Targeted combinational therapy inducing mitochondrial dysfunction

Weon Sup Shin, Soon Ki Park, Peter Verwilst, Seyoung Koo, Joung Hae Lee, Sung-Gil Chi, Jong Seung Kim

Research output: Contribution to journalArticlepeer-review

30 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1281-1284
Number of pages4
JournalChemical Communications
Volume53
Issue number7
DOIs
Publication statusPublished - 2017

Bibliographical note

Funding Information:
This work was supported by the Ministry of Science, ICT and Future Planning (MSIP) of the National Research Foundation of Korea (No. 2009-0081566 for JSK and NRF-20158A2A1A01005389 for SGC). This research was supported by the Korea Research Fellowship Program funded by the Ministry of Science, ICT and Future Planning through the National Research Foundation of Korea (2016H1D3A1938052 for PV).

Publisher Copyright:
© The Royal Society of Chemistry.

Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.

ASJC Scopus subject areas

  • Catalysis
  • Electronic, Optical and Magnetic Materials
  • Ceramics and Composites
  • General Chemistry
  • Surfaces, Coatings and Films
  • Metals and Alloys
  • Materials Chemistry

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