Evaluation of a bispidine-based chelator for gallium-68 and of the porphyrin conjugate as PET/PDT theranostic agent.
Fiche publication
Date publication
février 2020
Journal
Chemistry (Weinheim an der Bergstrasse, Germany)
Auteurs
Membres identifiés du Cancéropôle Est :
Dr CHARBONNIERE Loïc
Tous les auteurs :
Price T, Yap S, Gillet R, Savoie H, Charbonnière L, Boyle R, Nonat A, Stasiuk GJ
Lien Pubmed
Résumé
In this study a bispidine ligand has been applied to the complexation of gallium(III) and radiolabelled with gallium-68 for the first time. Despite its 5-coordinate nature, the resulting complex is stable in serum for over two hours, demonstrating a ligand system well matched to the imaging window of gallium-68 positron emission tomography (PET). To show the versatility of the bispidine ligand and its potential use in PET, the bifunctional chelator was conjugated to a porphyrin, producing a PET/PDT-theranostic, which showed the same level of stability to serum as the non-conjugated gallium-68 complex. The PET/PDT complex killed >90% of HT-29 cells upon light irradiation at 50 µM. This study shows bispidines have the versatility to be used as a ligand system for gallium-68 in PET.
Mots clés
Gallium-68* Bispidine * PET * PDT * theranostic
Référence
Chemistry. 2020 Feb 18;: