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Literature summary for 1.1.1.146 extracted from
- Inhibitory effects of gossypol on corticosteroid 11beta-hydroxysteroid dehydrogenase from guinea pig kidney: A possible mechanism for causing hypokalemia (1991), J. Steroid Biochem. Mol. Biol., 39, 169-176.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| glycyrrhizic acid | dose-dependent competitive inhibition, IC50: 1.994 mM | Cavia porcellus |  |
| gossypol acetic acid | dose-dependent competitive inhibition, IC50: 0.297 mM, (+)-isomer more potent inhibitor than (-)-isomer, mutant hairless strain more sensitive to inhibition than haired strain due to pharmacogenetic differences between the strains | Cavia porcellus | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0027 | - |
11beta,21-dihydroxypregn-4-en-3,20-dione | - |
Cavia porcellus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+ | Cavia porcellus | - |
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH + H+ | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Cavia porcellus | - |
guinea pig | - |
| Cavia porcellus | - |
haired and hairless strains | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| kidney | cortex | Cavia porcellus | - |
Storage Stability
| Storage Stability | Organism |
|---|---|
| -70°C, 0.01 M sodium phosphate, pH 7.0, 0.25 M sucrose, 6 weeks | Cavia porcellus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+ | - |
Cavia porcellus | 21-hydroxy-pregn-4-en-3,11,20-trione + NADPH + H+ | - |
? | |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NADP+ | - |
Cavia porcellus | |
| NADPH | - |
Cavia porcellus | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.297 | - |
dose-dependent competitive inhibition, IC50: 0.297 mM, (+)-isomer more potent inhibitor than (-)-isomer, mutant hairless strain more sensitive to inhibition than haired strain due to pharmacogenetic differences between the strains | Cavia porcellus | gossypol acetic acid | |
| 1.994 | - |
dose-dependent competitive inhibition, IC50: 1.994 mM | Cavia porcellus | glycyrrhizic acid | |
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