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双头阳离子脂肽:一类新兴的抗菌剂。

Double-Headed Cationic Lipopeptides: An Emerging Class of Antimicrobials.

机构信息

Faculty of Chemistry, University of Gdansk, Wita Stwosza 63, 80-308 Gdansk, Poland.

Faculty of Pharmacy, Medicinal University of Gdansk, Al. Gen. J. Hallera 107, 80-416 Gdansk, Poland.

出版信息

Int J Mol Sci. 2020 Nov 25;21(23):8944. doi: 10.3390/ijms21238944.

DOI:10.3390/ijms21238944
PMID:33255674
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7728077/
Abstract

Antimicrobial peptides (AMPs) constitute a promising tool in the development of novel therapeutic agents useful in a wide range of bacterial and fungal infections. Among the modifications improving pharmacokinetic and pharmacodynamic characteristics of natural AMPs, an important role is played by lipidation. This study focuses on the newly designed and synthesized lipopeptides containing multiple Lys residues or their shorter homologues with palmitic acid (C) attached to the side chain of a residue located in the center of the peptide sequence. The approach resulted in the development of lipopeptides representing a model of surfactants with two polar headgroups. The aim of this study is to explain how variations in the length of the peptide chain or the hydrocarbon side chain of an amino acid residue modified with C, affect biological functions of lipopeptides, their self-assembling propensity, and their mode of action.

摘要

抗菌肽 (AMPs) 是一种很有前途的工具,可用于开发针对各种细菌和真菌感染的新型治疗药物。在提高天然 AMPs 的药代动力学和药效学特性的修饰中,脂质化起着重要作用。本研究集中于新设计和合成的含有多个赖氨酸残基或其较短同源物的脂肽,这些残基带有棕榈酸 (C) 连接到肽序列中心残基的侧链上。这种方法开发了具有两个极性头基的表面活性剂模型的脂肽。本研究的目的是解释修饰后的氨基酸残基的肽链长度或碳氢侧链的变化如何影响脂肽的生物学功能、自组装倾向及其作用模式。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/5cb12c918e1b/ijms-21-08944-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/3a2c1be0f06b/ijms-21-08944-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/ada86d875657/ijms-21-08944-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/4e0cf67d85cd/ijms-21-08944-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/f004e11831b2/ijms-21-08944-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/788059d57219/ijms-21-08944-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/e77c978bd572/ijms-21-08944-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/5cb12c918e1b/ijms-21-08944-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/3a2c1be0f06b/ijms-21-08944-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/ada86d875657/ijms-21-08944-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/4e0cf67d85cd/ijms-21-08944-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/f004e11831b2/ijms-21-08944-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/788059d57219/ijms-21-08944-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/e77c978bd572/ijms-21-08944-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/591e/7728077/5cb12c918e1b/ijms-21-08944-g007.jpg

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