Targeting bromodomains: epigenetic readers of lysine acetylation

Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML)

(2015) Harald Herrmann et al.   Oncotarget

Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.

(2015) Anastasia Wyce et al.   Oncotarget

BET bromodomain protein inhibition is a therapeutic option for medulloblastoma

(2015) Anton George Henssen et al.   Oncotarget

c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells

(2014) J. E. Roderick et al.   BLOOD

BET bromodomain proteins are required for glioblastoma cell proliferation

(2014) Chiara Pastori et al.   Epigenetics

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

(2014) Pietro Ciceri et al.   Nature Chemical Biology

RVX-208, an Inducer of ApoA-I in Humans, Is a BET Bromodomain Antagonist

(2014) Kevin G. McLure et al.   PLoS One

The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains

(2013) Antje Dittmann et al.   ACS Chemical Biology

Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

(2013) Mathew P. Martin et al.   ACS Chemical Biology

4-Acyl Pyrroles: Mimicking Acetylated Lysines in Histone Code Reading

(2013) Xavier Lucas et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2013) A. Chaidos et al.   BLOOD

Discovery and Characterization of Super-Enhancer-Associated Dependencies in Diffuse Large B Cell Lymphoma

(2013) Bjoern Chapuy et al.   CANCER CELL

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

(2013) S. Picaud et al.   CANCER RESEARCH

BRD4 Sustains Melanoma Proliferation and Represents a New Target for Epigenetic Therapy

(2013) M. F. Segura et al.   CANCER RESEARCH

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure

(2013) Priti Anand et al.   CELL

BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism

(2013) Daniela Boehm et al.   CELL CYCLE

Naphthyridines as Novel BET Family Bromodomain Inhibitors

(2013) Olivier Mirguet et al.   ChemMedChem

Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma

(2013) Z. Cheng et al.   CLINICAL CANCER RESEARCH

Identification of a novel BET bromodomain inhibitor-sensitive, gene regulatory circuit that controls Rituximab response and tumour growth in aggressive lymphoid cancers

(2013) Anouk Emadali et al.   EMBO Molecular Medicine

In vitro biosynthesis, isolation, and identification of predominant metabolites of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one (RVX-208)

(2013) Yuri L. Khmelnitsky et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

BET bromodomain inhibition suppresses TH17-mediated pathology

(2013) Deanna A. Mele et al.   JOURNAL OF EXPERIMENTAL MEDICINE

BET Protein Function Is Required for Inflammation: Brd2 Genetic Disruption and BET Inhibitor JQ1 Impair Mouse Macrophage Inflammatory Responses

(2013) A. C. Belkina et al.   JOURNAL OF IMMUNOLOGY

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

(2013) Olivier Mirguet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Drug Discovery of 2-Thiazolidinones as Inhibitors of the Histone Reader BRD4 Bromodomain

(2013) Lele Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

(2013) Fleur M. Ferguson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

(2013) Lewis R. Vidler et al.   JOURNAL OF MEDICINAL CHEMISTRY

[1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains

(2013) Oleg Fedorov et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

(2013) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains

(2013) Guangtao Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bromo- and Extraterminal Domain Chromatin Regulators Serve as Cofactors for Murine Leukemia Virus Integration

(2013) Saumya Shree Gupta et al.   JOURNAL OF VIROLOGY

Recruitment of Brd4 to the Human Papillomavirus Type 16 DNA Replication Complex Is Essential for Replication of Viral DNA

(2013) X. Wang et al.   JOURNAL OF VIROLOGY

BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms

(2013) B S Wyspiańska et al.   LEUKEMIA

Regulation of NO Synthesis, Local Inflammation, and Innate Immunity to Pathogens by BET Family Proteins

(2013) S. Wienerroither et al.   MOLECULAR AND CELLULAR BIOLOGY

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

(2013) Anastasia Wyce et al.   PLoS One

BET proteins promote efficient murine leukemia virus integration at transcription start sites

