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Literature summary for 1.3.1.22 extracted from
- Theaflavin-3,3'-digallate and penta-O-galloyl-beta-D-glucose inhibit rat liver microsomal 5alpha-reductase activity and the expression of androgen receptor in LNCaP prostate cancer cells (2004), Carcinogenesis, 25, 1109-1118.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (-)-epigallocatechin-3-gallate | i.e. EGCG, from Thea sativa, slightly inhibits the liver microsomal enzyme | Rattus norvegicus |  |
| additional information | theaflavin, gallic acid, and n-propyl gallate are poor inhibitors, physiological effects of inhibitors in vivo, overview | Rattus norvegicus | |
| penta-O-galloyl-beta-D-glucose | from Thea sativa, inhibits the expression of androgen receptor and reduce secretion of prostate-specific antigen in LNCaP prostate cancer cells | Homo sapiens | |
| penta-O-galloyl-beta-D-glucose | i.e. 5GG, from Thea sativa, inhibits the liver microsomal enzyme | Rattus norvegicus | |
| theaflavin-3'-gallate | i.e. TF2b, from Thea sativa, inhibits the liver microsomal enzyme | Rattus norvegicus | |
| theaflavin-3,3'-digallate | from Thea sativa, inhibits the expression of androgen receptor and reduce secretion of prostate-specific antigen in LNCaP prostate cancer cells | Homo sapiens | |
| theaflavin-3,3'-digallate | i.e. TF3, from Thea sativa, inhibits the liver microsomal enzyme | Rattus norvegicus | |
| theaflavin-3-gallate | i.e. TF2a, from Thea sativa, inhibits the liver microsomal enzyme | Rattus norvegicus | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00245 | - |
testosterone | pH 6.5, 37°C | Rattus norvegicus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Rattus norvegicus | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| testosterone + NADPH + H+ | Rattus norvegicus | - |
5alpha-dihydrotestosterone + NADP+ | 5alpha-dihydrotestosterone is a more potent androgen, regulatory function, overview | ? | |
| testosterone + NADPH + H+ | Homo sapiens | - |
5alpha-dihydrotestosterone + NADP+ | dihydrotestosterone is a more potent androgen, regulatory function, overview | ? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
2 isozymes 5alpha-R1 and 5alpha-R2 | - |
| Rattus norvegicus | - |
2 isozymes 5alpha-R1 and 5alpha-R2 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| liver | only isozyme 5alpha-R1 | Rattus norvegicus | - |
| LNCaP cell | prostate cancer cell line | Homo sapiens | - |
| prostate | - |
Homo sapiens | - |
| prostate | - |
Rattus norvegicus | - |
| prostate carcinoma cell | - |
Homo sapiens | - |
| prostate carcinoma cell | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| testosterone + NADPH + H+ | - |
Homo sapiens | 5alpha-dihydrotestosterone + NADP+ | - |
? | |
| testosterone + NADPH + H+ | - |
Rattus norvegicus | 5alpha-dihydrotestosterone + NADP+ | - |
? | |
| testosterone + NADPH + H+ | - |
Rattus norvegicus | 5alpha-dihydrotestosterone + NADP+ | 5alpha-dihydrotestosterone is a more potent androgen, regulatory function, overview | ? | |
| testosterone + NADPH + H+ | - |
Homo sapiens | 5alpha-dihydrotestosterone + NADP+ | dihydrotestosterone is a more potent androgen, regulatory function, overview | ? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| steroid 5alpha-reductase | - |
Homo sapiens |
| steroid 5alpha-reductase | - |
Rattus norvegicus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
| 37 | - |
assay at | Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 6.5 | - |
assay at | Homo sapiens |
| 6.5 | - |
assay at | Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NADPH | - |
Homo sapiens | |
| NADPH | - |
Rattus norvegicus | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Rattus norvegicus | |
| 0.00036 | - |
theaflavin-3,3'-digallate | pH 6.5, 37°C, versus NADPH | Rattus norvegicus | |
| 0.00048 | - |
penta-O-galloyl-beta-D-glucose | pH 6.5, 37°C, versus NADPH | Rattus norvegicus | |
| 0.0026 | - |
theaflavin-3'-gallate | pH 6.5, 37°C, versus NADPH | Rattus norvegicus | |
| 0.0027 | - |
penta-O-galloyl-beta-D-glucose | pH 6.5, 37°C, versus testosterone | Rattus norvegicus | |
| 0.0056 | - |
theaflavin-3,3'-digallate | pH 6.5, 37°C, versus testosterone | Rattus norvegicus | |
| 0.0065 | - |
theaflavin-3'-gallate | pH 6.5, 37°C, versus testosterone | Rattus norvegicus | |
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