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Literature summary for 1.14.15.4 extracted from

  • Davioud, E.; Piffeteau, A.; Delorme, C.; Coustal, S.; Marquet, A.
    18-Vinyldeoxycorticosterone: a potent inhibitor of the bovine cytochrome P-45011beta (1998), Bioorg. Med. Chem., 6, 1781-1788.
    View publication on PubMed

Application

Application Comment Organism
medicine inhibitors for P-45011beta, against aldosterone overproduction which leads to oedematous diseases and hypertension Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
18-ethynylprogesterone suicide-substrate of aldosterone biosythesis, inhibits more strongly the 18-hydroxylation step Bos taurus
18-vinyldeoxycorticosterone deoxycorticosterone analog, very strong and reversible inhibitor for deoxycorticosterone and corticosterone oxidation, 0.001 mM leads to decrease in corticosterone production with 30% of total activity after 1 min, 100fold more efficient than 18-vinylprogesterone for inhibition of 11beta-hydroxylation step, only 6fold of more inhibition of 18-hydroxylation step Bos taurus
18-vinylprogesterone with 0.001 mM no inhibition detectable, with 0.01 mM 23% decrease in corticosterone production, better suicide-substrate of aldosterone biosythesis than 18-ethynylprogesterone, inhibits more strongly the 18-hydroxylation step Bos taurus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00197
-
11-deoxycorticosterone +/-0.00026 Bos taurus
0.0059
-
corticosterone +/-0.00018 Bos taurus

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
Bos taurus 5739
-

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
copurification of P-450 11beta-2 and 11beta-3, ammonium sulfate precipitation, octyl-Sepharose, separation of 2 isoforms by hydroxyapatite column connected to an FPLC system Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
adrenal cortex
-
Bos taurus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
11-deoxycorticosterone + reduced adrenal ferredoxin + O2 11beta-hydroxylation Bos taurus corticosterone + oxidized adrenal ferredoxin + H2O
-
?
corticosterone + reduced adrenal ferredoxin + O2 18-hydroxylation Bos taurus aldosterone + oxidized adrenal ferredoxin + H2O
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Bos taurus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Bos taurus

Cofactor

Cofactor Comment Organism Structure
NADPH adrenodoxin and NADPH-linked adrenodoxin reductase Bos taurus