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

Journal of biomolecular screening : the official journal of the Society for Biomolecular Screening

PubMedID: 19403925

Mori T, Itami S, Yanagi T, Tatara Y, Takamiya M, Uchida T. Use of a real-time fluorescence monitoring system for high-throughput screening for prolyl isomerase inhibitors. J Biomol Screen. 2009;14(4):419-24.
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.