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Literature summary for 1.1.1.145 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
Search for more literature for 1.1.1.145

Cloned(Commentary)

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

Protein Variants

Protein Variants Comment Organism
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
S124T mutant shows activity similar to the wild type enzyme Homo sapiens

Inhibitors

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

Molecular Weight [Da]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NAD+
-
 Homo sapiens

Ki Value [mM]

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