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Literature summary 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

EC Number Application Comment Organism
1.14.15.4 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)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.15.4 (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)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.15.4 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

EC Number Organism UniProt Comment Textmining
1.14.15.4 Homo sapiens P15538
-
-
1.14.15.4 Homo sapiens P19099
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.15.4 adrenal gland
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.15.4 11-deoxycorticosterone + reduced adrenal ferredoxin + O2
-
 Homo sapiens ?
-
 ?
1.14.15.4 11-deoxycortisol + reduced adrenal ferredoxin + O2 CYP11B1 Homo sapiens cortisol + oxidized adrenal ferredoxin + H2O
-
 ?
1.14.15.4 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

EC Number Synonyms Comment Organism
1.14.15.4 Aldosterone synthase
-
 Homo sapiens
1.14.15.4 CYP11B1
-
 Homo sapiens
1.14.15.4 CYP11B2
-
 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.14.15.4 7.4
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.14.15.4 0.0000008
-
 (R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile competitive inhibition, pH 7.4 Homo sapiens
1.14.15.4 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

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.15.4 0.0000016
-
 competitive inhibition, pH 7.4 Homo sapiens (R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile
1.14.15.4 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