Evaluation of a bispidine‐based chelator for gallium‐68 and of the porphyrin conjugate as PET/PDT theranostic agent

Price, Thomas; Yap, Steven Y.; Gillet, Raphaël; Savoie, Huguette; Charbonnière, Loïc J.; Boyle, Ross W.; Nonat, Aline M.; Stasiuk, Graeme J.

Abstract

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.

Citation

Price, T., Yap, S. Y., Gillet, R., Savoie, H., Charbonnière, L. J., Boyle, R. W., Nonat, A. M., & Stasiuk, G. J. (2020). Evaluation of a bispidine‐based chelator for gallium‐68 and of the porphyrin conjugate as PET/PDT theranostic agent. Chemistry: a European journal, 26(34), 7602-7608. https://doi.org/10.1002/chem.201905776

• Journal Article Type: Article
• Acceptance Date: Feb 17, 2020
• Online Publication Date: Feb 18, 2020
• Publication Date: Jun 18, 2020
• Deposit Date: Feb 20, 2020
• Publicly Available Date: Feb 19, 2021
• Journal: Chemistry - A European Journal
• Print ISSN: 0947-6539
• Publisher: Wiley
• Peer Reviewed: Peer Reviewed
• Volume: 26
• Issue: 34
• Pages: 7602-7608
• DOI: https://doi.org/10.1002/chem.201905776
• Keywords: Bispidine; Gallium-68; Porphyrin; Radiochemistry; Theranostic
• Public URL: https://hull-repository.worktribe.com/output/3439279
• Publisher URL: https://chemistry-europe.onlinelibrary.wiley.com/doi/abs/10.1002/chem.201905776
• Additional Information: Received: 2019-12-23; Accepted: 2020-02-17; Published: 2020-02-18