Table 1

Activities of a model androgen-responsive reporter gene in CV1 cells stably transfected with a cDNA encoding CYP1A2

ConcentrationLigand-stimulated Luciferase UnitsFold Induction(%)
pCMV 5 Mb (1)229,017510100
OH-F (1)4,346102
OH-F (2)4,920112
OH-F (5)15,689357
F (1)5161.10.1
F (2)4210.9
F (5)3240.7
pCMV Mb (1)488,828572100
CYP1A2 OH-F (1)14,644173
OH-F (2)20,175244
OH-F (5)47,2995510
F (1)4,83661
F (2)8,192102
F (5)15,259204
  • Cell populations previously stably transfected with pSV2neo and pCMV5 or pCMV CYP1A2 were transiently transfected with a cDNA encoding the human AR and the androgen-responsive reported plasmid MMTV luciferase. Twenty four hours following transfection, the cultures were treated with the ligands shown for 48 hr. At the end of the incubation, the cultures were harvested and assayed to measure the levels of luciferase activity. The concentrations of ligands used are indicated (nM for mibolerone [Mb], μM for the remaining ligands). Each of the experimental values is the average of single luciferase measurements of samples derived from three separate transfections (see Materials and Methods). The data presented are from a single representative experiment. Fold induction is the level of stimulated luciferase activity divided by the activity measured in cells incubated with no ligand (854 and 449 light units for cells transfected with pCMV 5 and pCMV CYP1A2, respectively). — indicates that the levels of luciferase were lower than those measured in the baseline (unstimulated) samples.