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    • 5. 发明申请
    • ACTIVATABLE TWO-COMPONENT PHOTOSENSITIZERS
    • 可激活的双组分光敏剂
    • WO2016081440A1
    • 2016-05-26
    • PCT/US2015/061051
    • 2015-11-17
    • CARNEGIE MELLON UNIVERSITY
    • BRUCHEZ, Marcel, P.HE, JianjunWANG, Yi
    • C07C233/36C07C233/40C07C211/43A61K41/00A61P35/00
    • A61K41/0057A61K47/64C07C211/43C07C233/36C07C233/40C09B11/10
    • Provided herein is a two-component photosensitizer, which demonstrated robust and selective killing effects for transfected HEK cells and affibody targeted A431 cancer cells when exposed to near infrared light excitation. Free MG2I is a pure and stable fluorogen; it is easy to synthesize and modify, and has no toxicity to cells. Unlike conventional photosensitizers, the dye and FAP itself has no photosensitizing effect until they are bound. Also unlike other activation methods, the activation step is achieved by adding the fluorogen, not the presence of the targeted molecule, requiring an 'active' activation instead of a 'passive' activation. This method offers the ability to locally switch-on and selective generation of singlet oxygen at the target site and can be used for a wide variety of molecular targets.
    • 本文提供了一种双组分光敏剂,当暴露于近红外光激发时,其显示了对转染的HEK细胞和亲和体靶向的A431癌细胞的鲁棒和选择性杀伤作用。 免费的MG2I是一种纯而稳定的荧光; 易于合成和修饰,对细胞无毒性。 与传统的光敏剂不同,染料和FAP本身在结合之前就没有光敏作用。 与其他活化方法不同,活化步骤通过添加荧光素而不是靶向分子的存在来实现,需要“活性”活化而不是“被动”激活。 该方法提供了在目标位点局部开启和选择性生成单线态氧的能力,可用于各种分子靶标。