R-6'-Me-α-L-LNA 修饰寡核苷酸的合成及生物物理特性分析。
Synthesis and biophysical characterization of R-6'-Me-α-L-LNA modified oligonucleotides.
机构信息
Department of Medicinal Chemistry, Isis Pharmaceuticals, 1891 Rutherford Road, Carlsbad, CA 92008, USA.
出版信息
Bioorg Med Chem Lett. 2011 Feb 15;21(4):1122-5. doi: 10.1016/j.bmcl.2010.12.119. Epub 2010 Dec 31.
The synthesis and biophysical properties of R-6'-Me-α-L-LNA, which has a methyl group in the (R) configuration on the 2',4'-bridging substituent of α-L-LNA, is reported. The synthesis of the uracil nucleobase phosphoramidite was efficiently accomplished in 14 steps and 8 chromatographic purifications starting from a known sugar intermediate. Biophysical evaluation revealed that substitution along the edge of the major groove does not impair the high affinity duplex forming ability of α-L-LNA modified oligonucleotides.
报道了 R-6'-Me-α-L-LNA 的合成及生物物理性质，R-6'-Me-α-L-LNA 是在 α-L-LNA 的 2'、4'-桥连取代基的（R）构型上具有甲基的化合物。从已知的糖中间体出发，经过 14 步反应和 8 次色谱纯化，高效地合成了尿嘧啶核苷亚磷酰胺。生物物理评价表明，在大沟边缘的取代不会损害 α-L-LNA 修饰寡核苷酸的高亲和力双链体形成能力。
Zotero 插件