High-throughput screening for Hsp90 ATPase inhibitors

被引：36

作者：

Avila, C

Hadden, MK

Ma, ZQ

Kornilayev, BA

Ye, QZ

Blagg, BSJ

机构：

[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA

[2] Univ Kansas, High Troughput Screening Lab, Lawrence, KS 66047 USA

[3] Univ Kansas, Biochen Res Serv Lab, Lawrence, KS 66047 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 11期

关键词：

Hsp90; high-throughput screening; inhibitors;

D O I：

10.1016/j.bmcl.2006.02.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of similar to 10,000 compounds was performed to determine the feasibility of this assay on large scale. Results from high-throughput screening indicated that the assay was reproducible (av Z-factor = 0.80) and identified 0.57% of the compounds as Hsp90 inhibitors that exhibited IC(50)s less than 20 mu M. The structures of several of these inhibitory scaffolds are reported along with their IC50 values. (c) 2006 Elsevier Ltd. All rights reserved.

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收藏

页码：3005 / 3008

页数：4

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