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首页> 外文期刊>RSC Advances >The impact of an extended nucleobase-2′-deoxyribose linker in the biophysical and biological properties of oligonucleotides
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The impact of an extended nucleobase-2′-deoxyribose linker in the biophysical and biological properties of oligonucleotides

机译：扩展的碱基2'-脱氧核糖接头对寡核苷酸的生物物理和生物学特性的影响

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摘要

Interest in artificial DNA mimetics has been triggered by the widespread applications of nucleic acids as they are useful tools for modulation of the biophysical and biological properties of oligonucleotides. In this article, we describe the synthesis and properties of a novel thymine derivative (T*) containing an extended linker between the thymine nucleobase and the 2′-deoxyribose moiety. The modified 2′-deoxyribosyl derivative was prepared via coupling of a functionalized nucleobase to the amino group of 1-aminomethyl-2-deoxyribose, which was synthesized starting from an easily accessible cyano sugar available on a large-scale. Corresponding phosphoramidite and succinyl derivatives have also been incorporated into oligonucleotides at predetermined sites and defined internucleotidic motifs using the solid-phase synthesis approach. This derivative pairs equally well with adenine and guanine and it can be safely introduced at the 3′-end of the siRNAs to generate potent inhibitors of gene expression by the RNA interference mechanism.
机译：核酸的广泛应用已经触发了对人工DNA模拟物的兴趣，因为它们是调节寡核苷酸的生物物理和生物学特性的有用工具。在本文中，我们描述了在胸腺嘧啶核苷碱基和2'-脱氧核糖部分之间包含扩展接头的新型胸腺嘧啶衍生物（T *）的合成和性质。修饰的2'-脱氧核糖基衍生物是通过将功能化的核碱基与1-氨基甲基-2-脱氧核糖的氨基偶联而制备的。规模。还使用固相合成方法将相应的亚磷酰胺和琥珀酰基衍生物掺入了预定位置的寡核苷酸中，并确定了核苷酸间的基序。该衍生物与腺嘌呤和鸟嘌呤同等地配对，可以安全地引入siRNA的3'端，通过RNA干扰机制产生有效的基因表达抑制剂。

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