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Fluorine-18 labelling of small interfering RNAs (siRNAs) for PET imaging

✍ Scribed by Thomas Viel; Bertrand Kuhnast; Françoise Hinnen; Raphaël Boisgard; Bertrand Tavitian; Frédéric Dollé

Publisher
John Wiley and Sons
Year
2007
Tongue
French
Weight
181 KB
Volume
50
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Small interfering RNAs (siRNAs), a class of macromolecules constituted by the association of two single‐stranded ribonucleic acids of short sequences, have been labelled with the positron‐emitter fluorine‐18 (T~1/2~: 109.8 min). The strategy involves (1) prosthetic conjugation of a single‐stranded oligonucleotide with [^18^F]FPyBrA (N‐[3‐(2‐[^18^F]fluoropyridin‐3‐yloxy)‐propyl]‐2‐bromoacetamide) followed by (2) formation of the target duplex by annealing with the complementary sequence, therefore, permitting parallel and combinatorial preparation of [^18^F]siRNAs. Pure fluorine‐18‐labelled siRNAs (0.55–1.11 GBq, specific activity: 74–148 GBq/µmol at EOB) could be obtained within 165 min starting from 37.0 GBq of starting [^18^F]fluoride (1.5–3.0%, non‐decay‐corrected isolated yields). Copyright © 2007 John Wiley & Sons, Ltd.

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