Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Flufenamic acid | a nonsteroidalanti-inflammatory drug, IC50: 1.084 mM | Homo sapiens | |
additional information | no inhibition by the bile acid 5beta-cholanic acid-3alpha,7alpha-diol | Homo sapiens | |
Phenolphthalein | AKR1C4-selective inhibitor, in vitro and in vivo inhibition, IC50: 0.0004 mM | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cytosol | - |
Homo sapiens | 5829 | - |
additional information | subcellular localization study, overview | Homo sapiens | - |
- |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
tibolone + NADPH + H+ | Homo sapiens | tibolone is used to treat climacteric symptoms and prevent osteoporosis, it exerts tissue-selective effects via site-specific metabolism into 3alpha- and 3beta-hydroxymetabolites and a DELTA4-isomer | 3-hydroxytibolone + NADP+ | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
hepatocyte | primary, high expression and activity in healthy hepatocytes | Homo sapiens | - |
liver | high expression and activity in female and male liver | Homo sapiens | - |
additional information | no activity in the hepatoma cell line Hep-G2 | Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
additional information | - |
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
tibolone + NADPH + H+ | tibolone is used to treat climacteric symptoms and prevent osteoporosis, it exerts tissue-selective effects via site-specific metabolism into 3alpha- and 3beta-hydroxymetabolites and a DELTA4-isomer | Homo sapiens | 3-hydroxytibolone + NADP+ | - |
? | |
tibolone + NADPH + H+ | i.e. [7alpha,17alpha]-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one, stereoselctive reaction to the 3alpha-hydroxytibolone product | Homo sapiens | 3-hydroxytibolone + NADP+ | - |
? | |
tibolone + NADPH + H+ | i.e. [7alpha,17alpha]-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one, stereoselective reaction to the 3alpha-hydroxytibolone product | Homo sapiens | 3-hydroxytibolone + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
AKR1C4 | - |
Homo sapiens |
More | cf. 1.1.1.213, the enzyme belongs to the aldo-keto reductase subfamily AKR1C | Homo sapiens |
More | cf. EC 1.1.1.213, the enzyme belongs to the aldo-keto reductase subfamily AKR1C | Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0004 | - |
AKR1C4-selective inhibitor, in vitro and in vivo inhibition, IC50: 0.0004 mM | Homo sapiens | Phenolphthalein | |
1.084 | - |
a nonsteroidalanti-inflammatory drug, IC50: 1.084 mM | Homo sapiens | Flufenamic acid |