Reference : Gallium-68-labelled NOTA-oligonucleotides: An optimized method for their preparation
Scientific journals : Article
Physical, chemical, mathematical & earth Sciences : Chemistry
Gallium-68-labelled NOTA-oligonucleotides: An optimized method for their preparation
Gijs, Marlies mailto [> >]
Dammicco, Sylvestre mailto [Université de Liège > Département de chimie (sciences) > Laboratoire de chimie organique de synthèse >]
Warnier, Corentin mailto [Université de Liège > > Centre de recherches du cyclotron >]
Aerts, An mailto [> >]
Impens, Nathalie mailto [> >]
Matthias, D'Huyvetter mailto [> >]
Léonard, Marc mailto [> >]
Baatout, Sarah mailto [> >]
Luxen, André mailto [Université de Liège > Département de chimie (sciences) > Laboratoire de chimie organique de synthèse >]
Journal of Labelled Compounds and Radiopharmaceuticals
John Wiley & Sons Ltd.
[en] DNA ; NOTA ; Gallium-68
[en] One of the most essential aspects to the success of radiopharmaceuticals is an easy and reliable radiolabelling protocol to obtain pure and stable products. In this study, we optimized the bioconjugation and gallium-68 ((68) Ga) radiolabelling conditions for a single-stranded 40-mer DNA oligonucleotide, in order to obtain highly pure and stable radiolabelled oligonucleotides. Quantitative bioconjugation was obtained for a disulfide-functionalized oligonucleotide conjugated to the macrocylic bifunctional chelator MMA-NOTA (maleimido-mono-amide (1,4,7-triazanonane-1,4,7-triyl)triacetic acid). Next, this NOTA-oligonucleotide bioconjugate was radiolabelled at room temperature with purified and pre-concentrated (68) Ga with quantitative levels of radioactive incorporation and high radiochemical and chemical purity. In addition, high chelate stability was observed in physiological-like conditions (37 °C, PBS and serum), in the presence of a transchelator (EDTA) and transferrin. A specific activity of 51.1 MBq/nmol was reached using a 1470-fold molar excess bioconjugate over (68) Ga. This study presents a fast, straightforward and reliable protocol for the preparation of (68) Ga-radiolabelled DNA oligonucleotides under mild reaction conditions and without the use of organic solvents. The methodology herein developed will be applied to the preparation of oligonucleotidic sequences (aptamers) targeting the human epidermal growth factor receptor 2 (HER2) for cancer imaging.

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