Synthesis and evaluation of zirconium-89 labelled and long-lived GLP-1 receptor agonists for PET imaging.
Fiche publication
Date publication
décembre 2019
Journal
Nuclear medicine and biology
Auteurs
Membres identifiés du Cancéropôle Est :
Pr DENAT Franck, Dr GONCALVES Victor, Dr VALVERDE Ibai
Tous les auteurs :
Jacobsen CB, Raavé R, Pedersen MØ, Adumeau P, Moreau M, Valverde IE, Bjørnsdottir I, Kristensen JB, Grove MF, Raun K, McGuire J, Goncalves V, Heskamp S, Denat F, Gustafsson M
Lien Pubmed
Résumé
Lately, zirconium-89 has shown great promise as a radionuclide for PET applications of long circulating biomolecules. Here, the design and synthesis of protracted and long-lived GLP-1 receptor agonists conjugated to desferrioxamine and labelled with zirconium-89 is presented with the purpose of studying their in vivo distribution by PET imaging. The labelled conjugates were evaluated and compared to a non-labelled GLP-1 receptor agonist in both in vitro and in vivo assays to certify that the modification did not significantly alter the peptides' structure or function. Finally, the zirconium-89 labelled peptides were employed in PET imaging, providing visual verification of their in vivo biodistribution.
Mots clés
Bioconjugation, GLP-1, Molecular imaging, PET, Radiolabelling, Zirconium-89
Référence
Nucl. Med. Biol.. 2019 Dec 4;82-83:49-56