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Literature summary extracted from
- Cinnamic acids as new inhibitors of 17beta-hydroxysteroid dehydrogenase type 5 (AKR1C3) (2006), Mol. Cell. Endocrinol., 248, 233-235.
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 1.1.1.62 | expression of AKR1C3 in Eschericha coli | Homo sapiens |
| 1.1.1.64 | expression of AKR1C3 in Eschericha coli | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.1.1.62 | 2-methylcinnamic acid | IC50: 0.0064 mM | Homo sapiens |  |
| 1.1.1.62 | 3,4,5-trimethoxycinnamic acid | IC50: 0.049 mM | Homo sapiens | |
| 1.1.1.62 | 3-coumaric acid | 34% inhibition at 0.05 mM | Homo sapiens | |
| 1.1.1.62 | 3-cyclohexylpropanoic acid | weak inhibition, IC50: 0.1 mM, above | Homo sapiens | |
| 1.1.1.62 | 3-trifluoromethylcinnamic acid | IC50: 0.043 mM | Homo sapiens | |
| 1.1.1.62 | caffeic acid | 18% inhibition at 0.05 mM | Homo sapiens | |
| 1.1.1.62 | Cinnamic acid | IC50: 0.050 mM | Homo sapiens | |
| 1.1.1.62 | coumarin-3-carboxylic acid | 30% inhibition at 0.05 mM | Homo sapiens | |
| 1.1.1.64 | 2-methylcinnamic acid | IC50: 0.0064 mM | Homo sapiens | |
| 1.1.1.64 | 3,4,5-trimethoxycinnamic acid | IC50: 0.049 mM | Homo sapiens | |
| 1.1.1.64 | 3-coumaric acid | 34% inhibition at 0.05 mM | Homo sapiens | |
| 1.1.1.64 | 3-cyclohexylpropanoic acid | weak inhibition, IC50: 0.1 mM, above | Homo sapiens | |
| 1.1.1.64 | 3-trifluoromethylcinnamic acid | IC50: 0.043 mM | Homo sapiens | |
| 1.1.1.64 | caffeic acid | 18% inhibition at 0.05 mM | Homo sapiens | |
| 1.1.1.64 | Cinnamic acid | IC50: 0.050 mM | Homo sapiens | |
| 1.1.1.64 | coumarin-3-carboxylic acid | 30% inhibition at 0.05 mM | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.1.1.62 | estrone + NADPH | Homo sapiens | convertion of the weak androgen estrone into the potent estrogen 17beta-estradiol | 17beta-estradiol + NADP+ | - |
? | |
| 1.1.1.64 | androst-4-ene-3,17-dione + NADPH | Homo sapiens | convertion of the weak androgen androstendione into the potent androgen testosterone | testosterone + NADP+ | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.1.1.62 | Homo sapiens | - |
- |
- |
| 1.1.1.64 | Homo sapiens | - |
- |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.1.1.62 | 9,10-phenanthrenequinone + NADPH | - |
Homo sapiens | ? | - |
? | |
| 1.1.1.62 | estrone + NADPH | - |
Homo sapiens | 17beta-estradiol + NADP+ | - |
? | |
| 1.1.1.62 | estrone + NADPH | convertion of the weak androgen estrone into the potent estrogen 17beta-estradiol | Homo sapiens | 17beta-estradiol + NADP+ | - |
? | |
| 1.1.1.64 | 9,10-phenanthrenequinone + NADPH | - |
Homo sapiens | ? | - |
? | |
| 1.1.1.64 | androst-4-ene-3,17-dione + NADPH | - |
Homo sapiens | testosterone + NADP+ | - |
? | |
| 1.1.1.64 | androst-4-ene-3,17-dione + NADPH | convertion of the weak androgen androstendione into the potent androgen testosterone | Homo sapiens | testosterone + NADP+ | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 1.1.1.62 | 17beta-HSD type 5 | - |
Homo sapiens |
| 1.1.1.62 | 17beta-hydroxysteroid dehydrogenase type 5 | - |
Homo sapiens |
| 1.1.1.62 | AKR1C3 | - |
Homo sapiens |
| 1.1.1.62 | More | the enzyme belongs to the aldo-keto reductase family | Homo sapiens |
| 1.1.1.64 | 17beta-HSD type 5 | - |
Homo sapiens |
| 1.1.1.64 | 17beta-hydroxysteroid dehydrogenase type 5 | - |
Homo sapiens |
| 1.1.1.64 | AKR1C3 | - |
Homo sapiens |
| 1.1.1.64 | More | the enzyme belongs to the aldo-keto reductase family | Homo sapiens |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 1.1.1.62 | 6.5 | - |
assay at | Homo sapiens |
| 1.1.1.64 | 6.5 | - |
assay at | Homo sapiens |
Cofactor
| EC Number | Cofactor | Comment | Organism | Structure |
|---|---|---|---|---|
| 1.1.1.62 | NADPH | - |
Homo sapiens | |
| 1.1.1.64 | NADPH | - |
Homo sapiens | |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 1.1.1.62 | 0.0064 | - |
IC50: 0.0064 mM | Homo sapiens | 2-methylcinnamic acid | |
| 1.1.1.62 | 0.043 | - |
IC50: 0.043 mM | Homo sapiens | 3-trifluoromethylcinnamic acid | |
| 1.1.1.62 | 0.049 | - |
IC50: 0.049 mM | Homo sapiens | 3,4,5-trimethoxycinnamic acid | |
| 1.1.1.62 | 0.05 | - |
IC50: 0.050 mM | Homo sapiens | Cinnamic acid | |
| 1.1.1.62 | 0.1 | - |
weak inhibition, IC50: 0.1 mM, above | Homo sapiens | 3-cyclohexylpropanoic acid | |
| 1.1.1.64 | 0.0064 | - |
IC50: 0.0064 mM | Homo sapiens | 2-methylcinnamic acid | |
| 1.1.1.64 | 0.043 | - |
IC50: 0.043 mM | Homo sapiens | 3-trifluoromethylcinnamic acid | |
| 1.1.1.64 | 0.049 | - |
IC50: 0.049 mM | Homo sapiens | 3,4,5-trimethoxycinnamic acid | |
| 1.1.1.64 | 0.05 | - |
IC50: 0.050 mM | Homo sapiens | Cinnamic acid | |
| 1.1.1.64 | 0.1 | - |
weak inhibition, IC50: 0.1 mM, above | Homo sapiens | 3-cyclohexylpropanoic acid | |
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