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. 2015 May 12;6(24):20474–20484. doi: 10.18632/oncotarget.4105

Figure 2. Topo II catalytic inhibitors suppress AR mutant and AR-V7 transcriptional activities.

Figure 2

(A) 293T cells were transfected with a PSA-luciferase reporter plus expression plasmids encoding the wild type AR, AR(F876L), AR(W741C) or AR-V7. Cells were treated with DMSO, 1nM of R1881, 10uM of ENZ or bicalutamide, 10uM of ENZ or Bicalutamdie plus 1uM of ICRF187 or ICRF193 for 24 hours. (B) 293T cells were cultured in medium containing 10% FBS, transfected with wild type AR and treated with vehicle, 0.01-10uM of ICRF187, ICRF193 or ENZ. 293T cells transfected with AR(F876L) were treated with 10uM of ENZ plus vehicle, 0.01-10uM of ICRF187 or ICRF193. 293T cells transfected with AR(W741C) were treated with 10uM of bicalutamide plus vehicle, 0.01-10uM of ICRF187 or ICRF193. PC3 cells transfected with AR-V7 were treated with vehicle, 0.01-10uM of ICRF187 or ICRF193. (C) LNCaP cells were transfected with a PSA-luciferase reporter and treated with 1nM of R1881. Cells were also treated with 0.01-10uM of ENZ, ICRF187 or ICRF193 (left panel). Cells were treated with 5uM of ENZ plus 0.01-10uM of ICRF187 or ICRF193 (right panel). (D) MR49F and LNCaP95 cells were transfected with a PSA-luciferase reporter. MR49F cells were treated with 10uM of ENZ plus 0.01-10uM of ICRF187 or ICRF193, while LNCaP95 cells were treated with 5uM of ENZ plus 0.01-10uM of ICRF187 or ICRF193 for 24 hours. Relative luciferase activities were calibrated with Renilla from three independent experiments and were presented as mean ± SEM (n = 3). Values from vehicle treatment were set as 100%.