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

doi:10.1016/j.bmcl.2013.12.100

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

Pharmacology and Toxicology

Research output: Contribution to journal › Article › peer-review

28 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 language	English (US)
Pages (from-to)	786-789
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2013.12.100
State	Published - 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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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.",

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AU - Johnson, Steven M.

AU - Sharif, Orzala

AU - Mak, Puiying Annie

AU - Wang, Hsiao Ting

AU - Engels, Ingo H.

AU - Brinker, Achim

AU - Schultz, Peter G.

AU - Horwich, Arthur L.

AU - Chapman, Eli

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KW - GroES

KW - High-throughput screening

KW - Small molecule inhibitors

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