Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release

Hua Tian,Shen You, Tianning Xiong,Ming Ji,Kehui Zhang,Lin Jiang,Tingting Du,Ying Li, Wenqian Liu,Songwen Lin,Xiaoguang Chen,Heng Xu

ACS medicinal chemistry letters（2023）

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摘要

A novel photocaged PI3K inhibitor 2 wasdesigned andsynthesized by introducing a cascade photocaging group to block itskey interaction with the kinase. Upon UV light irradiation, the photocagedcompound released a highly potent PI3K inhibitor to recover its anticancerproperties and a fluorescent dye for real-time reporting of drug release,providing a new approach for studying the PI3K signaling transductionpathway as well as developing precisely controlled cancer therapeutics.

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关键词

Phosphoinositide 3-kinase,Photocage,Drugrelease,Real-time reporting,Fluorescent dye

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