| Assay Method Information | |
| | Counter Screen for TR3-Based Bcl-B Inhibitors: Fluorescence Polarization Bcl-B/FITC-Bim-BH3 Assay |
| Description: | Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA). Network: NIH Molecular Libraries Screening Centers Network (MLSCN) Grant Number: XO1 MH077632-01 Assay Provider: Dr. John C. Reed, Sanford-Burnham Medical Research Institute This assay is a counter screen for compounds identified in the Bcl-B/FITC-TR3 fluorescence polarization assay (AID 1240). Bcl-B is an anti-apoptotic member of the Bcl-2 family that is prominently expressed in plasma and multiple myeloma cells. TR3 (also known under NR4A1, HMR, NP10, GFRP1, NAK1, NUR77, and 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 |
| Affinity data for this assay | |
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