论文部分内容阅读
多肽类药物的蛋白酶降解稳定性是决定该药物是否长效的重要因素。本文综述了近年来用以提高多肽药物蛋白酶降解稳定性的主要策略,尤其对特定位置如N端、C端及氨基酸侧链等的化学结构修饰进行了分类和概述,探讨了这些修饰方法对发展多肽药物的贡献及不足。
Peptide protease degradation stability is to determine the long-term effectiveness of the drug is an important factor. This review summarizes the major strategies used to improve the proteolytic stability of peptide drugs in recent years. In particular, the chemical structural modifications of specific sites such as N-terminal, C-terminal and amino acid side chains are reviewed and summarized. The effects of these modifications on development Polypeptide drug contributions and deficiencies.