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High-throughput docking for the identification of new influenza A virus polymerase inhibitors targeting the PA-PB1 protein-protein interaction.

Abstract
A high-throughput molecular docking approach was successfully applied for the selection of potential inhibitors of the Influenza RNA-polymerase which act by targeting the PA-PB1 protein-protein interaction. Commercially available compounds were purchased and biologically evaluated in vitro using an ELISA-based assay. As a result, some compounds possessing a 3-cyano-4,6-diphenyl-pyridine nucleus emerged as effective inhibitors with the best ones showing IC50 values in the micromolar range.
AuthorsCristina Tintori, Ilaria Laurenzana, Anna Lucia Fallacara, Ulrich Kessler, Beatrice Pilger, Lilli Stergiou, Maurizio Botta
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 24 Issue 1 Pg. 280-2 (Jan 01 2014) ISSN: 1464-3405 [Electronic] England
PMID24314669 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2013 Elsevier Ltd. All rights reserved.
Chemical References
  • Enzyme Inhibitors
  • PA protein, influenza viruses
  • PB2 protein, influenza virus
  • Pyridines
  • Viral Proteins
  • RNA-Dependent RNA Polymerase
Topics
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors (chemistry, pharmacology)
  • High-Throughput Screening Assays
  • Influenza A virus (enzymology)
  • Models, Molecular
  • Molecular Structure
  • Protein Binding (drug effects)
  • Pyridines (chemistry, pharmacology)
  • RNA-Dependent RNA Polymerase (antagonists & inhibitors, metabolism)
  • Structure-Activity Relationship
  • Viral Proteins (antagonists & inhibitors, metabolism)

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