Zhang Dan, He Yu, Ye Yang, Ma Yanni, Zhang Peng, Zhu Hongxia, Xu Ningzhi, Liang Shufang
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University / Collaborative Innovation Center for Biotherapy, Chengdu 610041, China.
Department of Urinary Surgery, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
Protein Pept Lett. 2019;26(8):564-578. doi: 10.2174/1573406415666190222141905.
Antimicrobial Peptides (AMPs) are short amphipathic biological molecules generally with less than 100 amino acids. AMPs not only present high bioactivities against bacteria, fungi or protists-induced infections, but also play important roles in anticancer activity, immune response and inflammation regulation. AMPs are classified as ribosomally synthesized, non-ribosomally synthesized and post-translationally modified, non-ribosomally synthesized ones and several synthetic or semisynthetic peptides according to their synthesis with or without the involvement of ribosomes. The molecular characterization and bioactivity action mechanisms are summarized for several ribosomally synthesized AMPs and main non-ribosomally synthesized members (cyclopeptides, lipopeptides, glycopeptides, lipoglycopeptides). We also analyze challenges and new strategies to overcome drug resistance and application limitations for AMP discovery. In conclusion, the growing novel small molecular AMPs have huge therapeutic potentials of antibacterial, antiviral, anticancer and immunoregulatory bioactivities through new techniquesdriven drug discovery strategy including bioinformatics prediction, de novo rational design and biosynthesis.
抗菌肽（AMPs）是一类短的两亲性生物分子，通常由少于100个氨基酸组成。抗菌肽不仅对细菌、真菌或原生生物引起的感染具有高生物活性，而且在抗癌活性、免疫反应和炎症调节中发挥重要作用。根据其合成是否涉及核糖体，抗菌肽可分为核糖体合成、非核糖体合成和翻译后修饰的非核糖体合成抗菌肽，以及几种合成或半合成肽。本文总结了几种核糖体合成抗菌肽和主要非核糖体合成成员（环肽、脂肽、糖肽、脂糖肽）的分子特征和生物活性作用机制。我们还分析了抗菌肽发现过程中克服耐药性和应用局限性的挑战及新策略。总之，通过包括生物信息学预测、从头合理设计和生物合成等新技术驱动的药物发现策略，越来越多新型小分子抗菌肽具有抗菌、抗病毒、抗癌和免疫调节生物活性的巨大治疗潜力。
