Rational design of potent sialidase-based inhibitors of influenza virus replication

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-assiste...

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Veröffentlicht in:Nature (London) 1993-06, Vol.363 (6428), p.418-423
Hauptverfasser: von Itzstein, Mark, Wu, Wen-Yang, Kok, Gaik B., Pegg, Michael S., Dyason, Jeffrey C., Jin, Betty, Van Phan, Tho, Smythe, Mark L., White, Hume F., Oliver, Stuart W., Colman, Peter M., Varghese, Joseph N., Ryan, D. Michael, Woods, Jacqueline M., Bethell, Richard C., Hotham, Vanessa J., Cameron, Janet M., Penn, Charles R.
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Sprache:eng
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Zusammenfassung: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.
ISSN:0028-0836
1476-4687
DOI:10.1038/363418a0