Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 12, Pages 2491-2496Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00484
Keywords
Photodynamic therapy; activatable photosensitizers; resorufin; cancer cell selectivity; monoamine oxidase
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Funding
- Koc University
- Middle East Technical University-BAP
- European Research Council (ERC) under the European Union's Horizon 2020 research and innovation program [852614]
- European Research Council (ERC) [852614] Funding Source: European Research Council (ERC)
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A red-absorbing, water-soluble, and iodinated resorufin derivative (R1) that can be selectively activated with a monoamine oxidase (MAO) enzyme was synthesized, and its potential as a photodynamic therapy (PDT) agent was evaluated. R1 showed high O-1(2) generation yields in aqueous solutions upon addition of MAO isoforms, and it was further tested in cell culture studies. R1 induced photocytotoxicity after being triggered by endogenous MAO enzyme in cancer cells with a much higher efficiency in SH-SYSY neuroblastoma cells with high MAO-A expression. Additionally, R1 displayed differential cytotoxicity between cancer and normal cells, without any considerable dark toxicity. To the best of our knowledge, R1 marks the first example of a resorufin-based photosensitizer (PS) as well as the first anticancer drug that is activated by a MAO enzyme. Remarkably, the target PDT agent was obtained only in three steps as a result of versatile resorufin chemistry.
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