A high-throughput screen to identify novel calcineurin inhibitors

Calcineurin is a eukaryotic protein phosphatase important for many signalling and developmental processes in cells. Inhibitors of this enzyme are used clinically and there is interest in identifying novel inhibitors for therapeutic applications. This report describes a high-throughput assay that can be used to screen natural or chemical libraries of compounds to identify new calcineurin inhibitors. The microtitre plate assay is based on a yeast reporter strain and was validated with known inhibitors and tested in a pilot screen of bacterial extracts.

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► There is a need to identify novel calcineurin inhibitors for therapeutic uses.
► A scalable HT screen for calcineurin inhibitors was developed and validated.
► The system makes use of a yeast reporter strain.
► The screen can be used to test libraries of synthesised or natural metabolites.
► The application was demonstrated in a pilot screen of bacterial extracts.