Cysteine-10 on 17β-Hydroxysteroid Dehydrogenase 1 Has Stabilizing Interactions in the Cofactor Binding Region and Renders Sensitivity to Sulfhydryl Modifying Chemicals

Figure 6

Inhibition of 17β-HSD1 and Cys¹⁰Ser mutant by dithiocarbamate chemicals. The conversion of estrone (200 nM) to estradiol in the presence of 400 μM NADPH and various dithiocarbamates (80 μM final concentration) was measured in lysates of transfected HEK-293 cells. Black bars, wild-type 17β-HSD1 enzyme (WT); white bars, Cys¹⁰Ser mutant 17β-HSD1 (C10S). The amount of total protein in the reaction was equalized to exclude differences due to unspecific binding of the inhibitors to cellular proteins.