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Issue 57, 2018
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Selective radiolabelling with 68Ga under mild conditions: a route towards a porphyrin PET/PDT theranostic agent

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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 rapid 68Ga 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).

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

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Article information


Submitted
15 May 2018
Accepted
25 Jun 2018
First published
25 Jun 2018

Chem. Commun., 2018,54, 7952-7954
Article type
Communication

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

S. Y. Yap, T. W. Price, H. Savoie, R. W. Boyle and G. J. Stasiuk, Chem. Commun., 2018, 54, 7952
DOI: 10.1039/C8CC03897J

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