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.

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
• Contract Date: Aug 7, 2018