一种基于2-人酚的碱性磷酸酶可激活光敏剂，用于选择性靶向癌细胞。

IF 2.2 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-08-12 DOI:10.1016/j.bmcl.2025.130371

Yusha Li, Yuki Masuda, Yuzuha Miyazawa, Daisuke Takahashi, Kazunobu Toshima

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引用次数: 0

摘要

发现2- anthrol(2)在中性条件下诱导蛋白质降解，在可见光照射下无需添加添加剂。在此基础上，设计并合成了一种新型光敏剂4，该光敏剂可被肿瘤相关生物标志物碱性磷酸酶（ALP）特异性激活。在可见光照射下，4对过度表达ALP的癌细胞表现出选择性光细胞毒性，表明其作为靶向光疗剂的潜力。

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

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

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.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.