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A review emphasizing on utility of heptad repeat sequence as a tool to design pharmacologically safe peptide-based antibiotics
Biochimie ( IF 3.3 ) Pub Date : 2021-09-04 , DOI: 10.1016/j.biochi.2021.09.001
Vikas Yadav 1 , Richa Misra 2
Affiliation  

Extensive usage of antibiotics has created an unprecedented scenario of the rapid emergence of many drug-resistant bacteria, which has become an alarming public health concern around the globe. Search for better alternatives that are as efficacious as antibiotics led to the discovery of antimicrobial peptides (AMPs). These small cationic amphiphilic peptides have emerged as a promising option as antimicrobial agents, owing to their multifaceted implications against varied pathogens. Recent years have witnessed tremendous growth in research on AMPs resulting in them being tested in clinical trials of which six got approved for topical application. The relatively less successful outcome has been attributed to the poor cell selectivity shown by most of the naturally occurring AMPs. This drawback needs to be circumvented by identifying strategies to design safe and effective peptides. In the present review, we have emphasized the importance of heptad repeat sequence (leucine and/or phenylalanine zipper motif) as a tool that has shown great promise in remodeling the toxic AMPs to safe antimicrobial agents.



中文翻译:

一篇强调七肽重复序列作为设计药理学安全的肽类抗生素工具效用的综述

抗生素的广泛使用造成了许多耐药细菌迅速出现的前所未有的局面,这已成为全球令人担忧的公共卫生问题。寻找与抗生素一样有效的更好替代品导致了抗菌肽 (AMP) 的发现。这些小的阳离子两亲肽已成为一种有前途的抗菌剂选择,因为它们对各种病原体具有多方面的影响。近年来,AMP 的研究取得了巨大的增长,导致它们在临床试验中进行了测试,其中六项被批准用于局部应用。相对不太成功的结果归因于大多数天然存在的 AMP 显示出较差的细胞选择性。需要通过确定设计安全有效肽的策略来规避这个缺点。在本综述中,我们强调了七肽重复序列(亮氨酸和/或苯丙氨酸拉链基序)作为一种工具的重要性,该工具在将有毒的 AMP 改造为安全的抗菌剂方面显示出巨大的前景。

更新日期:2021-09-19
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