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.