(Q38182138)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

title

Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands (English)

1 reference

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6 March 2020

4

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6 March 2020

author name string

Laura E Jennings

series ordinal

1

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

Angelina R Measures

series ordinal

2

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

Brian G Wilson

series ordinal

3

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

publication date

1 February 2014

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

Future Medicinal Chemistry

6 March 2020

published in

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

volume

6

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

issue

2

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

page(s)

179-204

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

Selective small molecules blocking HIV-1 Tat and coactivator PCAF association

6 March 2020

cites work

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Target structure-based discovery of small molecules that block human p53 and CREB binding protein association

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Suppression of inflammation by a synthetic histone mimic

21 January 2018

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Discovery and characterization of small molecule inhibitors of the BET family bromodomains

21 January 2018

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RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo

21 January 2018

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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).

21 January 2018

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Selective inhibition of BET bromodomains

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

21 January 2018

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Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery

21 January 2018

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Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides

21 January 2018

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3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

21 January 2018

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

21 January 2018

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

21 January 2018

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

21 January 2018

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Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain

21 January 2018

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Progress in the discovery of small-molecule inhibitors of bromodomain--histone interactions

21 January 2018

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Place your BETs: the therapeutic potential of bromodomains

21 January 2018

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Bromodomains: are readers right for epigenetic therapy?

21 January 2018

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Epigenetic protein families: a new frontier for drug discovery

21 January 2018

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Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions

21 January 2018

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Structural Basis for Acetylated Histone H4 Recognition by the Human BRD2 Bromodomain

21 January 2018

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

21 January 2018

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

21 January 2018

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Histone recognition and large-scale structural analysis of the human bromodomain family

21 January 2018

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Synthesis at the interface of chemistry and biology

21 January 2018

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

21 January 2018

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Structure and ligand of a histone acetyltransferase bromodomain

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.13.197

Structural basis of lysine-acetylated HIV-1 Tat recognition by PCAF bromodomain

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Structure-guided optimization of small molecules inhibiting human immunodeficiency virus 1 Tat association with the human coactivator p300/CREB binding protein-associated factor

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Target gene context influences the transcriptional requirement for the KAT3 family of CBP and p300 histone acetyltransferases.

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.13.197

Structural mechanism of the bromodomain of the coactivator CBP in p53 transcriptional activation

21 January 2018

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

21 January 2018

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Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

21 January 2018

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Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

21 January 2018

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Ligand efficiency: a useful metric for lead selection

21 January 2018

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PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

21 January 2018

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

21 January 2018

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Fragment screening to predict druggability (ligandability) and lead discovery success.

21 January 2018

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Efficacy and safety of a novel oral inducer of apolipoprotein a-I synthesis in statin-treated patients with stable coronary artery disease a randomized controlled trial

21 January 2018

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ApoA-I induction as a potential cardioprotective strategy: rationale for the SUSTAIN and ASSURE studies.

21 January 2018

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brahma: a regulator of Drosophila homeotic genes structurally related to the yeast transcriptional activator SNF2/SWI2

21 January 2018

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The bromodomain: a conserved sequence found in human, Drosophila and yeast proteins

21 January 2018

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The bromodomain: a chromatin-targeting module?

21 January 2018

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Small molecule bromodomain inhibitors: extending the druggable genome

21 January 2018

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

21 January 2018

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Targeting MYC dependence in cancer by inhibiting BET bromodomains

21 January 2018

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Inhibition of protein-protein interactions using designed molecules

21 January 2018

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Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites

21 January 2018

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Scaling the druggability landscape of human bromodomains, a new class of drug targets

21 January 2018

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Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains

21 January 2018

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The influence of drug-like concepts on decision-making in medicinal chemistry

21 January 2018

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Small-molecule inhibition of BRDT for male contraception

21 January 2018

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Targeting MYCN in neuroblastoma by BET bromodomain inhibition

21 January 2018

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Stability of nucleosomes containing homogenously ubiquitylated H2A and H2B prepared using semisynthesis

21 January 2018

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What an epigenome remembers

21 January 2018

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Bromodomain: an acetyl-lysine binding domain

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

The bromodomain interaction module

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Chromatin structure; oligomers of the histones

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Chromatin Structure: A Repeating Unit of Histones and DNA

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Crystal structure of the nucleosome core particle at 2.8 A resolution

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

ACETYLATION AND METHYLATION OF HISTONES AND THEIR POSSIBLE ROLE IN THE REGULATION OF RNA SYNTHESIS

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

The language of covalent histone modifications

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Signaling network model of chromatin

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Operating on chromatin, a colorful language where context matters

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Histone acetylation in chromatin structure and transcription

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Translating the Histone Code

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Global approaches to chromatin

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

The adjustable nucleosome: an epigenetic signaling module

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Perceptions of epigenetics

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Epigenetics: core misconcept

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Trial watch: phase II and phase III attrition rates 2011-2012.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Experiences in fragment-based drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Recent developments in fragment-based drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

A ‘Rule of Three’ for fragment-based lead discovery?

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Fragment-based approaches in drug discovery and chemical biology

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Fragment-based lead discovery grows up.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

MicroRNA therapeutics for cardiovascular disease: opportunities and obstacles.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

The therapeutic potential of acetyl-lysine and methyl-lysine effector domains

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.197

21 January 2018

Identifiers

DOI

10.4155/FMC.13.197

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24467243%20AND%20SRC:MED&resulttype=core&format=json

6 March 2020

1 reference