Evidence map›Paper›PMID 31124660›Full record

ArticleACS chemical neuroscience2019

Design and Synthesis of 2,3- trans-Proline Analogues as Ligands for Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters.

Christian B M Poulie, Anna Alcaide, Mikkel Krell-Jørgensen, Younes Larsen, Eloi Astier, Walden E Bjørn-Yoshimoto, Feng Yi, Jed T Syrenne, Morten Storgaard, Birgitte Nielsen and 5 more

Abstract read
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In one paragraph

Article in ACS chemical neuroscience, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

15 authors.

Christian B M PoulieDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Anna AlcaideDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Mikkel Krell-JørgensenDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Younes LarsenDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Eloi AstierDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Walden E Bjørn-YoshimotoDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Feng YiDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, and Center for Biomolecular Structure and Dynamics , University of Montana , Missoula , Montana 59812 , United States.
Jed T SyrenneDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, and Center for Biomolecular Structure and Dynamics , University of Montana , Missoula , Montana 59812 , United States.
Morten StorgaardDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Birgitte NielsenDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Karla A FrydenvangDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.ORCID 0000-0002-5823-3478
Anders A JensenDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.
Kasper B HansenDepartment of Biomedical and Pharmaceutical Sciences, Center for Structural and Functional Neuroscience, and Center for Biomolecular Structure and Dynamics , University of Montana , Missoula , Montana 59812 , United States.ORCID 0000-0002-3303-4819
Darryl S PickeringDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.ORCID 0000-0001-8687-6094
Lennart BunchDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen 2100 , Denmark.ORCID 0000-0002-0180-4639

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
Structural and functional investigation of negative allosteric NMDA receptor modulationR01NS097536 · NINDS · UNIVERSITY OF MONTANA · PI Kasper Boe Hansen · 2016 to 2026
$3.4M
NIGMS NIH HHS P20 GM103546NINDS NIH HHS R01 NS097536
6 · The paper itself

Abstract

Development of pharmacological tools for the ionotropic glutamate receptors (iGluRs) is imperative for the study and understanding of the role and function of these receptors in the central nervous system. We report the synthesis of 18 analogues of (2 S,3 R)-2-carboxy-3-pyrrolidine acetic acid (3a), which explores the effect of introducing a substituent on the ε-carbon (3c-q). A new synthetic method was developed for the efficient synthesis of racemic 3a and applied to give expedited access to 13 racemic analogues of 3a. Pharmacological characterization was carried out at native iGluRs, cloned homomeric kainate receptors (GluK1-3), NMDA receptors (GluN1/GluN2A-D), and excitatory amino acid transporters (EAAT1-3). From the structure-activity relationship studies, several new ligands emerged, exemplified by triazole 3p-d1, GluK3-preferring (GluK1/GluK3 K

Indexed as

AnimalsDrug DesignGlutamate Plasma Membrane Transport ProteinsHumansLigandsModels, MolecularProlineRatsReceptors, Ionotropic GlutamateStructure-Activity RelationshipGlutamate Plasma Membrane Transport ProteinsLigandsProlineReceptors, Ionotropic GlutamateCNSGlutamate receptorskainateNMDA receptorsproline analogues

Identifiers

PMID31124660
PMCPMC6597265

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.