Fig. 1. Transcriptional activities of AmphiRAR and AmphiTR2/4 on the consensus RARE (DR5) and IR7 elements expressed as the amount of chloramphenicol acetyl transferase (CAT) activity (A) or luciferase (Luc) activity (B-E) relative to control. Values are averages of three to five independent transfections in ROS17.2/8 cells. Error bars indicate ±one s.d. (A) Dose-dependent repression by AmphiTR2/4 (5-300 ng) of RA-induced transactivation and by AmphiRAR-AmphiRXR (10-500 ng each) on the DR5 element. (B) Dose-dependent repression by AmphiTR2/4 of RA-induced transactivation on the IR7 element (as in A, except for co-transfection with the IR7-containing pGL2 plasmid instead of pBLCAT). (C) Transactivation induced by AmphiTR2/4 on the IR7 element without RA or AmphiRAR-AmphiRXR. Conditions as in B. (D) Inhibition by AmphiRAR-AmphiRXR of transactivation induced by TR2/4 (100 ng) on the IR7 element without RA. AmphiRXR, 300 ng. AmphiRAR, 10-500 ng. (E) Antagonism by BMS009 on transcription induced by RA. Dark bars on left represent activation by RAR-RXR±RA. Light gray bars represent activity with added BMS009. White bars represent activity with BMS009, no RA.
