Mitochondria-targeted aggregation induced emission theranostics: crucial importance of in situ activation.

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 s

SUBMITTER: Shin WS 

PROVIDER: S-EPMC6022148 | biostudies-literature | 2016 Sep

REPOSITORIES: biostudies-literature