Evidence map›Paper›PMID 33398639›Full record

ArticleNeurochemical research2021

Inhibition of the Vesicular Glutamate Transporter (VGLUT) with Congo Red Analogs: New Binding Insights.

David M Hitt, Jeffery D Zwicker, Chih-Kai Chao, Sarjubhai A Patel, John M Gerdes, Richard J Bridges, Charles M Thompson

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

Article in Neurochemical research, 2021. 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
0.2field-weighted citation impact, top 57% 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, 2 citations in OpenAlex.

  1. Review
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 2 institutions in 1 country.

David M HittDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, College of Health Professions and Biomedical Sciences, University of Montana, Missoula, MT, 59812, USA.ORCID http://orcid.org/0000-0002-7278-2684
Jeffery D ZwickerDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, College of Health Professions and Biomedical Sciences, University of Montana, Missoula, MT, 59812, USA.
Chih-Kai ChaoDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, College of Health Professions and Biomedical Sciences, University of Montana, Missoula, MT, 59812, USA.
Sarjubhai A PatelDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, College of Health Professions and Biomedical Sciences, University of Montana, Missoula, MT, 59812, USA.
John M GerdesDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, College of Health Professions and Biomedical Sciences, University of Montana, Missoula, MT, 59812, USA.ORCID http://orcid.org/0000-0002-2768-5754
Richard J BridgesDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, College of Health Professions and Biomedical Sciences, University of Montana, Missoula, MT, 59812, USA.ORCID http://orcid.org/0000-0002-7204-5086
Charles M ThompsonDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, College of Health Professions and Biomedical Sciences, University of Montana, Missoula, MT, 59812, USA. chuck.thompson@mso.umt.edu.ORCID http://orcid.org/0000-0003-0018-4973
University of Montana · USDeciphera Pharmaceuticals (United States) · US

Funding

Surveillance genome sequencing to detect SARS-CoV-2 virus variants in MontanaP20GM103546 · NIGMS · UNIVERSITY OF MONTANA · PI BOWLER, BRUCE E · 2012 to 2021
$19.2M
NIGMS NIH HHS P20 GM103546NIGMS NIH HHS P20GM103546
6 · The paper itself

Abstract

The vesicular glutamate transporter (VGLUT) facilitates the uptake of glutamate (Glu) into neuronal vesicles. VGLUT has not yet been fully characterized pharmacologically but a body of work established that certain azo-dyes bearing two Glu isosteres via a linker were potent inhibitors. However, the distance between the isostere groups that convey potent inhibition has not been delineated. This report describes the synthesis and pharmacologic assessment of Congo Red analogs that contain one or two glutamate isostere or mimic groups; the latter varied in the interatomic distance and spacer properties to probe strategic binding interactions within VGLUT. The more potent inhibitors had two glutamate isosteres symmetrically linked to a central aromatic group and showed IC

Indexed as

AnimalsCongo RedDrug DesignMolecular Docking SimulationMolecular StructureProtein BindingRatsStructure-Activity RelationshipVesicular Glutamate Transport ProteinsCongo RedVesicular Glutamate Transport ProteinsCongo red analogsDockingInhibitorIsostereVesicular glutamate transporterVGLUT

Identifiers

PMID33398639
PMCPMC7904594
OpenAlexW3118445993

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.