Use of a real-time fluorescence monitoring system for high-throughput screening for Prolyl isomerase inhibitors

Tadashi Mori, Seima Itami, Tomotaka Yanagi, Yota Tatara, Mari Takamiya, Takafumi Uchida

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)

Abstract

Cyclophilin is a ubiquitous peptidyl prolyl cis/trans isomerase that plays critical roles in many biological processes. A number of cyclophilin inhibitors have been designed based on the structure of the immunosuppressant cyclosporin A. To discover inhibitors that have other structures, the authors established the high-throughput screening (HTS) method using FDSS6000 real-time fluorescence detector. The inhibitors identified with this HTS showed significant correlation with direct interaction as measured by surface plasmon resonance. This high-throughput assay system is a powerful tool for the discovery of peptidylprolyl isomerase inhibitors.

Original languageEnglish
Pages (from-to)419-424
Number of pages6
JournalJournal of Biomolecular Screening
Volume14
Issue number4
DOIs
Publication statusPublished - 2009 Apr

Keywords

  • Cyclophilin
  • Cyclosporin A
  • High-throughput screening
  • Peptidyl prolyl cis/trans isomerase
  • Protease-coupled assay

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biotechnology
  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

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