抗菌肽的设计与优化研究进展

Progress on the design and optimization of antimicrobial peptides

抗菌肽是一类广泛存在于自然界,具有广谱抗菌活性的多肽类物质,因其独特的抗菌作用机制被视为传统抗生素的新型替代药物。由于天然抗菌肽往往存在活性不强、代谢不稳定等缺点,导致其开发与应用受到很多限制,因此基于天然抗菌肽的设计与优化成为了近期研究热点。本文主要针对核糖体抗菌肽展开,总结其相关的一些衍生肽的设计和优化策略,包括合理的一级结构改造、环化策略、计算机辅助策略等,通过分析总结,期望对抗菌肽设计以及抗感染药物的研发提供思路。

Antimicrobial peptides(AMPs)are a class of peptides widely existing in nature with broad-spectrum antimicrobial activity.It is considered as a new alternative to traditional antibiotics because of its unique mechanism of antimicrobial activity.The development and application of natural AMPs are limited due to their drawbacks such as low antimicrobial activity and unstable metabolism.Therefore,the design and optimization of derived peptides based on natural antimicrobial peptides have become recent research hotspots.In this paper,we focus on ribosomal AMPs and summarize the design and optimization strategies of some related derived peptides,which include reasonable primary structure modification,cyclization strategy and computer-aided strategy.We expect to provide ideas for the design and optimization of antimicrobial peptides and the development of anti-infective drugs through analysis and summary in this paper.