Evidence map›Paper›PMID 39044606›Full record

ArticleJournal of medicinal chemistry2024

Design, Synthesis, and Characterization of New δ Opioid Receptor-Selective Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors.

Antonios Drakopoulos, Zsombor Koszegi, Kerstin Seier, Harald Hübner, Damien Maurel, Rémy Sounier, Sébastien Granier, Peter Gmeiner, Davide Calebiro, Michael Decker

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. 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
–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

1 citing paper in PubMed.

  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

10 authors.

Antonios DrakopoulosPharmazeutische und Medizinische Chemie, Institut für Pharmazie und Lebensmittelchemie, Julius-Maximilians-Universität (JMU) Würzburg, Am Hubland, 97074 Würzburg, Germany.
Zsombor KoszegiInstitute of Metabolism and Systems Research, University of Birmingham, B15 2TT Birmingham, U.K.
Kerstin SeierInstitute of Pharmacology and Toxicology, Julius-Maximilians University of Würzburg, Versbacher Strasse 9, 97078 Würzburg, Germany.
Harald HübnerChair of Pharmaceutical Chemistry, Department of Chemistry and Pharmacy, Friedrich-Alexander University of Erlangen-Nürnberg, 91058 Erlangen, Germany.ORCID 0000-0002-7892-599X
Damien MaurelInstitut de Génomique Fonctionnelle, CNRS, INSERM, Université de Montpellier, 34094 Cedex 5 Montpellier, France.
Rémy SounierInstitut de Génomique Fonctionnelle, CNRS, INSERM, Université de Montpellier, 34094 Cedex 5 Montpellier, France.
Sébastien GranierInstitut de Génomique Fonctionnelle, CNRS, INSERM, Université de Montpellier, 34094 Cedex 5 Montpellier, France.
Peter GmeinerChair of Pharmaceutical Chemistry, Department of Chemistry and Pharmacy, Friedrich-Alexander University of Erlangen-Nürnberg, 91058 Erlangen, Germany.ORCID 0000-0002-4127-197X
Davide CalebiroInstitute of Metabolism and Systems Research, University of Birmingham, B15 2TT Birmingham, U.K.ORCID 0000-0002-3811-1553
Michael DeckerPharmazeutische und Medizinische Chemie, Institut für Pharmazie und Lebensmittelchemie, Julius-Maximilians-Universität (JMU) Würzburg, Am Hubland, 97074 Würzburg, Germany.ORCID 0000-0002-6773-6245

Funding

Wellcome Trust
6 · The paper itself

Abstract

The delta opioid receptor (δOR or DOR) is a G protein-coupled receptor (GPCR) showing a promising profile as a drug target for nociception and analgesia. Herein, we design and synthesize new fluorescent antagonist probes with high δOR selectivity that are ideally suited for single-molecule microscopy (SMM) applications in unmodified, untagged receptors. Using our new probes, we investigated wild-type δOR localization and mobility at low physiological receptor densities for the first time. Furthermore, we investigate the potential formation of δOR homodimers, as such a receptor organization might exhibit distinct pharmacological activity, potentially paving the way for innovative pharmacological therapies. Our findings indicate that the majority of δORs labeled with these probes exist as freely diffusing monomers on the cell surface in a simple cell model. This discovery advances our understanding of OR behavior and offers potential implications for future therapeutic research.

Indexed as

Drug DesignFluorescent DyesReceptors, Opioid, deltaAnimalsHEK293 CellsHumansMicroscopy, FluorescenceSingle Molecule ImagingFluorescent DyesReceptors, Opioid, delta

Identifiers

PMID39044606
PMCPMC11386433

What OpenQuestion holds

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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.