This invention presents oligonucleotide derivatives comprising a complementary purine part carrying one or more 8-aminopurines such as 8-aminoadenine, 8-aminoguanine and 8-aminohypoxanthine connected with a linker to an oligonucleotide carrying either GT or GA sequences. These oligonucleotide derivatives bind polypyrimidine sequences complementary (in the antiparallel sense) to the purine part by formation of purine-purine-pyrimidine triple helices. The oligonucleotides carrying 8-aminoguanines described in this invention have better binding properties than unmodified oligonucleotides. This enhancement in stability, coupled with the lack of an acidic pH requirement, makes the oligonucleotides carrying 8-aminopurines effective in applications involving oligonucleotide targeting of single stranded RNA in vitro and in vivo, as well as applications requiring triple helix formation.
本发明提出了寡核苷酸衍
生物,其包含的互补
嘌呤部分带有一个或多个
8-氨基嘌呤,如 8-
氨基
腺嘌呤、8-
氨基
鸟嘌呤和
8-氨基次黄嘌呤,并与带有 GT 或 GA 序列的寡核苷酸连接。这些寡核苷酸衍
生物通过形成
嘌呤-
嘌呤-
嘧啶三螺旋,与
嘌呤部分互补(反平行)的多
嘧啶序列结合。与未修饰的寡核苷酸相比,本发明所述的含有 8-
氨基
鸟嘌呤的寡核苷酸具有更好的结合性能。这种稳定性的提高,再加上不需要酸性 pH 值,使得携带
8-氨基嘌呤的寡核苷酸在涉及体外和体内单链 RNA 的寡核苷酸靶向应用以及需要形成三螺旋的应用中非常有效。