(2013) A. Sharma et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

(2013) S. Picaud et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

(2013) Victor S. Gehling et al.   ACS Medicinal Chemistry Letters

BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia

(2013) D Da Costa et al.   Blood Cancer Journal

Targeting MYCN in Neuroblastoma by BET Bromodomain Inhibition

(2013) Alexandre Puissant et al.   Cancer Discovery

BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1

(2013) Helen Jayne Susan Stewart et al.   Cancer Medicine

Brd2 is required for cell cycle exit and neuronal differentiation through the E2F1 pathway in mouse neuroepithelial cells

(2012) Mami Tsume et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

ChromoHub: a data hub for navigators of chromatin-mediated signalling

(2012) L. Liu et al.   BIOINFORMATICS

From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151

(2012) Olivier Mirguet et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)

(2012) Jonathan Seal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia

(2012) C. J. Ott et al.   BLOOD

ApoA-I Induction as a Potential Cardioprotective Strategy: Rationale for the SUSTAIN and ASSURE Studies

(2012) Stephen J. Nicholls et al.   CARDIOVASCULAR DRUGS AND THERAPY

Small-Molecule Inhibition of BRDT for Male Contraception

(2012) Martin M. Matzuk et al.   CELL

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

(2012) Panagis Filippakopoulos et al.   CELL

Bromodomain-dependent stage-specific male genome programming by Brdt

(2012) Jonathan Gaucher et al.   EMBO JOURNAL

Histone Deacetylases Activate Hepatocyte Growth Factor Signaling by Repressing MicroRNA-449 in Hepatocellular Carcinoma Cells

(2012) Reena Buurman et al.   GASTROENTEROLOGY

Bromodomain-containing Protein 4 (BRD4) Regulates RNA Polymerase II Serine 2 Phosphorylation in Human CD4+ T Cells

(2012) Weishi Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Down-regulation of NF-κB Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition

(2012) Guangtao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

(2012) Paul V. Fish et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone deacetylases and cancer

(2012) Bruna Barneda-Zahonero et al.   Molecular Oncology

The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation

(2012) Zichong Li et al.   NUCLEIC ACIDS RESEARCH

Novel HDL-based therapeutic agents

(2012) Tisha R. Joy   PHARMACOLOGY & THERAPEUTICS

Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors

(2012) H. S. Bandukwala et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

BRD4 is an atypical kinase that phosphorylates Serine2 of the RNA Polymerase II carboxy-terminal domain

(2012) B. N. Devaiah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Place your BETs: the therapeutic potential of bromodomains

(2012) R.K. Prinjha et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

(2012) Duncan Hay et al.   MedChemComm

Bromodomain Protein Brd4 Plays a Key Role in Merkel Cell Polyomavirus DNA Replication

(2012) Xin Wang et al.   PLoS Pathogens

Pathogenesis of NUT Midline Carcinoma

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

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

(2011) Panagis Filippakopoulos et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Differentiation of NUT Midline Carcinoma by Epigenomic Reprogramming

(2011) B. E. Schwartz et al.   CANCER RESEARCH

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

(2011) Jake E. Delmore et al.   CELL

Real-Time Imaging of Histone H4K12–Specific Acetylation Determines the Modes of Action of Histone Deacetylase and Bromodomain Inhibitors

(2011) Tamaki Ito et al.   CHEMISTRY & BIOLOGY

A Small Molecule Binding to the Coactivator CREB-Binding Protein Blocks Apoptosis in Cardiomyocytes

(2011) Jagat C. Borah et al.   CHEMISTRY & BIOLOGY

The first bromodomain of the testis-specific double bromodomain protein Brdt is required for chromocenter organization that is modulated by genetic background

(2011) Binyamin D. Berkovits et al.   DEVELOPMENTAL BIOLOGY

Bromodomains as therapeutic targets

(2011) Susanne Muller et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

Rational therapeutic combinations with histone deacetylase inhibitors for the treatment of cancer

(2011) K Ted Thurn et al.   Future Oncology

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

(2011) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2011) Chun-wa Chung 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

Fragment-Based Discovery of Bromodomain Inhibitors Part 2: Optimization of Phenylisoxazole Sulfonamides

