Figure 5. Functional validation of the AR-LBD dimer interface.

To investigate the impact of mutations predicted to influence dimerization of the full-length receptor, luciferase reporter and whole-cell competition assays were performed in PC-3 and COS-7 cells, respectively. The mean and s.e.m. of four independent experiments with three technical replicates each are shown for both assays. (a) Transactivation assays were performed with increasing concentrations of DHT (from 0.1 to 10 nM). (b,c) Determination of relative binding affinities for DHT and of maximum binding of mibolerone. (d,e) Western blot analysis of wild-type and mutant AR variants from the experiments shown in panels (a–c), respectively.