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J Biomol Screen DOI:10.1177/1087057103261039

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

Publication TypeJournal Article
Year of Publication2004
AuthorsZheng, W, Brandish, PE, D Kolodin, G, Scolnick, EM, Strulovici, B
JournalJ Biomol Screen
Date Published2004 Mar
KeywordsAtropine, Biological Assay, Carbachol, Cells, Cultured, Chromatography, High Pressure Liquid, Humans, Models, Biological, Phosphoric Monoester Hydrolases, Scintillation Counting

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.


Alternate JournalJ Biomol Screen
PubMed ID15006136