FIGURE
Fig. 7
Fig. 7
Concentration-dependent inhibition of 11β-HSD2 variants by itraconazole and posaconazole. Lysates of HEK-293 cells expressing recombinant 11β-HSD2 of the indicated species or the respective chimera were incubated for 10 min (human, chimera B) or 20 min (mouse, chimera A, E, F, H) with 50 nM radiolabeled cortisol, 500 μM NAD+ and increasing concentrations of itraconazole (A, B) and posaconazole (C, D). Substrate conversion was normalized to that of the vehicle control (0.6% DMSO for itraconazole and 0.3% DMSO for posaconazole). Data from three independent experiments are shown as mean ± SD. |
Expression Data
Expression Detail
Antibody Labeling
Phenotype Data
Phenotype Detail
Acknowledgments
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