文章基本信息

标题：Amino Group PEGylation of Bovine Lactoferrin by Linear Polyethylene Glycol-p-nitrophenyl Active Esters
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作者：Kanako Kato ; Naomi Tamaki ; Yoshiki Saito 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2010
卷号：33
期号：7
页码：1253-1255
DOI：10.1248/bpb.33.1253
出版社：The Pharmaceutical Society of Japan
摘要：PEGylation, the covalent attachment of polyethylene glycol (PEG) to pharmaceutical proteins, is regarded as an extremely useful procedure to generate protein drugs with intensified therapeutic properties. We examined the amino group modification of bovine lactoferrin (bLF) with linear PEG- p -nitrophenyl active esters. At pH 5.0, we specifically observed the formation of mono-PEGylated bLF in high yields. PEG-conjugation reactions advanced slowly and reached a steady state by 48 h in a buffer at pH 5.0. The hydrolysis half-lives of 5-kDa and 30-kDa PEG- p -nitrophenyl active esters at pH 5.0 were estimated to be approximately 117 and 136 h, respectively. The slow reaction and hydrolysis rates of PEG- p -nitrophenyl active esters may contribute to the formation of mono-PEGylated bLF that could not be obtained by PEGylation with linear N -hydroxysuccinimide (NHS) activated PEG.
关键词：p-nitrophenyl active ester;polyethylene glycol;pH;kinetic;lactoferrin;hydrolysis