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.
Steven Y. Yap
Loïc J. Charbonnière
Professor Ross Boyle R.W.Boyle@hull.ac.uk
Professor of Biological Chemistry
Aline M. Nonat
Graeme J. Stasiuk
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.
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|
|Peer Reviewed||Peer Reviewed|
|Keywords||Bispidine; Gallium-68; Porphyrin; Radiochemistry; Theranostic|
|Additional Information||Received: 2019-12-23; Accepted: 2020-02-17; Published: 2020-02-18|
This file is under embargo due to copyright reasons.
Contact G.Stasiuk@hull.ac.uk to request a copy for personal use.
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