Figure 2.
FRET identifies Cortivazol and AZD2906 as GR dimer-enhancing ligands. HEK293T cells were transfected with CFP-GR (donor) and YFP-GR (acceptor) and stimulated with 10−8 M of the compounds (1 h). (a) FRET efficiencies. (b) FRET image of NI cells. (c) FRET image of Dex stimulated cells. (d) FRET image of Cortivazol stimulated cells. (e) FRET image of AZD2906 stimulated cells. A Hierarchical Generalized Linear Mixed Model (HGLMM) was fitted to the FRET data. T statistics (unpaired, two-tailed) were used to assess the significance of fixed compound effects estimated as differences to the NI condition (significance levels above error bars) and Dex (significance levels indicated with−) set as reference. Estimated mean values were obtained as predictions from the HGLMM, formed on the scale of the response variable. P-values < 0.05, 0.01, 0.001 and 0.0001 are represented by *, **, *** or **** respectively. Non-significant differences are not indicated on the graph. Experiments were repeated at least twice with at least 15 technical replicates included. NI: Non-Induced, Dex: Dexamethasone.