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Rational design of potent sialidase-based inhibitors of influenza virus replication
Abstract
Two potent inhibitors based on the crystal structure of influenza virus sialidase have been designed. These compounds are effective inhibitors not only of the enzyme, but also of the virus in cell culture and in animal models. The results provide an example of the power of rational, computer-assisted drug design, as well as indicating significant progress in the development of a new therapeutic or prophylactic treatment for influenza infection.
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Metadata
- Authors
- von Itzstein, M., Wu, W.-Y., Kok, G. B., Pegg, M. S., Dyason, J. C., Jin, B., Van Phan, T., Smythe, M. L., White, H. F., Oliver, S. W., Colman, P. M., Varghese, J. N., Ryan, D. M., Woods, J. M., Bethell, R. C., Hotham, V. J., Cameron, J. M., & Penn, C. R.
- Affiliations
- Monash University (AU)
- Commonwealth Scientific and Industrial Research Organisation (AU)
- Venue
- Nature
- Published
- 1993-06
- Volume
- 363
- Issue
- 6428
- Pages
- 418-423
- ISSN
- 0028-0836 (ISSN-L)
- 1476-4687
- OpenAlex
- W2086358466
- Cited by
- 1,862
- References
- 38
- Citations by year
- 2026: 27 · 2025: 25 · 2024: 34 · 2023: 30 · 2022: 46 · 2021: 50 · 2020: 60 · 2019: 50 · 2018: 58 · 2017: 45 · 2016: 68 · 2015: 48 · 2014: 71 · 2013: 83 · 2012: 84
- FWCI
- 58.57
- Type
- journal article
- Language
- en
- Update notices
- correction (1993-10-28)
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Nature (publishedVersion)
- PubMed (publishedVersion)
- Griffith Research Online (submittedVersion)
- Topics
- Health Sciences › Medicine › Epidemiology › Influenza Virus Research Studies
- Physical Sciences › Chemistry › Organic Chemistry › Carbohydrate Chemistry and Synthesis
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
- Keywords
- influenza virus, sialidase inhibitors, neuraminidase, rational drug design, computer-aided drug design, antiviral agents, influenza treatment, prophylaxis, enzyme inhibition
- MeSH terms
- Animals, Antiviral Agents, Cell Line, Disease Models, Animal, Female, Ferrets, Guanidines, Humans, Influenza, Human, Models, Molecular, Neuraminidase, Influenza A virus, Viral Plaque Assay, Pyrans, Sheep, Sialic Acids, Virus Replication, Drug Design, Computer-Aided Design, Mice, Zanamivir
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