期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 13, 期 16, 页码 4912-4920出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.05.024
关键词
oligonuclcotide; conjugate; aldehyde; oxime; hydrazine
资金
- Wellcome Trust Funding Source: Medline
2'-O-[2-(2.3-Diacetoxypropyl)amino-2-oxoethyl]uridine 3'-phosphoramidite was prepared and used in solid-phase-synthesis to obtain oligonucleotides containing a 1,2-diol group. which may then be converted into it 2'-aldehyde group. The oligonucleotides were conjugated efficiently to various Molecules by chemoselective ligation that involves all addition elimination reaction between the 2'-aldehyde group and a suitable nucleophile such as it hydrazine, a O-alkylhydroxylamine or in 1,2-aminothiol. The method was applied Successfully to the conjugation of peptides to oligonucleotides at the T-position, (c) 2005 Elsevier Ltd. All rights reserved.
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