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Literature summary for 1.14.14.19 extracted from

  • Hartmann, R.W.; Hector, M.; Haidar, S.; Ehmer, P.B.; Reichert, W.; Jose, J.
    Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17alpha-hydroxylase/C17-20-lyase) and 5alpha-reductase types 1 and 2 (2000), J. Med. Chem., 43, 4266-4277.
    View publication on PubMed

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

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli XL1 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
20-hydroxyiminopregna-4,14,16-trien-3-one at 0.0002 mM 50% inhibition Homo sapiens
20-hydroxyiminopregna-4,16-dien-3-one at 0.0001 mM 50% inhibition Homo sapiens
20-hydroxyiminopregna-5,14,16-trien-3beta-ol at 0.0002 mM 50% inhibition Homo sapiens
20-hydroxyiminopregna-5,16-dien-3beta-ol at 0.00017 mM 50% inhibition Homo sapiens
21-hydroxyimino-21-methylpregn-4-en-3-one at 0.0036 mM 50% inhibition Rattus norvegicus
21-hydroxyiminopregn-4-en-3-one at 0.0003 mM 50% inhibition, also 5alpha-reductase inhibitor Homo sapiens
21-hydroxyiminopregn-4-en-3-one at 0.0003 mM 50% inhibition, also 5alpha-reductase inhibitor Rattus norvegicus
21-hydroxyiminopregn-5-en-3beta-ol at 0.00027 mM 50% inhibition Homo sapiens
21-hydroxyiminopregn-5-en-3beta-ol at 0.00276 mM 50% inhibition Rattus norvegicus
21-hydroxyiminopregna-4,17(20)-dien-3-one at 0.00018 mM 50% inhibition, also 5alpha-reductase inhibitor Homo sapiens
21-hydroxyiminopregna-4,17(20)-dien-3-one at 0.00014 mM 50% inhibition Rattus norvegicus
21-hydroxyiminopregna-5,17(29)-dien-3beta-ol at 0.000077 mM 50% inhibition Homo sapiens
21-hydroxyiminopregna-5,17(29)-dien-3beta-ol at 0.00052 mM 50% inhibition Rattus norvegicus
21-methylpregn-5-en-3beta-ol-21-one at 0.0098 mM 50% inhibition Rattus norvegicus

Localization

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
Homo sapiens
-
testis
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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 ?

Synonyms

Synonyms Comment Organism
CYP 17
-
Homo sapiens
P450 17
-
Homo sapiens
P450 17
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens
NADPH
-
Rattus norvegicus