Prosthetic groups for radioiodination and astatination of peptides and proteins: a comparative study of five potential bioorthogonal labeling strategies
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.
https://www.hal.inserm.fr/inserm-01939636
Contributor : Elizabeth Bernardo
<>
Submitted on : Thursday, November 29, 2018 - 3:56:57 PM
Last modification on : Monday, May 20, 2019 - 3:32:02 PM
File
Restricted access
To satisfy the distribution rights of the publisher, the document is embargoed
until : 2019-05-26
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 & medicinal chemistry, Elsevier, In press, pp.167-174. ⟨10.1016/j.bmc.2018.11.034⟩. ⟨inserm-01939636⟩
