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Bioconjug Chem. 2011 Jan 19;22(1):108-14. doi: 10.1021/bc100263y. Epub 2010 Dec 21.

General method for labeling siRNA by click chemistry with fluorine-18 for the purpose of PET imaging.

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1
Cyclotron Research Center, Université de Liège, Sart-Tilman B.30, B-4000 Liège, Belgium.

Abstract

The alkyne-azide Cu(I)-catalyzed Huisgen cycloaddition, a click-type reaction, was used to label a double-stranded oligonucleotide (siRNA) with fluorine-18. An alkyne solid support CPG for the preparation of monostranded oligonucleotides functionalized with alkyne has been developed. Two complementary azide labeling agents (1-(azidomethyl)-4-[(18)F]fluorobenzene) and 1-azido-4-(3-[(18)F]fluoropropoxy)benzene have been produced with 41% and 35% radiochemical yields (decay-corrected), respectively. After annealing with the complementary strand, the siRNA was directly labeled by click chemistry with [(18)F]fluoroazide to produce the [(18)F]-radiolabeled siRNA with excellent radiochemical yield and purity.

PMID:
21174402
DOI:
10.1021/bc100263y
[Indexed for MEDLINE]
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