Site-specific PEGylation of proteins containing unnatural amino acids

被引:207
作者
Deiters, A
Cropp, TA
Summerer, D
Mukherji, M
Schultz, PG
机构
[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA
关键词
D O I
10.1016/j.bmcl.2004.09.059
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Here, we report a generally applicable PEGylation methodology based on the site-specific incorporation of para-azidophenylalanine into proteins in yeast. The azido group was used in a mild [3+2] cycloaddition reaction with an alkyne derivatized PEG reagent to afford selectively PEGylated protein. This strategy should be useful for the generation of selectively PEGylated proteins for therapeutic applications. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:5743 / 5745
页数:3
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