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

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Dhagat U, Endo S, Hara A, El-Kabbani O

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

Bioorg Med Chem. 2008 Mar 15;16(6):3245-54. doi: 10.1016/j.bmc.2007.12.016. Epub 2007 Dec 15.

PubMed ID
18165015 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
(R)-minalrestatAldose reductaseIC 50 (nM)70N/AN/ADetails
(S,R)-fidarestatAldose reductaseIC 50 (nM)9N/AN/ADetails
SorbinilAldose reductaseIC 50 (nM)910N/AN/ADetails
TolrestatAldose reductaseIC 50 (nM)40N/AN/ADetails
ZopolrestatAldose reductaseIC 50 (nM)30N/AN/ADetails