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Bioconjugation Methods for Radiopharmaceutical Chemistry

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Radiopharmaceutical Chemistry

Abstract

Bioconjugation methods are critical for the stable conjugation of metallic and nonmetallic radionuclides to biomolecular targeting vectors. In contrast to the radiosynthesis of most small molecule tracers, the creation of biomolecular imaging agents typically employs biomolecules in their native form, eschews protective groups, and generally involves no more than one or two steps. Because the majority of biomolecules contain not only different functional groups but also multiple copies thereof at different positions, particular attention has to be paid to the chemoselectivity and site-specificity of bioconjugation reactions. In addition, the sensitivity of many biomolecules frequently means that mild aqueous reaction conditions must be used, a requirement which imposes further restrictions on radiolabeling protocols. Taken together, these factors combine to make the controlled functionalization of biomolecules a non-trivial task. In this chapter, we discuss the various bioconjugation methods that have been harnessed for the development of biomolecular radiopharmaceuticals. Several classical approaches based on bifunctional reactive probes will be discussed as well as a number of more recently developed strategies employing enzymes and biorthogonal chemistry. The strengths and limitations of each approach will be addressed, and examples of the application of each strategy to different classes of biomolecules will be provided.

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Authors and Affiliations

  1. Ludwig Boltzmann Institute Applied Diagnostics, General Hospital Vienna (AKH), Vienna, Austria

    Jens Cardinale, Carolina Giammei, Nedra Jouini & Thomas L. Mindt

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  1. Jens Cardinale
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  2. Carolina Giammei
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  3. Nedra Jouini
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  4. Thomas L. Mindt
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Corresponding author

Correspondence to Thomas L. Mindt .

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Editors and Affiliations

  1. Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, USA

    Jason S. Lewis

  2. Department of Radiology and Nuclear Medicine, VU University Medical Center, Amsterdam, The Netherlands

    Albert D. Windhorst

  3. Department of Chemistry, Hunter College, City University of New York, New York, NY, USA

    Brian M. Zeglis

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Cardinale, J., Giammei, C., Jouini, N., Mindt, T.L. (2019). Bioconjugation Methods for Radiopharmaceutical Chemistry. In: Lewis, J., Windhorst, A., Zeglis, B. (eds) Radiopharmaceutical Chemistry. Springer, Cham. https://doi.org/10.1007/978-3-319-98947-1_25

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  • DOI: https://doi.org/10.1007/978-3-319-98947-1_25

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  • Online ISBN: 978-3-319-98947-1

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