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The bromodomain: from epigenome reader to druggable target
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title
The bromodomain: from epigenome reader to druggable target
(English)
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author name string
Roberto Sanchez
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1
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Jamel Meslamani
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2
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Ming-Ming Zhou
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3
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language of work or name
English
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PubMed
publication date
August 2014
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PubMed
published in
Biochimica et Biophysica Acta
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PubMed
volume
1839
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stated in
PubMed
page(s)
676-85
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stated in
PubMed
issue
8
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PubMed
cites work
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Down-regulation of NF-κB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition
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21 March 2017
Histone recognition and large-scale structural analysis of the human bromodomain family
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21 March 2017
Identification of 67 histone marks and histone lysine crotonylation as a new type of histone modification
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21 March 2017
Selective inhibition of BET bromodomains
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21 March 2017
Structural implications for K5/K12-di-acetylated histone H4 recognition by the second bromodomain of BRD2
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Regulation of cellular metabolism by protein lysine acetylation
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21 March 2017
The role of human bromodomains in chromatin biology and gene transcription
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21 March 2017
Structural insights into human KAP1 PHD finger-bromodomain and its role in gene silencing
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21 March 2017
PHD domain-mediated E3 ligase activity directs intramolecular sumoylation of an adjacent bromodomain required for gene silencing
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PubMed Central
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21 March 2017
ACETYLATION AND METHYLATION OF HISTONES AND THEIR POSSIBLE ROLE IN THE REGULATION OF RNA SYNTHESIS
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21 March 2017
Translating the Histone Code
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21 March 2017
The structural basis for the recognition of acetylated histone H4 by the bromodomain of histone acetyltransferase gcn5p
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21 March 2017
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21 March 2017
Structure and ligand of a histone acetyltransferase bromodomain
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21 March 2017
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors
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21 March 2017
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
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21 March 2017
Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors
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21 March 2017
The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains
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21 March 2017
Structural Insights into Acetylated-Histone H4 Recognition by the Bromodomain-PHD Finger Module of Human Transcriptional Coactivator CBP
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21 March 2017
Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
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21 March 2017
4-Acyl pyrroles: mimicking acetylated lysines in histone code reading
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21 March 2017
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
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21 March 2017
Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains
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21 March 2017
Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening
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21 March 2017
Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains
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21 March 2017
Naphthyridines as novel BET family bromodomain inhibitors
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21 March 2017
Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain
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21 March 2017
Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands
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21 March 2017
Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
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21 March 2017
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)
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21 March 2017
A Poised Chromatin Platform for TGF-β Access to Master Regulators
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21 March 2017
Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides
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21 March 2017
Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery
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21 March 2017
Discovery and characterization of small molecule inhibitors of the BET family bromodomains
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21 March 2017
A Small Molecule Binding to the Coactivator CREB-Binding Protein Blocks Apoptosis in Cardiomyocytes
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21 March 2017
Suppression of inflammation by a synthetic histone mimic
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21 March 2017
Structural insights into selective histone H3 recognition by the human Polybromo bromodomain 2
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21 March 2017
Structural Basis for Acetylated Histone H4 Recognition by the Human BRD2 Bromodomain
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21 March 2017
Cooperative binding of two acetylation marks on a histone tail by a single bromodomain
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21 March 2017
Structural Basis of Site-Specific Histone Recognition by the Bromodomains of Human Coactivators PCAF and CBP/p300
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21 March 2017
Autoregulation of the Rsc4 Tandem Bromodomain by Gcn5 Acetylation
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21 March 2017
Structural mechanism of the bromodomain of the coactivator CBP in p53 transcriptional activation
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21 March 2017
Structure and function of a human TAFII250 double bromodomain module
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21 March 2017
Lysine acetylation targets protein complexes and co-regulates major cellular functions
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21 March 2017
Chromatin modifications and their function
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21 March 2017
Cellular memory and the histone code
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21 March 2017
Bromodomain: an acetyl-lysine binding domain
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21 March 2017
BET bromodomain inhibition as a therapeutic strategy to target c-Myc
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21 March 2017
Structural basis and specificity of acetylated transcription factor GATA1 recognition by BET family bromodomain protein Brd3
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21 March 2017
A PHD finger of NURF couples histone H3 lysine 4 trimethylation with chromatin remodelling
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21 March 2017
Bromodomain protein Brd4 plays a key role in Merkel cell polyomavirus DNA replication
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21 March 2017
Epigenetic protein families: a new frontier for drug discovery
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7 April 2017
Targeting MYC dependence in cancer by inhibiting BET bromodomains
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7 April 2017
UniProt Knowledgebase: a hub of integrated protein data
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7 April 2017
Histone modifications in transcriptional regulation
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7 April 2017
Acetylation: a regulatory modification to rival phosphorylation?
