| 蛋白药物的聚乙二醇定点修饰策略与最佳位点 |
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| 引用本文： | 王旭东,李晓晖,苏志国,修志龙. 蛋白药物的聚乙二醇定点修饰策略与最佳位点[J]. 中国生物工程杂志, 2010, 30(4): 101-109 |
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| 作者姓名： | 王旭东 李晓晖 苏志国 修志龙 |
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| 作者单位： | 1.大连理工大学环境与生命学院 大连 116024 2.中国科学院过程工程研究所生化工程国家重点实验室 北京 100190 |
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| 基金项目： | 国家“863”计划资助项目(2007AA021604) |
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| 摘 要： | 聚乙二醇修饰是一种改善蛋白质药物临床药效行之有效的方法。聚乙二醇修饰具有延长蛋白质药物在体内的半衰期、降低免疫原性和延缓蛋白酶降解、提高稳定性和溶解性等优点。而聚乙二醇的定点修饰由于能够获得均一性和高活性保留率的产物，并能提高产率，已经引起了广泛关注。综述了近年来聚乙二醇定点修饰蛋白质药物方面的研究进展，着重介绍了聚乙二醇定点修饰的策略及最佳修饰位点，并对聚乙二醇定点修饰技术的发展趋势进行了展望。
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| 关 键 词： | 聚乙二醇定点修饰 固相修饰 位置异构体 分子模拟 |
| 收稿时间： | 2009-12-30 |
| 修稿时间： | 2010-03-01 |
Site-specific PEGylation Strategies and Suitable Modified Sites of Protein Drugs |
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| WANG Xu-dong,LI Xiao-hui,SU Zhi-guo,XIU Zhi-long. Site-specific PEGylation Strategies and Suitable Modified Sites of Protein Drugs[J]. China Biotechnology, 2010, 30(4): 101-109 |
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| Authors: | WANG Xu-dong LI Xiao-hui SU Zhi-guo XIU Zhi-long |
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| Affiliation: | 1.School of Environmental and Biological Science and Technology, Dalian University of Technology, Dalian 116024, China.2.State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, Chinese Academy of Sciences, Beijing 100190, China |
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| Abstract: | PEGylation,the covalent attachment of polyethylene glycol (PEG) to proteins,has been used as an effective strategy to overcome several shortcomings of proteins for therapeutic uses.The therapeutic efficacy of PEGylated protein drugs can be improved through prolonging their circulating half-life,reducing their immunogenicity and proteolysis,and increasing their stability and solubility.Furthermore,site-specific PEGylation is an attractive approach for the maximizing the bioavailability of drugs,because a hom... |
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| Keywords: | Site-specific PEGylation Solid phase PEGylation Positional isomer Molecular simulation |
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