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Journal of Biomolecular Screening
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High-Throughput Cell-Based Screening Using Scintillation Proximity Assay for the Discovery of Inositol Phosphatase Inhibitors

Wei Zheng

Department of Automated Biotechnology, Merck & Co., North Wales, PA wei_zheng{at}merck.com

Philip E. Brandish

Department of Neurobiology, Merck & Co., North Wales, PA

D. Garrett Kolodin

Department of Automated Biotechnology, Merck & Co., North Wales, PA

Edward M. Scolnick

Department of Neurobiology, Merck & Co., North Wales, PA

Berta Strulovici

Department of Automated Biotechnology, Merck & Co., North Wales, PA

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. (Journal of Biomolecular Screening 2004:132-140)

Key Words: inositol monophosphatase • bipolar disorder • phosphatidylinositol turnover • IP • assay • cell-based enzyme assay

Journal of Biomolecular Screening, Vol. 9, No. 2, 132-140 (2004)
DOI: 10.1177/1087057103261039
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