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Evaluation of a Bispidine‐Based Chelator for Gallium‐68 and of the Porphyrin Conjugate as PET/PDT Theranostic Agent
Author(s) -
Price Thomas W.,
Yap Steven Y.,
Gillet Raphaël,
Savoie Huguette,
Charbonnière Loïc J.,
Boyle Ross W.,
at Aline M.,
Stasiuk Graeme J.
Publication year - 2020
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201905776
Subject(s) - gallium , porphyrin , ligand (biochemistry) , conjugate , chelation , conjugated system , bifunctional , photodynamic therapy , positron emission tomography , chemistry , materials science , combinatorial chemistry , photochemistry , nuclear medicine , inorganic chemistry , medicine , receptor , organic chemistry , biochemistry , mathematical analysis , mathematics , catalysis , polymer
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 μ m . This study shows bispidines have the versatility to be used as a ligand system for gallium‐68 in PET.