4.5 Article

A biochemical screen for GroEL/GroES inhibitors

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 3, 页码 786-789

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.100

关键词

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

资金

  1. Genomics Institute of the Novartis Research Foundation (GNF)
  2. Scripps Research Institute

向作者/读者索取更多资源

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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