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See detailGallium-68-labelled NOTA-oligonucleotides: An optimized method for their preparation
Gijs, Marlies; Dammicco, Sylvestre ULg; Warnier, Corentin ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2016)

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 ... [more ▼]

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. [less ▲]

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See detailHigh output [18F]FDOPA on AllInOne (Trasis) at commercial scale
Otabashi, Muhammad; Cascione, Christian; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2015, May), 58

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See detailGuidance on current good radiopharmacy practice for the small-scale preparation of radiopharmaceuticals using automated modules: a European perspective
Aerts, Joël ULg; Ballinger, james; Behe, Martin et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2014), 57

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See detailTHE USEFULNESS OF AN ARTERIOVENOUS SHUNT COMBINED WITH A BETA MICROPROBE FOR THE MEASUREMENT OF INPUT FUNCTION IN RATS
Warnock, Geoffrey ULg; Goblet, David ULg; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 106

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See detailUSE OF A BETA MICROPROBE SYSTEM AS AN AFFORDABLE TRANSLATIONAL TOOL COMPARED TO PET – EXAMPLES USING FDG AND 18F-FALLYPRIDE BINDING
Warnock, Geoffrey ULg; Goblet, David ULg; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 55

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See detailTIME-DEPENDENT PREFERENTIAL IN VIVO D2 OCCUPANCY BY AMISULPRIDE IN THE MEDIAL STRIATUM – CONTINUOUS MEASUREMENT USING A BETA MICROPROBE SYSTEM
Warnock, Geoffrey ULg; Goblet, David ULg; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 105

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See detailNew Improvements in the Enantioselective Synthesis of 2-[18F]Fluoro-L-Tyrosine and 6-[18F]Fluoro-L-Dopa
Libert, Lionel ULg; Lemaire, Christian ULg; Denoël, Thibaut ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 196

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See detailTertiary Alcohols to Avoid Evaporation in Fluorine-18 Labeling
Aerts, Joël ULg; Voccia, Samuel; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 204

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See detailFast and Reliable Method for the Preparation of Various [18F]Fluorobenzyl Halides
Lemaire, Christian ULg; Libert, Lionel ULg; Plenevaux, Alain ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 178

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See detailUse of Organic Bases for 18F-Fluoride Anion Exchange Elution avoiding the Classical Azeotropic drying Step Before Labeling
Lemaire, Christian ULg; Aerts, Joël ULg; Voccia, Samuel et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 198

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See detailAre Ionic Liquid Useful for Fluorine-18 Labeling?
Aerts, Joël ULg; Lemaire, Christian ULg; Plenevaux, Alain ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 193

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See detailLarge Scale Preparation of [18]Fluoromethoxybenzyl Bromides, Key Precursors for 2-[18F]Fluoro-L-Tyrosine and 6-[18F]Fluoro-L-Dopa
Libert, Lionel ULg; Lemaire, Christian ULg; Wouters, Ludovic ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 292

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See detailModified Non-Ionic Solid Supports: a Way to High Activity Fluorine-18 Radiochemistry in Microfluidic Devices
Aerts, Joël ULg; Voccia, Samuel; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2009, July), 52(S1), 12

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See detailSynthesis, quality control and in vivo evaluation of [I-123] rhTIMP-2, a potential tumour-imaging agent
Oltenfreiter, R.; Burvenich, I.; Staelens, L. et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2005), 48(5), 387-396

Matrix metalloproteinases (MMPs) are enzymes involved in the turnover of the extracellular matrix. Their overexpression in tumours may provide a target for diagnostic imaging by using labelled MMP ... [more ▼]

Matrix metalloproteinases (MMPs) are enzymes involved in the turnover of the extracellular matrix. Their overexpression in tumours may provide a target for diagnostic imaging by using labelled MMP inhibitors. MMPs are inhibited by endogenous tissue inhibitors of metalloproteinases (TIMPs). The enhanced production of MT1-MMP, located on the surface of cells within or in the direct vicinity of the tumour, and the high affinity interaction between TIMP-2 and MT1-MMP suggested that TIMP-2 could be a potential agent for non-invasive monitoring of cancer MMP levels, diagnosis of primary and secondary tumours and tumour response to MMP inhibitor therapy. There is also evidence that I-125-rhTIMP-2 internalizes, which is an important feature for its possible use as a radiotherapeuticum if labelled with I-131. Labelling of rhTIMP-2 was performed using the iodogen method resulting in a radiochemical yield of 51.1 +/- 11.8% (n = 5) and a radiochemical purity of > 98%. The trichloroacetic acid (TCA) precipitability of I-123 rhTIMP-2 was 95.2%. SDS-PAGE confirmed the correct size (21 kDa) of the purified I-123 rhTIMP-2 without degradation. HPLC showed one radioactive peak with a retention time corresponding to the nonlabelled rhTIMP-2. In vivo biodistribution showed no long-term accumulation in organs and the possibility to accumulate in the tumour. These results show the potential of I-123 rhTIMP-2 as tumour-imaging agent. Copyright (c) 2005 John Wiley [less ▲]

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See detailNew Methods For Halogenation of [18F]Fluorinated Benzyl Derivatives.
Kech, C.; Lemaire, Christian ULg; Brichard, L. et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2005), 48

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See detailEx Vivo Evaluation of p-[18F]D-MPPF for the Study of 5-HT1A Receptors.
Defraiteur, C.; Lemaire, Christian ULg; Luxen, André ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2005), 48

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See detailRadiochemical Synthesis of OCH2F-[18F]MPPF a New Analogue of p-[18F]MPPF for the Study of 5-HT1A Receptors.
Defraiteur, C.; Lemaire, Christian ULg; Luxen, André ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2005), 48

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See detailRadiochemical Synthesis of p-[18F]Desmethyl-MPPF (p-[18F]D-MPPF) for the Study of 5-HT1A Receptors
Defraiteur, Caroline; Plenevaux, Alain ULg; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2003, August), 46(S1), 157

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See detailSynthesis of [18F]fluorinated a-methyl-a-amino acids by phase transfer catalysis for potential PET application.
Wouters, L.; Lemaire, Christian ULg; Plenevaux, Alain ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (2003), 46

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