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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.

Authors

Thomas Price

Steven Y. Yap

Raphaël Gillet

Huguette Savoie

Loïc J. Charbonnière

Ross W. Boyle

Aline M. Nonat

Graeme J. Stasiuk



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., …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
Electronic ISSN 1521-3765
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