Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

(2020) Emily J. Faivre et al.   NATURE

An Evolutionarily Conserved Function of Polycomb Silences the MHC Class I Antigen Presentation Pathway and Enables Immune Evasion in Cancer

(2019) Marian L. Burr et al.   CANCER CELL

Phase Ib Trial With Birabresib, a Small-Molecule Inhibitor of Bromodomain and Extraterminal Proteins, in Patients With Selected Advanced Solid Tumors

(2018) Jeremy Lewin et al.   JOURNAL OF CLINICAL ONCOLOGY

SLAM-seq defines direct gene-regulatory functions of the BRD4-MYC axis

(2018) Matthias Muhar et al.   SCIENCE

Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

(2018) Kristin M. Riching et al.   ACS Chemical Biology

BET Inhibition Improves NASH and Liver Fibrosis

(2018) Sarah A. Middleton et al.   Scientific Reports

The cancer epigenome: Concepts, challenges, and therapeutic opportunities

(2017) Mark A. Dawson   SCIENCE

Click chemistry enables preclinical evaluation of targeted epigenetic therapies

(2017) Dean S. Tyler et al.   SCIENCE

BET bromodomain inhibition suppresses innate inflammatory and profibrotic transcriptional networks in heart failure

(2017) Qiming Duan et al.   Science Translational Medicine

Thermal profiling reveals phenylalanine hydroxylase as an off-target of panobinostat

(2016) Isabelle Becher et al.   Nature Chemical Biology

Epigenetic drug discovery: breaking through the immune barrier

(2016) David F. Tough et al.   NATURE REVIEWS DRUG DISCOVERY

A bromodomain–DNA interaction facilitates acetylation-dependent bivalent nucleosome recognition by the BET protein BRDT

(2016) Thomas C. R. Miller et al.   Nature Communications

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

(2016) Céline Berthon et al.   Lancet Haematology

Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

(2016) Sandy Amorim et al.   Lancet Haematology

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

Apremilast for Behçet’s Syndrome — A Phase 2, Placebo-Controlled Study

(2015) Gulen Hatemi et al.   NEW ENGLAND JOURNAL OF MEDICINE

Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation

(2015) Ahmed Nadeem et al.   PHARMACOLOGICAL RESEARCH

The bromodomain protein inhibitor I-BET151 suppresses expression of inflammatory genes and matrix degrading enzymes in rheumatoid arthritis synovial fibroblasts

(2014) Kerstin Klein et al.   ANNALS OF THE RHEUMATIC DISEASES

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

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

A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

(2014) M. G. J. Baud et al.   SCIENCE

Role of SWI/SNF in acute leukemia maintenance and enhancer-mediated Myc regulation

(2013) J. Shi et al.   GENES & DEVELOPMENT

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

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

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

Data processing and analysis with theautoPROCtoolbox

(2011) Clemens Vonrhein et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Overview of theCCP4 suite and current developments

(2011) Martyn D. Winn et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

(2011) Jake E. Delmore et al.   CELL

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

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

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

The Identification of Markers of Macrophage Differentiation in PMA-Stimulated THP-1 Cells and Monocyte-Derived Macrophages

(2010) Marc Daigneault et al.   PLoS One

Brd2disruption in mice causes severe obesity without Type 2 diabetes

(2009) Fangnian Wang et al.   BIOCHEMICAL JOURNAL

Imiquimod-Induced Psoriasis-Like Skin Inflammation in Mice Is Mediated via the IL-23/IL-17 Axis

(2009) L. van der Fits et al.   JOURNAL OF IMMUNOLOGY

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

(2009) Jeanne Morinière et al.   NATURE