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Literature summary extracted from

  • Thomas, J.L.; Boswell, E.L.; Scaccia, L.A.; Pletnev, V.; Umland, T.C.
    Identification of key amino acids responsible for the substantially higher affinities of human type 1 3beta-hydroxysteroid dehydrogenase/isomerase (3b-HSD1) for substrates, coenzymes, and inhibitors relative to human 3b-HSD2 (2005), J. Biol. Chem., 280, 21321-21328.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.145 expression of soluble wild-type and mutant isozyme 3beta-HSD1 in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system Homo sapiens
1.1.1.145 expression of soluble wild-type and mutant isozyme 3beta-HSD2 in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.1.1.145 Q105M site-directed mutagenesis of isozyme 1, the mutants show altered kinetics compared to the wild-type isozymes Homo sapiens
1.1.1.145 Q105M site-directed mutagenesis of isozyme 2, the mutants show altered kinetics compared to the wild-type isozymes Homo sapiens
1.1.1.145 Q240R site-directed mutagenesis of isozyme 1, the mutant shows altered kinetics compared to the wild-type isozyme Homo sapiens
1.1.1.145 R240Q site-directed mutagenesis of isozyme 2, the mutant shows altered kinetics compared to the wild-type isozyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.145 epostane
-
 Homo sapiens
1.1.1.145 trilostane
-
 Homo sapiens
5.3.3.1 epostane
-
 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
1.1.1.145 additional information
-
 additional information kinetics, recombinant wild-type and mutant isozymes, overview, kinetics for the DELTA-5-3-ketosteroid isomerase, EC 5.3.3.1, activity Homo sapiens
1.1.1.145 0.0037
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD1 Homo sapiens
1.1.1.145 0.0061
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q240R Homo sapiens
1.1.1.145 0.025
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant Q105M Homo sapiens
1.1.1.145 0.0256
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q240R Homo sapiens
1.1.1.145 0.0327
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant R240Q Homo sapiens
1.1.1.145 0.0341
-
 NAD+ pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD1 Homo sapiens
1.1.1.145 0.0372
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant R240Q Homo sapiens
1.1.1.145 0.0388
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q105M Homo sapiens
1.1.1.145 0.0405
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q105M Homo sapiens
1.1.1.145 0.0473
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD2 Homo sapiens
1.1.1.145 0.0614
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant Q105M Homo sapiens
1.1.1.145 0.0863
-
 NAD+ pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD2 Homo sapiens
5.3.3.1 0.0175
-
 dehydroepiandrosterone mutant R240Q, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0279
-
 dehydroepiandrosterone wild-type, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.033
-
 dehydroepiandrosterone mutant Q105M, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0623
-
 dehydroepiandrosterone mutant Q240R, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0808
-
 dehydroepiandrosterone mutant Q105M, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0884
-
 dehydroepiandrosterone wild-type, isoform 2, 27°C, pH 7.4 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.145 Homo sapiens P14060 3beta-HSD1; isozyme 3beta-HSD1, bifunctional enzyme
-
1.1.1.145 Homo sapiens P26439 3beta-HSD2; isozyme 3beta-HSD2, bifunctional enzyme
-
5.3.3.1 Homo sapiens
-
 bifunctional 3beta-hydroxysteroid dehydrogenase/isomerase, isoforms type 1 and 2
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.145 recombinant soluble wild-type and mutant isozyme 3beta-HSD1 from Sf9 insect cells Homo sapiens
1.1.1.145 recombinant soluble wild-type and mutant isozyme 3beta-HSD2 from Sf9 insect cells Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.145 adrenal gland isozyme 3beta-HSD2 Homo sapiens
-
1.1.1.145 breast cancer cell isozyme 3beta-HSD1 Homo sapiens
-
1.1.1.145 gonad isozyme 3beta-HSD2 Homo sapiens
-
1.1.1.145 placenta isozyme 3beta-HSD1 Homo sapiens
-
1.1.1.145 prostate tumor cell isozyme 3beta-HSD1 Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.1.1.145 additional information
-
-
 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 ?
-
 r
1.1.1.145 additional information bifunctional enzyme that also catalyzes the reaction of the DELTA-5-3-ketosteroid isomerase, EC 5.3.3.1 Homo sapiens ?
-
 ?
5.3.3.1 dehydroepiandrosterone
-
 Homo sapiens 3beta-hydroxy-4-androsten-17-one
-
 ?

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.145 27
-
 assay at Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.1.1.145 0.022
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q240R Homo sapiens
1.1.1.145 0.023
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q240R Homo sapiens
1.1.1.145 0.038
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q105M Homo sapiens
1.1.1.145 0.055
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD1 Homo sapiens
1.1.1.145 0.058
-
 NAD+ pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD1 Homo sapiens
1.1.1.145 0.075
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant Q105M Homo sapiens
1.1.1.145 0.113
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD1 mutant Q105M Homo sapiens
1.1.1.145 0.118
-
 NAD+ pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD2 Homo sapiens
1.1.1.145 0.118
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant wild-type isozyme 3beta-HSD2 Homo sapiens
1.1.1.145 0.145
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant Q105M Homo sapiens
1.1.1.145 0.187
-
 NAD+ pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant R240Q Homo sapiens
1.1.1.145 0.217
-
 dehydroepiandrosterone pH 7.4, 27°C, recombinant isozyme 3beta-HSD2 mutant R240Q Homo sapiens
5.3.3.1 1990
-
 dehydroepiandrosterone mutant Q240R, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 2064
-
 dehydroepiandrosterone mutant R240Q, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 2088
-
 dehydroepiandrosterone mutant Q105M, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 3012
-
 dehydroepiandrosterone wild-type, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 4002
-
 dehydroepiandrosterone mutant Q105M, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 4890
-
 dehydroepiandrosterone wild-type, isoform 2, 27°C, pH 7.4 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.145 7.4
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.145 NAD+
-
 Homo sapiens
1.1.1.145 NADH
-
 Homo sapiens
5.3.3.1 NADH isomerase activity of enzyme requires NADH, Km- and kcat-value of isoform 1 wild-type are 0.0046 mM and 45 per min, resp. Km- and kcat-value of isoform 2 wild-type are 0.0126 mM and 99.1 per min, resp Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
5.3.3.1 0.00007
-
 epostane mutant Q240R, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00007
-
 epostane wild-type, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.0001
-
 trilostane wild-type, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00012
-
 trilostane mutant R240Q, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00013
-
 trilostane mutant Q240R, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00021
-
 epostane mutant R240Q, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00098
-
 epostane wild-type, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00164
-
 epostane mutant Q105M, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00166
-
 trilostane wild-type, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00184
-
 epostane mutant Q105M, isoform 1, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00207
-
 trilostane mutant Q105M, isoform 2, 27°C, pH 7.4 Homo sapiens
5.3.3.1 0.00208
-
 trilostane mutant Q105M, isoform 1, 27°C, pH 7.4 Homo sapiens