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

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

Author information

1
Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, Parkville, Vic. 3052, Australia.

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.

PMID:
18165015
DOI:
10.1016/j.bmc.2007.12.016
[Indexed for MEDLINE]

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