ArticleACS medicinal chemistry letters2015
Virtual Screening and Biological Validation of Novel Influenza Virus PA Endonuclease Inhibitors.
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.
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Who cites it
16 citing papers in PubMed.
- Pharmacophores of Influenza Virus PA Endonuclease Inhibitors.Advances in experimental medicine and biology · 2026Review
- Carboxamide: A Privileged Pharmacophore for the Development of Anti-infectious and Anti-cancer Drugs.Current topics in medicinal chemistry · 2026Review
- Data-driven discovery of chemical signatures for developing new inhibitors against human influenza viruses.BMC chemistry · 2025Article
- A Straightforward Access to New Amides of the Melanin Precursor 5,6-Dihydroxyindole-2-carboxylic Acid and Characterization of the Properties of the Pigments Thereof.Molecules (Basel, Switzerland) · 2022Article
- Recent Advances in Application of Computer-Aided Drug Design in Anti-Influenza A Virus Drug Discovery.International journal of molecular sciences · 2022Review
- Development of targeted nanoparticles loaded with antiviral drugs for SARS-CoV-2 inhibition.European journal of medicinal chemistry · 2022Article
- Synthesis and Antiviral Evaluation of Nucleoside Analogues Bearing One Pyrimidine Moiety and Two D-Ribofuranosyl Residues.Molecules (Basel, Switzerland) · 2021Article
- Synthesis of 1,2,3-triazolyl nucleoside analogues and their antiviral activity.Molecular diversity · 2021Article
- Exploring RdRp-remdesivir interactions to screen RdRp inhibitors for the management of novel coronavirus 2019-nCoV.SAR and QSAR in environmental research · 2020Article
- Expedient synthesis of eumelanin-inspired 5,6-dihydroxyindole-2-carboxylate ethyl ester derivatives.RSC advances · 2018Article
- Article
- Progress of small molecular inhibitors in the development of anti-influenza virus agents.Theranostics · 2017Review
- The Influenza Virus Polymerase Complex: An Update on Its Structure, Functions, and Significance for Antiviral Drug Design.Medicinal research reviews · 2016Review
- N-acylhydrazone inhibitors of influenza virus PA endonuclease with versatile metal binding modes.Scientific reports · 2016Article
- Atomic Structure and Biochemical Characterization of an RNA Endonuclease in the N Terminus of Andes Virus L Protein.PLoS pathogens · 2016Article
- Docking Screens for Novel Ligands Conferring New Biology.Journal of medicinal chemistry · 2016Review
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
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.
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