Title : Development of a coactivator displacement assay for the orphan receptor estrogen-related receptor-gamma using time-resolved fluorescence resonance energy transfer.

Pub. Date : 2006 Oct 1

PMID : 16889744






4 Functional Relationships(s)
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1 Although its physiological ligand is unknown, ERRgamma has been shown to interact with synthetic estrogenic compounds such as 4-hydroxytamoxifen (4-OHT), tamoxifen, and diethylstilbestrol (DES). 4,17 beta-dihydroxy-4-androstene-3-one estrogen related receptor gamma Homo sapiens
2 Fluorescein-labeled PGC1alpha peptide was displaced from the ERRgamma LBD in the presence of increasing concentrations of 4-OHT and tamoxifen, but DES was less effective in PGC1alpha displacement. 4,17 beta-dihydroxy-4-androstene-3-one estrogen related receptor gamma Homo sapiens
3 These findings also suggest that binding of 4-OHT, tamoxifen, or DES to ERRgamma results in differential affinity of coregulators for ERRgamma due to unique ligand-induced conformations. 4,17 beta-dihydroxy-4-androstene-3-one estrogen related receptor gamma Homo sapiens
4 These findings also suggest that binding of 4-OHT, tamoxifen, or DES to ERRgamma results in differential affinity of coregulators for ERRgamma due to unique ligand-induced conformations. 4,17 beta-dihydroxy-4-androstene-3-one estrogen related receptor gamma Homo sapiens