M. Hult et al., Selective inhibition of human type 1 11 beta-hydroxysteroid dehydrogenase by synthetic steroids and xenobiotics, FEBS LETTER, 441(1), 1998, pp. 25-28
Functional analyses were performed with microsomal human 11 beta-hydroxyste
roid dehydrogenase type 1 overexpressed in the yeast Pichia pastor is. Cell
extracts or microsomes from transformed strains displayed dehydrogenase an
d reductase activities, which were up to 10 times higher than in human live
r microsomes, while for whole cells cortisone reduction but no dehydrogenas
e activity was observed. The synthetic glucocorticoids prednisolone and pre
dnisone were efficiently metabolized by subcellular fractions, whereas no a
ctivity was observed with dexamethasone, budesonide and deflazacort. Inhibi
tors found to be effective towards the recombinant 11 beta-hydroxysteroid d
ehydrogenase include synthetic steroids and xenobiotic compounds, revealing
selective inhibition of the reaction direction, useful for development of
specific inhibitors. (C) 1998 Federation of European Biochemical Societies.