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 journalArticle

16 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

Fingerprint

Mitochondria
Chlorambucil
Prodrugs
Sulfhydryl Compounds
Agglomeration
Cell death
Caspases
Glutathione
Coloring Agents
Therapeutics
Dyes
Fluorescence
Chemical activation
Cells
Apoptosis
Cell Line
Neoplasms

ASJC Scopus subject areas

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

Cite this

Targeted combinational therapy inducing mitochondrial dysfunction. / Shin, Weon Sup; Park, Soon Ki; Verwilst, Peter; Koo, Seyoung; Lee, Joung Hae; Chi, Sung-Gil; Kim, Jong Seung.

In: Chemical Communications, Vol. 53, No. 7, 2017, p. 1281-1284.

Research output: Contribution to journalArticle

Shin, Weon Sup ; Park, Soon Ki ; Verwilst, Peter ; Koo, Seyoung ; Lee, Joung Hae ; Chi, Sung-Gil ; Kim, Jong Seung. / Targeted combinational therapy inducing mitochondrial dysfunction. In: Chemical Communications. 2017 ; Vol. 53, No. 7. pp. 1281-1284.
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