Evidence map›Paper›PMID 26288686›Full record

ArticleACS medicinal chemistry letters2015

Virtual Screening and Biological Validation of Novel Influenza Virus PA Endonuclease Inhibitors.

Nicolino Pala, Annelies Stevaert, Roberto Dallocchio, Alessandro Dessì, Dominga Rogolino, Mauro Carcelli, Vanna Sanna, Mario Sechi, Lieve Naesens

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
–field-weighted citation impact
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

16 citing papers in PubMed.

  1. Pharmacophores of Influenza Virus PA Endonuclease Inhibitors.Advances in experimental medicine and biology · 2026
    Review
  2. Review
  3. Article
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  5. Review
  6. Article
  7. Article
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  12. Review
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  15. Article
  16. Docking Screens for Novel Ligands Conferring New Biology.Journal of medicinal chemistry · 2016
    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

9 authors.

Nicolino PalaDipartimento di Chimica e Farmacia, Università di Sassari , Via Vienna 2, 07100 Sassari, Italy.
Annelies StevaertRega Institute for Medical Research, KU Leuven , Minderbroedersstraat 10, B-3000 Leuven, Belgium.
Roberto DallocchioIstituto di Chimica Biomolecolare, CNR-Consiglio Nazionale delle Ricerche , Sassari, 07100 Li Punti Italy.
Alessandro DessìIstituto di Chimica Biomolecolare, CNR-Consiglio Nazionale delle Ricerche , Sassari, 07100 Li Punti Italy.
Dominga RogolinoDipartimento di Chimica, Università di Parma , Parco Area delle Scienze 17/A, 43124 Parma, Italy.
Mauro CarcelliDipartimento di Chimica, Università di Parma , Parco Area delle Scienze 17/A, 43124 Parma, Italy.
Vanna SannaDipartimento di Chimica e Farmacia, Università di Sassari , Via Vienna 2, 07100 Sassari, Italy.
Mario SechiDipartimento di Chimica e Farmacia, Università di Sassari , Via Vienna 2, 07100 Sassari, Italy.
Lieve NaesensRega Institute for Medical Research, KU Leuven , Minderbroedersstraat 10, B-3000 Leuven, Belgium.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The influenza virus RNA-dependent RNA polymerase complex (RdRp), a heterotrimeric protein complex responsible for viral RNA transcription and replication, represents a primary target for antiviral drug development. One particularly attractive approach is interference with the endonucleolytic "cap-snatching" reaction by the RdRp subunit PA, more precisely by inhibiting its metal-dependent catalytic activity which resides in the N-terminal part of PA (PA-Nter). Almost all PA inhibitors (PAIs) thus far discovered bear pharmacophoric fragments with chelating motifs able to bind the bivalent metal ions in the catalytic core of PA-Nter. More recently, the availability of crystallographic structures of PA-Nter has enabled rational design of original PAIs with improved binding properties and antiviral potency. We here present a coupled pharmacophore/docking virtual screening approach that allowed us to identify PAIs with interesting inhibitory activity in a PA-Nter enzymatic assay. Moreover, antiviral activity in the low micromolar range was observed in cell-based influenza virus assays.

Indexed as

dihydroxy-1H-indole-2-carboxamidesInfluenza virus PA endonucleasemetal chelationPA inhibitors (PAIs)pharmacophore−structure virtual screeningpolymerase

Identifiers

PMID26288686
PMCPMC4538433

What OpenQuestion holds

Textmetadata
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.