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http://dx.doi.org/10.5012/bkcs.2011.32.9.3229

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

Oh, Sang-Mi (Department of Chemistry, Seoul National University)
Ko, Yeon-Jin (Department of Chemistry, Seoul National University)
Lee, Han-Jae (Department of Chemistry, Seoul National University)
Kim, Jong-Hoon (Department of Chemistry, Seoul National University)
Chung, Young-Sun (Department of Counseling, Korea Cyber University)
Park, Seung-Bum (Department of Chemistry, Seoul National University)
Publication Information
Bulletin of the Korean Chemical Society / v.32, no.9, 2011 , pp. 3229-3232 More about this Journal
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.
Keywords
Hsp90; FlAsH; Fluorescent resonance energy transfer (FRET); High throughput screening (HTS); Benzopyran analogs;
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