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

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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