Evidence map›Paper›PMID 30640473›Full record

ArticleJournal of medicinal chemistry2019

Antiproliferative and Antimigratory Effects of a Novel YAP-TEAD Interaction Inhibitor Identified Using in Silico Molecular Docking.

Sarah A Smith, Richard B Sessions, Deborah K Shoemark, Christopher Williams, Reza Ebrahimighaei, Madeleine C McNeill, Matthew P Crump, Tristan R McKay, Gemma Harris, Andrew C Newby and 1 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.

0numbers the graph read from it
0cells of the map it votes in
44citing papers in PubMed
5.9field-weighted citation impact, top 3% of its field
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

44 citing papers in PubMed, 81 citations in OpenAlex.

  1. The Regulation and Function of Hippo/YAP Pathway in Cancer.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026
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  12. New insights into the ambivalent role of YAP/TAZ in human cancers.Journal of experimental & clinical cancer research : CR · 2023
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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

11 authors at 4 institutions in 1 country.

Sarah A SmithSchool of Translational Health Sciences, Faculty of Health Sciences , University of Bristol , Research Floor Level 7, Bristol Royal Infirmary , Bristol BS2 8HW , U.K.
Richard B SessionsSchool of Biochemistry, Faculty of Biomedical Sciences , University of Bristol , Biomedical Sciences Building, University Walk , Bristol BS8 1TD , U.K.ORCID 0000-0003-0320-0895
Deborah K ShoemarkSchool of Biochemistry, Faculty of Biomedical Sciences , University of Bristol , Biomedical Sciences Building, University Walk , Bristol BS8 1TD , U.K.
Christopher WilliamsSchool of Chemistry, Faculty of Science , University of Bristol , Cantock's Close , Bristol BS8 1TS , U.K.ORCID 0000-0001-5806-9842
Reza EbrahimighaeiSchool of Translational Health Sciences, Faculty of Health Sciences , University of Bristol , Research Floor Level 7, Bristol Royal Infirmary , Bristol BS2 8HW , U.K.
Madeleine C McNeillSchool of Translational Health Sciences, Faculty of Health Sciences , University of Bristol , Research Floor Level 7, Bristol Royal Infirmary , Bristol BS2 8HW , U.K.
Matthew P CrumpSchool of Chemistry, Faculty of Science , University of Bristol , Cantock's Close , Bristol BS8 1TS , U.K.ORCID 0000-0002-7868-5818
Tristan R McKayCentre for Bioscience , Manchester Metropolitan University , John Dalton Building , Manchester M1 5GD , U.K.
Gemma HarrisResearch Complex at Harwell , Rutherford Appleton Laboratory , Harwell Campus , Didcot, Oxfordshire OX11 0FA , U.K.
Andrew C NewbySchool of Translational Health Sciences, Faculty of Health Sciences , University of Bristol , Research Floor Level 7, Bristol Royal Infirmary , Bristol BS2 8HW , U.K.
Mark BondSchool of Translational Health Sciences, Faculty of Health Sciences , University of Bristol , Research Floor Level 7, Bristol Royal Infirmary , Bristol BS2 8HW , U.K.ORCID 0000-0003-2788-278X
Bristol Royal Infirmary · GBUniversity of Bristol · GBManchester Metropolitan University · GBResearch Complex at Harwell · GB

Funding

Biotechnology and Biological Sciences Research Council BB/L01386X/1British Heart Foundation PG/15/100/31877
6 · The paper itself

Abstract

The Hippo pathway is an important regulator of cell growth, proliferation, and migration. TEAD transcription factors, which lie at the core of the Hippo pathway, are essential for regulation of organ growth and wound repair. Dysregulation of TEAD and its regulatory cofactor Yes-associated protein (YAP) have been implicated in numerous human cancers and hyperproliferative pathological processes. Hence, the YAP-TEAD complex is a promising therapeutic target. Here, we use in silico molecular docking using Bristol University Docking Engine to screen a library of more than 8 million druglike molecules for novel disrupters of the YAP-TEAD interaction. We report the identification of a novel compound (CPD3.1) with the ability to disrupt YAP-TEAD protein-protein interaction and inhibit TEAD activity, cell proliferation, and cell migration. The YAP-TEAD complex is a viable drug target, and CPD3.1 is a lead compound for the development of more potent TEAD inhibitors for treating cancer and other hyperproliferative pathologies.

Indexed as

Molecular Docking SimulationAdaptor Proteins, Signal TransducingCell MovementCell ProliferationComputer SimulationGene ExpressionHumansTranscription FactorsYAP-Signaling ProteinsAdaptor Proteins, Signal TransducingTranscription FactorsYAP1 protein, humanYAP-Signaling Proteins

Identifiers

PMID30640473
PMCPMC6701825
OpenAlexW2909855854

What OpenQuestion holds

Textmetadata
Read underepoch 390

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.