Figure 6.

VER-155008 inhibition of the transcriptional activity of GFP-NAR (mutant AR lacking LBD) in PSA promoter-driven luciferase assay. A. To determine GFP-NAR transcriptional activities, C4–2 cells were transfected with PSA 6.0 luciferase and Renilla plasmids, along with GFP or GFP-NAR, in RPMI1640 with 5% CSS for 48 hours and then the luciferase activities were measured. As controls, C4–2 cells were transfected with PSA 6.0 luciferase plasmid and Renilla plasmid in RPMI1640 with 5% CSS for 24 hours and then treated with 1 nM R1881 or vehicle for another 24 hours prior to luciferase assay. B. The luciferase assays in A were used to test the effects of VER-155008, 17-AAG, or MDV3100 on the transcriptional activity of androgen-induced endogenous AR or the transfected GFP-NAR. Twenty-four hours after the transfection, C4–2 cells were cultured for another 24 hours in the presence of 1 nM R1881 or ethanol vehicle plus indicated doses of VER-155008, 17-AAG or MDV3100 prior to harvest.