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Structural and Functional Analysis of Laninamivir and its Octanoate Prodrug Reveals Group Specific Mechanisms for Influenza NA Inhibition

Figure 5

Comparison of oseltamivir (yellow), laninamivir octanoate (magenta) and laninamivir (turquoise) binding to p09N1.

Laninamivir binds to p09N1 with a similar active site conformation to the uncomplexed structure. Both laninamivir octanoate and oseltamivir binding to p09N1 induces rotation of Glu276 toward Arg224 where they form a salt bridge. This Glu276 rotation creates a hydrophobic pocket that accommodates the hydrophobic pentyl ether side chain of oseltamivir, however results in a weaker overall binding mode of laninamivir octanoate. The terminal carbon of the oseltamivir side chain is 3.73 Å from the hydrophobic Glu276 Cβ.

Figure 5

doi: https://doi.org/10.1371/journal.ppat.1002249.g005