This review covers the most recent advances in the development of inhibitors for the bacterial enzyme sortase A (SrtA). Sortase A (SrtA) is a critical virulence factor present ubiquitously in Gram‐positive bacteria of which many are considered pathogenic. Sortases are key enzymes regulating bacterial adherence to host cells, by anchoring extracellular matrix‐binding proteins to the bacterial outer cell wall. By targeting virulence factors, effective treatment can be achieved, without inducing antibiotic resistance to the treatment. All in all, this would lead to a more sustainable, long‐term approach to treating bacterial infections, including ones that display multiple resistance to current therapeutics. Currently, it appears there are many promising approaches available that have the potential to advance into further clinical development, with peptidomimetic and in vivo active small molecules among the most promising. There are currently no approved drugs on the market targeting SrtA, despite its promise, adding to the relevance of this review article, as it extends to the pharmaceutical industry additionally to academic researchers.

中文翻译：

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分选酶 A 小分子和拟肽抑制剂抗毒治疗的完整评估

本综述涵盖了细菌酶分选酶 A (SrtA) 抑制剂开发的最新进展。分选酶 A (SrtA) 是革兰氏阳性菌中普遍存在的一种关键毒力因子，其中许多细菌被认为是致病性的。分选酶是通过将细胞外基质结合蛋白锚定到细菌外细胞壁来调节细菌粘附到宿主细胞的关键酶。通过针对毒力因子，可以实现有效的治疗，而不会引起对治疗的抗生素耐药性。总而言之，这将带来一种更可持续、更长期的方法来治疗细菌感染，包括对当前治疗方法表现出多重耐药性的细菌感染。目前，似乎有许多有前景的方法有可能进入进一步的临床开发，其中肽模拟物和体内活性小分子是最有前途的。尽管 SrtA 有前景，但目前市场上还没有批准的针对 SrtA 的药物，这增加了这篇综述文章的相关性，因为它除了学术研究人员之外还扩展到制药行业。