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

Urmi Dhagat; Satoshi Endo; Akira Hara; Ossama El-Kabbani

doi:10.1016/j.bmc.2007.12.016

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.

Authors

Urmi Dhagat¹, Satoshi Endo, Akira Hara, Ossama El-Kabbani

Affiliation

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

PMID: 18165015
DOI: 10.1016/j.bmc.2007.12.016

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

Enzyme Inhibitors
3-Hydroxysteroid Dehydrogenases
Aldehyde Reductase