%0 Journal Article
%T Investigation on Site-specific PEGylation of Glucagon-like Peptide-1<br>胰高血糖素样肽-1的聚乙二醇定点修饰
%A 张磊
%A 翟艳琴
%A 雷建都
%A 马光辉
%A 苏志国
%J 过程工程学报
%D 2009
%I 
%X 采用分子量为5 kDa的单甲氧基聚乙二醇琥珀酰亚胺碳酸酯(mPEG-SC)修饰胰高血糖素样肽-1(GLP-1),建立了GLP-1的定点修饰反应及分离纯化工艺,考察了修饰反应各因素对单修饰产物得率及体外活性的影响,得到优化修饰条件为:pH 7.5, 50 mmol/L Na_2HPO_4-NaH_2PO_4缓冲液,GLP-1浓度1 mg/mL, PEG/GLP-1摩尔比2:1,4℃下反应1 h.在此条件下,单修饰PEG-GLP-1得率达50%.反相高效液相色谱分离纯化所得单修饰产品纯度达98%,体外活性保留为未修饰GLP-1的86%,其在Sprague-Dawley远交群大鼠体内的循环半衰期为60 min,比原肽提高了20倍.
%K glucagon-like peptide-1
%K monomethoxy polyethylene glycol succinimidyl carbonate
%K site-specific PEGylation<br>胰高血糖素样肽-1
%K 聚乙二醇
%K 定点修饰
%U http://www.alljournals.cn/get_abstract_url.aspx?pcid=5B3AB970F71A803DEACDC0559115BFCF0A068CD97DD29835&cid=3FCF8B1A330466D5&jid=B9EE12934D19905403D996AE65CEEEED&aid=B1C359A84C27B3A5722D57E211A0FB8D&yid=DE12191FBD62783C&vid=9CF7A0430CBB2DFD&iid=B31275AF3241DB2D&sid=827D3389B7A27A64&eid=778972EBEFCE1267&journal_id=1009-606X&journal_name=过程工程学报&referenced_num=1&reference_num=11