Any feedback?
Literature summary for 1.3.1.3 extracted from
- Crystal structures of human Delta4-3-ketosteroid 5beta-reductase (AKR1D1) reveal the presence of an alternative binding site responsible for substrate inhibition (2008), Biochemistry, 47, 13537-13546.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of GST-tagged enzyme in Escherichia coli | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| purifed recombinant h5beta-red in ternary complex with NADPH and androstenedione, hanging-drop vapor diffusion technique, 2:1 v/v ratio of protein and well solution, about 5 days, X-ray diffraction structure determination and analysis at 2.0-2.3 A resolution | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| V309F | replacement of one of the residues delineating this site by a phenylalanine completely abolishes the enzyme's substrate inhibition, but the catalytic efficiency of the mutated enzyme is similar to that of the wild-type h5beta-red enzyme | Homo sapiens |
| Y132F | replacement of one of the residues delineating this site by a phenylalanine completely abolishes the enzyme's substrate inhibition, but the catalytic efficiency of the mutated enzyme is similar to that of the wild-type h5beta-red enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| androstenedione | the enzyme is rapidly inhibited by the substrate once its concentration reaches 2times the Km value. Androstenedione completely impedes the passage of another substrate molecule toward the catalytic site | Homo sapiens |  |
| additional information | structural features of substrate inhibition of h5beta-red by C19- and C21-steroids, overview | Homo sapiens | |
| progesterone | the enzyme is rapidly inhibited by the substrate once its concentration reaches 2times the Km value | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics for the reduction of androstenedione, overview | Homo sapiens | |
| 0.00037 | - |
androstenedione | pH 7.4, 37°C, wild-type enzyme | Homo sapiens | |
| 0.00094 | - |
androstenedione | pH 7.4, 37°C, mutant Y132F | Homo sapiens | |
| 0.01629 | - |
androstenedione | pH 7.4, 37°C, mutant V309F | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P51857 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant GST-tagged enzyme from Escherichia coli by glutathione affinity and anion exchange chromatography, and gel filtration | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 7alpha,12alpha-dihydroxy-4-cholesten-3-one + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| 7alpha-hydroxy-4-cholesten-3-one + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| androstenedione + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
| additional information | the large steroid-binding site of this enzyme also contains a subsite in which the androstenedione molecule is bound, steroid-binding cavity structure of h5 beta-red, structure comparison | Homo sapiens | ? | - |
? | |
| progesterone + NADPH + H+ | - |
Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | steroid-binding cavity structure of h5 beta-red, structure comparison | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AKR1D1 | - |
Homo sapiens |
| DELTA4-3-ketosteroid 5beta-reductase | - |
Homo sapiens |
| h5beta-red | - |
Homo sapiens |
| h5beta-reductase | - |
Homo sapiens |
| More | human 5beta-red belongs to the aldo-keto reductase, AKR, superfamily and is the first member of the 1D subfamily, AKR1D1 | Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.013 | - |
androstenedione | pH 7.4, 37°C, wild-type enzyme | Homo sapiens | |
| 0.0405 | - |
androstenedione | pH 7.4, 37°C, mutant Y132F | Homo sapiens | |
| 0.0425 | - |
androstenedione | pH 7.4, 37°C, mutant V309F | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.3 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NADPH | - |
Homo sapiens | |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 2.609 | - |
androstenedione | pH 7.4, 37°C, mutant V309F | Homo sapiens | |
| 35.13 | - |
androstenedione | pH 7.4, 37°C, wild-type enzyme | Homo sapiens | |
| 43.08 | - |
androstenedione | pH 7.4, 37°C, mutant Y132F | Homo sapiens | |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
