Evidence map›Paper›PMID 29282288›Full record

ArticleThe Journal of biological chemistry2018

Structure-based virtual screening identifies a small-molecule inhibitor of the profilin 1-actin interaction.

David Gau, Taber Lewis, Lee McDermott, Peter Wipf, David Koes, Partha Roy

Open access · hybridAbstract read
In one paragraph

Article in The Journal of biological chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.3field-weighted citation impact, top 22% 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

11 citing papers in PubMed, 20 citations in OpenAlex.

  1. Article
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  3. Review
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  5. Review
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  10. Profilin choreographs actin and microtubules in cells and cancer.International review of cell and molecular biology · 2020
    Article
  11. 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

6 authors at 1 institution in 1 country.

David GauFrom the Departments of Bioengineering.
Taber LewisChemistry.
Lee McDermottComputational and Systems Biology.
Peter WipfFrom the Departments of Bioengineering.
David KoesComputational and Systems Biology.
Partha RoyFrom the Departments of Bioengineering, Partha.Roy@pitt.edu par19@pitt.edu.
University of Pittsburgh · US

Funding

University of Pittsburgh Clinical and Translational Science InstituteUL1TR001857 · NCATS · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI REIS, STEVEN E · 2016 to 2025
$129.3M
Cardiovascular Bioengineering Training ProgramT32HL076124 · NHLBI · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI SANJEEV G SHROFF · 2005 to 2026
$7.0M
Profilin as a target to suppress Invasive breast cancerR01CA108607 · NCI · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI ROY, PARTHA · 2006 to 2017
$2.6M
Methods, Tools and Resources for Interactive Online Virtual Screening and Lead OptimizationR01GM108340 · NIGMS · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI KOES, DAVID RYAN · 2013 to 2020
$1.8M
NCATS NIH HHS UL1 TR001857NCI NIH HHS R01 CA108607NHLBI NIH HHS T32 HL076124NIGMS NIH HHS R01 GM108340
6 · The paper itself

Abstract

Profilin 1 (Pfn1) is an important regulator of the actin cytoskeleton and plays a vital role in many actin-based cellular processes. Therefore, identification of a small-molecule intervention strategy targeted against the Pfn1-actin interaction could have broad utility in cytoskeletal research and further our understanding of the role of Pfn1 in actin-mediated biological processes. Based on an already resolved Pfn1-actin complex crystal structure, we performed structure-based virtual screening of small-molecule libraries to seek inhibitors of the Pfn1-actin interaction. We identified compounds that match the pharmacophore of the key actin residues of Pfn1-actin interaction and therefore have the potential to act as competitive inhibitors of this interaction. Subsequent biochemical assays identified two candidate compounds with nearly identical structures that can mitigate the effect of Pfn1 on actin polymerization

Indexed as

Actin CytoskeletonActinsAnimalsAorta, ThoracicCell MovementCell ProliferationCrystallography, X-RayDrug Evaluation, PreclinicalEndothelial CellsHumansMiceMice, Inbred C57BLPolymerizationProfilinsProtein BindingSmall Molecule LibrariesActinsProfilinsSmall Molecule Librariesactinangiogenesiscell migrationendothelial cellmolecular dynamicspharmacophoreprofilinvirtual screening

Identifiers

PMID29282288
PMCPMC5818201
OpenAlexW2776414161

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.