High-throughput screening for Hsp90 ATPase inhibitors

Christopher Avila, M. Kyle Hadden, Zeqiang Ma, Boris A. Kornilayev, Qi Zhuang Ye, Brian S.J. Blagg

Research output: Contribution to journalArticle

33 Scopus citations

Abstract

Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of ∼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 IC50s less than 20 μM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.

Original languageEnglish (US)
Pages (from-to)3005-3008
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number11
DOIs
StatePublished - Jun 1 2006
Externally publishedYes

Keywords

  • High-throughput screening
  • Hsp90
  • Inhibitors

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Avila, C., Hadden, M. K., Ma, Z., Kornilayev, B. A., Ye, Q. Z., & Blagg, B. S. J. (2006). High-throughput screening for Hsp90 ATPase inhibitors. Bioorganic and Medicinal Chemistry Letters, 16(11), 3005-3008. https://doi.org/10.1016/j.bmcl.2006.02.063