A peptide nucleic acid-neamine conjugate that targets and cleaves HIV-1 TAR RNA inhibits viral replication.
A peptide nucleic acid-neamine conjugate that targets and cleaves HIV-1 TAR RNA inhibits viral replication.
复制标题
靶向并切割 HIV-1 TAR RNA 的肽核酸-新胺缀合物可抑制病毒复制。
DOI：
10.1021/jm049642d
复制
发表时间：
2004
影响因子：
7.3
通讯作者：
Decout,Jean-Luc
中科院分区：
文献类型：
--
作者：
Riguet,Emmanuel;Tripathi,Snehlata;Chaubey,Binay;Desire,Jerome;Pandey,VirendraN;Decout,Jean-Luc
将氨基糖苷类抗生素新霉素B的新霉胺部分与靶向HIV-1 TAR RNA的16聚体肽核酸（PNA）缀合。新霉胺核心的连接允许细胞摄取PNA并导致对HIV-1复制的有效抑制。聚阳离子新霉胺部分赋予PNA更大的溶解度，并且还赋予缀合物独特的RNA切割性质，其对其靶位点是特异性的并且在生理浓度的Mg 2+下是功能性的。这些性质表明这类化合物的潜在治疗应用。
The neamine part of the aminoglycoside antibiotic neomycin B was conjugated to a 16 mer peptide nucleic acid (PNA) targeting HIV-1 TAR RNA. Attachment of the neamine core allows cellular uptake of the PNA and results in potent inhibition of HIV-1 replication. The polycationic neamine moiety imparts greater solubility to the PNA and also confers a unique RNA cleavage property to the conjugate which is specific to its target site and functional at physiological concentrations of Mg2+. These properties suggest a potential therapeutic application for this class of compounds.