发现新型抗 HIV 活性 G-四链体形成寡核苷酸。

Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides.

机构信息

Dipartimento di Chimica Organica e Biochimica, Università degli Studi di Napoli Federico II, Complesso Universitario di Monte S. Angelo, via Cintia, 4, I-80126 Napoli, Italy.

出版信息

Chem Commun (Camb). 2011 Feb 28;47(8):2363-5. doi: 10.1039/c0cc04751a. Epub 2010 Dec 16.

DOI:10.1039/c0cc04751a

PMID:21305065

Abstract

A series of d((5')TGGGAG(3')) sequences, 5'-conjugated with a variety of aromatic groups through phosphodiester linkages, were synthesized, showing CD spectra diagnostic of parallel-stranded, tetramolecular G-quadruplex structures. When tested for anti-HIV-1 and HIV-2 activity, potent inhibition of HIV-1 infection in CEM cell cultures was found, associated with high selectivity index values. Surface Plasmon Resonance assays revealed specific binding to HIV-1 gp120 and gp41.

摘要

一系列 d((5')TGGGAG(3')) 序列通过磷酸二酯键与各种芳族基团 5'-连接，其 CD 谱显示出平行链、四分子 G-四链体结构的特征。当测试它们对 HIV-1 和 HIV-2 的活性时，发现它们在 CEM 细胞培养物中对 HIV-1 感染具有强烈的抑制作用，并且具有高选择性指数值。表面等离子体共振测定法显示出与 HIV-1 gp120 和 gp41 的特异性结合。