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[Establishment of a cell-based 2009 H1N1 influenza neuraminidase inhibitors evaluation system].
- Source :
-
Yao xue xue bao = Acta pharmaceutica Sinica [Yao Xue Xue Bao] 2010 Mar; Vol. 45 (3), pp. 383-7. - Publication Year :
- 2010
-
Abstract
- This study is to establish a cell-based model targeting to neuraminidase (NA) of the 2009 H1N1 influenza A virus. NA is an influenza virus structural protein with enzymatic activity of the cleavage of HA-sialic acid interaction to release new viral particles from cells. A model of HIV-1 (pNL4-3.Luc.R(-)E(-)) based pseudovirions packed with HA [hemagglutinin, A/VietNam/1203/2004 (H5N1)] and NA [A/California/04/2009 (H1N1)] was established to evaluate compounds activities on NA function. The viral release can be blocked by neuraminidase inhibitors, oseltamivir and oseltamivir carboxylate, with IC50 of (61 +/- 31) nmol L(-1) and (5.5 +/- 2.9) nmol L(-1) respectively. A point mutation of H275Y on NA leads oseltamivir-resistance. This corresponding mutation was introduced into the system which was also confirmed by oseltamivir and oseltamivir carboxylate.
- Subjects :
- Cell Line, Tumor
Drug Resistance, Viral genetics
Enzyme Inhibitors pharmacology
HEK293 Cells
HIV-1 genetics
Hemagglutinin Glycoproteins, Influenza Virus genetics
Hemagglutinin Glycoproteins, Influenza Virus metabolism
Humans
Influenza A Virus, H1N1 Subtype genetics
Influenza A Virus, H1N1 Subtype metabolism
Influenza A Virus, H5N1 Subtype genetics
Influenza A Virus, H5N1 Subtype metabolism
Mutation
Neuraminidase genetics
Neuraminidase metabolism
Plasmids
Transfection
Virus Internalization
Influenza A Virus, H1N1 Subtype drug effects
Influenza A Virus, H5N1 Subtype drug effects
Neuraminidase antagonists & inhibitors
Oseltamivir analogs & derivatives
Oseltamivir pharmacology
Subjects
Details
- Language :
- Chinese
- ISSN :
- 0513-4870
- Volume :
- 45
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Yao xue xue bao = Acta pharmaceutica Sinica
- Publication Type :
- Academic Journal
- Accession number :
- 21351517