Fig. 2: Evaluation of PXR modulation by chemical analogs.
From: Chemical manipulation of an activation/inhibition switch in the nuclear receptor PXR
a Chemical structures of designed antagonists and agonists. b TR-FRET PXR LBD binding assay measuring displacement of a fluorescent probe from PXR LBD. Data were normalized to 10 μM T0901317 as 100% binding and DMSO as 0% binding. c, d Compounds were evaluated for PXR agonism or antagonism in HepG2 cells stably expressing PXR and a firefly luciferase reporter under the control of the PXR-responsive CYP3A4 promoter. c Cellular assay in agonistic mode, where agonists increase signal. Data were normalized to 10 μM rifampicin as 100% activation and DMSO as 0% activation. d Cellular assay in antagonistic mode, where cells are incubated with rifampicin (5 μM), and antagonists reduce the rifampicin-induced signal. Data were normalized to 10 μM SPA70 as 100% inhibition and DMSO as 0% inhibition. Source data for (b–d) are provided as a Source Data file. Data were derived from n = 3 independent experiments and are presented as mean values +/- standard deviation (SD).
