Title : Tibolone is metabolized by the 3alpha/3beta-hydroxysteroid dehydrogenase activities of the four human isozymes of the aldo-keto reductase 1C subfamily: inversion of stereospecificity with a delta5(10)-3-ketosteroid.

Pub. Date : 2004 Dec

PMID : 15383625






4 Functional Relationships(s)
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1 Whereas AKR1C2 acted as a 3alpha-HSD toward 5alpha-DHT, it functioned exclusively as a 3beta-HSD on tibolone. tibolone aldo-keto reductase family 1 member C2 Homo sapiens
2 Furthermore, strong substrate inhibition was observed for the AKR1C2 catalyzed reduction of tibolone. tibolone aldo-keto reductase family 1 member C2 Homo sapiens
3 Molecular docking simulations using crystal structures of AKR1C1 and AKR1C2 explained why AKR1C2 inverted its stereospecificity from a 3alpha-HSD with 5alpha-DHT to a 3beta-HSD with tibolone. tibolone aldo-keto reductase family 1 member C2 Homo sapiens
4 Molecular docking simulations using crystal structures of AKR1C1 and AKR1C2 explained why AKR1C2 inverted its stereospecificity from a 3alpha-HSD with 5alpha-DHT to a 3beta-HSD with tibolone. tibolone aldo-keto reductase family 1 member C2 Homo sapiens