FIGURE 5.

Distal residues control corticosteroid specificity. A, key residues preceding β-sheet 1 and H7 in AncCR and human MR (hMR) were cross-mutated. The -fold activation (B) and potency (C) were measured via Dual-Luciferase reporter gene activation in transiently transfected CHO-K1 cells. Dex, dexamethasone. The same residues in GR and MR were cross-mutated, and the -fold activation (D) and potency (E) were measured via Dual-Luciferase reporter gene activation in transiently transfected CHO-K1 cells. The mean ± S.E. is shown (n = 3). Statistical analyses were performed using two-factor ANOVA, with Tukey's HSD post hoc tests used for individual comparisons. Comparisons found to be statistically significant to p < 0.05 are marked (*). hGR-HL, human GR-L647H/S651L; hMR-LS, human MR-H853L/L857S. X, no binding or activation observed.