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

Research output: Contribution to journalArticle

Thomas Price, Steven Yap, Raphaël Gillet, Huguette Savoie, Loic Charbonnière, Ross Boyle, Aline Nonat, Graeme J Stasiuk

Original languageEnglish
Pages (from-to)7602-7608
Number of pages7
JournalChemistry (Weinheim an der Bergstrasse, Germany)
Volume26
Issue number34
Early online date18 Feb 2020
DOIs
Publication statusPublished - 18 Jun 2020

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© 2020 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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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.

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