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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



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).

Journal Article Type Article
Publication Date Jun 25, 2018
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
Institution 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
DOI https://doi.org/10.1039/c8cc03897j
Publisher URL http://pubs.rsc.org/en/Content/ArticleLanding/2018/CC/C8CC03897J#!divAbstract
Copyright Statement ©2018 The authors

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