Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 3, Pages 786-789Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.100
Keywords
GroEL; GroES; Chaperonin; High-throughput screening; Small molecule inhibitors
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Funding
- Genomics Institute of the Novartis Research Foundation (GNF)
- Scripps Research Institute
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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 mu M). The screening results presented herein represent the first steps in a broader aim of developing molecular probes to study chaperonin biochemistry and physiology. (C) 2013 Elsevier Ltd. All rights reserved.
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