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Identification of a Tricyclic PIII Chiral Auxiliary for Solid-Supported Synthesis of Stereopure Phosphorothioate-Containing Oligonucleotides.
ChemBioChem ( IF 3.2 ) Pub Date : 2020-02-06 , DOI: 10.1002/cbic.201900631
Sukumar Sakamuri 1 , Dingguo Liu 1 , Laxman Eltepu 1 , Bin Liu 1 , Lisa Jo Reboton 1 , Ryan Preston 1 , Curt W Bradshaw 1
Affiliation  

Since the recognition of oligonucleotides as a therapeutic modality, significant work has been devoted to improving therapeutic properties, including nuclease stability. Phosphorothioate (PS) modifications of phosphodiesters are one of the most explored chemical modification and integral to currently approved oligonucleotide therapeutics, including antisense oligonucleotides (ASOs) and short interfering RNAs (siRNAs). Insertion of sulfur into the phosphate bridge in an n-mer leads to 2n isomeric mixtures of PSs, with different nuclease stability and protein-binding properties. Efforts to create stereopure PS-containing oligonucleotides has spurred interest in identifying new synthetic methods. Herein, work on a novel and practical tricyclic PIII chiral auxiliary and its application in solid-supported synthesis of stereopure PS-containing oligonucleotides is reported.

中文翻译:

固相合成含有立体硫代磷酸酯的寡核苷酸的三环PIII手性助剂的鉴定。

由于将寡核苷酸识别为治疗手段,因此已致力于改善包括核酸酶稳定性在内的治疗特性的大量工作。磷酸二酯的硫代磷酸酯(PS)修饰是研究最多的化学修饰之一,并且是当前批准的寡核苷酸治疗剂(包括反义寡核苷酸(ASO)和短干扰RNA(siRNA))不可或缺的组成部分。将硫插入n-mer的磷酸酯桥中会生成2n的PSs异构体混合物,具有不同的核酸酶稳定性和蛋白质结合特性。建立立体纯的含PS的寡核苷酸的努力激发了人们对鉴定新的合成方法的兴趣。在此处,
更新日期:2020-02-06
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