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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

High-throughput cell-based screening using scintillation proximity assay for the discovery of inositol phosphatase inhibitors.

Inositol monophosphatase is a potential drug target for developing lithium-mimetic agents for the treatment of bipolar disorder. Enzyme-based assays have been traditionally used in compound screening to identify inositol monophosphatase inhibitors. A cell-based screening assay in which the compound needs to cross the cell membrane before reaching the target enzyme offers a new approach for discovering novel structure leads of the inositol monophosphatase inhibitor. The authors have recently reported a high-throughput measurement of G-protein-coupled receptor activation by determining inositol phosphates in cell extracts using scintillation proximity assay. This cell-based assay has been modified to allow the determination of inositol monophosphatase activity instead of G-protein-coupled receptors. The enzyme is also assayed in its native form and physiological environment. The authors have applied this cell-based assay to the high-throughput screening of a large compound collection and identified several novel inositol monophosphatase inhibitors.[1]

References

  1. High-throughput cell-based screening using scintillation proximity assay for the discovery of inositol phosphatase inhibitors. Zheng, W., Brandish, P.E., Kolodin, D.G., Scolnick, E.M., Strulovici, B. Journal of biomolecular screening : the official journal of the Society for Biomolecular Screening. (2004) [Pubmed]
 
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