Development of a FRET-based high-throughput screening system for the discovery of Hsp90 inhibitors

…, HJ Lee, JH Kim, YS Chung, SB Park

Index: Oh, Sangmi; Ko, Yeonjin; Lee, Hanjae; Kim, Jonghoon; Chung, Young Sun; Park, Seung Bum Bulletin of the Korean Chemical Society, 2011 , vol. 32, # 9 p. 3229 - 3232

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Abstract

Abstract 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 ...