University of Hull logo

Development of PDT/PET theranostics: synthesis and biological evaluation of an ¹⁸F-radiolabeled water soluble porphyrin

Entract, Guy M.; Bryden, Francesca; Domarkas, Juozas; Savoie, Huguette; Allott, Louis; Archibald, Stephen J.; Cawthorne, Chris; Boyle, Ross W.

Authors

Guy M. Entract

Francesca Bryden

Juozas Domarkas

Huguette Savoie

Louis Allott

Chris Cawthorne

Professor Ross Boyle R.W.Boyle@hull.ac.uk
Professor of Biological Chemistry/ Module Coordinator for Biological Macromolecules/ Biological Safety and Genetic Modifications Committee Member

Abstract

Synthesis of the first water-soluble porphyrin radiolabeled with fluorine-18 is described: a new molecular theranostic agent which integrates the therapeutic selectivity of photodynamic therapy (PDT) with the imaging efficacy of positron emission tomography (PET). Generation of the theranostic was carried out through the conjugation of a cationic water-soluble porphyrin bearing an azide functionality to a fluorine-18 radiolabeled prosthetic bearing an alkyne functionality through click conjugation, with excellent yields obtained in both cold and hot synthesis. Biological evaluation of the synthesized structures shows the first example of an 18 F-radiolabeled porphyrin retaining photocytotoxicity following radiolabeling and demonstrable conjugate uptake and potential application as a radiotracer in vivo. The promising results gained from biological evaluation demonstrate the potential of this structure as a clinically relevant theranostic agent, offering exciting possibilities for the simultaneous imaging and photodynamic treatment of tumors.

Journal Article Type Article
Publication Date Dec 7, 2015
Journal Molecular pharmaceutics
Print ISSN 1543-8384
Electronic ISSN 1543-8392
Publisher American Chemical Society
Peer Reviewed Peer Reviewed
Volume 12
Issue 12
Pages 4414-4423
Institution Citation Entract, G. M., Bryden, F., Domarkas, J., Savoie, H., Allott, L., Archibald, S. J., …Boyle, R. W. (2015). Development of PDT/PET theranostics: synthesis and biological evaluation of an ¹⁸F-radiolabeled water soluble porphyrin. Molecular pharmaceutics, 12(12), 4414-4423. https://doi.org/10.1021/acs.molpharmaceut.5b00606
DOI https://doi.org/10.1021/acs.molpharmaceut.5b00606
Keywords Flourine-18, PET imaging, Photodynamic therapy, Porphyrins, Theranostics
Publisher URL http://pubs.acs.org/doi/abs/10.1021/acs.molpharmaceut.5b00606
Copyright Statement © 2015 The authors
Additional Information This document is the Accepted Manuscript version of a Published Work that appeared in final form in Molecular pharmaceutics, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.10...s.molpharmaceut.5b00606

Files




You might also like


Downloadable Citations