School of Chemistry and Chemical Engineering, David Keir Building, Stranmillis Road, Queen's University Belfast, Belfast BT9 5AG, UK.
Department of Ocean Science and Division of Life Science, Hong Kong University of Science and Technology, Clear Water Bay, Hong Kong, China.
Chem Commun (Camb). 2018 Sep 25;54(75):10634-10637. doi: 10.1039/c8cc05790g. Epub 2018 Sep 4.
Non-ribosomal peptides (NRPs) are a rich source of antibiotic candidates. However, it was recently discovered that resistance to NRPs can be mediated by d-stereoselective peptidases. The tridecaptins, a class of NRPs that selectively target Gram-negative bacteria, are degraded by the d-peptidase TriF. Through analysis of a solution NMR structure of tridecaptin A, we have rationally synthesized new cyclic tridecaptin analogues that retain strong antimicrobial activity and are resistant to TriF.
非核糖体肽 (NRPs) 是抗生素候选物的丰富来源。然而，最近发现，NPR 的耐药性可以由 d-立体选择性肽酶介导。十三肽，一类选择性针对革兰氏阴性菌的 NPR，被 d-肽酶 TriF 降解。通过对十三肽 A 的溶液 NMR 结构分析，我们合理合成了新的环状十三肽类似物，它们保留了强大的抗菌活性并能抵抗 TriF。
