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Strain-Promoted Copper-Free “Click” Chemistry for 18F Radiolabeling of Bombesin

Authors

  • Lachlan S. Campbell-Verduyn,

    1. Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 4, Groningen 9747AG (The Netherlands)
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    • These authors contributed equally to this work.

  • Leila Mirfeizi,

    1. Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Hanzeplein 1, Groningen, 9713GZ (The Netherlands)
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    • These authors contributed equally to this work.

  • Anne K. Schoonen,

    1. Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 4, Groningen 9747AG (The Netherlands)
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  • Prof. Dr. Rudi A. Dierckx,

    1. Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Hanzeplein 1, Groningen, 9713GZ (The Netherlands)
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  • Prof. Dr. Philip H. Elsinga,

    Corresponding author
    1. Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Hanzeplein 1, Groningen, 9713GZ (The Netherlands)
    • Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Hanzeplein 1, Groningen, 9713GZ (The Netherlands)
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  • Prof. Dr. Ben L. Feringa

    Corresponding author
    1. Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 4, Groningen 9747AG (The Netherlands)
    • Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 4, Groningen 9747AG (The Netherlands)
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Abstract

original image

Klick für PET: Das GRP-Rezeptor-spezifische Peptid Bombesin, das häufig in der nuklearmedizinischen Tumorbildgebung eingesetzt wird, kann durch eine kupferfreie Azid-Alkin-„Klick-Reaktion“ rasch und unter milden Bedingungen mit 18F markiert werden. Die Wahl des Azids bestimmt die Hydrophobie des erhaltenen Peptids. Die In-vitro-Affinität der 18F-markierten Radiopharmazeutika für den Zielrezeptor bleibt in menschlichen Prostatakrebszellen erhalten.

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