ArticleApplied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine2009
Automated synthesis of an 18F-labelled pyridine-based alkylating agent for high yield oligonucleotide conjugation.
Article in Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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4 citing papers in PubMed, 16 citations in OpenAlex.
- Light-Triggered Radiochemical Synthesis: A NovelContrast media & molecular imaging · 2018Article
- Review
- Ortho-Stabilized (18) F-Azido Click Agents and their Application in PET Imaging with Single-Stranded DNA Aptamers.Angewandte Chemie (International ed. in English) · 2015Article
- In vitro characterization of two novel biodegradable vectors for the delivery of radiolabeled antisense oligonucleotides.Cancer biotherapy & radiopharmaceuticals · 2010Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Alkylating agents have been shown to be very promising for the radiolabelling of oligonucleotides with fluorine-18. In this report we describe the fully automated synthesis of 2-bromo-N-[3-(2-[(18)F]fluoropyridin-3-yloxy)propyl]acetamide ([(18)F]FPyBrA) utilizing a modular synthesis unit. Reaction conditions for the coupling of this pyridine-based alkylating agent at the 5' end of a fully phosphorothioated random 20-mer DNA sequence were optimized to achieve very high radiochemical yields (>90%) and a maximum specific activity of 5-6 GBq/micromoL. The potential for rapid purification by solid phase extraction without need of chromatographic isolation of the radiolabelled oligonucleotide presents an overall benefit for the application of oligonucleotides in preclinical studies and potential clinical applications.
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