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

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.

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Publication Details

Journal
Bioorganic & Medicinal Chemistry Letters
Published
2026-03-01
DOI
https://doi.org/10.1016/j.bmcl.2026.130632
Primary Topic
Photodynamic Therapy Research Studies
Type
article
Field-Weighted Citation Impact
0.00
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article

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

Kazunobu Toshima, Yuri Miyazawa, Daisuke Takahashi
Bioorganic & Medicinal Chemistry Letters
Photodynamic Therapy Research Studies
article

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

Kazunobu Toshima, Yuri Miyazawa, Daisuke Takahashi
article en

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.

Bioorganic & Medicinal Chemistry Letters
Keio University (JP)
Good health and well-being
Openalex Percentile: Top 7%
Photodynamic Therapy Research Studies
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