Koide Yuichiro, Urano Yasuteru, Yatsushige Akira, Hanaoka Kenjiro, Terai Takuya, Nagano Tetsuo
Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan.
J Am Chem Soc. 2009 May 6;131(17):6058-9. doi: 10.1021/ja900443b.
A novel design strategy for controlling the fluorescence and photosensitizing ability of thiazole orange (TO) has been developed. The validity of this approach was demonstrated by the synthesis of a beta-galactosidase-activatable photosensitizer, PhoTO-Gal, in which fluorescence is simultaneously activated. PhoTO-Gal was demonstrated to kill HEK293 lacZ(+) cells, which express beta-galactosidase, but not HEK293 lacZ(-) cells, under light illumination. Such activatable photosensitizers should allow more refined PDT without the side effect of prolonged light sensitivity and should also be useful as tools for reporter enzyme expression-specific cell ablation.
已开发出一种用于控制噻唑橙（TO）荧光和光敏能力的新型设计策略。通过合成一种β-半乳糖苷酶可激活的光敏剂PhoTO-Gal证明了该方法的有效性，其中荧光同时被激活。在光照下，PhoTO-Gal被证明可杀死表达β-半乳糖苷酶的HEK293 lacZ(+)细胞，但不会杀死HEK293 lacZ(-)细胞。这种可激活的光敏剂应能实现更精确的光动力疗法，而不会产生长时间光敏感的副作用，并且还可用作报告酶表达特异性细胞消融的工具。
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