Phenyl Linker-Induced Dense PEG Conformation Improves the Efficacy of C-Terminally MonoPEGylated Staphylokinase | |
Xue, Xiaoying1,2; Li, Dongxia1; Yu, Jingkai1; Ma, Guanghui1; Su, Zhiguo1; Hu, Tao1 | |
刊名 | BIOMACROMOLECULES |
2013-02-01 | |
卷号 | 14期号:2页码:331-341 |
英文摘要 | PEGylation can improve the protein efficacy by prolonging serum half-life and reducing proteolytic sensitivity and immunogenicity. However, PEGylation may decrease the bioactivity of a protein by interfering with binding of its substrate or receptors. Here, staphylokinase (SAK), a thrombolysis agent for therapy of myocardial infarction, was mono-PEGylated at the C-terminus of SAK far from its bioactive domain. Phenyl, propyl, and amyl moieties were used as linkers between SAK and polyethylene glycol (PEG), respectively. Flexible propyl and amyl linkers lead to loose conformation. In contrast, rigid and hydrophobic phenyl linker induces dense PEG conformation that can extensively shield most domains adjacent to C-terminus (e.g., the antigen epitopes and proteolytic sites) of SAK and inefficiently shield its bioactive domain. As compared with loose PEG conformation, dense PEG conformation is more efficient to maintain the bioactivity, increase the plasma half-life, and decrease the proteolytic sensitivity and immunogenicity of the PEGylated SAK. |
WOS标题词 | Science & Technology ; Life Sciences & Biomedicine ; Physical Sciences |
类目[WOS] | Biochemistry & Molecular Biology ; Chemistry, Organic ; Polymer Science |
研究领域[WOS] | Biochemistry & Molecular Biology ; Chemistry ; Polymer Science |
关键词[WOS] | SITE-SPECIFIC PEGYLATION ; HUMAN GROWTH-HORMONE ; RECOMBINANT STAPHYLOKINASE ; THROMBOLYTIC PROPERTIES ; POLY(ETHYLENE GLYCOL) ; DRUG-DELIVERY ; GENETIC-CODE ; X-RAY ; HEMOGLOBIN ; CONJUGATION |
收录类别 | SCI |
语种 | 英语 |
WOS记录号 | WOS:000314908500006 |
公开日期 | 2015-05-27 |
内容类型 | 期刊论文 |
源URL | [http://ir.ipe.ac.cn/handle/122111/13559] |
专题 | 过程工程研究所_研究所(批量导入) |
作者单位 | 1.Chinese Acad Sci, Natl Key Lab Biochem Engn, Inst Proc Engn, Beijing 100190, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100190, Peoples R China |
推荐引用方式 GB/T 7714 | Xue, Xiaoying,Li, Dongxia,Yu, Jingkai,et al. Phenyl Linker-Induced Dense PEG Conformation Improves the Efficacy of C-Terminally MonoPEGylated Staphylokinase[J]. BIOMACROMOLECULES,2013,14(2):331-341. |
APA | Xue, Xiaoying,Li, Dongxia,Yu, Jingkai,Ma, Guanghui,Su, Zhiguo,&Hu, Tao.(2013).Phenyl Linker-Induced Dense PEG Conformation Improves the Efficacy of C-Terminally MonoPEGylated Staphylokinase.BIOMACROMOLECULES,14(2),331-341. |
MLA | Xue, Xiaoying,et al."Phenyl Linker-Induced Dense PEG Conformation Improves the Efficacy of C-Terminally MonoPEGylated Staphylokinase".BIOMACROMOLECULES 14.2(2013):331-341. |
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