Evidence map›Paper›PMID 30393515›Full record

ArticleMedChemComm2018

Discovery of new FXR agonists based on 6-ECDCA binding properties by virtual screening and molecular docking.

Antonella Giancristofaro, Arménio J M Barbosa, Alessandra Ammazzalorso, Pasquale Amoia, Barbara De Filippis, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini, Rosa Amoroso

Open access · bronzeAbstract read
In one paragraph

Article in MedChemComm, 2018. 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
0.8field-weighted citation impact, top 25% 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, 10 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

9 authors at 2 institutions in 4 countries.

Antonella GiancristofaroDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.
Arménio J M BarbosaChemistry Department , Faculdade de Ciências e Tecnologia , Universidade Nova de Lisboa , 2829-516 Caparica , Portugal.ORCID 0000-0002-9756-4958
Alessandra AmmazzalorsoDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.
Pasquale AmoiaDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.
Barbara De FilippisDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.
Marialuigia FantacuzziDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.
Letizia GiampietroDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.
Cristina MaccalliniDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.
Rosa AmorosoDepartment of Pharmacy , University of Chieti "G. d'Annunzio" , via dei vestini 31 , 66100 Chieti , Italy . Email: rosa.amoroso@unich.it.ORCID 0000-0002-8282-8535
University of Chieti-Pescara · ITDivision of Chemistry · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

FXR is a member of the nuclear receptor superfamily, which regulates the expression of various genes involved in bile acid, lipid and glucose metabolism. Targeting FXR with small molecules has been exploited to treat lipid-related disorders and diseases such as cholestasis, gallstones and hepatic disorders. In this work, we expand the existing pool of known FXR agonists using a fast hit-to-lead structure-based pharmacophore and docking screening protocol. A set of 25 molecules was selected after screening a large database of commercial chemicals, and experimental tests were carried out to demonstrate their ability to activate FXR. Three novel FXR agonists are reported, namely, one full agonist, more efficient than the endogenous ligand chenodeoxycholic acid, and two partial agonists.

Identifiers

PMID30393515
PMCPMC6194413
OpenAlexW2811079086

What OpenQuestion holds

Textmetadata
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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.