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

https://www.ncbi.nlm.nih.gov/pubmed/32068310

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.