Institute of Multidisciplinary Research for Advanced Materials, Tohoku University, Aoba-ku, Sendai-shi, Miyagi, Japan.
Bioorg Med Chem Lett. 2010 Oct 15;20(20):6121-4. doi: 10.1016/j.bmcl.2010.08.027. Epub 2010 Aug 10.
We previously reported that oligodeoxynucleotides containing 2-amino-6-vinylpurine (2-AVP: 1) exhibit efficient selective cross-linking to cytosine. In this study, the 2'-OMe nucleoside analogue (2) of 2-AVP was designed in order to increase its affinity to RNA and enhance metabolic stability. It has been demonstrated that 2'-OMe oligonucleotides bearing 2 achieve highly selective cross-linking to the thymine base in DNA and show higher antisense effect on luciferase production in cell lysate.
我们之前曾报道过，含有 2-氨基-6-乙烯基嘌呤（2-AVP：1）的寡核苷酸可有效地与胞嘧啶选择性交联。在这项研究中，设计了 2-AVP 的 2'-O-甲氧基核苷类似物（2），以增加其对 RNA 的亲和力并提高代谢稳定性。已经证明，带有 2 的 2'-O-甲氧基寡核苷酸可高度选择性地与 DNA 中的胸腺嘧啶碱基交联，并在细胞裂解物中对荧光素酶的产生表现出更高的反义效果。
