Mitochondria-targeted aggregation induced emission theranostics: Crucial importance of: In situ activation

Weon Sup Shin, Min Goo Lee, Peter Verwilst, Joung Hae Lee, Sung-Gil Chi, Jong Seung Kim

Research output: Contribution to journalArticle

55 Citations (Scopus)

Abstract

Tissue selective targeting and specific suborganellular localization combined with an efficient pathology associated enzymatic activation of drugs in drug delivery systems may exhibit a clear advantage over conventional cancer treatment. Here, a mitochondria targeted aggregation induced emission (AIE) fluorophore further conjugated with an NAD(P)H:quinone oxidoreductase-1 (NQO1) cleavable masking unit showed preferential uptake in cancer cells and was selectively activated, resulting in bright AIE fluorescence and apoptosis via the caspase pathway, triggered by mitochondrial dysfunction. In vivo experimental data further support the conclusions from in vitro experiments, clearly showing the dependence of the therapy's success on both the suborganelle localization and specific in situ activation. And the site specific and enzyme dependent activation and aggregation was further supported by in vivo and ex vivo imaging. As a whole, the data comprised in this work represent a strong argument for the further development of this type of novel anticancer drugs.

Original languageEnglish
Pages (from-to)6050-6059
Number of pages10
JournalChemical Science
Volume7
Issue number9
DOIs
Publication statusPublished - 2016

ASJC Scopus subject areas

  • Chemistry(all)

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