Evidence map›Paper›PMID 33525941›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2021

Pharmacophore-guided repurposing of fibrates and retinoids as GPR40 allosteric ligands with activity on insulin release.

Erika Cione, Maria Cristina Caroleo, Hiroyuki Kagechika, Fabrizio Manetti

Open access · goldAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2021. 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
0.4field-weighted citation impact, top 42% 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, 6 citations in OpenAlex.

  1. Article
  2. 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

4 authors at 3 institutions in 2 countries.

Erika CioneDepartment of Pharmacy, Health and Nutritional Sciences (Department of Excellence 2018-2022), University of Calabria, Rende, Italy.ORCID https://orcid.org/0000-0002-0562-0597
Maria Cristina CaroleoDepartment of Pharmacy, Health and Nutritional Sciences (Department of Excellence 2018-2022), University of Calabria, Rende, Italy.
Hiroyuki KagechikaInstitute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU), Tokyo, Japan.ORCID https://orcid.org/0000-0002-6747-1013
Fabrizio ManettiDepartment of Biotechnology, Chemistry and Pharmacy (Department of Excellence 2018-2022), University of Siena, Siena, Italy.ORCID https://orcid.org/0000-0002-9598-2339
University of Calabria · ITTokyo Medical and Dental University · JPUniversity of Siena · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A classical drug repurposing approach was applied to find new putative GPR40 allosteric binders. A two-step computational protocol was set up, based on an initial pharmacophoric-based virtual screening of the DrugBank database of known drugs, followed by docking simulations to confirm the interactions between the prioritised compounds and GPR40. The best-ranked entries showed binding poses comparable to that of TAK-875, a known allosteric agonist of GPR40. Three of them (tazarotenic acid, bezafibrate, and efaproxiral) affect insulin secretion in pancreatic INS-1 832/13 β-cells with EC

Indexed as

Drug RepositioningAllosteric RegulationAniline CompoundsAnimalsBezafibrateCells, CulturedDose-Response Relationship, DrugFibric AcidsHumansInsulinLigandsMolecular Docking SimulationMolecular StructurePropionatesRatsReceptors, G-Protein-CoupledAniline CompoundsBezafibrateefaproxiralFFAR1 protein, humanFibric AcidsInsulinLigandsPropionatesReceptors, G-Protein-CoupledRetinoidsdrug repurposingGPR40insulin secretionpharmacophore modelVirtual screening

Identifiers

PMID33525941
PMCPMC8759729
OpenAlexW3128697892

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.