The TR-FRET Retinoic Acid Receptor (RAR) alpha Coactivator Assay Kit provides a sensitive and robust method for high-throughput screening of potential RAR alpha ligands as agonists of coactivator recruitment. The homogeneous mix-and-read assay format results in a ligand EC50 composite value representing the amount of ligand required to bind to receptor, effect a conformational change, and recruit coactivator peptide.
How it works
The TR-FRET RAR alpha Coactivator Assay Kit includes a terbium (Tb)-labeled anti-GST antibody, a fluorescein-labeled coactivator peptide, and a human RAR alpha ligand-binding domain (RAR alpha-LBD) that is tagged with glutathione-S-transferase (GST). To assay, RAR alpha-LBD is added to ligand test compounds, followed by addition of a mixture of the fluorescein-coactivator peptide and Tb-anti-GST antibody. After room temperature incubation, the TR-FRET 520: 495 emission ratio is calculated and used to determine the EC50 from a dose response curve of the compound.