2015
DOI: 10.1016/j.antiviral.2014.12.004
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Neuraminidase mutations conferring resistance to laninamivir lead to faster drug binding and dissociation

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Cited by 15 publications
(16 citation statements)
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“…So far, the only antiviral drugs approved by the FDA which successfully inhibit release of progeny virions are NAIs (neuraminidase inhibitors). The two effective drugs present in this class are oseltamivir (OTV) and zanamivir, with the availability of two newer drugs, peramivir and laninamivir, in Japan and South Korea since 2010 (McKimm-Breschkin & Barrett, 2015;Singh & Soliman, 2015). These drugs have been designed based on the crystal structures of group-2 NA (N2, N3, N6, N7 and N9) (von Itzstein, 2007).…”
Section: Introductionmentioning
confidence: 99%
“…So far, the only antiviral drugs approved by the FDA which successfully inhibit release of progeny virions are NAIs (neuraminidase inhibitors). The two effective drugs present in this class are oseltamivir (OTV) and zanamivir, with the availability of two newer drugs, peramivir and laninamivir, in Japan and South Korea since 2010 (McKimm-Breschkin & Barrett, 2015;Singh & Soliman, 2015). These drugs have been designed based on the crystal structures of group-2 NA (N2, N3, N6, N7 and N9) (von Itzstein, 2007).…”
Section: Introductionmentioning
confidence: 99%
“…Mutations at the location affecting the laninamivir dissociation rate can confer a dramatic resistance to laninamivir (46). Some studies have reported that mutations conferring zanamivir resistance also induce resistance to laninamivir with the loss of slow binding and/or faster dissociation (46), also relevant to our results (Table 1) Peramivir contains a guanidino group, as does zanamivir, and a hydrophobic group, as does oseltamivir; consequently, mutations affecting the activities of oseltamivir and zanamivir can also confer resistance to peramivir (47), and is supported by our results.…”
Section: Discussionmentioning
confidence: 99%
“…The IC 50 values generated in NI assays also provide information for comparison of inhibitory effects of different NAIs thus aiding in identification of cross-resistant viruses. Variations in IC 50 values determined for the same virus and drug can arise from sources such as use of different enzyme substrates (fluorescent vs chemiluminescent), buffer systems, time of incubation, and other assay conditions (Nguyen et al, 2010;McKimm-Breschkin et al, 2003;McKimm-Breschkin and Barrett, 2014;Tisdale, 2000). The goal of the standardization process was to achieve consistency of IC 50 data across participating laboratories through the application of uniform NI assay testing procedures (same kit and assay protocol) with support from the CDC reference laboratory.…”
Section: Discussionmentioning
confidence: 99%