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Literature summary extracted from

  • Njar, V.C.; Kato, K.; Nnane, I.P.; Grigoryev, D.N.; Long, B.J.; Brodie, A.M.
    Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17alpha-hydroxylase-C17,20-lyase (P450(17)alpha): potential agents for the treatment of prostate cancer (1998), J. Med. Chem., 41, 902-912.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
1.14.14.19 cytochrome b5
-
Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.19 17-(1H-1,2,3-triazol-1-yl)androsta-4,16-dien-3-one at 19 nM 50% inhibition, also potent inhibitor of 5alpha-reductase Homo sapiens
1.14.14.19 17-(1H-1,2,3-triazol-1-yl)androsta-4,16-dien-3-one at 9 nM 50% inhibition Rattus norvegicus
1.14.14.19 17-(1H-1,2,4-triazol-1-yl)androsta-4,16-dien-3-one at 55 nM 50% inhibition, also potent inhibitor of 5alpha-reductase Homo sapiens
1.14.14.19 17-(1H-1,2,4-triazol-1-yl)androsta-4,16-dien-3-one at 11 nM 50% inhibition Rattus norvegicus
1.14.14.19 17-(1H-imidazol-1-yl)androsta-4,16-dien-3-one at 7 nM 50% inhibition, also potent inhibitor of 5alpha-reductase Homo sapiens
1.14.14.19 17-(1H-imidazol-1-yl)androsta-4,16-dien-3-one at 8 nM 50% inhibition Rattus norvegicus
1.14.14.19 3beta-hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene at 150 nM 94% inhibition Homo sapiens
1.14.14.19 3beta-hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene at 10 nM 50% inhibition Rattus norvegicus
1.14.14.19 3beta-hydroxy-17-(1H-1,2,4-triazol-1-yl)androsta-5,16-diene at 150 nM 60% inhibition Homo sapiens
1.14.14.19 3beta-hydroxy-17-(1H-1,2,4-triazol-1-yl)androsta-5,16-diene at 26 nM 50% inhibition Rattus norvegicus
1.14.14.19 3beta-hydroxy-17-(1H-imidazol-1-yl)androsta-5,16-diene at 150 nM 97% inhibition Homo sapiens
1.14.14.19 3beta-hydroxy-17-(1H-imidazol-1-yl)androsta-5,16-diene at 9 nM 50% inhibition Rattus norvegicus
1.14.14.19 ketoconazole at 150 nM 67% inhibition Homo sapiens
1.14.14.19 ketoconazole
-
Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.14.14.19 0.00056
-
17-hydroxypregnenolone
-
Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.14.19 microsome
-
Homo sapiens
-
-
1.14.14.19 microsome
-
Rattus norvegicus
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.14.14.19 Fe3+
-
Homo sapiens
1.14.14.19 Fe3+
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.14.19 additional information Homo sapiens it catalyzes steroid 17alpha-hydroxylase and 17,20-lyase activities in the biosynthesis of androgens, estrogens and cortisol ?
-
?
1.14.14.19 additional information Rattus norvegicus it catalyzes steroid 17alpha-hydroxylase and 17,20-lyase activities in the biosynthesis of androgens, estrogens and cortisol ?
-
?
1.14.14.19 pregnenolone + AH2 + O2 Rattus norvegicus
-
17alpha-hydroxypregnenolone + A + H2O
-
?
1.14.14.19 pregnenolone + AH2 + O2 Homo sapiens
-
17alpha-hydroxypregnenolone + A + H2O cytochrome b5 also as cofactor ?

Organism

EC Number Organism UniProt Comment Textmining
1.14.14.19 Homo sapiens
-
-
-
1.14.14.19 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.14.19 testis
-
Homo sapiens
-
1.14.14.19 testis
-
Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.19 additional information it catalyzes steroid 17alpha-hydroxylase and 17,20-lyase activities in the biosynthesis of androgens, estrogens and cortisol Homo sapiens ?
-
?
1.14.14.19 additional information it catalyzes steroid 17alpha-hydroxylase and 17,20-lyase activities in the biosynthesis of androgens, estrogens and cortisol Rattus norvegicus ?
-
?
1.14.14.19 pregnenolone + AH2 + O2
-
Rattus norvegicus 17alpha-hydroxypregnenolone + A + H2O
-
?
1.14.14.19 pregnenolone + AH2 + O2
-
Homo sapiens 17alpha-hydroxypregnenolone + A + H2O cytochrome b5 also as cofactor ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.14.14.19 0.0000012
-
3beta-hydroxy-17-(1H-imidazol-1-yl)androsta-5,16-diene noncompetitive inhibitor Homo sapiens
1.14.14.19 0.0000014
-
3beta-hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene noncompetitive inhibitor Homo sapiens
1.14.14.19 0.0000019
-
17-(1H-imidazol-1-yl)androsta-4,16-dien-3-one noncompetitive inhibitor Homo sapiens
1.14.14.19 0.000023
-
3beta-hydroxy-17-(1H-1,2,4-triazol-1-yl)androsta-5,16-diene noncompetitive inhibitor Homo sapiens
1.14.14.19 0.000041
-
17-(1H-1,2,4-triazol-1-yl)androsta-4,16-dien-3-one noncompetitive inhibitor Homo sapiens
1.14.14.19 0.00008
-
17-(1H-1,2,3-triazol-1-yl)androsta-4,16-dien-3-one noncompetitive inhibitor Homo sapiens