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Fluorine‐18 labelling of oligonucleotides: Prosthetic labelling at the 5′‐end using the N ‐(4‐[ 18 F]fluorobenzyl)‐2‐bromoacetamide reagent
Author(s) -
Kuhnast B.,
Hinnen F.,
Boisgard R.,
Tavitian B.,
Dollé F.
Publication year - 2003
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.742
Subject(s) - labelling , chemistry , oligonucleotide , reagent , fluorine , radiochemistry , nucleic acid , conjugated system , specific activity , combinatorial chemistry , organic chemistry , biochemistry , enzyme , dna , polymer
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.