摘要
抗菌肽因其作用机制独特,不易产生耐药性,有望成为替代传统抗生素的新型候选药物。天然抗菌肽在动物、植物和微生物等生物体内广泛存在,但因细胞选择性差、体内不稳定以及生产成本高等问题限制了其开发应用。从头设计具有重复单元的新型抗菌肽,与天然抗菌肽相比具有序列短、二级结构特征明显、抗菌活性高以及毒性低等优势,逐渐成为新型抗菌药物开发的热点。本文作者对抗菌肽的基本概念、结构类型和作用机制进行概括,对具备重复单元特征的新型抗菌肽的设计策略以及其在改善细胞毒性和蛋白酶稳定性等方面采取的修饰方法进行总结,以期为新型抗菌肽的设计与开发提供有价值的参考。
Antimicrobial peptides(AMPs)are expected to be the novel candidate drugs to replace traditional antibiotics due to their unique mechanisms and ability to combat drug-resistant bacteria.Natural AMPs were widely distributed in animals,plants,microorganisms and other organisms,but poor cellular selectivity,instability in vivo and high production costs have limited their development and application.Compared with natural AMPs,novel AMPs designed with repeat units have the advantages of short sequences,significant secondary structures,high antimicrobial activity and low toxicity,which are gradually becoming a hot spot for the development of new antimicrobial agents.The basic concepts,the structure types and mechanisms of AMPs were outlined,the design strategies of novel AMPs with repeat units and the peptide modification methods in terms of improving cytotoxicity and protease stability were summarized in this article,in order to provide an important reference for the design and development of novel AMPs.
作者
娜黑芽
NA Heiya(College of Life Sciences,Inner Mongolia Agricultural University,Hohhot 010018,China)
出处
《中国药物化学杂志》
2025年第3期226-241,共16页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(82060624)。
关键词
抗菌肽
结构
从头设计
重复单元
antimicrobial peptide
structure
de novo design
repeat units
