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J Biomol Screen. 2009 Apr;14(4):419-24. doi: 10.1177/1087057109333979.

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

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Molecular Enzymology, Graduate School of Agricultural Science, Tohoku University, Sendai, Japan.


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.

[Indexed for MEDLINE]

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