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

被引：2
|
作者：
Oh, Sangmi [1 ]
Ko, Yeonjin [1 ]
Lee, Hanjae [1 ]
Kim, Jonghoon [1 ]
Chung, Young Sun [3 ]
Park, Seung Bum [1 ,2 ]
机构：
[1] Seoul Natl Univ, Dept Chem, Seoul 151747, South Korea
[2] Seoul Natl Univ, Dept Biophys & Chem Biol, Seoul 151747, South Korea
[3] Korea Cyber Univ, Dept Counseling, Seoul 110340, South Korea
来源：
BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2011年 / 32卷 / 09期
基金：
新加坡国家研究基金会;
关键词：
Hsp90; FlAsH; Fluorescent resonance energy transfer (FRET); High throughput screening (HTS); Benzopyran analogs; DIVERSITY-ORIENTED SYNTHESIS; RESONANCE ENERGY-TRANSFER; SHOCK-PROTEIN; 90; MOLECULAR CHAPERONE; FLUORESCENT PROTEIN; BINDING ASSAY; HEAT-SHOCK-PROTEIN-90; CANCER; GELDANAMYCIN; AGENT;
D O I：
10.5012/bkcs.2011.32.9.3229
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A FRET-based high-throughput screening system was developed for the discovery of competitive small-molecule 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.
引用
收藏
页码：3229 / 3232
页数：4
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