| Solution Information | help | |
| Enzyme: | Photoreceptor-specific nuclear receptor | |
| inhibitor: | BDBM75958 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: The purpose of this biochemical assay is to determine dose response curves for compounds presenting an inverse agonist profile as active in a previous set of experiments entitled, TR-FRET-based primary biochemical high throughput screening assay to identify agonists of nuclear receptor subfamily 2, group E, member 3 (NR2E3) (AID 2300). This assay assesses the ability of compounds to disrupt NR2E3 transcriptional activity through the enhancement of binding to its corepressor, RetCOR. In this assay, GST-NR2E3 and its interaction partner, a biotinylated corepressor RetCOR, are incubated together in the presence of test compounds, Eu(K)-anti GST antibody, and Streptavidin-D2. Interaction between the RetCOR and NR2E3 partners brings the fluorophore-tagged antibodies together, leading to FRET between the fluorophores. As designed, test compounds that act as NR2E3 inverse agonists will lead to strengthening of RetCOR and NR2E3 interaction, thereby increasing the interaction | |
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