Bacteriocins are potent antimicrobial peptides that are produced by bacteria. Since their discovery almost a century ago, diverse peptides have been discovered and described, and some are currently used as commercial food preservatives. Many bacteriocins exhibit extensively post-translationally modified structures encoded on complex gene clusters, whereas others have simple linear structures. The molecular structures, mechanisms of action and resistance have been determined for a number of bacteriocins, but most remain incompletely characterized. These gene-encoded peptides are amenable to bioengineering strategies and heterologous expression, enabling metagenomic mining and modification of novel antimicrobials. The ongoing global antimicrobial resistance crisis demands that novel therapeutics be developed to combat infectious pathogens. New compounds that are target-specific and compatible with the resident microbiota would be valuable alternatives to current antimicrobials. As bacteriocins can be broad or narrow spectrum in nature, they are promising tools for this purpose. However, few bacteriocins have gone beyond preclinical trials and none is currently used therapeutically in humans. In this Review, we explore the broad diversity in bacteriocin structure and function, describe identification and optimization methods and discuss the reasons behind the lack of translation beyond the laboratory of these potentially valuable antimicrobials.

细菌素是由细菌产生的有效抗菌肽。自从近一个世纪前发现以来，已经发现和描述了多种肽，其中一些目前被用作商业食品防腐剂。许多细菌素表现出在复杂基因簇上编码的广泛翻译后修饰结构，而其他细菌素则具有简单的线性结构。许多细菌素的分子结构、作用机制和耐药性已经确定，但大多数仍不完全表征。这些基因编码的肽适合生物工程策略和异源表达，从而能够进行宏基因组挖掘和新型抗菌药物的修饰。持续的全球抗菌素耐药性危机要求开发新的疗法来对抗传染性病原体。具有特定靶点且与常驻微生物群相容的新化合物将成为当前抗菌药物的有价值的替代品。由于细菌素本质上可以是广谱或窄谱，因此它们是用于此目的的有前途的工具。然而，很少有细菌素经过临床前试验，目前还没有一种细菌素用于人类治疗。在这篇综述中，我们探讨了细菌素结构和功能的广泛多样性，描述了鉴定和优化方法，并讨论了这些潜在有价值的抗菌药物在实验室之外缺乏转化的原因。