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肽核酸(PNAs):目前有潜力的杀菌剂。

Peptide nucleic acids (PNAs): currently potential bactericidal agents.

机构信息

Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

Hematology and Oncology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran; Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Biomed Pharmacother. 2017 Sep;93:580-588. doi: 10.1016/j.biopha.2017.06.092. Epub 2017 Jul 4.

Abstract

In recent years, the emergence of ESBL-producing and multi-drug resistant bacteria have been increased and designing novel components is necessary for confrontation these bacteria. Peptide nucleic acids (PNAs) are one of the synthetic components that bind to single strand DNA and RNA. Applications of these components are wide while, and one of the important applications of these components is inhibition of gene expression and knock downing the target gene follow as inhibition of bacterial growth. For PNA targeting gene, peptide-PNAs (PPNA) activity cannot be occurred without sequence homology, at the same time, it has been affected by sequence-based specific target and dose-dependent-based manner. Choosing the conserved sequence in different bacterial genus can provide broad-spectrum antimicrobial activity. In this review article, we studied several research papers and extract PNA targeting genes that cause gene knock down and inhibition of bacterial growth. Some novel opportunities for advancement and the design ultra-narrow-spectrum antimicrobial drugs against multi-drug can be accessible by utilizing PNA against necessary genes of pathogens. These results open novel vision for therapeutic intervention. Future researches are required to evaluate the safety, toxicity and pharmacokinetics properties of PPNAs in order to be utilized in clinical treatment.

摘要

近年来,产生 ESBL 和多药耐药菌的情况有所增加,因此有必要设计新型成分来对抗这些细菌。肽核酸 (PNA) 是一种与单链 DNA 和 RNA 结合的合成成分之一。这些成分的应用非常广泛,其中一个重要的应用是抑制基因表达和敲低目标基因,从而抑制细菌生长。对于针对基因的 PNA(肽 -PNA [PPNA]),如果没有序列同源性,其活性就无法发挥,同时它还受到基于序列特异性和剂量依赖性的靶标影响。选择不同细菌属中的保守序列可以提供广谱抗菌活性。在这篇综述文章中,我们研究了几篇研究论文,并提取了导致基因敲低和细菌生长抑制的 PNA 靶向基因。通过利用 PNA 针对病原体的必要基因,可以为开发针对多药的超窄谱抗菌药物提供新的机会。这些结果为治疗干预开辟了新的视野。需要进一步研究以评估 PPNAs 的安全性、毒性和药代动力学特性,以便在临床治疗中应用。

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