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A biochemical screen for GroEL/GroES inhibitors.
Johnson, Steven M; Sharif, Orzala; Mak, Puiying Annie; Wang, Hsiao-Ting; Engels, Ingo H; Brinker, Achim; Schultz, Peter G; Horwich, Arthur L; Chapman, Eli.
Afiliação
  • Johnson SM; Indiana University, School of Medicine, Department of Biochemistry and Molecular Biology, 635 Barnhill Dr., Indianapolis, IN 46202, USA.
  • Sharif O; The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Dr., San Diego, CA 92121, USA.
  • Mak PA; The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Dr., San Diego, CA 92121, USA.
  • Wang HT; The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Dr., San Diego, CA 92121, USA.
  • Engels IH; The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Dr., San Diego, CA 92121, USA.
  • Brinker A; The Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Dr., San Diego, CA 92121, USA.
  • Schultz PG; The Scripps Research Institute, Department of Chemistry, 10550 North Torrey Pines Rd., La Jolla, CA 92037, USA.
  • Horwich AL; 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.
  • Chapman E; 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.
Bioorg Med Chem Lett ; 24(3): 786-9, 2014 Feb 01.
Article em En | MEDLINE | ID: mdl-24418775
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Chaperonina 60 / Chaperonina 10 / Bibliotecas de Moléculas Pequenas Idioma: En Ano de publicação: 2014 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Chaperonina 60 / Chaperonina 10 / Bibliotecas de Moléculas Pequenas Idioma: En Ano de publicação: 2014 Tipo de documento: Article