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Mono-N-terminal poly(ethylene glycol)-protein conjugates

被引：242
作者：
Kinstler, O [1 ]
Molineux, G [1 ]
Treuheit, M [1 ]
Ladd, D [1 ]
Gegg, C [1 ]
机构：
[1] Amgen Inc, Thousand Oaks, CA 91320 USA
来源：
ADVANCED DRUG DELIVERY REVIEWS | 2002年 / 54卷 / 04期
关键词：
poly(ethylene glycol); polymer-modified proteins; site-specific conjugation; therapeutic proteins;
D O I：
10.1016/S0169-409X(02)00023-6
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A site-directed method of joining proteins to poly(ethylene glycol) is presented which allows for the preparation of essentially homogeneous PEG-protein derivatives with a single PEG chain conjugated to the amine terminus of the protein. This selectivity is achieved by conducting the reductive alkylation of proteins with PEG-aldehydes at lower pH. Working examples demonstrating the application of this method to improve the delivery characteristics and therapeutic value of several proteins are provided. (C) 2002 Published by Elsevier Science B.V.
引用
收藏
页码：477 / 485
页数：9
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