Rational design of potent sialidase-based inhibito...[Nature. 1993]

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1: Nature. 1993 Jun 3;363(6428):418-23. Links

Comment in:: Nature. 1993 Jun 3;363(6428):401-2.

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

von Itzstein M, Wu WY, Kok GB, Pegg MS, Dyason JC, Jin B, Van Phan T, Smythe ML, White HF, Oliver SW, et al.

Department of Pharmaceutical Chemistry, Victorian College of Pharmacy, Monash University, Parkville, Australia.

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.

PMID: 8502295 [PubMed - indexed for MEDLINE]

Inhibition of replication of avian influenza viruses by the neuraminidase inhibitor 4-guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid. [Virology. 1995]
Zanamivir. A potent and selective inhibitor of influenza A and B viruses. [Clin Pharmacokinet. 1999]
'Flu' and structure-based drug design. [Structure. 1997]
Zanamivir: from drug design to the clinic. [Philos Trans R Soc Lond B Biol Sci. 2001]
4-Guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid is a highly effective inhibitor both of the sialidase (neuraminidase) and of growth of a wide range of influenza A and B viruses in vitro. [Antimicrob Agents Chemother. 1993]
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Rational design of potent sialidase-based inhibitors of influenza virus replication.

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