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Fluorine‐18 labelling of small interfering RNAs (siRNAs) for PET imaging
Author(s) -
Viel Thomas,
Kuhnast Bertrand,
Hinnen Françoise,
Boisgard Raphaël,
Tavitian Bertrand,
Dollé Frédéric
Publication year - 2007
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.1411
Subject(s) - chemistry , small interfering rna , oligonucleotide , fluorine , rna , specific activity , radiochemistry , combinatorial chemistry , dna , biochemistry , enzyme , organic chemistry , gene
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.