Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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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)
  • Received : 2011.06.30
  • Accepted : 2011.07.13
  • Published : 2011.09.20
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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.

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References

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