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抗菌肽迈向临床应用——漫长的历史即将结束。

Antimicrobial Peptides towards Clinical Application-A Long History to Be Concluded.

机构信息

Medical Biotechnology Department, University of Siena, Via A Moro 2, 53100 Siena, Italy.

SetLance srl, Via Fiorentina 1, 53100 Siena, Italy.

出版信息

Int J Mol Sci. 2024 Apr 29;25(9):4870. doi: 10.3390/ijms25094870.

Abstract

Antimicrobial peptides (AMPs) are molecules with an amphipathic structure that enables them to interact with bacterial membranes. This interaction can lead to membrane crossing and disruption with pore formation, culminating in cell death. They are produced naturally in various organisms, including humans, animals, plants and microorganisms. In higher animals, they are part of the innate immune system, where they counteract infection by bacteria, fungi, viruses and parasites. AMPs can also be designed de novo by bioinformatic approaches or selected from combinatorial libraries, and then produced by chemical or recombinant procedures. Since their discovery, AMPs have aroused interest as potential antibiotics, although few have reached the market due to stability limits or toxicity. Here, we describe the development phase and a number of clinical trials of antimicrobial peptides. We also provide an update on AMPs in the pharmaceutical industry and an overall view of their therapeutic market. Modifications to peptide structures to improve stability in vivo and bioavailability are also described.

摘要

抗菌肽(AMPs)是一种具有两亲性结构的分子,使其能够与细菌膜相互作用。这种相互作用可能导致膜穿透和孔形成,最终导致细胞死亡。它们在各种生物体中自然产生,包括人类、动物、植物和微生物。在高等动物中,它们是先天免疫系统的一部分,能够抵抗细菌、真菌、病毒和寄生虫的感染。抗菌肽也可以通过生物信息学方法从头设计或从组合文库中选择,然后通过化学或重组程序进行生产。自发现以来,抗菌肽作为潜在抗生素引起了人们的兴趣,尽管由于稳定性限制或毒性,很少有抗菌肽进入市场。在这里,我们描述了抗菌肽的开发阶段和一些临床试验。我们还提供了制药行业中抗菌肽的最新情况以及它们治疗市场的总体情况。还描述了对肽结构的修饰,以提高体内稳定性和生物利用度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f40a/11084544/3f0357df9ff1/ijms-25-04870-g001.jpg

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