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]
- 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
Drug Target Property Measurement pH Temperature (°C) (R)-minalrestat Aldose reductase IC 50 (nM) 70 N/A N/A Details (S,R)-fidarestat Aldose reductase IC 50 (nM) 9 N/A N/A Details Sorbinil Aldose reductase IC 50 (nM) 910 N/A N/A Details Tolrestat Aldose reductase IC 50 (nM) 40 N/A N/A Details Zopolrestat Aldose reductase IC 50 (nM) 30 N/A N/A Details