Result: Next, one of the NA inhibitor-resistant mutations, NA/H274Y, was introduced in A/H1N1 and the susceptibility to BXA was determined.
Result: Whilst NA/H274Y results in a more than 200-fold reduction in susceptibility to oseltamivir acid, BXA showed potent activity against these viruses.
Table: H274Y
Anti-Influenza A Viral Butenolide from Streptomyces sp. Smu03 Inhabiting the Intestine of Elephas maximus.
Abstract: In addition, 1 was also active against oseltamivir-resistant influenza virus strain of A/PR/8/34 with NA-H274Y mutation.
Method: Influenza virus including A/FM/1/47 (H1N1) mouse adapted strain, A/Puerto Rico/8/34 (H1N1), A/Puerto Rico/8/34 (H1N1) with NA-H274Y mutation and A/Aichi/2/68 (H3N2), clinical isolates of 690 (H3 subtype), 699 (H3 subtype), and the influenza B virus.
Result: The viral strains were influenza A/PR/8/34 (H1N1), A/Aichi/2/68 (H3N2), A/FM/1/47 (H1N1) mouse adapted strains, and oseltamivir-resistant influenza virus strains of A/PR/8/34 with NA-H274Y mutation.
Dynamic residue interaction network analysis of the oseltamivir binding site of N1 neuraminidase and its H274Y mutation site conferring drug resistance in influenza A virus.
PMID: 30365885
2018
Journal of medicinal chemistry
Abstract: Besides, 21h was 5- to 86-fold more potent than OSC toward N1, N8, and N1-H274Y mutant NAs in the inhibitory assays.
Abstract: Computational studies provided a plausible rationale for the high potency of 21h against group-1 and N1-H274Y NAs.
Antiviral resistance markers in influenza virus sequences in Mexico, 2000-2017.
Conclusion: These resistant viruses increased their presence as of 2009; among them, H275Y (or H274Y) has been maintained and disseminated by different influenza virus subtypes around the world.
Result: The most frequent codon in H274Y change was UAU (9/10), while the other viruses had CAC (7/10) and CAU (3/10).
Discussion: In the sequences analyzed in this work, the predominant mutation was H275Y in both the H1N1 pdm09 and seasonal H1N1 subtypes, while the H3N2 subtype did not present this mutation (H274Y), and its overall resistance proportion was lower than that of the other two influenza A viruses.
Development of a quadruple qRT-PCR assay for simultaneous identification of highly and low pathogenic H7N9 avian influenza viruses and characterization against oseltamivir resistance.
Introduction: However, studies have shown that the NA R292K (N2 numbering) mutation in H3N2 and H7N9 viruses, H274Y (N2 numbering) mutation in the seasonal H1N1, H1N1pdm09 and H5N1 viruses, emerged during the treatments or through spontaneous changes, resulted in a high level of resistance to oseltamivir and other NAIs.
Structurally Diverse Polyketides From the Mangrove-Derived Fungus Diaporthe sp. SCSIO 41011 With Their Anti-influenza A Virus Activities.
Method: Meanwhile, different influenza A virus subtypes, including A/Puerto Rico/8/34 H274Y (H1N1), A/FM-1/1/47 (H1N1), and A/Aichi/2/68 (H3N2), were multiplied in 10-day-old chick embryo at 37 C.
Result: Antiviral effect of the isolated compounds 1-28 and 5-chloroisorotiorin against different IAV subtypes, including A/Puerto Rico/8/34 H274Y (H1N1), A/FM-1/1/47 (H1N1), and A/Aichi/2/68 (H3N2), were then evaluated.
Result: By the way, 5-chloroisorotiorin (Luo et al.,), a recently reported co-isolated chloroazaphilone derivative obtained with major amount, was also screened for anti-IAV activity, which presented selective inhibition activities against the two IAV subtypes of A/Puerto Rico/8/34 H274Y (H1N1) and A/Aichi/2/68 (H3N2) with the IC50 values of 2.52 +- 0.21 and 10.10 +- 1.84 muM, respectively.
Result: Notably, among the three xanthones (25-27), only 3,8-dihydroxy-6
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
PMID: 29965752
2018
Journal of medicinal chemistry
Abstract: They also showed greater inhibitory activity than OSC toward H274Y and E119V variant.
"A Small-Molecule Compound Has Anti-influenza A Virus Activity by Acting as a ''PB2 Inhibitor""."
Abstract: Our results revealed that D715-2441 possessed antiviral activities against multiple subtypes of influenza A viruses (IAVs) strains, including H1N1, H5N1, H7N9, H3N2, the clinical isolate 690 (H3), and oseltamivir-resistant strains with the H274Y NA mutation, and suppressed the early steps in the virus replication cycle.
Pharmacokinetics and safety of intravenous peramivir, neuraminidase inhibitor of influenza virus, in healthy Japanese subjects.
Abstract: The peramivir plasma and upper respiratory tract fluid levels were significantly higher than the 50% inhibition concentrations for NA enzyme activity (IC50) of epidemic influenza viruses, including those harbouring the H274Y mutation.
Evolution of the neuraminidase gene of seasonal influenza A and B viruses in Thailand between 2010 and 2015.
Method: We analyzed for the presence of NA substitutions associated with either NAI-resistant genotype in different NA subtypes (E119V/I/A/G, H274Y, R292K, and N294S: N2 numbering) or reduced susceptibility genotype to NAIs (Q136K, D151E/V/D, D198N/G/E/Y, I222V/T/K/R/M, S246N, E276D, and R371K: N2 numbering) among influenza A and B viruses.
IV mutation literature information.
PMID: 
2018
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