Evidence map›Paper›PMID 34885825›Full record

ArticleMolecules (Basel, Switzerland)2021

Identification of a Novel Delta Opioid Receptor Agonist Chemotype with Potential Negative Allosteric Modulator Capabilities.

Yazan J Meqbil, Hongyu Su, Robert J Cassell, Kendall L Mores, Anna M Gutridge, Benjamin R Cummins, Lan Chen, Richard M van Rijn

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

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 32% 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

5 citing papers in PubMed, 10 citations in OpenAlex.

  1. Review
  2. Identification of 1,3,8-Triazaspiro[4.5]Decane-2,4-Dione Derivatives as a NovelThe Journal of pharmacology and experimental therapeutics · 2024
    Article
  3. Review
  4. Article
  5. 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

8 authors at 1 institution in 1 country.

Yazan J MeqbilDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN 47907, USA.ORCID 0000-0001-5801-1608
Hongyu SuDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN 47907, USA.
Robert J CassellDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN 47907, USA.
Kendall L MoresDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN 47907, USA.
Anna M GutridgeDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN 47907, USA.
Benjamin R CumminsDepartment of Chemistry, College of Science, Purdue University, West Lafayette, IN 47907, USA.
Lan ChenPurdue Institute for Drug Discovery, Purdue University, West Lafayette, IN 47907, USA.
Richard M van RijnDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN 47907, USA.ORCID 0000-0002-9957-1633
Purdue University West Lafayette · US

Funding

G-protein-, beta-arrestin- and ERK-signaling in alcohol use- and anxiety-disordersR01AA025368 · NIAAA · PURDUE UNIVERSITY · PI CHESTER, JULIA ANN · 2017 to 2021
$1.7M
Opioidergic alkaloids from Mitragynia Speciosa (kratom) as novel treatment for alcohol use disorderR21AA026949 · NIAAA · PURDUE UNIVERSITY · PI VAN RIJN, RICHARD M. · 2018 to 2019
$421k
The influence of alcohol on the metastatic dormancy of breast cancerR21AA026675 · NIAAA · PURDUE UNIVERSITY · PI VAN RIJN, RICHARD M., WENDT, MICHAEL KEITH · 2018 to 2019
$280k
Development of G-protein biased delta opioid receptor agonist with analgesic potencyR03DA045897 · NIDA · PURDUE UNIVERSITY · PI VAN RIJN, RICHARD M. · 2018 to 2019
$149k
NIAAA NIH HHS AA025368NIAAA NIH HHS AA026675NIAAA NIH HHS AA026949NIAAA NIH HHS R01 AA025368NIAAA NIH HHS R21 AA026949NIDA NIH HHS DA045897NIDA NIH HHS R03 DA045897
6 · The paper itself

Abstract

The δ-opioid receptor (δOR) holds great potential as a therapeutic target. Yet, clinical drug development, which has focused on δOR agonists that mimic the potent and selective tool compound SNC80 have largely failed. It has increasingly become apparent that the SNC80 scaffold carries with it potent and efficacious β-arrestin recruitment. Here, we screened a relatively small (5120 molecules) physical drug library to identify δOR agonists that underrecruit β-arrestin, as it has been suggested that compounds that efficaciously recruit β-arrestin are proconvulsant. The screen identified a hit compound and further characterization using cellular binding and signaling assays revealed that this molecule (R995045, compound

Indexed as

Allosteric RegulationAmino Acidsbeta-ArrestinsBinding SitesCyclic AMPEnkephalin, LeucineHEK293 CellsHumansInhibitory Concentration 50Molecular Dynamics SimulationReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muAmino Acidsbeta-ArrestinsCyclic AMPEnkephalin, LeucineReceptors, Opioid, deltaReceptors, Opioid, kappaReceptors, Opioid, muallosteric modulationbeta-arrestinchemotypedelta opioid receptorhigh-throughput screenmolecular dynamics

Identifiers

PMID34885825
PMCPMC8659279
OpenAlexW3217070909

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.