Evidence map›Paper›PMID 26169596›Full record

ArticleVirology journal2015

In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses.

Céline Lacroix, Samuela Laconi, Fabrizio Angius, Antonio Coluccia, Romano Silvestri, Raffaello Pompei, Johan Neyts, Pieter Leyssen

Open access · goldAbstract read
In one paragraph

Article in Virology journal, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
2.4field-weighted citation impact, top 11% 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

15 citing papers in PubMed, 36 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Enterovirus A71 antivirals: Past, present, and future.Acta pharmaceutica Sinica. B · 2022
    Article
  5. Review
  6. Anno 2021: Which antivirals for the coming decade?Annual reports in medicinal chemistry · 2021
    Article
  7. Review
  8. Article
  9. Article
  10. [Rhinoviruses].Der Internist · 2019
    Review
  11. Cryo-EM structure of pleconaril-resistant rhinovirus-B5 complexed to the antiviral OBR-5-340 reveals unexpected binding site.Proceedings of the National Academy of Sciences of the United States of America · 2019
    Article
  12. Article
  13. Review
  14. Article
  15. 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

8 authors at 3 institutions in 2 countries.

Céline LacroixDepartment of Microbiology and Immunology, Laboratory for Virology and Chemotherapy, KU Leuven, Rega Institute for Medical Research, B-3000, Leuven, Belgium. lacroixceline@gmail.com.
Samuela LaconiDepartment of Biomedical Sciences, University of Cagliari, I-09124, Cagliari, Italy. lsamuela@tiscali.it.
Fabrizio AngiusDepartment of Biomedical Sciences, University of Cagliari, I-09124, Cagliari, Italy. fangius@unica.it.
Antonio ColucciaIstituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185, Rome, Italy. antonio.coluccia@uniroma1.it.
Romano SilvestriIstituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185, Rome, Italy. romano.silvestri@uniroma1.it.
Raffaello PompeiDepartment of Biomedical Sciences, University of Cagliari, I-09124, Cagliari, Italy. pompei@unica.it.
Johan NeytsDepartment of Microbiology and Immunology, Laboratory for Virology and Chemotherapy, KU Leuven, Rega Institute for Medical Research, B-3000, Leuven, Belgium. johan.neyts@rega.kuleuven.be.
Pieter LeyssenDepartment of Microbiology and Immunology, Laboratory for Virology and Chemotherapy, KU Leuven, Rega Institute for Medical Research, B-3000, Leuven, Belgium. pieter.leyssen@rega.kuleuven.be.
Rega Institute for Medical Research · BEUniversity of Cagliari · ITIstituto Pasteur · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundRhinovirus infections do not only cause common colds, but may also trigger severe exacerbations of asthma and chronic obstructive pulmonary disease (COPD). Even though rhinoviruses have been the focus of extensive drug development efforts in the past, an anti-rhinoviral drug still has to make it to the market. In the past, the viral capsid protein VP1 has been shown to be an important target for the development of antiviral molecules. Furthermore, many different chemical scaffolds appear to possess the properties that are required to inhibit virus replication by this mechanism of action. I-6602, an analogue of the rhinovirus inhibitor pirodavir, was previously identified as a potent inhibitor of rhinovirus infection. Here, we describe the antiviral activity of its analogue ca603, a molecule with a modified linker structure, and corroborate its mechanism of action as a capsid binder.

findingsThe molecule ca603 shows antiviral activity against a panel of rhino-and enteroviruses. Cross-resistance is observed against viruses with mutations that render them resistant to the inhibitory effect of the capsid binder pleconaril and thermostability assays demonstrate that the compound binds and stabilizes the viral capsid. Binding of the molecule to the VP1 protein is corroborated by in silico modeling.

conclusionsIt is confirmed that ca603 inhibits rhinovirus replication by interaction with the VP1 protein and, by this, allows to further expand the chemical diversity of capsid-binding molecules.

Indexed as

Antiviral AgentsCapsid ProteinsHumansMicrobial Sensitivity TestsOxadiazolesOxazolesPiperidinesProtein BindingPyridazinesRhinovirusAntiviral AgentsCapsid ProteinsOxadiazolesOxazolesPiperidinespirodavirpleconarilPyridazines

Identifiers

PMID26169596
PMCPMC4501209
OpenAlexW2137873490

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.