Evidence map›Paper›PMID 27203574›Full record

ArticleChemical biology & drug design2016

Various modifications of the amphipathic dynorphin A pharmacophore for rat brain bradykinin receptors.

Yeon Sun Lee, Robert Kupp, Michael V Remesic, Cyf Ramos-Colon, Sara M Hall, Christopher Chan, David Rankin, Josephine Lai, Frank Porreca, Victor J Hruby

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

Article in Chemical biology & drug design, 2016. 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
0.3field-weighted citation impact, top 39% 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. Cyclic non-opioid dynorphin A analogues for the bradykinin receptors.Bioorganic & medicinal chemistry letters · 2016
    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 at 1 institution in 1 country.

Yeon Sun LeeDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ, USA. yeon@email.arizona.edu.
Robert KuppDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ, USA.
Michael V RemesicDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ, USA.
Cyf Ramos-ColonDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ, USA.
Sara M HallDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ, USA.
Christopher ChanDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ, USA.
David RankinDepartment of Pharmacology, University of Arizona, Tucson, AZ, USA.
Josephine LaiDepartment of Pharmacology, University of Arizona, Tucson, AZ, USA.
Frank PorrecaDepartment of Pharmacology, University of Arizona, Tucson, AZ, USA.
Victor J HrubyDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ, USA.
University of Arizona · US

Funding

THERAPEUTIC PROFILES OF OPIOID DELTA RECEPTORS--NEW MODALITIESP01DA006284 · NIDA · UNIVERSITY OF ARIZONA · PI HRUBY, VICTOR J · 1989 to 2015
$14.8M
NOVEL NON-PEPTIDE OPIOID LIGANDS FOR PAINR01DA013449 · NIDA · UNIVERSITY OF ARIZONA · PI HRUBY, VICTOR J · 2000 to 2015
$6.8M
NIDA NIH HHS P01 DA006284NIDA NIH HHS R01 DA013449
6 · The paper itself

Abstract

As a unique endogenous opioid ligand, dynorphin A shows paradoxical neuroexcitatory effects at bradykinin receptors, and the effects are known to be amplified by the upregulation of dynorphin A under chronic pain and inflammatory conditions. In our earlier structure-activity relationship studies, the amphipathic dynorphin A fragment, [Des-Arg(7) ]-Dyn A-(4-11), was identified as a pharmacophore for the bradykinin receptors along with key structural features. Here, further modifications of the pharmacophore showed that the position of a Pro residue is also an important feature because of its role in making (or disrupting) a β-turn or 310 helix structure which is crucial for receptor recognition.

Indexed as

AnimalsDynorphinsInhibitory Concentration 50LigandsRatsReceptors, BradykininStructure-Activity RelationshipDynorphinsLigandsReceptors, Bradykininamphipathicitybradykinin receptorschronic painnon-opioid dynorphin Aprolinestructure-activity relationship

Identifiers

PMID27203574
PMCPMC5025351
OpenAlexW2407222510

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.