Evidence map›Paper›PMID 30125504›Full record

ArticleJournal of medicinal chemistry2018

Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.

Shuai Liu, Hailemichael O Yosief, Lingling Dai, He Huang, Gagan Dhawan, Xiaofeng Zhang, Alex M Muthengi, Justin Roberts, Dennis L Buckley, Jennifer A Perry and 4 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.

0numbers the graph read from it
0cells of the map it votes in
23citing 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

23 citing papers in PubMed.

  1. Review
  2. Review
  3. Article
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  5. Article
  6. Review
  7. Signaling Modulation via Minimal C-Terminal Modifications of Apelin-13.ACS pharmacology & translational science · 2023
    Article
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  10. Review
  11. Article
  12. Review
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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

14 authors.

Shuai LiuDepartment of Chemistry , University of Massachusetts-Boston , Boston , Massachusetts 02125 , United States.
Hailemichael O YosiefDepartment of Chemistry , University of Massachusetts-Boston , Boston , Massachusetts 02125 , United States.
Lingling DaiPhase I Clinical Trial Center & Department of Clinical Pharmacology, Xiangya Hospital , Central South University , Changsha , Hunan 410008 , P.R. China.
He HuangDepartment of Chemistry , Stony Brook University , Stony Brook , New York 11794-3400 , United States.
Gagan DhawanDepartment of Chemistry , University of Massachusetts-Boston , Boston , Massachusetts 02125 , United States.
Xiaofeng ZhangDepartment of Chemistry , University of Massachusetts-Boston , Boston , Massachusetts 02125 , United States.
Alex M MuthengiDepartment of Chemistry , University of Massachusetts-Boston , Boston , Massachusetts 02125 , United States.
Justin Roberts
Dennis L Buckley
Jennifer A Perry
Lei Wu
James E BradnerNovartis Institutes for Biomedical Research , Cambridge , Massachusetts 02139 , United States.ORCID 0000-0002-2718-4415
Jun QiDepartment of Medicine , Harvard Medical School , Boston , Massachusetts 02115 , United States.ORCID 0000-0002-1461-3356
Wei ZhangDepartment of Chemistry , University of Massachusetts-Boston , Boston , Massachusetts 02125 , United States.ORCID 0000-0002-6097-2763

Funding

TYROSINE KINASE ONCOGENESIS IN MYELOID LEUKEMIAP01CA066996 · NCI · DANA-FARBER CANCER INSTITUTE · PI SCOTT A ARMSTRONG · 1996 to 2026
$52.5M
U Mass Boston / DFHCC U54 Partnership (1 of 2)U54CA156732 · NCI · DANA-FARBER CANCER INST · PI WENDY Beth LONDON · 2010 to 2026
$25.6M
Understanding Behavioral Patterns in Contraceptive UseU54HD093540 · NICHD · UNIVERSITY OF MINNESOTA · PI BARBER, JENNIFER S. · 2017 to 2018
$4.4M
Understanding Behavioral Patterns in Contraceptive UseP50HD093540 · NICHD · UNIVERSITY OF MINNESOTA · PI GEORG, GUNDA I. · 2019 to 2020
$3.9M
NCI NIH HHS P01 CA066996NCI NIH HHS U54 CA156732NICHD NIH HHS P50 HD093540NICHD NIH HHS U54 HD093540
6 · The paper itself

Abstract

The simultaneous inhibition of polo-like kinase 1 (PLK1) and BRD4 bromodomain by a single molecule could lead to the development of an effective therapeutic strategy for a variety of diseases in which PLK1 and BRD4 are implicated. Compound 23 has been found to be a potent dual kinase-bromodomain inhibitor (BRD4-BD1 IC

Indexed as

Drug DesignProtein ConformationBromodomain Containing ProteinsCell Cycle ProteinsHumansLeukemia, Myeloid, AcuteModels, MolecularMolecular Docking SimulationMolecular StructureNuclear ProteinsPolo-Like Kinase 1Protein DomainsProtein Kinase InhibitorsProtein Serine-Threonine KinasesProto-Oncogene ProteinsStructure-Activity RelationshipBRD4 protein, humanBromodomain Containing ProteinsCell Cycle ProteinsNuclear ProteinsPolo-Like Kinase 1Protein Kinase InhibitorsProtein Serine-Threonine KinasesProto-Oncogene ProteinsTranscription Factors

Identifiers

PMID30125504
PMCPMC6309379

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.