Inhibitors | Comment | Organism | Structure |
---|---|---|---|
17(E)-picolinyliden-androst-4-en-3beta-ol | - |
Rattus norvegicus | |
17(E)-picolinyliden-androst-5-en-3beta-ol | - |
Rattus norvegicus | |
abiraterone | - |
Rattus norvegicus | |
ketoconazole | - |
Rattus norvegicus | |
additional information | picolyl derivatives exert no significant inhibition either on the 17alpha-hydroxylase or the C17,20-lyase activities | Rattus norvegicus |
Organic Solvent | Comment | Organism |
---|---|---|
dimethyl sulfoxide | 5% v/v, no significant reduction of activity | Rattus norvegicus |
propylene glycol | 3% v/v, no significant reduction of activity | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
testis | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
17alpha-hydroxyprogesterone + [reduced NADPH-hemoprotein reductase] + O2 | - |
Rattus norvegicus | androstenedione + acetate + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? | |
17alpha-picolyl-androst-4-en-3beta,17beta-diol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Rattus norvegicus | ? + acetate + [oxidized NADPH-hemoprotein reductase] + H2O | 66% conversion in 17,20-lyase reaction | ? | |
17beta-hydroxy-17alpha-picolyl-androst-4-en-3-one + [reduced NADPH-hemoprotein reductase] + O2 | - |
Rattus norvegicus | ? + acetate + [oxidized NADPH-hemoprotein reductase] + H2O | 73% conversion in 17,20-lyase reaction | ? | |
additional information | the enzyme catalyses two independent reactions at the same active site, the 17-hydroxylation of pregnenolone and progesterone (reaction of EC 1.14.14.19), and the conversion of the 17-hydroxylated products via a 17,20-lyase reaction. The C17,20-lyase reaction is rate limiting, and 525% of the 17OH-progesterone product is converted to 4-en-dione | Rattus norvegicus | ? | - |
? |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000012 | - |
C17,20-lyase activity, pH 7.3, 37°C | Rattus norvegicus | abiraterone | |
0.00032 | - |
C17,20-lyase activity, pH 7.3, 37°C | Rattus norvegicus | ketoconazole | |
0.0082 | - |
C17,20-lyase activity, pH 7.3, 37°C | Rattus norvegicus | 17(E)-picolinyliden-androst-5-en-3beta-ol | |
0.014 | - |
C17,20-lyase activity, pH 7.3, 37°C | Rattus norvegicus | 17(E)-picolinyliden-androst-4-en-3beta-ol |