(2011) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis and Specificity of Acetylated Transcription Factor GATA1 Recognition by BET Family Bromodomain Protein Brd3

(2011) R. Gamsjaeger et al.   MOLECULAR AND CELLULAR BIOLOGY

Inactivating mutations of acetyltransferase genes in B-cell lymphoma

(2011) Laura Pasqualucci et al.   NATURE

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

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

(2011) Mark A. Dawson et al.   NATURE

ChEMBL: a large-scale bioactivity database for drug discovery

(2011) A. Gaulton et al.   NUCLEIC ACIDS RESEARCH

Targeting MYC dependence in cancer by inhibiting BET bromodomains

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

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

Oncogenesis by sequestration of CBP/p300 in transcriptionally inactive hyperacetylated chromatin domains

(2010) Nicolas Reynoird et al.   EMBO JOURNAL

Mixed lineage leukemia: histone H3 lysine 4 methyltransferases from yeast to human

(2010) Shivani Malik et al.   FEBS Journal

RVX-208

(2010) Dana Bailey et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Regulation of Cellular Metabolism by Protein Lysine Acetylation

(2010) S. Zhao et al.   SCIENCE

The molecular biology of HIV latency: breaking and restoring the Tat-dependent transcriptional circuit

(2010) Jonathan Karn   Current Opinion in HIV and AIDS

Brd2disruption in mice causes severe obesity without Type 2 diabetes

(2009) Fangnian Wang et al.   BIOCHEMICAL JOURNAL

Control of Inducible Gene Expression by Signal-Dependent Transcriptional Elongation

(2009) Diana C. Hargreaves et al.   CELL

Management of Prolonged Seizures and Status Epilepticus in Childhood: A Systematic Review

(2009) Kalliopi Sofou et al.   JOURNAL OF CHILD NEUROLOGY

Abrogation of the Brd4-Positive Transcription Elongation Factor b Complex by Papillomavirus E2 Protein Contributes to Viral Oncogene Repression

(2009) J. Yan et al.   JOURNAL OF VIROLOGY

Catalytic activity of the proteasome fine-tunes Brg1-mediated chromatin remodeling to regulate the expression of inflammatory genes

(2009) Sarah J. Cullen et al.   MOLECULAR IMMUNOLOGY

Cooperative binding of two acetylation marks on a histone tail by a single bromodomain

(2009) Jeanne Morinière et al.   NATURE

Specific interaction between genotype, smoking and autoimmunity to citrullinated α-enolase in the etiology of rheumatoid arthritis

(2009) Hiba Mahdi et al.   NATURE GENETICS

Real-time imaging of histone H4 hyperacetylation in living cells

(2009) K. Sasaki et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2009) C. Choudhary et al.   SCIENCE

The Challenge of Finding a Cure for HIV Infection

(2009) D. D. Richman et al.   SCIENCE

Roles of the histone acetyltransferase monocytic leukemia zinc finger protein in normal and malignant hematopoiesis

(2008) Takuo Katsumoto et al.   CANCER SCIENCE

The multi-tasking P-TEFb complex

(2008) Vanessa Brès et al.   CURRENT OPINION IN CELL BIOLOGY

A complex t(1;22;11)(q44;q13;q23) translocation causingMLL-p300fusion gene in therapy-related acute myeloid leukemia

(2008) Hiroaki Ohnishi et al.   EUROPEAN JOURNAL OF HAEMATOLOGY

Demystified molecular pathology of NUT midline carcinomas

(2008) C. A. French   JOURNAL OF CLINICAL PATHOLOGY

Incidence and diversity of PAX5 fusion genes in childhood acute lymphoblastic leukemia

(2008) K Nebral et al.   LEUKEMIA

Brd4 Coactivates Transcriptional Activation of NF- B via Specific Binding to Acetylated RelA

(2008) B. Huang et al.   MOLECULAR AND CELLULAR BIOLOGY

Therapeutic application of histone deacetylase inhibitors for central nervous system disorders

(2008) Aleksey G. Kazantsev et al.   NATURE REVIEWS DRUG DISCOVERY