Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
H156Y | 5fold decrease in catalytic efficiency | Homo sapiens |
Q105M1 | 5fold decrease in catalytic efficiency | Homo sapiens |
Q105M1 | mutant retains the lower affinity profile of inhibition by epostane that is observed with wild-type 3beta-HSD2 | Homo sapiens |
R195P | mutation of isoform 3betaHSD1 to corresponding residue in isoform 3betaHSD2. Mutation shifts the dehydroepiandrosterone substrate kinetics to the lower affinity profile of isoform 3beta-HSD2 | Homo sapiens |
R195P | mutation of isoform 3betaHSD2 to corresponding residue in isoform 3betaHSD1. Mutation shifts the dehydroepiandrosterone substrate kinetics to the higher affinity profile of isoform 3beta-HSD1 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
epostane | inhibits the dehydroepiandrosterone-induced proliferation of MCF-7 cells expressing isoform 3beta-HSD1 with 12- to 16fold lower IC50 values compared to the MCF-7 cells expressing isoform 3beta-HSD2. Epostane also competitively inhibits purified human 3beta-HSD1 with 12fold to 16fold lower Ki values compared to the noncompetitive Ki values measured for human 3beta-HSD2; inhibits the dehydroepiandrosterone-induced proliferation of MCF-7 cells expressing isoform 3beta-HSD1 with 12- to 16fold lower IC50 values compared to the MCF-7 cells expressing isoform 3beta-HSD. Epostane also competitively inhibits purified human 3beta-HSD1 with 12fold to 16fold lower Ki values compared to the noncompetitive Ki values measured for human 3beta-HSD2 | Homo sapiens | |
trilostane | inhibits the dehydroepiandrosterone-induced proliferation of MCF-7 cells expressing isoform 3beta-HSD1 with 12- to 16fold lower IC50 values compared to the MCF-7 cells expressing isoform 3beta-HSD2. Trilostane also competitively inhibits purified human 3beta-HSD1 with 12fold to 16fold lower Ki values compared to the noncompetitive Ki values measured for human 3beta-HSD2; inhibits the dehydroepiandrosterone-induced proliferation of MCF-7 cells expressing isoform 3beta-HSD1 with 12- to 16fold lower IC50 values compared to the MCF-7 cells expressing isoform 3beta-HSD2. Trilostane also competitively inhibits purified human 3beta-HSD1 with 12fold to 16fold lower Ki values compared to the noncompetitive Ki values measured for human 3beta-HSD2. Trilostane is docked in the active site of isoform 3beta-HSD1, and residue Arg195 in 3beta-HSD1 is a potentially critical residue | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00164 | - |
dehydroepiandrosterone | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.0037 | - |
dehydroepiandrosterone | wild-type, pH 7.4, 27°C | Homo sapiens | |
0.0077 | - |
dehydroepiandrosterone | mutant P195R, pH 7.4, 27°C | Homo sapiens | |
0.0107 | - |
dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.0156 | - |
dehydroepiandrosterone | wild-type, pH 7.4, 27°C | Homo sapiens | |
0.04 | - |
dehydroepiandrosterone | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.0424 | - |
dehydroepiandrosterone | mutant H156Y, pH 7.4, 27°C | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P14060 | isoform 3betaHSD1 | - |
Homo sapiens | P26439 | isoform 3betaHSD2 | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
dehydroepiandrosterone + NAD+ | - |
Homo sapiens | androst-5-en-3,17-dione + NADH + H+ | - |
? |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.055 | - |
dehydroepiandrosterone | wild-type, pH 7.4, 27°C | Homo sapiens | |
0.075 | - |
dehydroepiandrosterone | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.093 | - |
dehydroepiandrosterone | mutant P195R, pH 7.4, 27°C | Homo sapiens | |
0.113 | - |
dehydroepiandrosterone | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.118 | - |
dehydroepiandrosterone | mutant H156Y, pH 7.4, 27°C | Homo sapiens | |
0.13 | - |
dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.145 | - |
dehydroepiandrosterone | wild-type, pH 7.4, 27°C | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00007 | - |
epostane | wild-type, pH 7.4, 27°C | Homo sapiens | |
0.0001 | - |
trilostane | wild-type, pH 7.4, 27°C | Homo sapiens | |
0.00098 | - |
epostane | wild-type, pH 7.4, 27°C | Homo sapiens | |
0.00118 | - |
epostane | mutant H156Y, pH 7.4, 27°C | Homo sapiens | |
0.00164 | - |
epostane | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.00184 | - |
epostane | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.0019 | - |
trilostane | mutant P195R, pH 7.4, 27°C | Homo sapiens | |
0.00256 | - |
trilostane | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.016 | - |
trilostane | wild-type, pH 7.4, 27°C | Homo sapiens |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0028 | - |
dehydroepiandrosterone | mutant H156Y, pH 7.4, 27°C | Homo sapiens | |
0.0028 | - |
dehydroepiandrosterone | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.003 | - |
dehydroepiandrosterone | mutant Q105M, pH 7.4, 27°C | Homo sapiens | |
0.0073 | - |
dehydroepiandrosterone | wild-type, pH 7.4, 27°C | Homo sapiens | |
0.012 | - |
dehydroepiandrosterone | mutant P195R, pH 7.4, 27°C | Homo sapiens | |
0.012 | - |
dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.015 | - |
dehydroepiandrosterone | wild-type, pH 7.4, 27°C | Homo sapiens |