碳水化合物功能化的锁核酸：具有非凡结合亲和力、靶标特异性和酶稳定性的寡核苷酸。

Carbohydrate-functionalized locked nucleic acids: oligonucleotides with extraordinary binding affinity, target specificity, and enzymatic stability.

机构信息

Department of Chemistry, University of Idaho , Moscow, Idaho 83844-2343, United States.

出版信息

Org Lett. 2014 Jun 20;16(12):3308-11. doi: 10.1021/ol501306u. Epub 2014 Jun 3.

Abstract

Three different C5-carbohydrate-functionalized LNA uridine phosphoramidites were synthesized and incorporated into oligodeoxyribonucleotides. C5-Carbohydrate-functionalized LNA display higher affinity toward complementary DNA/RNA targets (ΔTm/modification up to +11.0 °C), more efficient discrimination of mismatched targets, and superior resistance against 3'-exonucleases compared to conventional LNA. These properties render C5-carbohydrate-functionalized LNAs as promising modifications in antisense technology and other nucleic acid targeting applications.

摘要

合成了三种不同的 C5-碳水化合物功能化 LNA 尿嘧啶磷酰胺，并将其掺入寡脱氧核苷酸中。C5-碳水化合物功能化 LNA 与互补的 DNA/RNA 靶标具有更高的亲和力（ΔTm/修饰高达+11.0°C），对错配靶标的识别效率更高，对 3'-核酸外切酶的抗性也优于常规 LNA。这些特性使 C5-碳水化合物功能化 LNA 成为反义技术和其他核酸靶向应用中很有前途的修饰物。