Taniguchi Yosuke, Nakamura Ayako, Senko Yusuke, Sasaki Shigeki
Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
Nucleic Acids Symp Ser (Oxf). 2004(48):69-70. doi: 10.1093/nass/48.1.69.
Triplex-forming oligonucleotides (TFOs) are potential DNA-targeting molecules, but their recognizable duplexes are limited to homopurine:homopyrimidine sequences by interruption of pyrimidine bases in the purine strand. Despite numerous studies, this problem has not been generally solved. We have recently demonstrated that the new nucleoside analogues, WNA-betaT and WNA-betaC exhibit selective stabilization of the triplexes at a TA and a CG interrupting site, respectively. However, subsequent investigations have shown that there are limitations in recognizable sequences by these analogs. In this study, we performed further systematic investigation on WNA analogs by synthesizing a variety of WNA analogs having 5-substituted cytosine and uracil, and found that WNA-betaFU exhibit high CG-selectivity.
三链形成寡核苷酸（TFOs）是潜在的DNA靶向分子，但其可识别的双链体限于同型嘌呤：同型嘧啶序列，因为嘌呤链中的嘧啶碱基会中断。尽管进行了大量研究，但这个问题尚未得到普遍解决。我们最近证明，新的核苷类似物WNA-βT和WNA-βC分别在TA和CG中断位点表现出三链体的选择性稳定。然而，随后的研究表明，这些类似物在可识别序列方面存在局限性。在本研究中，我们通过合成多种具有5-取代胞嘧啶和尿嘧啶的WNA类似物，对WNA类似物进行了进一步的系统研究，发现WNA-βFU表现出高CG选择性。
