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PEGylated recombinant human interferon-omega as a long-acting antiviral agent: Structure, antiviral activity and pharmacokinetics
Alternative TitleAntiviral Res.
Yu, Weili1,3; Yu, Changming2; Wu, Ling1,3; Fang, Ting2; Qiu, Rui1; Zhang, Jinlong2; Yu, Ting2; Fu, Ling2; Chen, Wei2; Hu, Tao1
2014-08-01
Source PublicationANTIVIRAL RESEARCH
ISSN0166-3542
Volume108Issue:AUGPages:142-147
AbstractRecombinant human interferon-omega (rhIFN-omega) exhibits a potent antiviral activity. Because of poor pharmacokinetics (PK) of rhIEN-omega, frequent dosing of rhIFN-omega is necessitated to achieve the sustained antiviral efficacy. PEGylation can efficiently improve the PK of rhIFN-omega while substantially decrease its bioactivity. The structure, antiviral activity and PK of the PEGylated rhIEN-omega were measured to establish their relationship with PEGylation sites, polyethylene glycol (PEG) mass and PEG structure. Accordingly, N-terminus and the lysine residues were selected as the PEGylation sites. PEGs with M-w of 20 kDa and 40 kDa were used to investigate the effect of PEG mass. Linear and branched PEGs were used to investigate the effect of PEG structure. PEGylation decreased the antiviral activity of rhIEN-omega and improved its PK. The PEGylation sites determine the bioactivity of the PEGylated rhIFN-omega and the conjugated PEG mass determines the PK. N-terminally PEGylated rhIFN-omega with 40 kDa linear PEG maintains 21.7% of the rhIFN-omega antiviral activity with a half-life of 139.6 h. Thus, N-terminally PEGylated rhIFN-omega with linear 40 kDa PEG is a potential antiviral agent for long-acting treatment of the viral diseases. (C) 2014 Elsevier B.V. All rights reserved.; Recombinant human interferon-omega (rhIFN-omega) exhibits a potent antiviral activity. Because of poor pharmacokinetics (PK) of rhIEN-omega, frequent dosing of rhIFN-omega is necessitated to achieve the sustained antiviral efficacy. PEGylation can efficiently improve the PK of rhIFN-omega while substantially decrease its bioactivity. The structure, antiviral activity and PK of the PEGylated rhIEN-omega were measured to establish their relationship with PEGylation sites, polyethylene glycol (PEG) mass and PEG structure. Accordingly, N-terminus and the lysine residues were selected as the PEGylation sites. PEGs with M-w of 20 kDa and 40 kDa were used to investigate the effect of PEG mass. Linear and branched PEGs were used to investigate the effect of PEG structure. PEGylation decreased the antiviral activity of rhIEN-omega and improved its PK. The PEGylation sites determine the bioactivity of the PEGylated rhIFN-omega and the conjugated PEG mass determines the PK. N-terminally PEGylated rhIFN-omega with 40 kDa linear PEG maintains 21.7% of the rhIFN-omega antiviral activity with a half-life of 139.6 h. Thus, N-terminally PEGylated rhIFN-omega with linear 40 kDa PEG is a potential antiviral agent for long-acting treatment of the viral diseases. (C) 2014 Elsevier B.V. All rights reserved.
KeywordInterferon-omega Antiviral Agent Pegylation Pharmacokinetics
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
DOI10.1016/j.antiviral.2014.06.003
URL查看原文
Indexed BySCI
Language英语
WOS KeywordCHRONIC HEPATITIS-C ; VIRUS ; ALPHA ; STAPHYLOKINASE
WOS Research AreaPharmacology & Pharmacy ; Virology
WOS SubjectPharmacology & Pharmacy ; Virology
WOS IDWOS:000340220400017
Citation statistics
Cited Times:3[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Version出版稿
Identifierhttp://ir.ipe.ac.cn/handle/122111/11594
Collection研究所(批量导入)
Affiliation1.Chinese Acad Sci, Inst Proc Engn, Natl Key Lab Biochem Engn, Beijing 100190, Peoples R China
2.Beijing Inst Biotechnol, Beijing 100071, Peoples R China
3.Univ Chinese Acad Sci, Beijing 100190, Peoples R China
Recommended Citation
GB/T 7714
Yu, Weili,Yu, Changming,Wu, Ling,et al. PEGylated recombinant human interferon-omega as a long-acting antiviral agent: Structure, antiviral activity and pharmacokinetics[J]. ANTIVIRAL RESEARCH,2014,108(AUG):142-147.
APA Yu, Weili.,Yu, Changming.,Wu, Ling.,Fang, Ting.,Qiu, Rui.,...&Hu, Tao.(2014).PEGylated recombinant human interferon-omega as a long-acting antiviral agent: Structure, antiviral activity and pharmacokinetics.ANTIVIRAL RESEARCH,108(AUG),142-147.
MLA Yu, Weili,et al."PEGylated recombinant human interferon-omega as a long-acting antiviral agent: Structure, antiviral activity and pharmacokinetics".ANTIVIRAL RESEARCH 108.AUG(2014):142-147.
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