Fig. 6
Comparison of the posaconazole-, itraconazole- and OHI-dependent inhibition of human and mouse 11β-HSD2 with that of chimera E, F and H. Lysates of HEK-293 cells expressing recombinant 11β-HSD2 of the indicated species or the respective chimera were incubated for 10 min (human) or 20 min (mouse, chimeras) with 50 nM cortisol, 500 μM NAD+ and 1 μM or 10 μM of the test compounds. Substrate conversion was normalized to that of the vehicle control (0.4% DMSO). Data represent mean ± SD from three independent experiments. Data were analyzed by two-way ANOVA with Bonferroni's post hoc test. P values: * < 0.05, ** < 0.01, **** < 0.0001 and ns (not significant), n.d. (not detected). |