Hikishima Sadao, Minakawa Noriaki, Kuramoto Kazuyuki, Ogata Shintaro, Matsuda Akira
Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
Chembiochem. 2006 Dec;7(12):1970-5. doi: 10.1002/cbic.200600318.
We describe the synthesis and properties of oligodeoxynucleotides (ODNs) containing 1,8-naphthyridine C-nucleoside (Na-NO) and imidazo[5',4':4,5]pyrido[2,3-d]pyrimidine nucleoside (Im-ON) at the termini. The modified ODNs were more resistant (6 to 40 times) than natural DNA to snake venom phosphodiesterase (SVPD). Although incorporation of one pair each of Na-NO:Im-ON on the sticky ends of the duplex was insufficient for thermal stabilization (+2.5 degrees C per pair relative to the G:C pair), the duplex containing two consecutive Na-NO:Im-ON pairs at its sticky ends was markedly stabilized thermally. The stabilizing effect of the incorporation of additional Na-NO:Im-ON pairs is estimated to be +7.8 degrees C per pair. Application as thermally stabilized decoy molecules to NF-kappaB (p50) was also demonstrated. The DNA duplexes containing the Na-NO:Im-ON pairs (ODN I:ODN II and ODN III:ODN IV) acted as competitors to the natural NF-kappaB-binding duplex (ODN V: ODN VI), and the calculated IC50 values of ODN I:ODN II and ODN III:ODN IV were 20.1+/-13.3 and 10.9+/-4.8 nM, respectively, greater than that of ODN V:ODN VI.
我们描述了在末端含有1,8-萘啶C-核苷(Na-NO)和咪唑并[5',4':4,5]吡啶并[2,3-d]嘧啶核苷(Im-ON)的寡脱氧核苷酸(ODN)的合成及其性质。修饰后的ODN对蛇毒磷酸二酯酶(SVPD)的抗性比天然DNA高(6至40倍)。尽管在双链体的粘性末端各掺入一对Na-NO:Im-ON对热稳定性的提升不足(相对于G:C对,每对提升2.5摄氏度),但在其粘性末端含有两个连续Na-NO:Im-ON对的双链体在热稳定性上有显著提升。额外掺入Na-NO:Im-ON对的稳定作用估计为每对提升7.8摄氏度。还展示了其作为热稳定的诱饵分子对NF-κB(p50)的应用。含有Na-NO:Im-ON对的DNA双链体(ODN I:ODN II和ODN III:ODN IV)作为天然NF-κB结合双链体(ODN V:ODN VI)的竞争者,ODN I:ODN II和ODN III:ODN IV的计算IC50值分别为20.1±13.3和10.9±4.8 nM,高于ODN V:ODN VI的IC50值。