A high-throughput screen to identify novel calcineurin inhibitors

Lekha Menon Margassery; Jonathan Kennedy; Fergal O'Gara; Alan D Dobson; John P Morrissey

doi:10.1016/j.mimet.2011.10.012

A high-throughput screen to identify novel calcineurin inhibitors

J Microbiol Methods. 2012 Jan;88(1):63-6. doi: 10.1016/j.mimet.2011.10.012. Epub 2011 Oct 26.

Authors

Lekha Menon Margassery¹, Jonathan Kennedy, Fergal O'Gara, Alan D Dobson, John P Morrissey

Affiliation

¹ Marine Biotechnology Centre, Environmental Research Institute, Microbiology Department, University College Cork, Ireland.

PMID: 22056231
DOI: 10.1016/j.mimet.2011.10.012

Abstract

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.

Publication types

Evaluation Study
Research Support, Non-U.S. Gov't

MeSH terms

Calcineurin Inhibitors*
Drug Evaluation, Preclinical / methods*
Enzyme Inhibitors / pharmacology*
Genes, Reporter
High-Throughput Screening Assays / methods*
Humans
Saccharomyces cerevisiae / drug effects*
Saccharomyces cerevisiae / genetics
Saccharomyces cerevisiae / metabolism

Substances

Calcineurin Inhibitors
Enzyme Inhibitors