Evidence map›Paper›PMID 35082341›Full record

ArticleScientific reports2022

GLUT3 inhibitor discovery through in silico ligand screening and in vivo validation in eukaryotic expression systems.

Cristina V Iancu, Giovanni Bocci, Mohd Ishtikhar, Moumita Khamrai, Mislav Oreb, Tudor I Oprea, Jun-Yong Choe

Open access · goldAbstract readValidation Study
In one paragraph

Article in Scientific reports, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.7field-weighted citation impact, top 15% 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

13 citing papers in PubMed, 19 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

7 authors at 3 institutions in 2 countries.

Cristina V Iancu *East Carolina Diabetes and Obesity Institute, East Carolina University, Greenville, NC, 27834, USA.
Giovanni Bocci *Translational Informatics Division, Department of Internal Medicine, The University of New Mexico School of Medicine, Albuquerque, NM, 87131, USA.
Mohd Ishtikhar *East Carolina Diabetes and Obesity Institute, East Carolina University, Greenville, NC, 27834, USA.
Moumita KhamraiEast Carolina Diabetes and Obesity Institute, East Carolina University, Greenville, NC, 27834, USA.
Mislav OrebInstitute of Molecular Biosciences, Faculty of Biological Sciences, Goethe University Frankfurt, Frankfurt am Main, Germany.
Tudor I OpreaTranslational Informatics Division, Department of Internal Medicine, The University of New Mexico School of Medicine, Albuquerque, NM, 87131, USA. toprea@salud.unm.edu.
Jun-Yong ChoeEast Carolina Diabetes and Obesity Institute, East Carolina University, Greenville, NC, 27834, USA. choej18@ecu.edu.
East Carolina University · USUniversity of New Mexico · USGoethe University Frankfurt · DE

Funding

Ligand Specificity In Human Glucose Transporters GLUT1-5 and GLUT9R01GM123103 · NIGMS · ROSALIND FRANKLIN UNIV OF MEDICINE & SCI · PI CHOE, JUN-YONG, OPREA, TUDOR I · 2017 to 2020
$1.3M
NIGMS NIH HHS R01 GM123103NIGMS NIH HHS R01-GM123103
6 · The paper itself

Abstract

The passive transport of glucose and related hexoses in human cells is facilitated by members of the glucose transporter family (GLUT, SLC2 gene family). GLUT3 is a high-affinity glucose transporter primarily responsible for glucose entry in neurons. Changes in its expression have been implicated in neurodegenerative diseases and cancer. GLUT3 inhibitors can provide new ways to probe the pathophysiological role of GLUT3 and tackle GLUT3-dependent cancers. Through in silico screening of an ~ 8 million compounds library against the inward- and outward-facing models of GLUT3, we selected ~ 200 ligand candidates. These were tested for in vivo inhibition of GLUT3 expressed in hexose transporter-deficient yeast cells, resulting in six new GLUT3 inhibitors. Examining their specificity for GLUT1-5 revealed that the most potent GLUT3 inhibitor (G3iA, IC

Indexed as

Drug DiscoveryBinding SitesBiological TransportCell Line, TumorCell SurvivalGlucose Transporter Type 1Glucose Transporter Type 2Glucose Transporter Type 3Glucose Transporter Type 4Glucose Transporter Type 5Heterocyclic Compounds, 3-RingHigh-Throughput Screening AssaysHumansModels, MolecularNeoplasmsProtein BindingGlucose Transporter Type 1Glucose Transporter Type 2Glucose Transporter Type 3Glucose Transporter Type 4Glucose Transporter Type 5Heterocyclic Compounds, 3-RingSaccharomyces cerevisiae ProteinsSmall Molecule Libraries

Identifiers

PMID35082341
PMCPMC8791944
OpenAlexW4210574246

What OpenQuestion holds

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LicenceCC BY
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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.