Prosthetic groups for radioiodination and astatination of peptides and proteins: a comparative study of five potential bioorthogonal labeling strategies

Laurent Navarro 1 Marion Berdal 1 Michel Chérel 1 Frédéric Pecorari 1 Jean-François Gestin 1 François Guérard 1, *
* Corresponding author
1 CRCINA - Département NOHMAD - Equipe 13 - Oncologie nucléaire
CRCINA - Centre de recherche de Cancérologie et d'Immunologie / Nantes - Angers
Abstract : 125I- and 211At-labeled azide and tetrazine (Tz) based prosthetic groups for bioorthogonal conjugation were designed and tested in a comparative study of five bioorthogonal systems. All five bioconjugation reactions conducted on a model clickable peptide led to quantitative yields within less than a minute to several hours depending on the system used. Transferability to the labeling of an IgG was demonstrated with one of the bioorthogonal system. This study provides several new alternatives to the conventional and suboptimal approach currently in use for radioiodination and astatination of biomolecules and should accelerate the development of new probes with these radionuclides for applications in nuclear imaging and targeted alpha-therapy.
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Submitted on : Thursday, November 29, 2018 - 3:56:57 PM
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Laurent Navarro, Marion Berdal, Michel Chérel, Frédéric Pecorari, Jean-François Gestin, et al.. Prosthetic groups for radioiodination and astatination of peptides and proteins: a comparative study of five potential bioorthogonal labeling strategies. Bioorganic and Medicinal Chemistry, Elsevier, In press, pp.167-174. ⟨10.1016/j.bmc.2018.11.034⟩. ⟨inserm-01939636⟩

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