[关键词]
[摘要]
随着耐药致病菌的传播和致病菌耐药谱的扩大,抗菌药物的临床选择已经非常有限,不寻求直接杀灭病原菌而仅抑制其致病能力正成为一种新的抗感染策略。分泌系统是革兰阴性菌最为重要的毒力因子之一,承担各种致病相关效应蛋白和遗传物质的分泌和转运,在不同病原菌中结构和功能相对保守,因而被认为是抗毒力因子药物的理性靶标,受到越来越多研究者的重视。按照化合物的结构类型,总结了目前在研革兰阴性菌分泌系统小分子抑制剂的结构特征和构效关系,并对此类抑制剂的开发难点进行了探讨,旨在为更多分泌系统抑制剂的研发提供参考。
[Key word]
[Abstract]
With the spread of drug-resistant pathogens and the expansion of drug resistance spectrum, the clinical choice of antibacterial drugs has been quite restricted. To inhibit the pathogenicity instead of directly killing pathogens became a new anti-infective strategy. As the vital virulence factors of Gram-negative bacteria, secretion systems are responsible for the secretion and translocation of various pathogenic effector proteins and genetic material, with relatively conserved structures and functions among different pathogens, and thus were believed as potential drug targets by researchers. According to the type of compounds, structural characteristics and structure-function relationship of the small molecule inhibitors of the main secretory systems of Gram-negative bacteria are reviewed, and the limitation and development prospects of these inhibitors are discussed for further research.
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