Evidence map›Paper›PMID 39274873›Full record

ArticleMolecules (Basel, Switzerland)2024

Identification of Novel Bromodomain-Containing Protein 4 (BRD4) Binders through 3D Pharmacophore-Based Repositioning Screening Campaign.

Ester Colarusso, Erica Gazzillo, Eleonora Boccia, Stefania Terracciano, Ines Bruno, Giuseppe Bifulco, Maria Giovanna Chini, Gianluigi Lauro

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Ester ColarussoDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.ORCID 0000-0002-4193-1659
Erica GazzilloDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.
Eleonora BocciaDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.
Stefania TerraccianoDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.
Ines BrunoDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.
Giuseppe BifulcoDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.
Maria Giovanna ChiniDepartment of Biosciences and Territory, University of Molise, Contrada Fonte Lappone, 86090 Pesche, Italy.
Gianluigi LauroDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, Italy.ORCID 0000-0001-5065-9717

Funding

Italian Association for Cancer Research MFAG 2017 - ID. 20160 project
6 · The paper itself

Abstract

A 3D structure-based pharmacophore model built for bromodomain-containing protein 4 (BRD4) is reported here, specifically developed for investigating and identifying the key structural features of the (+)-JQ1 known inhibitor within the BRD4 binding site. Using this pharmacophore model, 273 synthesized and purchased compounds previously considered for other targets but yielding poor results were screened in a drug repositioning campaign. Subsequently, only six compounds showed potential as BRD4 binders and were subjected to further biophysical and biochemical assays. Compounds

Indexed as

Cell Cycle ProteinsTranscription FactorsAzepinesBinding SitesBromodomain Containing ProteinsDrug Evaluation, PreclinicalDrug RepositioningHumansLigandsModels, MolecularMolecular Docking SimulationNuclear ProteinsPharmacophoreProtein BindingStructure-Activity RelationshipTriazolesAzepinesBRD3 protein, humanBRD4 protein, humanBRD9 protein, humanBromodomain Containing ProteinsCell Cycle Proteins(+)-JQ1 compoundLigandsNuclear ProteinsTranscription FactorsTriazolesanticancer agentsbromodomainchemical synthesiscomputational techniquesdrug discoverydrug repositioning

Identifiers

PMID39274873
PMCPMC11397543

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.