- Home
- Publications
- Publication Search
- Publication Details
Title
Potent and selective bivalent inhibitors of BET bromodomains
Authors
Keywords
-
Journal
Nature Chemical Biology
Volume 12, Issue 12, Pages 1097-1104
Publisher
Springer Nature
Online
2016-10-24
DOI
10.1038/nchembio.2210
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)
- (2016) Robert H. Bradbury et al. JOURNAL OF MEDICINAL CHEMISTRY
- Segmental Isotope Labelling of an Individual Bromodomain of a Tandem Domain BRD4 Using Sortase A
- (2016) Felix P. Williams et al. PLoS One
- NanoBRET—A Novel BRET Platform for the Analysis of Protein–Protein Interactions
- (2015) Thomas Machleidt et al. ACS Chemical Biology
- The promise and peril of chemical probes
- (2015) Cheryl H Arrowsmith et al. Nature Chemical Biology
- HISAT: a fast spliced aligner with low memory requirements
- (2015) Daehwan Kim et al. NATURE METHODS
- Target engagement and drug residence time can be observed in living cells with BRET
- (2015) Matthew B. Robers et al. Nature Communications
- Advanced ensemble modelling of flexible macromolecules using X-ray solution scattering
- (2015) Giancarlo Tria et al. IUCrJ
- Abstract 5475: Interrogation of NCI-60 patterns of growth inhibition in conjunction with investigational oncology agents kinase profiling for the elucidation of mechanistic targets
- (2015) Joel Morris et al. CANCER RESEARCH
- Abstract 4238: BROMOscan- a high throughput, quantitative ligand binding platform identifies best-in-class bromodomain inhibitors from a screen of mature compounds targeting other protein classes.
- (2014) Elizabeth Quinn et al. CANCER RESEARCH
- 5LBA Results of a first-in-man phase I trial assessing OTX015, an orally available BET-bromodomain (BRD) inhibitor, in advanced hematologic malignancies
- (2014) A. Stathis et al. EUROPEAN JOURNAL OF CANCER
- Abstract A102: NCI-60 response profiles of >400 investigational oncology agents: A resource enabling drug and biomarker discovery.
- (2014) J. Morris et al. MOLECULAR CANCER THERAPEUTICS
- Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer
- (2014) Irfan A. Asangani et al. NATURE
- 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
- Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer
- (2013) Robert H. Bradbury et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers
- (2013) Jakob Lovén et al. CELL
- Master Transcription Factors and Mediator Establish Super-Enhancers at Key Cell Identity Genes
- (2013) Warren A. Whyte et al. CELL
- Super-Enhancers in the Control of Cell Identity and Disease
- (2013) Denes Hnisz et al. CELL
- The machinery of macroautophagy
- (2013) Yuchen Feng et al. CELL RESEARCH
- Nmrglue: an open source Python package for the analysis of multidimensional NMR data
- (2013) Jonathan J. Helmus et al. JOURNAL OF BIOMOLECULAR NMR
- 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
- Upgraded ESRF BM29 beamline for SAXS on macromolecules in solution
- (2013) Petra Pernot et al. JOURNAL OF SYNCHROTRON RADIATION
- AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function In Vitro and In Vivo
- (2013) S. A. Loddick et al. MOLECULAR CANCER THERAPEUTICS
- Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites
- (2012) Lewis R. Vidler et al. JOURNAL OF MEDICINAL CHEMISTRY
- Automated acquisition and analysis of small angle X-ray scattering data
- (2012) Daniel Franke et al. NUCLEAR INSTRUMENTS & METHODS IN PHYSICS RESEARCH SECTION A-ACCELERATORS SPECTROMETERS DETECTORS AND ASSOCIATED EQUIPMENT
- Place your BETs: the therapeutic potential of bromodomains
- (2012) R.K. Prinjha et al. TRENDS IN PHARMACOLOGICAL SCIENCES
- Prediction of Hydrodynamic and Other Solution Properties of Rigid Proteins from Atomic- and Residue-Level Models
- (2011) A. Ortega et al. BIOPHYSICAL JOURNAL
- Recognition of a Mononucleosomal Histone Modification Pattern by BPTF via Multivalent Interactions
- (2011) Alexander J. Ruthenburg et al. CELL
- BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc
- (2011) Jake E. Delmore et al. CELL
- Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
- (2011) Mark A. Dawson et al. NATURE
- XDS
- (2010) Wolfgang Kabsch ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY
- Features and development ofCoot
- (2010) P. Emsley et al. ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY
- A combined spectroscopic and crystallographic approach to probing drug–human serum albumin interactions
- (2010) David Buttar et al. BIOORGANIC & MEDICINAL CHEMISTRY
- Structural characterization of proteins and complexes using small-angle X-ray solution scattering
- (2010) Haydyn D.T. Mertens et al. JOURNAL OF STRUCTURAL BIOLOGY
- 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
- Histone H3K27ac separates active from poised enhancers and predicts developmental state
- (2010) M. P. Creyghton et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Structures of the Dual Bromodomains of the P-TEFb-activating Protein Brd4 at Atomic Resolution
- (2009) Friederike Vollmuth et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Cooperative binding of two acetylation marks on a histone tail by a single bromodomain
- (2009) Jeanne Morinière et al. NATURE
- Modern analytical ultracentrifugation in protein science: A tutorial review
- (2002) Jacob Lebowitz et al. PROTEIN SCIENCE
Publish scientific posters with Peeref
Peeref publishes scientific posters from all research disciplines. Our Diamond Open Access policy means free access to content and no publication fees for authors.
Learn MoreAsk a Question. Answer a Question.
Quickly pose questions to the entire community. Debate answers and get clarity on the most important issues facing researchers.
Get Started