摘要
聚乙二醇修饰具有抵抗蛋白酶降解、提高稳定性、延长体内半衰期、降低免疫原性等优点,能够有效地改善蛋白质多肽类药物的临床药效。而聚乙二醇的定点修饰由于能够获得均一性和高活性保留率的产物,并能提高产物的产率,已经引起了广泛关注。本文概述近年来聚乙二醇定点修饰蛋白质多肽类药物方面的研究进展,并对聚乙二醇定点修饰技术的发展趋势进行了展望。
PEGylation has been used as an effective strategy to overcome several shortcomings of pro teins and pepetides for therapeutic uses. The therapeutic efficacy of PEGylated protein and peptide drugs can be improved through reducing their immunogenicity and proteolysis, increasing their stability and pro longing their circulating halflife. Furthermore, sitespecific PEGylation is an attractive approach for the maximizing the bioavailability of drugs, because a homogeneously modified product with high activity reten tion and yield can be achieved. Recent advances in sitespecific PEGylation were reviewed and the future trends in sitespecific PEGylation were discussed.
出处
《药学与临床研究》
2013年第4期360-365,共6页
Pharmaceutical and Clinical Research
基金
"重大新药创制"科技重大专项(编号:2012ZX09103-101-016)
关键词
聚乙二醇
定点修饰
蛋白质
Polyethylene glycol
Site-specific PEGylation
Protein
