Oligonucleotides hold great promise as therapeutic agents but poor bioavailability limits their utility. Hence, new analogues with improved cell uptake are urgently needed. Here, we report the synthesis and physical study of reduced-charge oligonucleotides containing artificial LNA-sulfamate and sulfamide linkages combined with 2′-O-methyl sugars and phosphorothioate backbones. These oligonucleotides have high affinity for RNA and excellent nuclease resistance.

中文翻译：

---

含有 LNA-氨基磺酸盐和磺酰胺主链键的寡核苷酸的合成和性质

寡核苷酸作为治疗剂具有广阔的前景，但生物利用度差限制了其实用性。因此，迫切需要具有改善细胞摄取的新类似物。在此，我们报告了含有人工 LNA-氨基磺酸盐和磺酰胺键以及 2'-O-甲基糖和硫代磷酸酯主链的减电荷寡核苷酸的合成和物理研究。这些寡核苷酸对RNA具有高亲和力，并且具有优异的核酸酶抗性。