Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors |
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| Authors: | Dhagat Urmi Endo Satoshi Hara Akira El-Kabbani Ossama |
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| Institution: | Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, Parkville, Vic. 3052, Australia. |
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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. |
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