Ueno Yoshihito, Shibata Aya, Matsuda Akira, Kitade Yukio
Department of Biomolecular Science, Faculty of Engineering, Gifu University, Yanagido, Gifu 501-1193, Japan.
Bioconjug Chem. 2003 May-Jun;14(3):684-9. doi: 10.1021/bc020059q.
Synthesis of 3'-3'-linked oligonucleotides branched by a pentaerythritol linker is described. The branched oligonucleotides were synthesized on a DNA/RNA synthesizer using a controlled pore glass (CPG) with a pentaerythritol linker carrying 4,4'-dimethoxytrityl (DMTr) and levulinyl (Lev) groups. The stability of the triplexes between the branched oligonucleotides and the target single-stranded DNA or RNA was studied by thermal denaturation. The oligonucleotides with the pentaerythritol linker formed thermally stable triplexes with the single-stranded DNA and RNA. Furthermore, the branched oligonucleotides containing 2'-O-methylribonucleosides, especially the oligonucleotide composed of 2'-deoxyribonucleosides and 2'-O-methylribonucleosides, stabilized the triplexes with the single-stranded DNA or RNA. Thus, the branched oligonucleotide containing 2'-O-methylribonucleosides may be a candidate for a novel antisense molecule by the triplex formation.
描述了由季戊四醇连接基支化的3'-3'-连接的寡核苷酸的合成。使用带有携带4,4'-二甲氧基三苯甲基(DMTr)和乙酰丙酸基(Lev)基团的季戊四醇连接基的可控孔玻璃(CPG),在DNA/RNA合成仪上合成支化寡核苷酸。通过热变性研究了支化寡核苷酸与靶单链DNA或RNA之间三链体的稳定性。带有季戊四醇连接基的寡核苷酸与单链DNA和RNA形成了热稳定的三链体。此外,含有2'-O-甲基核糖核苷的支化寡核苷酸,尤其是由2'-脱氧核糖核苷和2'-O-甲基核糖核苷组成的寡核苷酸,稳定了与单链DNA或RNA的三链体。因此,含有2'-O-甲基核糖核苷的支化寡核苷酸可能是通过三链体形成的新型反义分子的候选物。