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研究抗菌 AA 肽及其衍生物的指标的进展。

Developments with investigating descriptors for antimicrobial AApeptides and their derivatives.

机构信息

a Department of Chemistry , University of South Florida , Tampa , FL , USA.

出版信息

Expert Opin Drug Discov. 2018 Aug;13(8):727-739. doi: 10.1080/17460441.2018.1487950. Epub 2018 Jun 22.

DOI:10.1080/17460441.2018.1487950
PMID:29933702
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6301047/
Abstract

The development of multidrug-resistant strains of bacteria resulting from prolonged treatment with conventional antibiotics has necessitated the need for continuous research for better antibiotic strategies. One of these alternatives is evolutionary antimicrobial peptides also known as host-defense peptides (HDPs). HDPs are an integral part of the innate defense system in multicellular eukaryotes. Although HDPs can largely circumvent the persistent problem of antibiotic resistance due to their bacteriolytic membrane mechanism, they have some drawbacks including a low activity profile and protease instability. AApeptides have recently been introduced as a new class of peptidomimetics with resistance to proteolysis, improved activity profile, and limitless possibilities for structural diversity. Furthermore, they have shown excellent antimicrobial activity. Areas covered: This review updates the reader on the latest developments of antimicrobial AApeptides, the various derivatizations, and their development for antimicrobial applications. The most recent findings on the heterogeneous γ-AA backbone are also outlined. Expert opinion: AApeptides have found diverse applications in antimicrobial studies. AApeptides are believed to exhibit bactericidal properties by imitating the membranolytic action of HDPs. They have shown broad-spectrum antimicrobial activity and are active against medicinally relevant drug-resistant pathogens. AApeptides and their derivatives could gain therapeutic relevance in the design and development of antibiotic agents.

摘要

由于长期使用传统抗生素导致耐药菌株的发展,因此需要不断研究更好的抗生素策略。其中一种替代方法是进化抗菌肽,也称为宿主防御肽 (HDP)。HDP 是多细胞真核生物先天防御系统的重要组成部分。尽管 HDP 由于其溶菌膜机制在很大程度上避免了抗生素耐药性的持续问题,但它们存在一些缺点,包括活性谱低和蛋白酶不稳定。AApeptides 最近被引入作为一种新型的肽模拟物,具有抗蛋白水解、改善的活性谱和结构多样性的无限可能性。此外,它们表现出优异的抗菌活性。涵盖领域:本综述更新了读者对最新抗菌 AApeptides 发展、各种衍生化及其在抗菌应用中的开发的了解。还概述了最近关于异质 γ-AA 主链的发现。专家意见:AApeptides 在抗菌研究中找到了多种应用。AApeptides 被认为通过模拟 HDP 的膜溶解作用表现出杀菌特性。它们具有广谱抗菌活性,对医学相关的耐药病原体有效。AApeptides 及其衍生物可能在抗生素药物的设计和开发中获得治疗相关性。

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Linear peptidomimetics as potent antagonists of Staphylococcus aureus agr quorum sensing.线性肽拟似物作为金黄色葡萄球菌 agr 群体感应的有效拮抗剂。
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