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.
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Authors | Cristina Tintori, Ilaria Laurenzana, Anna Lucia Fallacara, Ulrich Kessler, Beatrice Pilger, Lilli Stergiou, Maurizio Botta |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 24
Issue 1
Pg. 280-2
(Jan 01 2014)
ISSN: 1464-3405 [Electronic] England |
PMID | 24314669
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 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
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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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