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Basic Characteristics of Mutations
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Mutation Site
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H274Y |
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Mutation Site Sentence
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CS-8958 also significantly reduced the titers of an oseltamivir-resistant H1N1 virus with a neuraminidase H274Y substitution in a mouse infection model. |
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Mutation Level
|
Amino acid level |
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Mutation Type
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Nonsynonymous substitution |
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Gene/Protein/Region
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NA |
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Standardized Encoding Gene
|
NA
|
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Genotype/Subtype
|
H1N1 |
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Viral Reference
|
-
|
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Functional Impact and Mechanisms
|
|
Disease
|
Influenza A
|
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Immune
|
- |
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Target Gene
|
-
|
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Clinical and Epidemiological Correlations
|
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Clinical Information
|
- |
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Treatment
|
oseltamivir |
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Location
|
- |
|
Literature Information
|
|
PMID
|
20047917
|
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Title
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Laninamivir prodrug CS-8958, a long-acting neuraminidase inhibitor, shows superior anti-influenza virus activity after a single administration
|
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Author
|
Kubo S,Tomozawa T,Kakuta M,Tokumitsu A,Yamashita M
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Journal
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Antimicrobial agents and chemotherapy
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Journal Info
|
2010 Mar;54(3):1256-64
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Abstract
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Two neuraminidase (NA) inhibitors, zanamivir (Relenza) and oseltamivir phosphate (Tamiflu), have been licensed for use for the treatment and prophylaxis of influenza. We have reported on laninamivir (code name, R-125489), a novel neuraminidase inhibitor, and have discovered that the laninamivir prodrug CS-8958 worked as a long-acting neuraminidase inhibitor in a mouse influenza virus infection model when it is intranasally administered. In this study, CS-8958 was administered just once 7 days before infection and showed significant efficacy in vivo. The efficacy of a single administration of CS-8958 after viral infection was then compared with that of repeated administrations of oseltamivir phosphate or zanamivir in mice and ferrets. CS-8958 showed efficacy superior or similar to the efficacies of the two licensed NA inhibitors. CS-8958 also significantly reduced the titers of an oseltamivir-resistant H1N1 virus with a neuraminidase H274Y substitution in a mouse infection model. These results suggest that since CS-8958 is characteristically long lasting in the lungs, it may be ideal for the prophylaxis and treatment of influenza.
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Sequence Data
|
-
|