Bulletin of the Korean Chemical Society

  • 제32권9호
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  • Pages.3229-3232
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  • 2011
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  • 0253-2964(pISSN)
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  • 1229-5949(eISSN)
대한화학회 (Korean Chemical Society)
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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)
  • 투고 : 2011.06.30
  • 심사 : 2011.07.13
  • 발행 : 2011.09.20
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초록

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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피인용 문헌

  1. Biarsenical fluorescent probes for multifunctional site-specific modification of proteins applicable in life sciences: an overview and future outlook vol.12, pp.8, 2020, https://doi.org/10.1039/d0mt00093k