Cloned (Comment) | Organism |
---|---|
expressed in Sf9 cells using the baculovirus system | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D61N | D61N mutation produces a 1.3fold increase in Km for the dehydroepiandrosterone substrate, a 1.9fold increase in Km for NAD+ utilization by the 3beta-HSD activity and little change in isomerase kinetics for either substrate or cofactor | Homo sapiens |
D61V | mutant shows no enzymatic activity | Homo sapiens |
E192A | the E192A mutation causes an 8.2fold increase in Km (dehydroepiandrosterone) and no change in the Km for NAD+ | Homo sapiens |
R195P | R195P mutation shifts the high-affinity, competitive inhibition profile of 3beta-HSD1 to a low-affinity (Ki= 2.56 microM), noncompetitive inhibition profile. R195P mutant has a 10.4fold higher Km value for 16beta-hydroxy-dehydroepiandrosterone compared to wild-type 3beta-HSD1. Km values for 16alpha-hydroxy-dehydroepiandrosterone and dehydroepiandrosterone are also inreased compared to wild-type (kcat values are decreased compared to wild-type) | Homo sapiens |
R195R | the P195R mutation shifts the low-affinity, noncompetitive inhibition profile of 3beta-HSD2 to a high affinity (Ki= 0.19 microM), competitive inhibition profile. The P195R mutant has a 12.2fold lower Km value for 16beta-hydroxy-dehydroepiandrosterone compared to wild-type 3beta-HSD2. The coenzyme values measured for P195R mutant are similar to those measured for wildtype 3beta-HSD2 | Homo sapiens |
T8A | mutant shows almost similar kinetic values as wild-type | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
trilostane | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0014 | - |
16beta-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.0015 | - |
16beta-hydroxy-dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.0025 | - |
NADH | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.0036 | - |
NADH | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.0037 | - |
dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.004 | - |
16alpha-hydroxy-dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.0046 | - |
NADH | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.0055 | - |
NADH | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.0064 | - |
16alpha-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.0065 | - |
NADH | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.0072 | - |
NADH | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
0.0077 | - |
dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.0082 | - |
dehydroepiandrosterone | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.0107 | - |
dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.0126 | - |
NADH | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.0148 | - |
16alpha-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.015 | - |
16beta-hydroxy-dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.0156 | - |
dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.0184 | - |
16beta-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.0196 | - |
16alpha-hydroxy-dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.0205 | - |
NAD+ | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.0333 | - |
NAD+ | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.0341 | - |
NAD+ | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.0351 | - |
NAD+ | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.0351 | - |
dehydroepiandrosterone | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.0564 | - |
NAD+ | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.0643 | - |
NAD+ | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
0.0643 | - |
dehydroepiandrosterone | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
0.0863 | - |
NAD+ | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
42000 | - |
SDS-PAGE | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P14060 | - |
- |
Homo sapiens | P26439 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
16alpha-hydroxy-dehydroepiandrosterone + NAD+ | - |
Homo sapiens | ? | - |
? | |
16alpha-hydroxy-dehydroepiandrosterone + NAD+ | - |
Homo sapiens | ? + NADH | - |
? | |
16beta-hydroxy-dehydroepiandrosterone + NAD+ | - |
Homo sapiens | ? | - |
? | |
16beta-hydroxy-dehydroepiandrosterone + NAD+ | - |
Homo sapiens | ? + NADH | - |
? | |
androst-5-en-3,17-dione + NADH | - |
Homo sapiens | dehydroepiandrosterone + NAD+ | - |
r | |
dehydroepiandrosterone + NAD+ | - |
Homo sapiens | androst-5-en-3,17-dione + NADH + H+ | - |
? | |
dehydroepiandrosterone + NAD+ | - |
Homo sapiens | androst-5-en-3,17-dione + NADH + H+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
3beta-HSD1 | - |
Homo sapiens |
3beta-HSD2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
27 | - |
assay at | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.02 | - |
NAD+ | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.03 | - |
dehydroepiandrosterone | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.04 | - |
dehydroepiandrosterone | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
0.04 | - |
NAD+ | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.04 | - |
16beta-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.05 | - |
16beta-hydroxy-dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.05 | - |
NAD+ | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.05 | - |
dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.06 | - |
NAD+ | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
0.06 | - |
dehydroepiandrosterone | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.07 | - |
16alpha-hydroxy-dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.09 | - |
dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.09 | - |
16alpha-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.1 | - |
NAD+ | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.11 | - |
NAD+ | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.12 | - |
dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.14 | - |
dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.14 | - |
16beta-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.15 | - |
16beta-hydroxy-dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.15 | - |
16alpha-hydroxy-dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
0.15 | - |
16alpha-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
0.17 | - |
NAD+ | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
0.31 | - |
NADH | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.69 | - |
NADH | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
0.75 | - |
NADH | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
0.76 | - |
NADH | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
1.03 | - |
NADH | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
1.49 | - |
NADH | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
1.65 | - |
NADH | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00001 | - |
trilostane | pH 7.4, 27°C, wild-tpye 3beta-HSD1 | Homo sapiens | |
0.00002 | - |
trilostane | pH 7.4, 27°C, mutant R195R | Homo sapiens | |
0.0001 | - |
trilostane | pH 7.4, 27°C, wild-tpye 3beta-HSD2 | Homo sapiens | |
0.00022 | - |
trilostane | pH 7.4, 27°C, mutant R195P | Homo sapiens |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.83 | - |
NAD+ | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
1 | - |
NAD+ | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
1 | - |
dehydroepiandrosterone | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
1.33 | - |
NAD+ | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
1.33 | - |
NAD+ | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
1.66 | - |
NAD+ | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
3.16 | - |
NAD+ | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
4.83 | - |
NAD+ | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
7.33 | - |
dehydroepiandrosterone | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
7.33 | - |
dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
7.66 | - |
16beta-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
7.83 | - |
16alpha-hydroxy-dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
10 | - |
dehydroepiandrosterone | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
10.16 | - |
16alpha-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
10.33 | - |
16beta-hydroxy-dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
11.21 | - |
dehydroepiandrosterone | mutant R195P, pH 7.4, 27°C | Homo sapiens | |
12.16 | - |
dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
14.83 | - |
dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
15 | - |
16alpha-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
19.1 | - |
16alpha-hydroxy-dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
34.5 | - |
16beta-hydroxy-dehydroepiandrosterone | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
35.5 | - |
16beta-hydroxy-dehydroepiandrosterone | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
106 | - |
NADH | mutant D61N, pH 7.4, 27°C | Homo sapiens | |
106 | - |
NADH | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
125 | - |
NADH | mutant E192A, pH 7.4, 27°C | Homo sapiens | |
131 | - |
NADH | wild-type 3beta-HSD2, pH 7.4, 27°C | Homo sapiens | |
163 | - |
NADH | wild-type 3beta-HSD1, pH 7.4, 27°C | Homo sapiens | |
271 | - |
NADH | mutant R195R, pH 7.4, 27°C | Homo sapiens | |
280 | - |
NADH | mutant R195P, pH 7.4, 27°C | Homo sapiens |