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Literature summary for 1.14.15.4 extracted from

  • LaSala, D.; Shibanaka, Y.; Jeng, A.Y.
    Coexpression of CYP11B2 or CYP11B1 with adrenodoxin and adrenodoxin reductase for assessing the potency and selectivity of aldosterone synthase inhibitors (2009), Anal. Biochem., 394, 56-61.
    View publication on PubMed

Application

Application Comment Organism
additional information assays can be used for assessing the potency and selectivity of CYP11B2 inhibitors for the treatment of hypertension and heart failure Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
overexpressed in V79-4 Chinese hamster lung cell line Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile FAD286; FAD286, CYP11B2 inhibitor, inhibited CYP11B2 and CYP11B1 activities Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens enzyme is responsible for the final step of aldosterone synthesis. It requires electron transfer from the adrenodoxin/adrenodoxin reductase system to catalyze the production of aldosterone ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P15538
-
-
Homo sapiens P19099
-
-

Source Tissue

Source Tissue Comment Organism Textmining
adrenal gland
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
11-deoxycorticosterone + reduced adrenal ferredoxin + O2
-
Homo sapiens ?
-
?
11-deoxycortisol + reduced adrenal ferredoxin + O2 CYP11B1 Homo sapiens cortisol + oxidized adrenal ferredoxin + H2O
-
?
additional information enzyme is responsible for the final step of aldosterone synthesis. It requires electron transfer from the adrenodoxin/adrenodoxin reductase system to catalyze the production of aldosterone Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Aldosterone synthase
-
Homo sapiens
CYP11B1
-
Homo sapiens
CYP11B2
-
Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000008
-
(R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile competitive inhibition, pH 7.4 Homo sapiens
0.0000022
-
(R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile competitive inhibition, pH 7.4, 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000016
-
competitive inhibition, pH 7.4 Homo sapiens (R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile
0.0000099
-
competitive inhibition, pH 7.4, 25°C Homo sapiens (R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile