Fluorine-18 labelling of oligonucleotides: Prosthetic labelling at the 5′-end using the N-(4-[18F]fluorobenzyl)-2-bromoacetamide reagent

✍ Scribed by B. Kuhnast; F. Hinnen; R. Boisgard; B. Tavitian; F. Dollé

• Publisher: John Wiley and Sons
• Year: 2003
• Tongue: French
• Weight: 124 KB
• Volume: 46
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.742

✦ Synopsis

Abstract

Labelled oligonucleotides are new imaging tools to study gene expression at the nucleic acid and protein levels. We have previously developed a universal method to label oligonucleotides at their 3′‐end with radiohalogens and particularly with fluorine‐18, the most widely used positron‐emitter, t~1/2~: 109.8 min. Using the same strategy, we herein report the fluorine‐18 labelling of oligonucleotides at their 5′‐end. A 18‐mer 2′O‐methyl modified oligoribonucleotide, bearing a phosphorothioate group at its 5′‐end, was conjugated to our fluorine‐18‐labelled reagent N‐(4‐[^18^F]fluorobenzyl)‐2‐bromoacetamide. The whole synthetic procedure yielded up to 1 GBq of fluorine‐18‐labelled oligonucleotide with a specific radioactivity of 37–74 GBq/μmol in 160 min. Copyright © 2003 John Wiley & Sons, Ltd.