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Bioorg Med Chem Lett. 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.

Author information

1
Indiana University, School of Medicine, Department of Biochemistry and Molecular Biology, 635 Barnhill Dr., Indianapolis, IN 46202, USA.
2
The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Dr., San Diego, CA 92121, USA.
3
The Scripps Research Institute, Department of Chemistry, 10550 North Torrey Pines Rd., La Jolla, CA 92037, USA.
4
HHMI, Department of Genetics, Yale School of Medicine, Boyer Center for Molecular Medicine, 295 Congress Ave., New Haven, CT 06510, USA. Electronic address: arthur.horwich@yale.edu.
5
The University of Arizona, College of Pharmacy, Department of Pharmacology and Toxicology, 1703 E. Mabel St., PO Box 210207, Tucson, AZ 85721-0207, USA. Electronic address: chapman@pharmacy.arizona.edu.

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

PMID:
24418775
DOI:
10.1016/j.bmcl.2013.12.100
[Indexed for MEDLINE]

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