Evidence map›Paper›PMID 32957550›Full record

ArticleMolecules (Basel, Switzerland)2020

Design, Synthesis and Functional Analysis of Cyclic Opioid Peptides with Dmt-Tic Pharmacophore.

Arijit Sarkar, Anna Adamska-Bartlomiejczyk, Justyna Piekielna-Ciesielska, Karol Wtorek, Alicja Kluczyk, Attila Borics, Anna Janecka

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.2field-weighted citation impact, top 53% 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

2 citing papers in PubMed, 3 citations in OpenAlex.

  1. Article
  2. Chemical tools for the opioids.Molecular and cellular neurosciences · 2023
    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 3 institutions in 2 countries.

Arijit SarkarLaboratory of Chemical Biology, Institute of Biochemistry, Biological Research Centre, Szeged, 62. Temesvári krt., H-6726 Szeged, Hungary.ORCID 0000-0002-3447-1295
Anna Adamska-BartlomiejczykDepartment of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Justyna Piekielna-CiesielskaDepartment of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Karol WtorekDepartment of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Alicja KluczykFaculty of Chemistry, University of Wroclaw, F. Joliot-Curie 14, 50-383 Wroclaw, Poland.ORCID 0000-0003-2943-2782
Attila BoricsLaboratory of Chemical Biology, Institute of Biochemistry, Biological Research Centre, Szeged, 62. Temesvári krt., H-6726 Szeged, Hungary.ORCID 0000-0002-6331-3536
Anna JaneckaDepartment of Biomolecular Chemistry, Faculty of Medicine, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Medical University of Lodz · PLUniversity of Szeged · HUUniversity of Wrocław · PL

Funding

The National Science Center (Poland) 2015/17/B/ST5/00153
6 · The paper itself

Abstract

The opioid receptors are members of the G-protein-coupled receptor (GPCR) family and are known to modulate a variety of biological functions, including pain perception. Despite considerable advances, the mechanisms by which opioid agonists and antagonists interact with their receptors and exert their effect are still not completely understood. In this report, six new hybrids of the Dmt-Tic pharmacophore and cyclic peptides, which were shown before to have a high affinity for the µ-opioid receptor (MOR) were synthesized and characterized pharmacologically in calcium mobilization functional assays. All obtained ligands turned out to be selective antagonists of the δ-opioid receptor (DOR) and did not activate or block the MOR. The three-dimensional structural determinants responsible for the DOR antagonist properties of these analogs were further investigated by docking studies. The results indicate that these compounds attach to the DOR in a slightly different orientation with respect to the Dmt-Tic pharmacophore than Dmt-TicΨ[CH

Indexed as

Analgesics, OpioidAnimalsDipeptidesHumansLigandsMolecular Docking SimulationNarcotic AntagonistsOpioid PeptidesPeptides, CyclicReceptors, OpioidReceptors, Opioid, deltaStructure-Activity RelationshipTetrahydroisoquinolines2',6'-dimethyltyrosyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acidAnalgesics, OpioidDipeptidesLigandsNarcotic AntagonistsOpioid PeptidesPeptides, CyclicphenylalanylphenylalanineReceptors, OpioidReceptors, Opioid, deltaTetrahydroisoquinolinesfunctional assaymolecular modelingopioid receptorspeptide synthesisδ opioid receptor antagonists

Identifiers

PMID32957550
PMCPMC7570497
OpenAlexW3084818663

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.