A biochemical screen for GroEL/GroES inhibitors

Bioorg Med Chem Lett. 2014 Feb 1;24(3):786-9. doi: 10.1016/j.bmcl.2013.12.100. Epub 2014 Jan 2.

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.

Keywords: Chaperonin; GroEL; GroES; High-throughput screening; Small molecule inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chaperonin 10 / antagonists & inhibitors*
  • Chaperonin 60 / antagonists & inhibitors*
  • Dose-Response Relationship, Drug
  • Inhibitory Concentration 50
  • Models, Biological
  • Protein Folding / drug effects
  • Small Molecule Libraries / pharmacology*

Substances

  • Chaperonin 10
  • Chaperonin 60
  • Small Molecule Libraries