A biochemical screen for GroEL/GroES inhibitors

Steven M. Johnson, Orzala Sharif, Puiying Annie Mak, Hsiao Ting Wang, Ingo H. Engels, Achim Brinker, Peter G. Schultz, Arthur L. Horwich, Eli Chapman

Research output: Contribution to journalArticle

22 Scopus citations

Abstract

High-throughput screening of 700,000 small molecules has identified 235 inhibitors of the GroEL/GroES-mediated refolding cycle. Dose-response analysis of a subset of these hits revealed that 21 compounds are potent inhibitors of GroEL/GroES-mediated refolding (IC50 <10 μM). The screening results presented herein represent the first steps in a broader aim of developing molecular probes to study chaperonin biochemistry and physiology.

Original languageEnglish (US)
Pages (from-to)786-789
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number3
DOIs
StatePublished - Feb 1 2014

Keywords

  • Chaperonin
  • GroEL
  • GroES
  • High-throughput screening
  • Small molecule inhibitors

ASJC Scopus subject areas

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

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  • Cite this

    Johnson, S. M., Sharif, O., Mak, P. A., Wang, H. T., Engels, I. H., Brinker, A., Schultz, P. G., Horwich, A. L., & Chapman, E. (2014). A biochemical screen for GroEL/GroES inhibitors. Bioorganic and Medicinal Chemistry Letters, 24(3), 786-789. https://doi.org/10.1016/j.bmcl.2013.12.100