Short Antimicrobial Peptides.

Q3 Medicine
Komal Sharma, Shams Aaghaz, Kitika Shenmar, Rahul Jain
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引用次数: 23

Abstract

Background: After the era of serendipitous discovery of penicillin and outburst in the discovery and development of highly efficient antibiotics, a surge in resistance against the target specific drugs was observed, primarily due to a combination of selective pressure of antibiotics use and spontaneous mutations. As per the World Health Organization, antibiotic resistance is one of the greatest threats to the mankind.

Objective: Short antimicrobial peptides (SAMPs) can be considered as a viable therapeutic alternative to conventional antibiotics in tackling resistant microbes. The ubiquitous nature of SAMPs combined with their ability to act via non-specific modes of action, high activity against a wide spectrum of drug-sensitive and drug-resistant microbes, and relative insusceptibility against the development of resistance adds to their desirability as new generation antibiotics.

Results: Due to the natural tendency of peptides to get metabolized by proteolytic enzymes, modification of naturally occurring SAMPs is desirable. The modifications can be done either by incorporating unnatural or modified amino acids into the peptide chain or by protecting C and N termini. The characteristic feature of SAMPs is their hydrophobicity and cationicity, which aid in the effective killing of microbes by selectively binding target and lysing the microbial cells with less deleterious effects on the host cells as compared to AMPs and other conventional antibiotics.

Conclusion: Herein, we discussed the arsenal of short peptides and peptidomimetics starting from the smallest unit possible - a dipeptide to a decapeptide along with their activity profiles as antimicrobials. Recently, various SAMPs have paved their ways from in vitro studies to clinical trials, as evident from the most recent patent (EP1951194) on oral hygiene. This step by step growth of SAMPs has restored the hope in peptide-based therapeutics, which may prove an essential tool in eradicating antimicrobial resistance and tackling various microbial infections.

短抗菌肽。
背景:在偶然发现青霉素和发现和开发高效抗生素的爆发时代之后,观察到对目标特异性药物的耐药性激增,主要是由于抗生素使用的选择压力和自发突变的结合。据世界卫生组织称,抗生素耐药性是人类面临的最大威胁之一。目的:短抗菌肽(SAMPs)可以被认为是治疗耐药微生物的一种可行的替代方法。SAMPs的普遍特性,加上它们通过非特异性作用方式起作用的能力,对广泛的药物敏感和耐药微生物的高活性,以及对耐药性发展的相对不敏感,这些都增加了它们作为新一代抗生素的可取性。结果:由于多肽自然倾向于被蛋白水解酶代谢,因此需要对天然存在的SAMPs进行修饰。修饰可以通过在肽链中加入非天然或修饰的氨基酸或通过保护C和N端来完成。SAMPs的特点是其疏水性和阳离子性,与AMPs和其他常规抗生素相比,SAMPs通过选择性结合靶点并裂解微生物细胞来有效杀死微生物,对宿主细胞的有害作用较小。结论:在这里,我们讨论了短肽和仿肽的武器库,从最小的单位开始-二肽到十肽,以及它们作为抗菌剂的活性概况。最近,各种samp已经从体外研究到临床试验铺平了道路,这一点从最近的口腔卫生专利(EP1951194)中可以看出。SAMPs的逐步增长恢复了基于肽的治疗方法的希望,这可能被证明是消除抗菌素耐药性和解决各种微生物感染的重要工具。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Recent patents on anti-infective drug discovery
Recent patents on anti-infective drug discovery Medicine-Pharmacology (medical)
CiteScore
2.40
自引率
0.00%
发文量
1
期刊介绍: Recent Patents on Anti-Infective Drug Discovery publishes review articles on recent patents in the field of anti-infective drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on anti-infective drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-infective drug design and discovery.
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