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

A biochemical screen for GroEL/GroES inhibitors

Steven M Johnson  1 , Orzala Sharif  2 , Puiying Annie Mak  2 , Hsiao-Ting Wang  2 , Ingo H Engels  2 , Achim Brinker  2 , Peter G Schultz  3 , Arthur L Horwich  4 , Eli Chapman  5
Affiliations

A biochemical screen for GroEL/GroES inhibitors

Steven M Johnson et al. Bioorg Med Chem Lett. .

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.

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