Fluorine‐18 labelling of small interfering RNAs (siRNAs) for PET imaging |
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| Authors: | Thomas Viel Bertrand Kuhnast Françoise Hinnen Raphaël Boisgard Bertrand Tavitian Frédéric Dollé |
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| Affiliation: | 1. CEA, DSV, I2BM, SHFJ, LIEG ‐ INSERM U803, Institut d'Imagerie Biomédicale, Service Hospitalier Frédéric Joliot, Laboratoire d'Imagerie de l'Expression des Gènes, 4 Place du Général Leclerc, F‐91401 Orsay, France;2. CEA, DSV, I2BM, SHFJ, LIME, Institut d'Imagerie Biomédicale, Service Hospitalier Frédéric Joliot, Laboratoire d'Imagerie Moléculaire Expérimentale, 4 Place du Général Leclerc, F‐91401 Orsay, France |
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| 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 (T1/2: 109.8 min). The strategy involves (1) prosthetic conjugation of a single‐stranded oligonucleotide with [18F]FPyBrA (N‐[3‐(2‐[18F]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 [18F]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 [18F]fluoride (1.5–3.0%, non‐decay‐corrected isolated yields). Copyright © 2007 John Wiley & Sons, Ltd. |
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| Keywords: | fluorine‐18 siRNA oligonucleotide FPyBrA |
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