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Literature summary for 5.3.3.1 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 5.3.3.1

Crystallization (Commentary)

Crystallization (Comment) Organism
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

Protein Variants Comment Organism
M187T increase in affinity for NADH as an allosteric activator Homo sapiens
S124T 11fold decrease in affinity to substrate Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4alpha,5alpha-epoxy-testosterone
-
 Homo sapiens
trilostane
-
 Homo sapiens

KM Value [mM]

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

Organism

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

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5-Androstene-3,17-dione
-
 Homo sapiens 4-Androstene-3,17-dione
-
 ?

Turnover Number [1/s]

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

Cofactor

Cofactor Comment Organism Structure
NADH Km value 0.0126 mM, pH 7.4, 27°C Homo sapiens
NADH Km value of wild-type 0.0046 mM, pH 7.4, 27°C Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0001
-
 trilostane wild-type, 27°C, pH 7.4 Homo sapiens
0.00041
-
 trilostane mutant S124T, 27°C, pH 7.4 Homo sapiens
0.00083
-
 trilostane mutant M187T, 27°C, pH 7.4 Homo sapiens
0.0016
-
 trilostane 27°C, pH 7.4 Homo sapiens
0.0028
-
 4alpha,5alpha-epoxy-testosterone mutant M187T, 27°C, pH 7.4 Homo sapiens
0.00375
-
 4alpha,5alpha-epoxy-testosterone 27°C, pH 7.4 Homo sapiens
0.0041
-
 4alpha,5alpha-epoxy-testosterone wild-type, 27°C, pH 7.4 Homo sapiens
0.0043
-
 4alpha,5alpha-epoxy-testosterone mutant S124T, 27°C, pH 7.4 Homo sapiens