The AR is a ligand-dependent transcription factor that controls the expression of specific genes. The binding of the AR to its native ligands 5α-dihydrotestosterone (DHT) and testosterone initiates male sexual development and differentiation.
2Tan MHE et al., (2015) Androgen receptor: structure, role in prostate cancer and drug discovery. Acta Pharmacologica Sinica 36: 3-23
Test Method | AR Redistribution Assay (ThermoScientific) |
---|---|
Cell Type | Recombinant U2OS cells stably expressing human androgen receptor |
Test Article Concentrations | 10 µM in quadruplicate (alternative concentrations or dose curves available on request) |
Test Article Exposure | Overnight |
Reference Controls | Dihydrotestosterone (agonist) Mifepristone (antagonist) |
Typical Vehicle Control | 0.5% DMSO |
Analysis Method | ThermoScientific ArrayScan® VTi High Content Imaging |
Data Delivery | % Effect compared to control (single concentration) EC50 (dose response) |
1 Hua Y, et al, (2014) High-content positional biosensor screening assay for compounds to prevent or disrupt androgen receptor and transcriptional intermediary factor 2 protein-protein interactions. ASSAY Drug Dev Technol 12(7); 395-418
2 Tan MHE et al., (2015) Androgen receptor: structure, role in prostate cancer and drug discovery. Acta Pharmacologica Sinica 36; 3-23
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