Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.

Authors :: Dhagat U
Endo S
Hara A
El-Kabbani O
Source :: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2008 Mar 15; Vol. 16 (6), pp. 3245-54. Date of Electronic Publication: 2007 Dec 15.
Publication Year :: 2008
Abstract: Mouse 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) is a member of the aldo-keto reductase superfamily that catalyses the oxido-reduction of steroid hormones such as estrogens, androgens and neurosteroids. Inhibitors of aldose reductase (AR), a member of the same superfamily, were evaluated against AKR1C21. Models of the enzyme-inhibitor complexes suggest that Tyr118 and Phe311 are important residues for inhibitor recognition and orientation in the active site of AKR1C21.

Subjects :: 3-Hydroxysteroid Dehydrogenases chemistry
Aldehyde Reductase chemistry
Animals
Binding Sites
Mice
Models, Molecular
Protein Binding
Substrate Specificity
3-Hydroxysteroid Dehydrogenases antagonists & inhibitors
Aldehyde Reductase antagonists & inhibitors
Enzyme Inhibitors chemistry

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