Hydroxysteroid dehydrogenase

About: Hydroxysteroid dehydrogenase is a research topic. Over the lifetime, 1087 publications have been published within this topic receiving 28468 citations. The topic is also known as: hydroxysteroid dehydrogenase.

Characterization of hamster NAD+-dependent 3(17)β-hydroxysteroid dehydrogenase belonging to the aldo-keto reductase 1C subfamily

Abstract: The cDNAs for morphine 6-dehydrogenase (AKR1C34) and its homologous aldo-keto reductase (AKR1C35) were cloned from golden hamster liver, and their enzymatic properties and tissue distribution were compared. AKR1C34 and AKR1C35 similarly oxidized various xenobiotic alicyclic alcohols using NAD(+), but differed in their substrate specificity for hydroxysteroids and inhibitor sensitivity. While AKR1C34 showed 3α/17β/20α-hydroxysteroid dehydrogenase activities, AKR1C35 efficiently oxidized various 3β- and 17β-hydroxysteroids, including biologically active 3β-hydroxy-5α/β-dihydro-C19/C21-steroids, dehydroepiandrosterone and 17β-estradiol. AKR1C35 also differed from AKR1C34 in its high sensitivity to flavonoids, which inhibited competitively with respect to 17β-estradiol (Ki 0.11-0.69 μM). The mRNA for AKR1C35 was expressed liver-specific in male hamsters and ubiquitously in female hamsters, whereas the expression of the mRNA for AKR1C34 displayed opposite sexual dimorphism. Because AKR1C35 is the first 317Β-HYDROXYSTEROID DEHYDROGENASE IN THE AKR SUPERFAMILY: , we also investigated the molecular determinants for the 3β-hydroxysteroid dehydrogenase activity by replacement of Val54 and Cys310 in AKR1C35 with the corresponding residues in AKR1C34, Ala and Phe, respectively. The mutation of Val54Ala, but not Cys310Phe, significantly impaired this activity, suggesting that Val54 plays a critical role in recognition of the steroidal substrate.

Effect of ergocornine on the luteal 20alpha-hydroxysteroid dehydrogenase in pseudopregnant and pregnant rats.

Abstract: Trattando ratte gravide o pseudogravide con ergocornina si puo osservare la comparsa dell'attivita 20α-idrossisteroide-deidrogenasica nei corpi lutei rispettivamente gravidici o pseudogravidici nei quali tale attivita normalmente manca. Perche questo effetto si manifesti sono necessari 2–3 giorni di trattamento. Si constata che l'ergocornina causa la comparsa dell'attivita enzimatica sopra indicata in qualsiasi periodo della pseudogravidanza, e nel periodo della gravidanza precedente l'impianto dell'uovo. L'ergocornina quindi agirebbe tramite l'ipofisi dalla cui regolazione dipende l'attivita 20α-idrossisteroide-deidrogenasica dell'ovaio.

3 alpha-hydroxysteroid dehydrogenase inhibitory activity of some N(3)-(1-R-4-carboxypyrazol-5-yl)-1,2,3-benzotriazin-4(3H)-one and quinazolin-4(3H)-one acids.

Abstract: Some carboxylic acids of N(3)-pyrazole substituted 1,2,3-benzotriazin-4-(3H)-ones and- quinazolin-4-(3H)-ones were prepared and tested for the inhibitory property of 3 alpha-hydroxysteroid dehydrogenase of rat liver cytosol. The results indicated that the degree of inhibition can be used to predict the antiinflammatory potency of the compounds described.

New 12alpha-hydroxysteroid dehydrogenase mutants, method for their manufacture and application thereof

Abstract: 12alpha -Hydroxysteroid dehydrogenase (12alpha -HSDH) mutant catalyzing at least stereospecific enzymatic oxidation of a 12-hydroxysteroid to the corresponding 12-ketosteroid, is new, where the mutant exhibits an increased specific activity (U/mg) in the presence of NADP +>cofactor in comparison to non-mutated enzyme. Independent claims are included for: (1) a nucleic acid sequence encoding the 12alpha -HSDH mutant; (2) an expression cassette comprising the nucleic acid sequence under the genetic control of at least one regulatory nucleic acid sequence; (3) a vector comprising at least one expression cassette; (4) a recombinant microorganism which carries at least one nucleic acid sequence or at least one expression cassette or is transformed with at least one vector; (5) enzymatic synthesis of 12alpha -hydroxysteroids, comprising reacting the corresponding 12-ketosteroid in the presence of 12alpha -HSDH mutant, and optionally isolating at least one reduction product formed from the reaction mixture; (6) enzymatic oxidation of 12alpha -hydroxysteroids, comprising reacting the hydroxysteroid in the presence of 12alpha -hydroxysteroid dehydrogenase, and optionally isolating an oxidation product formed from the reaction mixture; and (7) preparing ursodeoxycholic acid of formula (I), comprising oxidizing a cholic acid of formula (II) in the presence of 12alpha -hydroxysteroid dehydrogenase mutant for the corresponding 12-ketochenodeoxycholic acid of formula (III), and subsequently reacting (III) by deoxygenation to chenodeoxycholic acid of formula (IV), chemically oxidizing (IV) in position 7 to 7-keto-lithocholic acid of formula (V), reducing (V) and optionally further purifying the reaction product. R : alkyl, NR1R2, H, alkali metal ion or N(R3) 4+>; R3 : H or alkyl; and R1a : H or acyl. [Image] [Image] ACTIVITY : Hepatotropic; Litholytic. MECHANISM OF ACTION : None given.