title: Use of a real-time fluorescence monitoring system for high-throughput screening for prolyl isomerase inhibitors.
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.
authors.affiliation: Molecular Enzymology, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan.
authors.forename: Tadashi
authors.initials: T
authors.lastname: Mori
authors.forename: Seima
authors.initials: S
authors.lastname: Itami
authors.forename: Tomotaka
authors.initials: T
authors.lastname: Yanagi
authors.forename: Yota
authors.initials: Y
authors.lastname: Tatara
authors.forename: Mari
authors.initials: M
authors.lastname: Takamiya
authors.forename: Takafumi
authors.initials: T
authors.lastname: Uchida
mesh_terms: D021983:Cyclophilins / Q000037:antagonists & inhibitors; D004791:Enzyme Inhibitors / Q000032:analysis* / Q000494:pharmacology*; D005470:Fluorometry / Q000379:methods*; D007700:Kinetics; D019696:Peptidylprolyl Isomerase / Q000037:antagonists & inhibitors*; D015203:Reproducibility of Results; D054852:Small Molecule Libraries / Q000032:analysis / Q000494:pharmacology; D020349:Surface Plasmon Resonance; D013997:Time Factors
chemical_list: D004791:Enzyme Inhibitors; D054852:Small Molecule Libraries; D021983:Cyclophilins; D019696:Peptidylprolyl Isomerase