Ueno Y, Mikawa M, Hoshika S, Takeba M, Kitade Y, Matsuda A
Graduate School of Pharmaceutical Sciences, Hokkaido University.
Nucleic Acids Res Suppl. 2001(1):11-2. doi: 10.1093/nass/1.1.11.
3'-3'-Linked oligodeoxynucleotides (ODNs) with the anthraquinonyl group at the junction point were synthesized on a DNA synthesizer using a controlled pore glass (CPG), which has pentaerythritol carrying the intercalator at one of the four hydroxymethyl groups. Stability of the triplexes with the target duplexes was studied by thermal denaturation. The 3'-3'-linked ODNs with the anthraquinonyl group enhanced the thermal stability of the triplexes when compared with those without the intercalator and the unmodified nonamer. The inhibitory activity of the 3'-3'-linked ODNs against the cleavage of the target DNA by the restriction enzyme Hind III was tested. It was found that the 3'-3'-linked ODN with the anthraquinonyl group at the junction point inhibited the cleavage by the enzyme more effectively than the nonamer and the 3'-3'-linked ODN without the intercalator.
在DNA合成仪上,使用可控孔玻璃(CPG)合成了在连接点带有蒽醌基的3'-3'-连接的寡脱氧核苷酸(ODN),该CPG在四个羟甲基之一上带有携带嵌入剂的季戊四醇。通过热变性研究了与靶双链体形成的三链体的稳定性。与没有嵌入剂的那些和未修饰的九聚体相比,带有蒽醌基的3'-3'-连接的ODN增强了三链体的热稳定性。测试了3'-3'-连接的ODN对限制性内切酶Hind III切割靶DNA的抑制活性。发现连接点带有蒽醌基的3'-3'-连接的ODN比九聚体和没有嵌入剂的3'-3'-连接的ODN更有效地抑制酶的切割。