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提高抗菌肽抗酶解稳定性的结构修饰策略研究进展

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随着抗生素耐药性问题日益严重,抗菌肽作为一种新型抗生素替代药物引起广泛关注,然而抗菌肽较低的抗酶解稳定性严重限制了其临床应用。为提高抗菌肽的抗酶解稳定性,目前已开发多种结构修饰策略。本文综述了其中3种修饰策略——引入非天然氨基酸、肽链环化和化学基团修饰的基本原理及应用实例,分析其优缺点和潜在的优化方向,同时对抗菌肽酶稳定性增强策略的发展趋势和潜在挑战进行展望,旨在为抗菌肽的进一步研究和开发提供有效策略。
Modification strategies for improving anti-enzymatic stability of antimicrobial peptides
As antibiotic resistance becomes increasingly concerning,antimicrobial peptides,as a new type of antibiotic alternative,have attracted more attention.However,the low enzymatic stability of antimicrobial peptides severely limits their clinical applications.To address this issue,researchers have developed various structural modification strategies,including the introduction of unnatural amino acids,peptide chain cyclization and chemical group modification.This article reviews the basic principles and cases of the above modification strategies analyzes the advantages and disadvantages of different modification strategies and recommends ways these strategies can be optimized.In addition,this article predicts the developments of and potential challenges to strategies for enhancing enzymatic stability of antimicrobial peptides in the hope of providing references for subsequent research and development of antimicrobial peptides.

antimicrobial peptidesenzymatic stabilitystructural optimization strategy

姜淑元、张昌浩、王陶然

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延边大学药学院,吉林 延吉 133002

军事医学研究院国家安全特需药品全国重点实验室,北京 100850

抗菌肽 酶稳定性 结构优化策略

2025

中国药理学与毒理学杂志
军事医学科学院毒物药物研究所,中国药理学会,中国毒理学会

中国药理学与毒理学杂志

北大核心
影响因子:1.182
ISSN:1000-3002
年,卷(期):2025.39(1)