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Literature summary extracted from

  • Thomas, J.L.; Mack, V.L.; Glow, J.A.; Moshkelani, D.; Terrell, J.R.; Bucholtz, K.M.
    Structure/function of the inhibition of human 3beta-hydroxysteroid dehydrogenase type 1 and type 2 by trilostane (2008), J. Steroid Biochem. Mol. Biol., 111, 66-73.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.145 expressed in Sf9 insect cells Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
5.3.3.1 identification of potentially critical residues M187 and S124 by docking of trilostane or 4alpha,5alpha-epoxy-testosterone into the active site Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.1.1.145 M187T the 3beta-HSD1 mutant shows 16fold lower affinity inhibition by trilostane compared to the wild type enzyme, and produces a 2.2fold decrease in the Km value for the NAD+ utilization by of 3beta-HSD1 and a 9.2fold decrease in the Km measured for NADH Homo sapiens
1.1.1.145 S124T mutant shows activity similar to the wild type enzyme Homo sapiens
5.3.3.1 M187T increase in affinity for NADH as an allosteric activator Homo sapiens
5.3.3.1 S124T 11fold decrease in affinity to substrate Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.145 4alpha,5alpha-epoxy-testosterone
-
 Homo sapiens
1.1.1.145 trilostane i.e. 2alpha-cyano-4alpha,5alpha-epoxy-17beta-ol-androstane-3-one Homo sapiens
5.3.3.1 4alpha,5alpha-epoxy-testosterone
-
 Homo sapiens
5.3.3.1 trilostane
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
5.3.3.1 0.0001
-
 5-androstene-3,17-dione wild-type, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00041
-
 5-androstene-3,17-dione mutant S124T, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00083
-
 5-androstene-3,17-dione mutant M187T, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.088
-
 5-androstene-3,17-dione 27°C, pH 7.4 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.1.1.145 42000
-
 SDS-PAGE Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.145 Homo sapiens
-
-
-
5.3.3.1 Homo sapiens
-
 bifunctional 3beta-hydroxysteroid dehydrogenase/DELTA5-DELTA4-isomerase, isoform 3betaHSD1
-
5.3.3.1 Homo sapiens
-
 bifunctional 3beta-hydroxysteroid dehydrogenase/DELTA5-DELTA4-isomerase, isoform 3betaHSD2
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.145 adrenal gland isoform 3beta-hydroxysteroid dehydrogenase type 2 Homo sapiens
-
1.1.1.145 breast cancer cell 3beta-hydroxysteroid dehydrogenase type 1 Homo sapiens
-
1.1.1.145 gonad isoform 3beta-hydroxysteroid dehydrogenase type 2 Homo sapiens
-
1.1.1.145 mammary gland 3beta-hydroxysteroid dehydrogenase type 1 Homo sapiens
-
1.1.1.145 placenta 3beta-hydroxysteroid dehydrogenase type 1 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.145 dehydroepiandrosterone + NAD+
-
 Homo sapiens androst-5-en-3,17-dione + NADH + H+
-
 ?
5.3.3.1 5-Androstene-3,17-dione
-
 Homo sapiens 4-Androstene-3,17-dione
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.145 3beta-HSD1 isoform Homo sapiens
1.1.1.145 3beta-HSD2 isoform Homo sapiens
1.1.1.145 3beta-hydroxysteroid dehydrogenase type 1 isoform Homo sapiens
1.1.1.145 3beta-hydroxysteroid dehydrogenase type 2 isoform Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
5.3.3.1 0.83
-
 5-androstene-3,17-dione wild-type, 27°C, pH 7.4 Homo sapiens
5.3.3.1 1.46
-
 5-androstene-3,17-dione mutant M187T, 27°C, pH 7.4 Homo sapiens
5.3.3.1 1.56
-
 5-androstene-3,17-dione mutant S124T, 27°C, pH 7.4 Homo sapiens
5.3.3.1 13.6
-
 5-androstene-3,17-dione 27°C, pH 7.4 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.145 NAD+
-
 Homo sapiens
5.3.3.1 NADH Km value 0.0126 mM, pH 7.4, 27°C Homo sapiens
5.3.3.1 NADH Km value of wild-type 0.0046 mM, pH 7.4, 27°C Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.145 0.0001
-
 trilostane wild type enzyme 3beta-HSD1, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
1.1.1.145 0.00041
-
 trilostane mutant enzyme S124T, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
1.1.1.145 0.00083
-
 trilostane mutant enzyme M187T, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
1.1.1.145 0.0016
-
 trilostane wild type enzyme 3beta-HSD2, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
1.1.1.145 0.0028
-
 4alpha,5alpha-epoxy-testosterone mutant enzyme M187T, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
1.1.1.145 0.00375
-
 4alpha,5alpha-epoxy-testosterone wild type enzyme 3beta-HSD2, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
1.1.1.145 0.00408
-
 4alpha,5alpha-epoxy-testosterone wild type enzyme 3beta-HSD1, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
1.1.1.145 0.00434
-
 4alpha,5alpha-epoxy-testosterone mutant enzyme S124T, in 0.02 M potassium phosphate, pH 7.4, at 27°C Homo sapiens
5.3.3.1 0.0001
-
 trilostane wild-type, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00041
-
 trilostane mutant S124T, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00083
-
 trilostane mutant M187T, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0016
-
 trilostane 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0028
-
 4alpha,5alpha-epoxy-testosterone mutant M187T, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00375
-
 4alpha,5alpha-epoxy-testosterone 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0041
-
 4alpha,5alpha-epoxy-testosterone wild-type, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0043
-
 4alpha,5alpha-epoxy-testosterone mutant S124T, 27°C, pH 7.4 Homo sapiens