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Journal of Biomolecular Screening
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A High-Content Glucocorticoid Receptor Translocation Assay for Compound Mechanism-of-Action Evaluation

Michele Agler

Lead Discovery & Profiling, Wallingford, Connecticut, michele.agler{at}bms.com

Margaret Prack

Lead Discovery & Profiling, Wallingford, Connecticut

Yingjie Zhu

Lead Discovery & Profiling, Wallingford, Connecticut

Janet Kolb

Lead Discovery & Profiling, Wallingford, Connecticut

Kimberly Nowak

Lead Discovery & Profiling, Wallingford, Connecticut

Rolf Ryseck

Immunology & Oncology Drug Discovery, Princeton, New Jersey

Ding Shen

Lead Evaluation, Princeton, New Jersey

Mary Ellen Cvijic

Lead Evaluation, Princeton, New Jersey

John Somerville

Immunology & Oncology Drug Discovery, Princeton, New Jersey

Steve Nadler

Immunology & Oncology Drug Discovery, Princeton, New Jersey

Taosheng Chen

Department of Chemical Biology & Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee

Ligand-induced cytoplasm to nucleus translocation is a critical event in the nuclear receptor (NR) signal transduction cascade. The development of green fluorescent proteins and their color variants fused with NRs, along with the recent developments in automated cellular imaging technologies, has provided unique tools to monitor and quantify the NR translocation events. These technology developments have important implications in the mechanistic evaluation of NR signaling and provide a powerful tool for drug discovery. The unique challenges for developing a robust NR translocation assay include cytotoxicity accompanied with chronic overexpression of NRs, basal translocation induced by serum present in culture medium, and interference from endogenous NRs, as well as subcellular dynamics. The authors have developed a robust assay system for the glucocorticoid receptor (GR) that was applied to a panel of nuclear receptor ligands. Using a high-content imaging system, ligand-induced, dose-dependent GR nuclear translocation was quantified and a correlation with other conventional assays established. (Journal of Biomolecular Screening 2007:1029-1041)

Key Words: glucocorticoid receptor • nuclear translocation • high content screening • green fluorescent proteins • androgen receptor

This version was published on December 1, 2007

Journal of Biomolecular Screening, Vol. 12, No. 8, 1029-1041 (2007)
DOI: 10.1177/1087057107309353
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