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Literature summary for 1.14.14.19 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-3-one complete inhibition at 0.05 mM Rattus norvegicus
17(E)-picolinyliden-androst-4-en-3beta-ol 52% inhibition at 0.05 mM Rattus norvegicus
17(E)-picolinyliden-androst-5-en-3beta-ol 55% inhibition at 0.05 mM Rattus norvegicus
17alpha-picolyl-androst-4-en-3beta,17beta-diol 10% inhibition at 0.05 mM Rattus norvegicus
17alpha-picolyl-androst-5-en-3beta,17beta-diol 5% inhibition at 0.05 mM Rattus norvegicus
17beta-hydroxy-17alpha-picolyl-androst-4-en-3-one 13% inhibition at 0.05 mM Rattus norvegicus
abiraterone
-
 Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
pregnenolone + [reduced NADPH-hemoprotein reductase] + O2 Rattus norvegicus
-
 17alpha-hydroxypregnenolone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
progesterone + [reduced NADPH-hemoprotein reductase] + O2 Rattus norvegicus
-
 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

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.
pregnenolone + [reduced NADPH-hemoprotein reductase] + O2
-
 Rattus norvegicus 17alpha-hydroxypregnenolone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
progesterone + [reduced NADPH-hemoprotein reductase] + O2
-
 Rattus norvegicus 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

Synonyms

Synonyms Comment Organism
17alpha-hydroxylase-C17,20-lyase
-
 Rattus norvegicus
P45017alpha
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0059
-
 at pH 7.3 and 37°C Rattus norvegicus 17(E)-picolinyliden-androst-4-en-3-one
0.038
-
 at pH 7.3 and 37°C Rattus norvegicus 17(E)-picolinyliden-androst-5-en-3beta-ol
0.048
-
 at pH 7.3 and 37°C Rattus norvegicus 17(E)-picolinyliden-androst-4-en-3beta-ol