肽菌素：多样性、生物活性与生物合成。

Hou Xuewen, Sun Ruonan, Feng Yanyan, Zhang Runfang, Zhu Tianjiao, Che Qian, Zhang Guojian, Li Dehai

Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.

Laboratory for Marine Drugs and Bioproducts, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China.

Eng Microbiol. 2022 Jun 5;2(3):100026. doi: 10.1016/j.engmic.2022.100026. eCollection 2022 Sep.

Peptaibols are a large family of linear, amphipathic polypeptides consisting of 5-20 amino acid residues generated from the fungal nonribosomal peptide synthetase (NRPS) pathway. With a relatively high content of non-proteinogenic amino acids such as -aminoisobutyrate (Aib) and isovaline (Iva) in the skeleton, peptaibols exhibit a wide range of biological activities, including anti-microbial, cytotoxic, and neuroleptic effects. With five peptaibols brought to market for use as biocontrol agents, this class of peptides has received increasing attention from both biochemists and pharmacologists. In this review, we summarized the progress made in structural characterization, elucidation of biosynthetic pathways, and investigation of biosynthesis elucidation and bioactivities, to promote further efforts to develop peptaibols as pharmaceuticals.

短杆菌肽是一大类线性两亲性多肽，由5至20个氨基酸残基组成，通过真菌非核糖体肽合成酶（NRPS）途径产生。由于其骨架中含有相对较高含量的非蛋白质氨基酸，如α-氨基异丁酸（Aib）和异缬氨酸（Iva），短杆菌肽具有广泛的生物活性，包括抗菌、细胞毒性和抗精神病作用。随着五种短杆菌肽作为生物防治剂上市，这类肽受到了生物化学家和药理学家越来越多的关注。在这篇综述中，我们总结了在结构表征、生物合成途径阐明以及生物合成阐明和生物活性研究方面取得的进展，以促进进一步努力将短杆菌肽开发成药物。