Application | Comment | Organism |
---|---|---|
medicine | the selective inhibition of human 3beta-HSD1 in breast tumors represents a potential treatment for hormone-sensitive breast cancer | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression of wild-type and mutant enzymes in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D61N | site-directed mutagenesis, mutation in isozyme 3beta-HSD1 | Homo sapiens |
D61V | site-directed mutagenesis, mutation in isozyme 3beta-HSD1 | Homo sapiens |
E192A | site-directed mutagenesis, mutation in isozyme 3beta-HSD1 | Homo sapiens |
P195R | site-directed mutagenesis, mutation in isozyme 3beta-HSD2 | Homo sapiens |
R195P | site-directed mutagenesis, mutation in isozyme 3beta-HSD1 | Homo sapiens |
T8A | site-directed mutagenesis, mutation in isozyme 3beta-HSD1 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
trilostane | competitive for 3beta-HSD1, noncompetitive for 3beta-HSD2 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant wild-type and mutant enzymes from Sf9 insect cells by ultracentrifugation | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
breast cancer cell | selective expression of 3beta-HSD1 | Homo sapiens | - |
mammary gland | selective expression of 3beta-HSD1 | Homo sapiens | - |
additional information | isozymes 3beta-HSD1 and 3beta-HSD2 are encoded by two distinct genes which are expressed in a tissue-specific pattern | Homo sapiens | - |
placenta | selective expression of 3beta-HSD1 | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
16alpha-hydroxy-dehydroepiandrosterone + NADH + H+ | - |
Homo sapiens | ? | - |
? | |
16beta-hydroxy-dehydroepiandrosterone + NADH + H+ | - |
Homo sapiens | ? | - |
? | |
17alpha-hydroxypregnenolone + NADH + H+ | - |
Homo sapiens | 17alpha-hydroxyprogesterone + NAD+ | - |
? | |
5-androstene-3,17-dione + NAD+ | - |
Homo sapiens | dehydroepiandrosterone + NADH + H+ | - |
? | |
dehydroepiandrosterone + NADH + H+ | - |
Homo sapiens | 5-androstene-3,17-dione + NAD+ | - |
? | |
additional information | both isoforms of the enzyme catalyze the conversion of 3beta-hydroxy-5-ene-steroids (dehydroepiandrosterone, 17alpha-hydroxypregnenolone, pregnenolone) to 3-oxo-4-ene-steroids (androstenedione, 17alpha-hydroxyprogestrone, progesterone) on a single, dimeric protein containing both enzyme activities | Homo sapiens | ? | - |
? | |
pregnenolone + NADH + H+ | - |
Homo sapiens | progesterone + NAD+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
3beta-HSD1 | - |
Homo sapiens |
3beta-HSD2 | - |
Homo sapiens |
3beta-hydroxysteroid dehydrogenase type 1 | - |
Homo sapiens |
3beta-hydroxysteroid dehydrogenase/Delta 5->4-isomerase type 1 | - |
Homo sapiens |
3beta-hydroxysteroid dehydrogenase/Delta 5->4-isomerase type 2 | - |
Homo sapiens |
SDR11E1 | - |
Homo sapiens |
SDR11E2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
27 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NAD+ | - |
Homo sapiens | |
NADH | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0001 | - |
trilostane | 3beta-HSD1 wild-type, pH 7.4, 27°C | Homo sapiens | |
0.00019 | - |
trilostane | 3beta-HSD2 mutant P195R, pH 7.4, 27°C | Homo sapiens | |
0.0016 | - |
trilostane | 3beta-HSD2 wild-type, pH 7.4, 27°C | Homo sapiens | |
0.00256 | - |
trilostane | 3beta-HSD1 mutant R195P, pH 7.4, 27°C | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
evolution | human 3beta-hydroxysteroid dehydrogenase is a member of the short-chain dehydrogenase/reductase (SDR) family of enzymes, all of which contain the Rossmann-fold domain with a beta-alpha-beta-alpha-beta-alpha-beta-alpha-beta folding pattern that binds cofactor and substrate | Homo sapiens |
metabolism | the enzyme catalyzes the first step in the conversion of dehydroepiandrosterone to estradiol | Homo sapiens |
physiological function | the enzyme promotes tumor growth in placenta, mammary glands, and breasts. In human adrenals, 3beta-HSD2 is required for the production of cortisol and aldosterone | Homo sapiens |