A biochemical screen for GroEL/GroES inhibitors

Steven 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

19 Citations (Scopus)

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

Fingerprint

Chaperonins
Molecular Probes
Biochemistry
Inhibitory Concentration 50
Screening
Physiology
Throughput
Molecules

Keywords

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

ASJC Scopus subject areas

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

Cite this

Johnson, S., Sharif, O., Mak, P. A., Wang, H. T., Engels, I. H., Brinker, A., ... 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

A biochemical screen for GroEL/GroES inhibitors. / Johnson, Steven; Sharif, Orzala; Mak, Puiying Annie; Wang, Hsiao Ting; Engels, Ingo H.; Brinker, Achim; Schultz, Peter G.; Horwich, Arthur L.; Chapman, Eli.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 24, No. 3, 01.02.2014, p. 786-789.

Research output: Contribution to journalArticle

Johnson, S, Sharif, O, Mak, PA, Wang, HT, Engels, IH, Brinker, A, Schultz, PG, Horwich, AL & Chapman, E 2014, 'A biochemical screen for GroEL/GroES inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 24, no. 3, pp. 786-789. https://doi.org/10.1016/j.bmcl.2013.12.100
Johnson, Steven ; Sharif, Orzala ; Mak, Puiying Annie ; Wang, Hsiao Ting ; Engels, Ingo H. ; Brinker, Achim ; Schultz, Peter G. ; Horwich, Arthur L. ; Chapman, Eli. / A biochemical screen for GroEL/GroES inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2014 ; Vol. 24, No. 3. pp. 786-789.
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