钙依赖性脂肽抗生素：结构、作用机制与药物化学
The calcium-dependent lipopeptide antibiotics: structure, mechanism, & medicinal chemistry.
作者信息
Wood Thomas M, Martin Nathaniel I
机构信息
Department of Chemical Biology & Drug Discovery , Utrecht Institute for Pharmaceutical Sciences , Utrecht University , Universiteitsweg 99 , 3584 CG Utrecht , The Netherlands.
Biological Chemistry Group , Institute of Biology Leiden , Leiden University , Sylvius Laboratories , Sylviusweg 72 , 2333 BE Leiden , The Netherlands . Email:
出版信息
Medchemcomm. 2019 Mar 21;10(5):634-646. doi: 10.1039/c9md00126c. eCollection 2019 May 1.
To push back the growing tide of antibacterial resistance the discovery and development of new antibiotics is a must. In recent years the calcium-dependent lipopeptide antibiotics (CDAs) have emerged as a potential source of new antibacterial agents rich in structural and mechanistic diversity. All CDAs share a common lipidated cyclic peptide motif containing amino acid side chains that specifically chelate calcium. It is only in the calcium bound state that the CDAs achieve their potent antibacterial activities. Interestingly, despite their common structural features, the mechanisms by which different CDAs target bacteria can vary dramatically. This review provides both a historic context for the CDAs while also addressing the state of the art with regards to their discovery, optimization, and antibacterial mechanisms.
为了击退日益增长的抗菌耐药性浪潮，必须发现和开发新的抗生素。近年来，钙依赖性脂肽抗生素（CDAs）已成为一种潜在的新型抗菌剂来源，其结构和作用机制具有丰富的多样性。所有CDAs都有一个共同的脂化环肽基序，其氨基酸侧链能特异性螯合钙。只有在与钙结合的状态下，CDAs才能发挥其强大的抗菌活性。有趣的是，尽管它们具有共同的结构特征，但不同CDAs靶向细菌的机制可能有很大差异。本综述既为CDAs提供了历史背景，也探讨了它们在发现、优化和抗菌机制方面的最新进展。
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