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含精氨酸核肽的固相合成及RNA结合活性

Solid phase synthesis and RNA-binding activity of an arginine-containing nucleopeptide.

作者信息

Roviello G N, Vicidomini C, Di Gaetano S, Capasso D, Musumeci D, Roviello V

机构信息

CNR , Istituto di Biostrutture e Bioimmagini - (Mezzacannone site and Headquarters) , 80134 Napoli , Italy . Email:

Università di Napoli "Federico II" , Dipartimento di Farmacia , 80134 Napoli , Italy.

出版信息

RSC Adv. 2016 Feb 2;6(17):14140-14148. doi: 10.1039/c5ra25809j. Epub 2016 Jan 26.

Abstract

Here we report the solid phase synthesis and characterization (LC-ESIMS, CD) of a cationic nucleobase-containing α-peptide, composed of both l-arginine residues and l-lysine-based nucleoamino acids sequentially present in the structure. The binding properties of this novel basic nucleopeptide towards nucleic acids were investigated by CD spectroscopy which revealed the ability of the thymine-containing oligomer to bind both adenine-containing DNA (dA) and RNA (poly rA) molecules inducing high conformational variations in the nucleic acid structures. Moreover, the artificial oligonucleotide inhibited the enzymatic activity of HIV reverse transcriptase, opening the door to the exploitation of novel antiviral strategies inspired to this molecular tool.

摘要

在此,我们报告了一种含阳离子核碱基的α-肽的固相合成及表征(液相色谱-电喷雾离子化质谱法、圆二色光谱法),该α-肽由结构中依次存在的L-精氨酸残基和基于L-赖氨酸的核氨基酸组成。通过圆二色光谱法研究了这种新型碱性核肽与核酸的结合特性,结果表明含胸腺嘧啶的低聚物能够结合含腺嘌呤的DNA(dA)和RNA(聚rA)分子,从而在核酸结构中诱导高度的构象变化。此外,这种人工寡核苷酸抑制了HIV逆转录酶的酶活性,为基于这一分子工具开发新型抗病毒策略打开了大门。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f963/5635565/750afc9bfb87/c5ra25809j-s1.jpg

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