Design and development of enzymatically activatable photosensitizer based on unique characteristics of thiazole orange.
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.
Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan.
Yuichiro
Y
Koide
Yasuteru
Y
Urano
Akira
A
Yatsushige
Kenjiro
K
Hanaoka
Takuya
T
Terai
Tetsuo
T
Nagano
D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry*; D004247:DNA / Q000737:chemistry; D005453:Fluorescence; D006367:HeLa Cells; D006801:Humans; D006868:Hydrolysis; D015394:Molecular Structure; D010316:Particle Size; D017319:Photosensitizing Agents / Q000138:chemical synthesis* / Q000737:chemistry*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry*; D015203:Reproducibility of Results; D013499:Surface Properties; D001616:beta-Galactosidase / Q000737:chemistry / Q000378:metabolism*
D052160:Benzothiazoles; D017319:Photosensitizing Agents; D011804:Quinolines; C051000:thiazole orange; D004247:DNA; D001616:beta-Galactosidase