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7 April 2017
ChEpiMod: a knowledgebase for chemical modulators of epigenome reader domains
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28 September 2017
ChromoHub V2: cancer genomics
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28 September 2017
[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains
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28 September 2017
BET bromodomain inhibition of MYC-amplified medulloblastoma.
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28 September 2017
Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer
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28 September 2017
BET bromodomain protein inhibition is a therapeutic option for medulloblastoma.
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28 September 2017
Bromodomain and extraterminal (BET) protein inhibition suppresses human T cell leukemia virus 1 (HTLV-1) Tax protein-mediated tumorigenesis by inhibiting nuclear factor κB (NF-κB) signaling
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28 September 2017
BET bromodomain inhibition suppresses TH17-mediated pathology
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28 September 2017
Cancer-associated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition
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28 September 2017
Bromo- and extraterminal domain chromatin regulators serve as cofactors for murine leukemia virus integration
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28 September 2017
Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer
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28 September 2017
BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms
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28 September 2017
BET bromodomains mediate transcriptional pause release in heart failure
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PubMed Central
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28 September 2017
BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia.
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PubMed Central
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28 September 2017
Identification of a novel BET bromodomain inhibitor-sensitive, gene regulatory circuit that controls Rituximab response and tumour growth in aggressive lymphoid cancers.
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28 September 2017
BET proteins promote efficient murine leukemia virus integration at transcription start sites
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28 September 2017
Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors
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28 September 2017
PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains
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28 September 2017
Bromodomains as therapeutic targets in cancer
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retrieved
28 September 2017
Targeting MYCN in neuroblastoma by BET bromodomain inhibition
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Inhibition of BET bromodomain targets genetically diverse glioblastoma
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
BET bromodomain inhibition rescues erythropoietin differentiation of human erythroleukemia cell line UT7.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Reactivation of latent HIV-1 by inhibition of BRD4.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Scaling the druggability landscape of human bromodomains, a new class of drug targets
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Contraception for men: a breakthrough new approach
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
BET bromodomain inhibition as a novel strategy for reactivation of HIV-1
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
ChromoHub: a data hub for navigators of chromatin-mediated signalling
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
The bromodomain interaction module
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Lysine acetylation: enzymes, bromodomains and links to different diseases
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Place your BETs: the therapeutic potential of bromodomains
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Bromodomains as therapeutic targets
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Rational design of cyclic peptide modulators of the transcriptional coactivator CBP: a new class of p53 inhibitors
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Domain mobility in proteins: functional and evolutionary implications
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Evolution of protein domain promiscuity in eukaryotes
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Structure and acetyl-lysine recognition of the bromodomain
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Histone modifications: signalling receptors and potential elements of a heritable epigenetic code
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Target structure-based discovery of small molecules that block human p53 and CREB binding protein association
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Histone arginine methylation and its dynamic regulation
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Selective small molecules blocking HIV-1 Tat and coactivator PCAF association
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Histone acetylation and chromatin remodeling: which comes first?
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 September 2017
Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
31 May 2018
Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosis
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
31 May 2018
BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
31 May 2018
Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
31 May 2018
Histone acetylation as an epigenetic determinant of long-term transcriptional competence
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
31 May 2018
Reading signals on the nucleosome with a new nomenclature for modified histones
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 November 2018
The bromodomain revisited.
1 reference
stated in
PubMed Central
reference URL
https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4099289
retrieved
28 November 2018
Identifiers
DOI
10.1016/J.BBAGRM.2014.03.011
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
1304342
OpenCitations bibliographic resource ID
1304342
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
1304342
PMCID
4099289
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
1304342
PubMed ID
24686119
1 reference
stated in
Consolidated OpenCitations Corpus – April 2017
OpenCitations bibliographic resource ID
1304342
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