Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

(2017) Bing Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural basis of PROTAC cooperative recognition for selective protein degradation

(2017) Morgan S Gadd et al.   Nature Chemical Biology

BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice

(2017) Kalung Cheung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Chemical genetics approaches for selective intervention in epigenetics

(2016) Andrew C Runcie et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Clinical progress and pharmacology of small molecule bromodomain inhibitors

(2016) Natalie H Theodoulou et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology

(2016) Carles Galdeano et al.   Future Medicinal Chemistry

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins

(2016) Brigitt Raux et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

(2016) Brian K. Albrecht et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and characterization of bivalent BET inhibitors

(2016) Minoru Tanaka et al.   Nature Chemical Biology

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

(2016) Paul Bamborough et al.   ACS Medicinal Chemistry Letters

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

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

Clinical Response of Carcinomas Harboring the BRD4-NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628

(2016) A. Stathis et al.   Cancer Discovery

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

BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell

(2016) Jude T. Deeney et al.   PLoS One

The Bromodomain: A New Target in Emerging Epigenetic Medicine

(2015) Steven G. Smith et al.   ACS Chemical Biology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors

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

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition

(2015) Matthias G. J. Baud 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

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

Allele-Specific Chemical Genetics: Concept, Strategies, and Applications

(2014) Kabirul Islam   ACS Chemical Biology

Disrupting the Interaction of BRD4 with Diacetylated Twist Suppresses Tumorigenesis in Basal-like Breast Cancer

(2014) Jian Shi et al.   CANCER CELL

Selective Chemical Modulation of Gene Transcription Favors Oligodendrocyte Lineage Progression

(2014) Mar Gacias et al.   CHEMISTRY & BIOLOGY

“Minimalist” Cyclopropene-Containing Photo-Cross-Linkers Suitable for Live-Cell Imaging and Affinity-Based Protein Labeling

(2014) Zhengqiu Li et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

CRISPR-Cas systems for editing, regulating and targeting genomes

(2014) Jeffry D Sander et al.   NATURE BIOTECHNOLOGY

Accelerated chromatin biochemistry using DNA-barcoded nucleosome libraries

(2014) Uyen T T Nguyen et al.   NATURE METHODS

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

(2014) M. G. J. Baud et al.   SCIENCE

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching

(2014) Martin Philpott et al.   Epigenetics & Chromatin

Inducible In Vivo Silencing of Brd4 Identifies Potential Toxicities of Sustained BET Protein Inhibition

(2014) Jessica E. Bolden et al.   Cell Reports

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

Genome-wide localization of small molecules

(2013) Lars Anders et al.   NATURE BIOTECHNOLOGY

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA

(2013) Z Zou et al.   ONCOGENE

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 of BET bromodomain inhibitors and their role in target validation

(2013) S. Müller et al.   MedChemComm

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

(2012) Panagis Filippakopoulos et al.   CELL

Profiling Genome-Wide Chromatin Methylation with Engineered Posttranslation Apparatus within Living Cells

(2012) Rui Wang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2011) Jake E. Delmore et al.   CELL

Two-pronged Binding with Bromodomain-containing Protein 4 Liberates Positive Transcription Elongation Factor b from Inactive Ribonucleoprotein Complexes

(2011) Sebastian Schröder et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Efficacy and Safety of a Novel Oral Inducer of Apolipoprotein A-I Synthesis in Statin-Treated Patients With Stable Coronary Artery Disease

(2011) Stephen J. Nicholls et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

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

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

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

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

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