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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

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. (in press). Evaluation of a bispidine‐based chelator for gallium‐68 and of the porphyrin conjugate as PET/PDT theranostic agent. Chemistry : a European journal, https://doi.org/10.1002/chem.201905776

Journal Article Type Article
Acceptance Date Feb 17, 2020
Online Publication Date Feb 18, 2020
Deposit Date Feb 20, 2020
Publicly Available Date Nov 30, -0001
Journal Chemistry - A European Journal
Print ISSN 0947-6539
Electronic ISSN 1521-3765
Publisher Wiley
Peer Reviewed Peer Reviewed
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