Shanmugasundaram Muthian, Charles Irudaya, Kore Anilkumar R
Life Sciences Solutions Group, Thermo Fisher Scientific, 2130 Woodward Street, Austin, TX 78744-1832, USA.
Life Sciences Solutions Group, Thermo Fisher Scientific, 2130 Woodward Street, Austin, TX 78744-1832, USA.
Bioorg Med Chem. 2016 Mar 15;24(6):1204-8. doi: 10.1016/j.bmc.2016.01.048. Epub 2016 Jan 29.
The first example of the synthesis of new dinucleotide cap analog containing propargyl group such as m(7,3'-O-propargyl)G[5']ppp[5']G is reported. The effect of propargyl cap analog with standard cap was evaluated with respect to their capping efficiency, in vitro T7 RNA polymerase transcription efficiency, and translation activity using cultured HeLa cells. It is noteworthy that propargyl cap analog outperforms standard cap by 3.1 fold in terms of translational properties. The propargyl cap analog forms a more stable complex with translation initiation factor eIF4E based on the molecular modeling studies.
报道了含炔丙基的新型二核苷酸帽类似物如m(7,3'-O-炔丙基)G[5']ppp[5']G合成的首个实例。就其封端效率、体外T7 RNA聚合酶转录效率以及使用培养的HeLa细胞的翻译活性而言，评估了炔丙基帽类似物与标准帽的效果。值得注意的是，就翻译特性而言，炔丙基帽类似物比标准帽的性能高出3.1倍。基于分子模拟研究，炔丙基帽类似物与翻译起始因子eIF4E形成更稳定的复合物。
