Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.
本发明揭示了一种新型寡聚物,与仅含传统碱基的寡聚物相比,具有增强的形成双链或三链的能力。该寡聚物包含5-(1-
丙炔基)尿
嘧啶,5-(1-
丙炔基)
胞嘧啶或相关类似物的碱基。本发明的寡聚物能够(i)通过在生理pH值下与靶DNA双链的主沟结合,形成与各种靶序列(如病毒或癌
基因序列)的三链,或(ii)通过结合单链DNA或靶
基因编码的RNA而形成双链。本发明的寡聚物可以被纳入药学可接受的载体中,并且可以构建任何所需的序列,只要序列通常包括一个或多个被本发明类似物替换的碱基。本发明的组合物可以用作制药剂治疗各种由病毒引起的疾病,并可用于诊断目的,以检测病毒或疾病情况。