Evidence map›Paper›PMID 28320616›Full record

ArticleBioorganic & medicinal chemistry letters2017

High-content screen using zebrafish (Danio rerio) embryos identifies a novel kinase activator and inhibitor.

Werner J Geldenhuys, Sadie A Bergeron, Jackie E Mullins, Rowaa Aljammal, Briah L Gaasch, Wei-Chi Chen, June Yun, Lori A Hazlehurst

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. 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
0.4field-weighted citation impact, top 39% 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

1 citing paper in PubMed, 4 citations in OpenAlex.

  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 at 2 institutions in 1 country.

Werner J GeldenhuysDepartment of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, Morgantown, WV 26506, United States. Electronic address: werner.geldenhuys@hsc.wvu.edu.
Sadie A BergeronDepartment of Biology, Eberly College of Arts and Sciences, West Virginia University, Morgantown, WV 26506, United States.
Jackie E MullinsDepartment of Biology, Eberly College of Arts and Sciences, West Virginia University, Morgantown, WV 26506, United States.
Rowaa AljammalDepartment of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, Morgantown, WV 26506, United States.
Briah L GaaschDepartment of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, Morgantown, WV 26506, United States.
Wei-Chi ChenDepartment of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, Morgantown, WV 26506, United States.
June YunDepartment of Integrative Medical Sciences, College of Medicine, Northeast Ohio Medical University, Rootstown, OH 44272, United States.
Lori A HazlehurstDepartment of Pharmaceutical Sciences, School of Pharmacy, West Virginia University, Morgantown, WV 26506, United States.
West Virginia University · USNortheast Ohio Medical University · US

Funding

West Virginia IDEA-CTRU54GM104942 · NIGMS · WEST VIRGINIA UNIVERSITY · PI Sally Lynn Hodder · 2012 to 2026
$81.0M
Targeting CD44-mediated calcium signaling for the treatment of relapsed myelomaR01CA195727 · NCI · WEST VIRGINIA UNIVERSITY · PI HAZLEHURST, LORI A · 2015 to 2019
$1.7M
NCI NIH HHS R01 CA195727NIGMS NIH HHS U54 GM104942
6 · The paper itself

Abstract

In this report we utilized zebrafish (Danio rerio) embryos in a phenotypical high-content screen (HCS) to identify novel leads in a cancer drug discovery program. We initially validated our HCS model using the flavin adenosine dinucleotide (FAD) containing endoplasmic reticulum (ER) enzyme, endoplasmic reticulum oxidoreductase (ERO1) inhibitor EN460. EN460 showed a dose response effect on the embryos with a dose of 10μM being significantly lethal during early embryonic development. The HCS campaign which employed a small library identified a promising lead compound, a naphthyl-benzoic acid derivative coined compound 1 which had significant dosage and temporally dependent effects on notochord and muscle development in zebrafish embryos. Screening a 369 kinase member panel we show that compound 1 is a PIM3 kinase inhibitor (IC

Indexed as

AnimalsAntineoplastic AgentsBenzoic AcidDeath-Associated Protein KinasesDrug DiscoveryDrug Screening Assays, AntitumorEmbryo, NonmammalianEnzyme ActivationEnzyme ActivatorsNeoplasmsProtein Kinase InhibitorsProtein Serine-Threonine KinasesZebrafishZebrafish ProteinsAntineoplastic AgentsBenzoic AcidDeath-Associated Protein KinasesEnzyme ActivatorsProtein Kinase InhibitorsProtein Serine-Threonine KinasesZebrafish ProteinsCancerCompound libraryKinaseNotochordPhenotypic screenSomitesZebrafish

Identifiers

PMID28320616
PMCPMC5435482
OpenAlexW2592489006

What OpenQuestion holds

Textmetadata
LicenceTDM
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.