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作为新一代抗菌药物的肽模拟物:最新进展。

Peptidomimetics as a new generation of antimicrobial agents: current progress.

机构信息

Department of Immunology, National School of Biological Sciences, National Polytechnic Institute, Mexico City, Mexico.

出版信息

Infect Drug Resist. 2014 Aug 30;7:229-37. doi: 10.2147/IDR.S49229. eCollection 2014.

Abstract

Antibiotic resistance is an increasing public health concern around the world. Rapid increase in the emergence of multidrug-resistant bacteria has been the target of extensive research efforts to develop a novel class of antibiotics. Antimicrobial peptides (AMPs) are small cationic amphiphilic peptides, which play an important role in the defense against bacterial infections through disruption of their membranes. They have been regarded as a potential source of future antibiotics, owing to a remarkable set of advantageous properties such as broad-spectrum activity, and they do not readily induce drug-resistance. However, AMPs have some intrinsic drawbacks, such as susceptibility to enzymatic degradation, toxicity, and high production cost. Currently, a new class of AMPs termed "peptidomimetics" have been developed, which can mimic the bactericidal mechanism of AMPs, while being stable to enzymatic degradation and displaying potent activity against multidrug-resistant bacteria. This review will focus on current findings of antimicrobial peptidomimetics. The potential future directions in the development of more potent analogs of peptidomimetics as a new generation of antimicrobial agents are also presented.

摘要

抗生素耐药性是全球日益严重的公共卫生问题。多药耐药菌的迅速出现已成为广泛研究努力的目标,旨在开发一类新型抗生素。抗菌肽 (AMPs) 是小的阳离子两亲肽,通过破坏细菌的膜在抵御细菌感染方面发挥重要作用。由于具有广谱活性等一系列显著优势,并且不易产生耐药性,因此它们被视为未来抗生素的潜在来源。然而,AMPs 也存在一些内在的缺点,例如易被酶降解、毒性和高生产成本。目前,已经开发出一类新型的 AMPs,称为“肽模拟物”,它们可以模拟 AMPs 的杀菌机制,同时对酶降解稳定,并对多药耐药菌具有强大的活性。本综述将重点介绍抗菌肽模拟物的最新研究发现。还提出了作为新一代抗菌药物开发更有效类似物的潜在未来方向。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/237c/4155802/d1fb4d6ed858/idr-7-229Fig1.jpg

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