The tridecaptins: non-ribosomal peptides that selectively target Gram-negative bacteria.

The tridecaptins: non-ribosomal peptides that selectively target Gram-negative bacteria.
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Tridecaptins:选择性靶向革兰氏阴性细菌的非核糖体肽。

DOI:
10.1039/d0md00413h
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发表时间:
2021-01-22
影响因子:
4.1
通讯作者:
Cochrane SA
Cochrane SA
中科院分区:
医学3区
文献类型:
--
作者:
Bann SJ;Ballantine RD;Cochrane SA

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tridecaptin是一类重新出现的非核糖体抗菌肽(NRAP),对革兰氏阴性菌的高度问题菌株具有有效活性。已经报道了一种复杂的作用模式来解释这些NRAP的杀菌活性,其中它们选择性地与内膜的外小叶上的革兰氏阴性形式的肽聚糖前体脂质II结合并破坏质子动力。由于其线性结构,十三肽非常适合合成修饰,因此,已经报道了各种合成类似物,其中一些具有增强的抗微生物活性、降低的合成成本和/或改善的对d-肽酶介导的水解的稳定性。还已经证明,未酰化的tridecaptin可以通过使外膜敏化而与临床相关的抗生素协同作用。本综述将总结过去关于开发/发现新型tridecaptin类似物的文献(截至2020年底),其中一些可能是治疗隐伏革兰氏阴性细菌感染的有用治疗药物。tridecaptin是一类重新出现的非核糖体抗菌肽(NRAP),对革兰氏阴性菌的高度问题菌株具有有效活性。
Tridecaptins are a re-emerging class of non-ribosomal antibacterial peptides (NRAPs) with potent activity against highly problematic strains of Gram-negative bacteria. An intricate mode of action has been reported to explain the bactericidal activity of these NRAPs, wherein they bind selectivity to the Gram-negative version of the peptidoglycan precursor lipid II on the outer leaflet of the inner membrane and disrupt the proton-motive force. Tridecaptins are highly amenable to synthetic modification owing to their linear structure, therefore, various synthetic analogues have been reported, several of which have enhanced antimicrobial activity, reduced cost of synthesis and/or improved stability towards d-peptidase mediated hydrolysis. It has also been demonstrated that unacylated tridecaptins can act synergistically with clinically relevant antibiotics by sensitizing the outer membrane. This review will summarize past literature on the development/discovery of novel tridecaptin analogues (up until the end of 2020), some of which may be useful therapeutic agents to treat insidious Gram-negative bacterial infections. Tridecaptins are a re-emerging class of non-ribosomal antibacterial peptides (NRAPs) with potent activity against highly problematic strains of Gram-negative bacteria.
DOI: 10.1039/c9md00031c
发表时间: 2019-03-01
期刊: MEDCHEMCOMM
影响因子: --
作者:
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影响因子: 7.3
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