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Literature summary for 1.14.14.14 extracted from
- Inhibition of aromatase cytochrome P-450 (estrogen synthetase) by derivatives of alpha-naphthoflavone (1986), Biochem. Pharmacol., 35, 2887-2891.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 7,8-Benzoflavone | competitive inhibitor, induces spectral changes in the aromatase cytochrome P450 | Homo sapiens |  |
| apigenin | - |
Homo sapiens | |
| chrysin | competitive inhibitor, induces spectral changes in the aromatase cytochrome P450 | Homo sapiens | |
| flavanone | - |
Homo sapiens | |
| flavone | - |
Homo sapiens | |
| additional information | not inhibitory: 5,6-benzoflavone | Homo sapiens | |
| quercetin | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| microsome | - |
Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| androst-4-ene-3,17-dione + 3 O2 + 3 reduced flavoproteins | Homo sapiens | overall reaction | estrone + formate + 4 H2O + 3 oxidized flavoproteins | - |
? | |
| testosterone + 3 O2 + 3 reduced flavoproteins | Homo sapiens | overall reaction | 17beta-estradiol + formate + 4 H2O + 3 oxidized flavoproteins | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| ovary | - |
Homo sapiens | - |
| placenta | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| androst-4-ene-3,17-dione + 3 O2 + 3 reduced flavoproteins | overall reaction | Homo sapiens | estrone + formate + 4 H2O + 3 oxidized flavoproteins | - |
? | |
| testosterone + 3 O2 + 3 reduced flavoproteins | overall reaction | Homo sapiens | 17beta-estradiol + formate + 4 H2O + 3 oxidized flavoproteins | - |
? | |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| cytochrome P450 | inhibitors 7,8-benzoflavone and chrysin induce spectral changes in the aromatase cytochrome P450 | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00006 | - |
substrate testosterone, pH 7.2, 37°C | Homo sapiens | 7,8-Benzoflavone | |
| 0.00007 | - |
substrate androst-4-ene-3,17-dione, pH 7.2, 37°C | Homo sapiens | 7,8-Benzoflavone | |
| 0.0004 | - |
substrate testosterone, pH 7.2, 37°C | Homo sapiens | chrysin | |
| 0.0005 | - |
substrate androst-4-ene-3,17-dione, pH 7.2, 37°C | Homo sapiens | chrysin | |
| 0.001 | - |
substrate testosterone, pH 7.2, 37°C | Homo sapiens | apigenin | |
| 0.0012 | - |
substrate androst-4-ene-3,17-dione, pH 7.2, 37°C | Homo sapiens | apigenin | |
| 0.005 | - |
substrate testosterone, pH 7.2, 37°C | Homo sapiens | flavone | |
| 0.005 | - |
substrate testosterone, pH 7.2, 37°C | Homo sapiens | flavanone | |
| 0.008 | - |
substrate androst-4-ene-3,17-dione, pH 7.2, 37°C | Homo sapiens | flavone | |
| 0.008 | - |
substrate androst-4-ene-3,17-dione, pH 7.2, 37°C | Homo sapiens | flavanone | |
| 0.01 | - |
substrate testosterone, pH 7.2, 37°C | Homo sapiens | quercetin | |
| 0.012 | - |
substrate androst-4-ene-3,17-dione, pH 7.2, 37°C | Homo sapiens | quercetin | |
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