Fig. 2.
GRL604 is active at 10-fold lower steroid concentrations than GRWT. The ability of wild-type and mutant GRs to induce luciferase expressed under control of the mouse mammary tumor virus promoter was assessed in Cos7 cells in the absence or presence of the indicated steroids. Luciferase activity is expressed as percent of maximal induction of GRWT by dexamethasone (10 nM). All data points represent the mean of at least nine independent transfections. (A) Schematic of the GR mutants studied. (B–D) Dose–response curves for induction of luciferase by GRWT, GRL604, GRL604A567, and GRA567 in response to cortisol (B), dexamethasone (C), and corticosterone (D). (E) Dose–response curves for induction of luciferase by GRWT, GRA604, and GRA604A567 by dexamethasone. *, P < 0.001 vs. GRWT...., P < 0.01 vs. GRWT.