Figure 4. Crossreactivity Studies of the Identified FXR Ligands with Other Nuclear Hormone Receptors.
CV-1 cells were cotransfected with a reporter gene containing the (A) MH2004 promoter that contains four GAL4 binding sites with pCMXGAL4-FXR LBD chimeric expression construct or (B) MH2004 promoter with pCMXGAL4-FXR LBD/RXRα constructs and treated with increasing amounts of the compounds fexaramine, fexarine, fexarene, SRI-1, SRI-2, and GW4064. (C, D, and E) CV-1 cells were transiently transfected with the indicated plasmids and treated with either DMSO or 10 μM of the compounds fexaramine, fexarine, and fexarene. Reporter activity was normalized to the internal control, and the data were plotted as fold activation relative to untreated cells. All transfections contained CMX-gal as an internal control.