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  2. A glutathione-activated anthraquinone-based photosensitizer for selective photodynamic therapy of cancer cells overexpressing glutathione

A glutathione-activated anthraquinone-based photosensitizer for selective photodynamic therapy of cancer cells overexpressing glutathione

  • Bioorg Med Chem Lett. 2026 Mar 26:137:130632. doi: 10.1016/j.bmcl.2026.130632.
Yuzuha Miyazawa 1 Daisuke Takahashi 1 Kazunobu Toshima 2
Affiliations

Affiliations

  • 1 Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan.
  • 2 Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan. Electronic address: toshima@applc.keio.ac.jp.
Abstract

An anthraquinone derivative 2 was found to induce protein degradation under neutral conditions and without additives upon visible light irradiation. Based on this finding, a glutathione (GSH)-activatable Photosensitizer 3 was designed and synthesized. 3 showed minimal photoactivity in the absence of GSH, but upon reaction with GSH, it generated a highly active species that caused selective photo-cytotoxicity toward Cancer cells with elevated intracellular GSH levels. These results demonstrate the potential of anthraquinone-based systems as tunable and tumor-selective photosensitizers for photodynamic therapy.

Keywords

Activatable photosensitizer; Anthraquinone; Cancer cell; Glutathione; Photodynamic therapy.

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