Evidence map›Paper›PMID 27736766›Full record

ArticleAntimicrobial agents and chemotherapy2016

A Novel Fluorescence Resonance Energy Transfer-Based Screen in High-Throughput Format To Identify Inhibitors of Malarial and Human Glucose Transporters.

Thomas E Kraft, Monique R Heitmeier, Marina Putanko, Rachel L Edwards, Ma Xenia G Ilagan, Maria A Payne, Joseph M Autry, David D Thomas, Audrey R Odom, Paul W Hruz

Open access · bronzeAbstract read
In one paragraph

Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
0.9field-weighted citation impact, top 23% 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

14 citing papers in PubMed, 17 citations in OpenAlex.

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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

10 authors at 3 institutions in 1 country.

Thomas E KraftDepartment of Pediatrics, Washington University School of Medicine, St. Louis, Missouri, USA thomas.e.kraft@gmail.com hruz_p@kids.wustl.edu.ORCID 0000-0002-5528-3197
Monique R HeitmeierDepartment of Pediatrics, Washington University School of Medicine, St. Louis, Missouri, USA.
Marina PutankoDepartment of Pediatrics, Washington University School of Medicine, St. Louis, Missouri, USA.
Rachel L EdwardsDepartment of Pediatrics, Washington University School of Medicine, St. Louis, Missouri, USA.
Ma Xenia G IlaganHigh Throughput Screening Core, Washington University School of Medicine, St. Louis, Missouri, USA.
Maria A PayneDepartment of Pediatrics, Washington University School of Medicine, St. Louis, Missouri, USA.
Joseph M AutryDepartment of Biochemistry, Molecular Biology and Biophysics, University of Minnesota, Minneapolis, Minnesota, USA.
David D ThomasDepartment of Biochemistry, Molecular Biology and Biophysics, University of Minnesota, Minneapolis, Minnesota, USA.
Audrey R OdomDepartment of Pediatrics, Washington University School of Medicine, St. Louis, Missouri, USA.
Paul W HruzDepartment of Pediatrics, Washington University School of Medicine, St. Louis, Missouri, USA thomas.e.kraft@gmail.com hruz_p@kids.wustl.edu.
Washington University in St. Louis · USUniversity of Minnesota · USHigh Throughput Biology (United States) · US

Funding

Washington University Institute of Clinical and Translational SciencesUL1TR000448 · NCATS · WASHINGTON UNIVERSITY · PI EVANOFF, BRADLEY A · 2012 to 2016
$41.4M
MEP pathway resistance in Plasmodium falciparumR01AI103280 · NIAID · WASHINGTON UNIVERSITY · PI Audrey Ragan Odom John · 2013 to 2026
$5.5M
NCATS NIH HHS UL1 TR000448NIAID NIH HHS R01 AI103280
6 · The paper itself

Abstract

The glucose transporter PfHT is essential to the survival of the malaria parasite Plasmodium falciparum and has been shown to be a druggable target with high potential for pharmacological intervention. Identification of compounds against novel drug targets is crucial to combating resistance against current therapeutics. Here, we describe the development of a cell-based assay system readily adaptable to high-throughput screening that directly measures compound effects on PfHT-mediated glucose transport. Intracellular glucose concentrations are detected using a genetically encoded fluorescence resonance energy transfer (FRET)-based glucose sensor. This allows assessment of the ability of small molecules to inhibit glucose uptake with high accuracy (Z' factor of >0.8), thereby eliminating the need for radiolabeled substrates. Furthermore, we have adapted this assay to counterscreen PfHT hits against the human orthologues GLUT1, -2, -3, and -4. We report the identification of several hits after screening the Medicines for Malaria Venture (MMV) Malaria Box, a library of 400 compounds known to inhibit erythrocytic development of P. falciparum Hit compounds were characterized by determining the half-maximal inhibitory concentration (IC

Indexed as

High-Throughput Screening AssaysAntimalarialsCells, CulturedErythrocytesFluorescence Resonance Energy TransferGene ExpressionGlucoseGlucose Transporter Type 1Glucose Transporter Type 2Glucose Transporter Type 3Glucose Transporter Type 4HEK293 CellsHumansMonosaccharide Transport ProteinsPlasmodium falciparumProtozoan ProteinsAntimalarialsGlucoseGlucose Transporter Type 1Glucose Transporter Type 2Glucose Transporter Type 3Glucose Transporter Type 4hexose transporter 1 protein, Plasmodium falciparumMonosaccharide Transport ProteinsProtozoan ProteinsSLC2A1 protein, humanSLC2A2 protein, humanSLC2A3 protein, humanSLC2A4 protein, humanSmall Molecule LibrariesTritium

Identifiers

PMID27736766
PMCPMC5119023
OpenAlexW2554412450

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.