Issue 7, 2017

Targeted combinational therapy inducing mitochondrial dysfunction

Abstract

We report on a mitochondria-specific combinational theranostic agent, 1. This system contains a chlorambucil prodrug and an aggregation induced emission dye. In addition, compound 1 bears both an intracellular thiol-triggered moiety and a mitochondria targeting unit (triphenylphosphonium). Glutathione (GSH) is the most abundant thiol and its concentrations are significantly higher in a great number of cancer cell lines, compared to normal cells. The GSH-induced prodrug 1 upon activation releases chlorambucil and exhibits mitochondria targeted aggregation induced emission (AIE) fluorescence, resulting in cell apoptosis via the caspase pathway due to mitochondrial dysfunction.

Graphical abstract: Targeted combinational therapy inducing mitochondrial dysfunction

Supplementary files

Article information

Article type
Communication
Submitted
10 nov 2016
Accepted
22 dec 2016
First published
22 dec 2016

Chem. Commun., 2017,53, 1281-1284

Targeted combinational therapy inducing mitochondrial dysfunction

W. S. Shin, S. K. Park, P. Verwilst, S. Koo, J. H. Lee, S. Chi and J. S. Kim, Chem. Commun., 2017, 53, 1281 DOI: 10.1039/C6CC08977A

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