Fig. 1
From: Defining a conformational ensemble that directs activation of PPARγ
Nuclear receptor co-regulator interaction differentiates pharmacologically distinct PPARγ ligands. TR-FRET biochemical assay shows the effect of the compounds on the interaction between PPARγ LBD and peptides derived from the a MED1 coactivator and b NCoR corepressor, plotted as TR-FRET ratio (665 nm/620 nm) vs. ligand concentration (n = 2, standard deviation). The data shown represents technical replicates from a single experiment and the experiment was repeated four times with similar results. The window of efficacy in these data is representative of ligand-induced changes in co-regulator affinity for PPARγ. An increase in TR-FRET ratio indicates a strengthening of affinity for MED1/NCoR compared to apo while a decrease indicates a ligand-induced weakening of affinity for the co-regulator. The effect of vehicle (DMSO) is negligible (Supplementary Fig. 5); furthermore, the DMSO concentration is constant across the titration both in this figure and all other TR-FRET data presented
