Attaching zanamivir to a polymer markedly enhances its activity against drug-resistant strains of influenza a virus
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Klibanov_Attaching Zanamivir.pdf
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255.91 KB
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Author(s)
Weight, Alisha Kessel
Haldar, Jayanta
Cienfuegos, Luis Álvarez de
Gubareva, Larisa V.
Tumpey, Terrence M.
Chen, Jianzhu
Klibanov, Alexander M.
Date Issued
August 2010
Journal
Journal of Pharmaceutical Sciences
Publisher
Wiley Blackwell (John Wiley & Sons)
Citation
Weight, Alisha K. et al. “Attaching Zanamivir to a Polymer Markedly Enhances Its Activity Against Drug-resistant Strains of Influenza a Virus.” Journal of Pharmaceutical Sciences 100.3 (2011): 831–835.
Version
Author's final manuscript
Abstract
Effects of the commercial drug zanamivir (Relenza™) covalently attached to poly-l-glutamine on the infectivity of influenza A viruses are examined using the plaque reduction assay and binding affinity to viral neuraminidase (NA). These multivalent drug conjugates exhibit (i) up to a 20,000-fold improvement in anti-influenza potency compared with the zanamivir parent against human and avian viral strains, including both wild-type and drug-resistant mutants, and (ii) superior neuraminidase (NA) inhibition constants, especially for the mutants. These findings provide a basis for exploring polymer-attached inhibitors as more efficacious therapeutics, particularly against drug-resistant influenza strains.
MIT Department
Massachusetts Institute of Technology. Department of Biological Engineering
Massachusetts Institute of Technology. Department of Biology
Massachusetts Institute of Technology. Department of Chemistry
Koch Institute for Integrative Cancer Research at MIT
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Creative Commons Attribution-Noncommercial-Share Alike 3.0
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DOI of Published Version
https://doi.org/10.1002/jps.22338
