Department of Medicinal Chemistry, Isis Pharmaceuticals, Inc., 2855 Gazelle Court, Carlsbad, California 92010, USA.
Org Lett. 2013 Sep 6;15(17):4316-9. doi: 10.1021/ol401730d. Epub 2013 Aug 13.
The first synthesis of constrained altritol nucleic acids (cANA) containing antisense oligonucleotides (ASOs) was carried out to ascertain how conformationally restricting the D-altritol backbone-containing ASO (Me-ANA) would affect their ability to form duplexes with RNA. It was found that the thermal stability was reduced (cANA/RNA -1.1 °C/modification) compared to DNA/RNA, suggesting the constrained system results in a small destabilizing perturbation in the duplex structure.
首次合成了含有反义寡核苷酸 (ASO) 的约束性阿卓糖醇核酸 (cANA)，以确定 D-阿卓糖醇骨架 ASO (Me-ANA) 的构象限制程度如何影响其与 RNA 形成双链的能力。结果发现，与 DNA/RNA 相比，热稳定性降低 (cANA/RNA -1.1°C/修饰)，这表明约束系统导致双链结构的小的不稳定扰动。
