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The Remarkable Cationic Peptides: A Boon to Pharmaceutical Sciences?

机译:杰出的阳离子肽:药物科学的福音吗?

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In this opinion article, the authors discuss a number of interesting, beneficial properties of naturally occurring and synthetic cationic antimicrobial peptides (AMPs) with the prospective aim of bringing these compounds into therapeutic use to avoid antibiotic resistance and utilize their numerous properties. The structural diversity and the conformational freedom of these compounds adversely affects their mechanistic elucidation. Our molecular level mechanistic exploration of these peptides has shown their ion carriage properties and systematically explains their antibiotic activity through disruption of bacterial cell homeostasis and inhibition of 14-α demethylase enzyme. We have also shown self-assemblage in AMPs in different nanoparticulate and tubular forms. Some AMPs possess cell penetration capability and their co-administration with drug enhances antibacterial activity through a non-disruptive mechanism. The anti-HIV activity of AMPs has been explained based on their non-covalent, non-base-pair base-pair type interactions with HIV viral ssRNA template. Design of peptidomimetic compounds with enhanced druggability based on our mechanistic explorations will definitely lead to better non-toxic drugs with antibacterial, anti-HIV activity and may contribute towards development of efficient drug delivery systems.?This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.
机译:在这篇观点文章中,作者讨论了天然存在的和合成的阳离子抗菌肽(AMPs)的许多有趣的有益特性,其预期目标是将这些化合物用于治疗用途以避免抗生素耐药性并利用其众多特性。这些化合物的结构多样性和构象自由度不利地影响了它们的机理阐明。我们对这些肽的分子水平机理研究表明它们具有离子运输特性,并通过破坏细菌细胞稳态和抑制14-α脱甲基酶来系统地解释其抗生素活性。我们还显示了不同纳米颗粒和管状形式的AMP中的自组装。一些AMP具有细胞穿透能力,它们与药物的共同给药通过无干扰机制增强抗菌活性。 AMPs的抗HIV活性已根据其与HIV病毒ssRNA模板的非共价,非碱基对碱基对类型相互作用进行了解释。根据我们的机理研究,设计具有增强可药物性的拟肽化合物肯定会产生具有抗菌,抗HIV活性的更好的无毒药物,并可能有助于开发有效的药物递送系统。本文接受后发表评论。已注册的读者(请参阅“针对读者”)可以通过在问题目录页面上单击摘要来发表评论。

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