多肽和蛋白质的聚乙二醇化修饰方法

聚乙二醇是一类具有独特理化性质的大分子聚合物。多肽和蛋白质类药物经聚 乙二醇共价修饰后能明显改善其药代学和药效学性质，如降低免疫原性、增加对蛋 白水解酶的稳定性、增加水溶性及延长体内的半衰期等。蛋白质的聚乙二醇化修饰 研究已取得较好的效果，多肽的聚乙二醇化修饰研究起步较晚。对近年来多肽和蛋 白质的聚乙二醇化修饰方法进行了综述，主要介绍了对多肽和蛋白质的N端、C端及 某些氨基酸侧链进行选择性聚乙二醇化修饰的方法。

Methods of Peptide and Protein Pegylation

With typical molecular weights of 500 ～20000, polyethylene glycol (PEG) is nontoxic, nonimmunogenic and soluble in aqueous solutions as well as in most organic solvents. The covalent attachment of PEG (pegylation) to peptides and proteins can significantly improve their pharmacological and biological properties, such as shielding immunogenic epitopes, preventing degradation by proteolytic enzymes, increasing solubility, reducing renal filtration and altering biodistribution. Some methods in this field especially on site- directed pegylation for amino, carboxyl and thiol groups of peptides and proteins are reviewed.