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从具有不同亲核或亲电官能团的未保护寡核苷酸和配体快速合成寡核苷酸缀合物的方法。

Rapid routes of synthesis of oligonucleotide conjugates from non-protected oligonucleotides and ligands possessing different nucleophilic or electrophilic functional groups.

作者信息

Grimm G N, Boutorine A S, Hélène C

机构信息

Laboratoire de Biophysique, INSERM U201, CNRS UMR 8646, Muséum National d'Histoire Naturelle, Paris, France.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2000 Oct-Dec;19(10-12):1943-65. doi: 10.1080/15257770008045470.

DOI:10.1080/15257770008045470
PMID:11200283
Abstract

Optimized methods are described for post-synthetic conjugation of non-protected oligodeoxyribonucleotides to different ligands. Methods for the terminal functionalization of oligonucleotides by amino, sulfhydryl, thiophosphate or carboxyl groups using different chemical reactions and linkers in both organic and aqueous media are described and compared. Experimental conditions for subsequent coupling of ligands containing aliphatic and aromatic amines, aromatic alcohols, carboxylic, sulfhydryl, alkylating, aldehydic and other reactive nucleophilic and electrophilic groups to oligonucleotides were established, including covalent linkage to other oligonucleotides.

摘要

本文描述了用于将未保护的寡脱氧核糖核苷酸与不同配体进行合成后共轭的优化方法。阐述并比较了在有机和水性介质中,利用不同化学反应和连接体通过氨基、巯基、硫代磷酸酯或羧基对寡核苷酸进行末端功能化的方法。确定了含有脂肪族和芳香族胺、芳香醇、羧基、巯基、烷基化、醛基及其他活性亲核和亲电基团的配体与寡核苷酸后续偶联的实验条件,包括与其他寡核苷酸的共价连接。

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Nucleosides Nucleotides Nucleic Acids. 2000 Oct-Dec;19(10-12):1943-65. doi: 10.1080/15257770008045470.
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