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Selective radiolabelling with 68Ga under mild conditions: a route towards a porphyrin PET/PDT theranostic agent

Yap, Steven Y.; Price, Thomas W.; Savoie, Huguette; Boyle, Ross W.; Stasiuk, Graeme J.

Authors

Steven Y. Yap

Thomas W. Price

Huguette Savoie

Graeme J. Stasiuk



Abstract

A theranostic conjugate for use as a positron emission tomography (PET) radiotracer and as a photosensitiser for photodynamic therapy (PDT) has been synthesised. A water-soluble porphyrin was coupled with the bifunctional chelate, H4Dpaa.ga. This conjugate is capable of rapid68Ga complexation under physiological conditions; with 93% and 80% radiochemical yields achieved, at pH 4.5 and pH 7.4 respectively, in 15 min at 25 °C. Photocytotoxicity was evaluated on HT-29 cells and showed the conjugate was capable of >50% cell death at 50 μM upon irradiation with light, while causing minimal toxicity in the absence of light (>95% cell survival).

Citation

Yap, S. Y., Price, T. W., Savoie, H., Boyle, R. W., & Stasiuk, G. J. (2018). Selective radiolabelling with 68Ga under mild conditions: a route towards a porphyrin PET/PDT theranostic agent. Chemical communications : Chem comm / the Royal Society of Chemistry, 54(57), 7952-7954. https://doi.org/10.1039/c8cc03897j

Journal Article Type Article
Acceptance Date Jun 25, 2018
Online Publication Date Jun 25, 2018
Publication Date Jun 25, 2018
Deposit Date Aug 7, 2018
Publicly Available Date Jun 26, 2019
Journal Chemical Communications
Print ISSN 1359-7345
Electronic ISSN 1364-548X
Publisher Royal Society of Chemistry
Peer Reviewed Peer Reviewed
Volume 54
Issue 57
Pages 7952-7954
DOI https://doi.org/10.1039/c8cc03897j
Public URL https://hull-repository.worktribe.com/output/939038
Publisher URL http://pubs.rsc.org/en/Content/ArticleLanding/2018/CC/C8CC03897J#!divAbstract
Copyright Statement ©2018 The authors

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