Development of a FRET-based High-Throughput Screening System for the Discovery of Hsp90 Inhibitors

Bulletin of the Korean chemical society

Jonghoon Kim¹  Yeonjin Ko¹  Young Sun Chung¹  Sangmi Oh¹  Hanjae Lee¹  Seung Bum Park¹ 

关键词: Hsp90;    FlAsH;    Fluorescent resonance energy transfer (FRET);    High throughput screening (HTS);    Benzopyran analogs;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A FRET-based high-throughput screening system was developed for the discovery of competitive smallmolecule Hsp90 inhibitors. The biarsenical fluorescein derivative FlAsH and dabcyl-conjugated Hsp90 inhibitor GM were employed as the FRET donor and quencher, respectively. The spatial proximity perturbation between FlAsH-labeled Hsp90N and GM-dabcyl upon treatment of a small molecule led to changes in the FRET-induced fluorescence, monitored in a high-throughput fashion.

【 授权许可】

Unknown