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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (08): 1167-1174.    下一篇

综述与进展

药物的聚乙二醇修饰研究进展

路 娟a; 刘清飞b; 罗国安*,a ; 王义明a   

  1. (a清华大学化学系 北京 100084)
    (b清华大学医学院 北京 100084)
  • 收稿日期:2008-09-20 修回日期:2008-11-08 发布日期:2009-08-30
  • 通讯作者: 罗国安

Advances in PEGylation of Drug Conjugates

Lu, Juan a; Liu, Qingfei b; Luo, Guoan*,a; Wang, Yiminga   

  1. (a Department of Chemistry, Tsinghua University, Beijing 100084)
    (b Institute of Biomedicine, Tsinghua University, Beijing 10084)
  • Received:2008-09-20 Revised:2008-11-08 Published:2009-08-30
  • Contact: Luo, Guoan

PDF

8547

被引次数

136 | 13

简要介绍了聚乙二醇(polyethylene glycol, PEG)的生理化学特性, 药物的聚乙二醇修饰的优势, 详细介绍了蛋白质药物和小分子药物的聚乙二醇修饰技术及其在药物研究中的应用进展, 认为药物的聚乙二醇修饰技术通过改变药物的分子结构, 可以有效地改善药物动力学和药效等性质, 增加注射药物的临床应用范围. 同时基于药物的聚乙二醇修饰技术的优势和研究现状, 评述了药物的聚乙二醇修饰技术的发展前景.

关键词: 聚乙二醇修饰技术, 蛋白质, 小分子药物

The current review presents the advances in PEGylation of drug conjugates based on plentiful literatures up to date. The physiochemical properties of PEG [poly(ethylene glycol)] and advantages of PEGylation for drug conjugates are introduced briefly. The technology of PEGylation of protein and small molecular drug conjugates and application to drug investigation are presented in detail. It is found that PEGylation technology can effectively improve the pharmacokinetic and pharmacodynamic properties of drugs by altering the structures of drug conjugates. It also presents a method to extend the area of clinic application of drug conjugates. The foresight of development and investigation of PEGylation of drug conjugates is also brought forward based on the discussion of advantages and investigation status in quo of PEGylation tech-nology.

Key words: small molecular drug, protein, PEGylation