期刊
BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 33, 期 7, 页码 1253-1255出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.33.1253
关键词
p-nitrophenyl active ester; polyethylene glycol; pH; kinetic; lactoferrin; hydrolysis
资金
- New Energy and Industrial Technology Development Organization (NEDO)
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 136h, 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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据