Issue 5, 2019

The calcium-dependent lipopeptide antibiotics: structure, mechanism, & medicinal chemistry

Abstract

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.

Graphical abstract: The calcium-dependent lipopeptide antibiotics: structure, mechanism, & medicinal chemistry

Article information

Article type
Review Article
Submitted
01 Mar 2019
Accepted
20 Mar 2019
First published
21 Mar 2019

Med. Chem. Commun., 2019,10, 634-646

The calcium-dependent lipopeptide antibiotics: structure, mechanism, & medicinal chemistry

T. M. Wood and N. I. Martin, Med. Chem. Commun., 2019, 10, 634 DOI: 10.1039/C9MD00126C

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