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Literature summary for 1.14.14.19 extracted from
- Inhibitors of 17alpha-hydroxylase/17,20-lyase (CYP17): potential agents for the treatment of prostate cancer (1999), Curr. Pharm. Des., 5, 163-180.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | inhibition of steroid 17alpha-monooxygenase is an important therapeutic strategy in order to inhibit tumor growth in prostate cancer | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 17-(1H-imidazol-1-yl)androsta-4,16-dien-3-one | - |
Homo sapiens |  |
| 17-(1H-imidazol-1-yl)androsta-4,16-dien-3-one | - |
Rattus norvegicus | |
| 17-(2-amino-4-thiazolyl)-androsta-5,16-dien-3beta-ol | type II competitive inhibitor | Macacine alphaherpesvirus 1 | |
| 17-(3'-pyrazolyl)androsta-4,16-dien-3beta-one | type II competitive inhibitor | Homo sapiens | |
| 17-(3'-pyrazolyl)androsta-4,16-dien-3beta-one | type II competitive inhibitor | Rattus norvegicus | |
| 17-(3'-pyrazolyl)androsta-5,16-dien-3beta-ol | type II competitive inhibitor | Homo sapiens | |
| 17-(3'-pyrazolyl)androsta-5,16-dien-3beta-ol | type II competitive inhibitor | Rattus norvegicus | |
| 17-(3-pyridyl)androsta-5,6-dien-3beta-ol | - |
Homo sapiens | |
| 17-(5'-isooxazoloyl)androsta-4,16-dien-3-one | type II competitive inhibitor | Homo sapiens | |
| 17-(5'-isooxazoloyl)androsta-4,16-dien-3-one | type II competitive inhibitor | Rattus norvegicus | |
| 17-(methylthio)androst-5-en-3beta-ol S-oxide | type I competitive inhibitor | Sus scrofa | |
| 17beta-acetamidoandrost-4-en-3-one | - |
Homo sapiens | |
| 17beta-ureidoandrosta-1,4-dien-3-one | - |
Homo sapiens | |
| 2-(1H-imidazol-4-ylmethyl)-9H-carbazole | suicide inhibitor | Rattus norvegicus | |
| 20(S)-20,21-aziridinylpregn-5-en-3beta-ol | type II competitive inhibitor | Rattus norvegicus | |
| 20xi-hydroxy-21-trifluoropregn-4-en-3-one | type I competitive inhibitor | Rattus norvegicus | |
| 3-pyridyl-1a,2,3,7b-tetrahydro-1H-cyclopropa[a]naphthalene | suicide inhibitor | Rattus norvegicus | |
| 3beta-hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene | type II competitive inhibitor | Homo sapiens | |
| 3beta-hydroxy-17-(1H-imidazol-1-yl)androsta-5,16-diene | type II competitive inhibitor | Homo sapiens | |
| 4-amino-17beta-(cyclopropylamino)-androst-4-en-3-one | suicide inhibitor | Macacine alphaherpesvirus 1 | |
| 4-amino-17beta-(cyclopropyloxy)-androst-4,6-dien-3-one | suicide inhibitor | Macacine alphaherpesvirus 1 | |
| 4-amino-17beta-(cyclopropyloxy)-androst-4-en-3-one | suicide inhibitor | Macacine alphaherpesvirus 1 | |
| 5-[(3-chlorophenyl-1H-imidazole-1-yl)methyl]-1H-benzimidazole | suicide inhibitor | Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| pregnenolone + AH2 + O2 | Homo sapiens | - |
17alpha-hydroxypregnenolone + A + H2O | - |
? | |
| pregnenolone + AH2 + O2 | Rattus norvegicus | - |
17alpha-hydroxypregnenolone + A + H2O | - |
? | |
| pregnenolone + AH2 + O2 | Sus scrofa | - |
17alpha-hydroxypregnenolone + A + H2O | - |
? | |
| progesterone + [reduced NADPH-hemoprotein reductase] + O2 | Homo sapiens | - |
17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O | product eliminates at C20,21 acetate to yield androstenedione | ? | |
| progesterone + [reduced NADPH-hemoprotein reductase] + O2 | Rattus norvegicus | - |
17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O | product eliminates at C20,21 acetate to yield androstenedione | ? | |
| progesterone + [reduced NADPH-hemoprotein reductase] + O2 | Sus scrofa | - |
17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O | product eliminates at C20,21 acetate to yield androstenedione | ? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Macacine alphaherpesvirus 1 | - |
cynomolgus monkey | - |
| Rattus norvegicus | - |
- |
- |
| Sus scrofa | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| testis | - |
Rattus norvegicus | - |
| testis | - |
Sus scrofa | - |
| testis | adult and foetal | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| pregnenolone + AH2 + O2 | - |
Homo sapiens | 17alpha-hydroxypregnenolone + A + H2O | - |
? | |
| pregnenolone + AH2 + O2 | - |
Rattus norvegicus | 17alpha-hydroxypregnenolone + A + H2O | - |
? | |
| pregnenolone + AH2 + O2 | - |
Sus scrofa | 17alpha-hydroxypregnenolone + A + H2O | - |
? | |
| progesterone + [reduced NADPH-hemoprotein reductase] + O2 | - |
Homo sapiens | 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O | product eliminates at C20,21 acetate to yield androstenedione | ? | |
| progesterone + [reduced NADPH-hemoprotein reductase] + O2 | - |
Rattus norvegicus | 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O | product eliminates at C20,21 acetate to yield androstenedione | ? | |
| progesterone + [reduced NADPH-hemoprotein reductase] + O2 | - |
Sus scrofa | 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O | product eliminates at C20,21 acetate to yield androstenedione | ? | |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 34 | - |
- |
Homo sapiens |
| 34 | - |
- |
Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| NADPH | - |
Homo sapiens | |
| NADPH | - |
Rattus norvegicus | |
| NADPH | - |
Sus scrofa | |
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