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

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

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.
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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