关键词: Aminoglycosides Antimicrobial activity Antisense oligonucleotides Cell-penetrating peptides Peptide nucleic acid (PNA) Vitamin B12

Mesh : Peptide Nucleic Acids / pharmacology chemistry Anti-Bacterial Agents / pharmacology Amino Acid Sequence Cell-Penetrating Peptides / pharmacology

来  源:   DOI:10.1007/s00249-023-01673-w   PDF(Pubmed)

Abstract:
Peptide nucleic acid (PNA) is a nucleic acid mimic with high specificity and binding affinity to natural DNA or RNA, as well as resistance to enzymatic degradation. PNA sequences can be designed to selectively silence gene expression, which makes PNA a promising tool for antimicrobial applications. However, the poor membrane permeability of PNA remains the main limiting factor for its applications in cells. To overcome this obstacle, PNA conjugates with different molecules have been developed. This mini-review focuses on covalently linked conjugates of PNA with cell-penetrating peptides, aminosugars, aminoglycoside antibiotics, and non-peptidic molecules that were tested, primarily as PNA carriers, in antibacterial and antiviral applications. The chemistries of the conjugation and the applied linkers are also discussed.
摘要:
肽核酸(PNA)是一种对天然DNA或RNA具有高特异性和结合亲和力的核酸模拟物,以及对酶降解的抗性。PNA序列可以被设计为选择性地沉默基因表达,这使得PNA成为抗菌应用的有前途的工具。然而,PNA的膜通透性差仍然是其在细胞中应用的主要限制因素。为了克服这个障碍,已经开发了具有不同分子的PNA缀合物。这篇小型综述侧重于PNA与细胞穿透肽的共价连接缀合物,氨基糖,氨基糖苷类抗生素,和测试过的非肽分子,主要作为PNA携带者,在抗菌和抗病毒应用。还讨论了缀合的化学性质和应用的接头。
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