A biochemical screen for GroEL/GroES inhibitors

作者:Johnson Steven M; Sharif Orzala; Mak Puiying Annie; Wang Hsiao Ting; Engels Ingo H; Brinker Achim; Schultz Peter G; Horwich Arthur L*; Chapman Eli
来源:Bioorganic & Medicinal Chemistry Letters, 2014, 24(3): 786-789.
DOI:10.1016/j.bmcl.2013.12.100

摘要

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.

  • 出版日期2014-2-1