蛋白质和肽类分子的聚乙二醇化化学

蛋白质和肽类生物大分子聚乙二醇化后，溶解行为改善，稳定性增强，免疫原 性消除或降低，循环半衰期延长，药物动力学优化，因而在生物技术和生物医学中 具有重要的应用前景，聚乙二醇化也逐渐发展成为一种平台技术．随着聚乙二醇化 蛋白质和肽类进入临床试验阶段，聚乙二醇化化学越来越引起研究者的重视．简要 评述第一代和第二代聚乙二醇化化学，主要包括聚乙二醇化学修饰剂的类型与性能 比较等．

Chemistry for Pegylation of Protein and Peptide Molecules

The pegylated proteins and peptides have found promising applications in biotechnological and biomedical fields due to the improved solubility, thermal and mechanical stability, reduced antigenicity and immunogenicity, enhanced circulating half lives, optimized pharmacokinetic and pharmacodynamic properties. Consequently, pegylation gradually becomes a platform technology. The importance of chemistry of protein and peptide pegylation has attracted more and more attentions as more PEG conjugates have reached late phase clinical trials. In this paper, the first generation and second generation pegylation chemistry is briefly reviewed, mainly including the different types of PEG chemical modifiers and their performance comparison.