Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.
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.
Dhagat
Urmi
U
Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, Parkville, Vic. 3052, Australia.
Endo
Satoshi
S
Hara
Akira
A
El-Kabbani
Ossama
O
D015096:3-Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000818:Animals; D001665:Binding Sites; D004791:Enzyme Inhibitors / Q000737:chemistry*; D051379:Mice; D008958:Models, Molecular; D011485:Protein Binding; D013379:Substrate Specificity
D004791:Enzyme Inhibitors; D015096:3-Hydroxysteroid Dehydrogenases; D000449:Aldehyde Reductase