药物的聚乙二醇修饰研究进展有机化学.pdfVIP

2009 年第 29 卷 有 机 化 学 Vol. 29, 2009 第 8 期, 1167～1174 Chinese Journal of Organic Chemistry No. 8, 1167～1174 ·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 a ( 清华大学化学系 北京 100084) (b 清华大学医学院 北京 100084) 摘要 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 , 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 Advances in PEGylation of Drug Conjugates Lu, Juana Liu, Qingfeib Luo, Guoan*,a Wang, Yiminga a ( Department of Chemistry, Tsinghua University, Beijing 100084) (b Institute of Biomedicine, Tsinghua University, Beijing 10084) Abstract 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 PE- Gylation for drug conjugates are introduced briefly. The technology of PEGylation of protein and small mo- lecular drug conjugates and application to drug investigation are presented in detail. It is found that PEGyla- tion 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 conjug