12:00 AM
Mar 21, 2013
 |  BC Innovations  |  Targets & Mechanisms

Trapping influenza neuraminidase

Researchers at The University of British Columbia have used a mechanism-based approach to design irreversible inhibitors of influenza virus neuraminidase that could have activity against flu strains resistant to marketed inhibitors of the target.1 The new molecules are being developed by CDRD Ventures Inc., the venture arm of The Centre for Drug Research and Development, a public-private partnership that commercializes discoveries from Canadian researchers.

Influenza virus uses neuraminidase to cleave sugars from host glycoproteins at the cell surface, allowing newly formed virions to escape from the infected cells and spread to others.

Two reversible inhibitors of influenza A virus neuraminidase-Roche and Gilead Sciences Inc.'s Tamiflu oseltamivir and Relenza zanamivir from GlaxoSmithKline plc and Biota Pharmaceuticals Inc.-are marketed in the U.S. to treat and prevent influenza A. Two other reversible neuraminidase inhibitors are marketed outside the U.S.-PeramiFlu peramivir from BioCryst Pharmaceuticals Inc., Green Cross Corp. and Shionogi & Co. Ltd., and Inavir laninamivir from Daiichi Sankyo Co. Ltd. and Biota.

Although these inhibitors bind tightly to the active site of the enzyme, mutations in nearby residues of the viral protein can reduce drug affinity and even lead to resistance.

Over time, widespread use of marketed neuraminidase inhibitors could favor the spread of resistant strains, similar to what occurs with...

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