Suppr超能文献

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.

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。

相似文献

1
Developments with investigating descriptors for antimicrobial AApeptides and their derivatives.研究抗菌 AA 肽及其衍生物的指标的进展。
Expert Opin Drug Discov. 2018 Aug;13(8):727-739. doi: 10.1080/17460441.2018.1487950. Epub 2018 Jun 22.
2
The development of antimicrobial γ-AApeptides.抗菌 γ-AApeptides 的研发。
Future Med Chem. 2016 Jun;8(10):1101-10. doi: 10.4155/fmc-2016-0034. Epub 2016 Jun 10.
3
Antimicrobial AApeptides.抗菌A肽
Curr Top Med Chem. 2017;17(11):1266-1279. doi: 10.2174/1568026616666161018145945.
4
Antimicrobial γ-AApeptides (WO2013112548): a patent evaluation.抗菌 γ-AApeptides(WO2013112548):专利评估。
Expert Opin Ther Pat. 2015 Jan;25(1):111-8. doi: 10.1517/13543776.2014.973855. Epub 2014 Oct 21.
5
AApeptides as a new class of antimicrobial agents.**抗菌肽**:一类新型的抗菌药物。
Org Biomol Chem. 2013 Jul 14;11(26):4283-90. doi: 10.1039/c3ob40444g. Epub 2013 May 31.
7
γ-AApeptides as a New Strategy for Therapeutic Development.γ-AA 肽作为治疗开发的新策略。
Curr Med Chem. 2019;26(13):2313-2329. doi: 10.2174/0929867324666171107095913.
10
The Activity of Small Urea-γ-AApeptides Toward Gram-Positive Bacteria.小尿素-γ-AA 肽对革兰氏阳性菌的活性。
ChemMedChem. 2019 Dec 4;14(23):1963-1967. doi: 10.1002/cmdc.201900520. Epub 2019 Nov 7.

本文引用的文献

2
Membrane-Active Hydantoin Derivatives as Antibiotic Agents.作为抗生素的膜活性乙内酰脲衍生物
J Med Chem. 2017 Oct 26;60(20):8456-8465. doi: 10.1021/acs.jmedchem.7b00847. Epub 2017 Oct 6.
4
Cadazolid for the treatment of Clostridium difficile.用于治疗艰难梭菌的卡达唑胺
Expert Opin Investig Drugs. 2017 Apr;26(4):509-514. doi: 10.1080/13543784.2017.1304538.
6
Structure and Function of AApeptides.A肽的结构与功能。
Biochemistry. 2017 Jan 24;56(3):445-457. doi: 10.1021/acs.biochem.6b01132. Epub 2017 Jan 13.
7
Antibiotic resistance: A current epilogue.抗生素耐药性:当前的尾声。
Biochem Pharmacol. 2017 Jun 15;134:139-146. doi: 10.1016/j.bcp.2016.12.005. Epub 2016 Dec 10.
8
Antimicrobial Peptides: Mechanisms of Action and Resistance.抗菌肽:作用机制与耐药性
J Dent Res. 2017 Mar;96(3):254-260. doi: 10.1177/0022034516679973. Epub 2016 Nov 25.
9
Antimicrobial AApeptides.抗菌A肽
Curr Top Med Chem. 2017;17(11):1266-1279. doi: 10.2174/1568026616666161018145945.
10
Small Antimicrobial Agents Based on Acylated Reduced Amide Scaffold.基于酰化还原酰胺骨架的小分子抗菌剂。
J Med Chem. 2016 Sep 8;59(17):7877-87. doi: 10.1021/acs.jmedchem.6b00640. Epub 2016 Aug 25.

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验