferase gene EZH2 in myelodysplastic syndromes

(2010) Gorica Nikoloski et al.   NATURE GENETICS

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

The metazoan Mediator co-activator complex as an integrative hub for transcriptional regulation

(2010) Sohail Malik et al.   NATURE REVIEWS GENETICS

Safety and Efficacy of INCB018424, a JAK1 and JAK2 Inhibitor, in Myelofibrosis

(2010) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Comparison of Azacitidine and Decitabine Activities in Acute Myeloid Leukemia Cell Lines

(2010) Paul W. Hollenbach et al.   PLoS One

The Novel Deacetylase Inhibitor AR-42 Demonstrates Pre-Clinical Activity in B-Cell Malignancies In Vitro and In Vivo

(2010) David M. Lucas et al.   PLoS One

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

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

L3MBTL1 polycomb protein, a candidate tumor suppressor in del(20q12) myeloid disorders, is essential for genome stability

(2010) N. Gurvich et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Histone deacetylase (HDAC) inhibitors in recent clinical trials for cancer therapy

(2010) Julia M. Wagner et al.   Clinical Epigenetics

Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells

(2009) W. Fiskus et al.   BLOOD

Analysis of VHL Gene Alterations and their Relationship to Clinical Parameters in Sporadic Conventional Renal Cell Carcinoma

(2009) A. C. Young et al.   CLINICAL CANCER RESEARCH

Double bromodomain-containing gene Brd2 is essential for embryonic development in mouse

(2009) Enyuan Shang et al.   DEVELOPMENTAL DYNAMICS

Multicenter Study of Decitabine Administered Daily for 5 Days Every 4 Weeks to Adults With Myelodysplastic Syndromes: The Alternative Dosing for Outpatient Treatment (ADOPT) Trial

(2009) David P. Steensma et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II Multi-Institutional Trial of the Histone Deacetylase Inhibitor Romidepsin As Monotherapy for Patients With Cutaneous T-Cell Lymphoma

(2009) Richard L. Piekarz et al.   JOURNAL OF CLINICAL ONCOLOGY

DNA Methylation Predicts Survival and Response to Therapy in Patients With Myelodysplastic Syndromes

(2009) Lanlan Shen et al.   JOURNAL OF CLINICAL ONCOLOGY

Multicenter, Phase II Study of Decitabine for the First-Line Treatment of Older Patients With Acute Myeloid Leukemia

(2009) Amanda F. Cashen et al.   JOURNAL OF CLINICAL ONCOLOGY

Efficacy of azacitidine compared with that of conventional care regimens in the treatment of higher-risk myelodysplastic syndromes: a randomised, open-label, phase III study

(2009) Pierre Fenaux et al.   LANCET ONCOLOGY

Histone modifications at human enhancers reflect global cell-type-specific gene expression

(2009) Nathaniel D. Heintzman et al.   NATURE

Acquired mutations in TET2 are common in myelodysplastic syndromes

(2009) Saskia M C Langemeijer et al.   NATURE GENETICS

Mutation inTET2in Myeloid Cancers

(2009) François Delhommeau et al.   NEW ENGLAND JOURNAL OF MEDICINE

Lysine Acetylation Targets Protein Complexes and Co-Regulates Major Cellular Functions

(2009) C. Choudhary et al.   SCIENCE

Conversion of 5-Methylcytosine to 5-Hydroxymethylcytosine in Mammalian DNA by MLL Partner TET1

(2009) M. Tahiliani et al.   SCIENCE

The Nuclear DNA Base 5-Hydroxymethylcytosine Is Present in Purkinje Neurons and the Brain

(2009) S. Kriaucionis et al.   SCIENCE

Therapeutic potential of JAK2 inhibitors

(2009) S. Verstovsek   Hematology-American Society of Hematology Education Program

Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases⊥

(2008) Nathan R. Rose et al.   JOURNAL OF MEDICINAL CHEMISTRY

MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo

(2008) M. Fournel et al.   MOLECULAR CANCER THERAPEUTICS

Chemical probes for histone-modifying enzymes

(2008) Philip A Cole   Nature Chemical Biology