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| | High Throughput Fluorescence Polarization Screen for Bcl-B Phenotype Converters |
| Description: | Sanford-Burnham Center for Chemical Genomics (SBCCG) Sanford-Burnham Medical Research Institute (San Diego, CA) NIH Molecular Libraries Screening Centers Network (MLSCN) Bcl-B is an anti-apoptotic member of the Bcl-2 family that is prominently expressed in plasma and multiple myeloma cells. TR3 (NR4A1; HMR; NP10; GFRP1; NAK1; NUR77; NGFIB) is an orphan member of the steroid/thyroid/retinoid nuclear receptor superfamily that translocates from cellular nuclei to mitochondria upon exposure to various pro-apoptotic stimuli. At mitochondria, TR3 binds to Bcl-B and converts it into a pro-apoptotic protein. A specific 9-amino acid sequence within the full length TR3 is able to form a complex with Bcl-B and induce its phenotypic conversion. This interaction forms the basis for a high throughput fluorescence polarization screen for compound mimetics. Such compounds may be useful as chemical probes for understanding the functional mechanism of Bcl-B, and may have therapeutic relevance in a |
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