An alkaline phosphatase-activatable photosensitizer based on 2-anthrol for selective targeting of cancer cells

  • Bioorg Med Chem Lett. 2025 Dec 15:129:130371. doi: 10.1016/j.bmcl.2025.130371.
Yusha Li  1 ,  Yuki Masuda  1 ,  Yuzuha Miyazawa  1 ,  Daisuke Takahashi  1 ,  Kazunobu Toshima  2
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: [email protected].
PMID: 40812517 DOI: 10.1016/j.bmcl.2025.130371
Abstract

2-Anthrol (2) was found to induce protein degradation under neutral conditions and without the need for additives upon visible light irradiation. Based on this simple and small scaffold, a novel Photosensitizer 4 was designed and synthesized, which is specifically activated by the tumor-associated biomarker Alkaline Phosphatase (ALP). Upon visible light exposure, 4 exhibited selective photo-cytotoxicity toward Cancer cells overexpressing ALP, demonstrating its potential as a targeted phototherapeutic agent.

Keywords
2-Anthrol; Activatable photosensitizer; Alkaline phosphatase; Cancer cell; Photodynamic therapy.
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