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    Automation of [(18) F]fluoroacetaldehyde synthesis: application to a recombinant human interleukin-1 receptor antagonist (rhIL-1RA).

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    Authors
    Morris, Olivia C
    McMahon, Adam
    Boutin, Herve
    Grigg, J
    Prenant, Christian
    Affiliation
    Wolfson Molecular Imaging Centre, CRUK and EPSRC Cancer Imaging Centre in Cambridge and Manchester, The University of Manchester, Manchester,
    Issue Date
    2016-04-06
    
    Metadata
    Show full item record
    Abstract
    [(18) F]Fluoroacetaldehyde is a biocompatible prosthetic group that has been implemented pre-clinically using a semi-automated remotely controlled system. Automation of radiosyntheses permits use of higher levels of [(18) F]fluoride whilst minimising radiochemist exposure and enhancing reproducibility. In order to achieve full-automation of [(18) F]fluoroacetaldehyde peptide radiolabelling, a customised GE Tracerlab FX-FN with fully programmed automated synthesis was developed. The automated synthesis of [(18) F]fluoroacetaldehyde is carried out using a commercially available precursor, with reproducible yields of 26% ± 3 (decay-corrected, n = 10) within 45 min. Fully automated radiolabelling of a protein, recombinant human interleukin-1 receptor antagonist (rhIL-1RA), with [(18) F]fluoroacetaldehyde was achieved within 2 h. Radiolabelling efficiency of rhIL-1RA with [(18) F]fluoroacetaldehyde was confirmed using HPLC and reached 20% ± 10 (n = 5). Overall RCY of [(18) F]rhIL-1RA was 5% ± 2 (decay-corrected, n = 5) within 2 h starting from 35 to 40 GBq of [(18) F]fluoride. Specific activity measurements of 8.11-13.5 GBq/µmol were attained (n = 5), a near three-fold improvement of those achieved using the semi-automated approach. The strategy can be applied to radiolabelling a range of peptides and proteins with [(18) F]fluoroacetaldehyde analogous to other aldehyde-bearing prosthetic groups, yet automation of the method provides reproducibility thereby aiding translation to Good Manufacturing Practice manufacture and the transformation from pre-clinical to clinical production.
    Citation
    Automation of [(18) F]fluoroacetaldehyde synthesis: application to a recombinant human interleukin-1 receptor antagonist (rhIL-1RA). 2016: J Labelled Comp Radiopharm
    Journal
    Journal of Labelled Compounds & Radiopharmaceuticals
    URI
    http://hdl.handle.net/10541/613332
    DOI
    10.1002/jlcr.3393
    PubMed ID
    27061216
    Type
    Article
    Language
    en
    ISSN
    1099-1344
    ae974a485f413a2113503eed53cd6c53
    10.1002/jlcr.3393
    Scopus Count
    Collections
    All Paterson Institute for Cancer Research

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