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Literature summary for 1.14.14.32 extracted from

  • Szabo, N.; Ajdukovic, J.J.; Djurendic, E.A.; Sakac, M.N.; Ignath, I.; Gardi, J.; Mahmoud, G.; Klisuric, O.R.; Jovanovic-Santa, S.; Penov Gasi, K.M.; Szecsi, M.
    Determination of 17alpha-hydroxylase-C17,20-lyase (P45017alpha) enzyme activities and their inhibition by selected steroidal picolyl and picolinylidene compounds (2015), Acta Biol. Hung., 66, 41-51.
    View publication on PubMed
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Inhibitors

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 Stability

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

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

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 5–25% of the 17OH-progesterone product is converted to 4-en-dione Rattus norvegicus ?
-
 ?

IC50 Value

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