A tetrazine-responsive isonitrile-caged photosensitiser for site-specific photodynamic therapy

Research output: Journal Publications and ReviewsRGC 21 - Publication in refereed journalpeer-review

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Original languageEnglish
Pages (from-to)663-674
Journal / PublicationJournal of Controlled Release
Online published14 Dec 2022
Publication statusPublished - Jan 2023



We report herein a versatile and efficient bioorthogonal strategy to actualise targeted delivery and site-specific activation of photosensitisers for precise antitumoural photodynamic therapy. The strategy involved the use of an isonitrile-caged distyryl boron dipyrromethene-based photosensitiser, labelled as NC-DSBDP, of which the photoactivities could be specifically activated upon conversion of the meso ester substituent to carboxylate initiated by the [4 + 1] cycloaddition with a tetrazine derivative. By using two tetrazines conjugated with a galactose moiety or the GE11 peptide, labelled as gal-Tz and GE11-Tz, we could selectively label the cancer cells overexpressed with the asialoglycoprotein receptor and the epidermal growth factor receptor respectively. Upon encountering the internalised NC-DSBDP, these tetrazines triggered the “ester-to-carboxylate” transformation of this compound, activating its fluorescence and reactive oxygen species generation inside the target cells. The bioorthogonal activation was also demonstrated in vivo, leading to effective photo-eradication of the tumour in nude mice.

Research Area(s)

  • Bioorthogonal chemistry, Boron dipyrromethene, Isonitrile, Photodynamic therapy, Tetrazine

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