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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 9
BKCSDE 32(9)
September 20, 2011 

 
Title
Development of a FRET-based High-Throughput Screening System for the Discovery of Hsp90 Inhibitors
Author
Sangmi Oh, Yeonjin Ko, Hanjae Lee, Jonghoon Kim, Young Sun Chung, Seung Bum Park,*,
Keywords
Hsp90, FlAsH, Fluorescent resonance energy transfer (FRET), High throughput screening (HTS), Benzopyran analogs
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 fluorescence, monitored in a high-throughput fashion.
Page
3229 - 3232
Full Text
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