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Literature summary for 1.14.14.25 extracted from

  • Shafaati, M.; Mast, N.; Beck, O.; Nayef, R.; Heo, G.Y.; Bjoerkhem-Bergman, L.; Lutjohann, D.; Bjoerkhem, I.; Pikuleva, I.A.
    The antifungal drug voriconazole is an efficient inhibitor of brain cholesterol 24S-hydroxylase (CYP46A1) in vitro and in vivo (2010), J. Lipid Res., 51, 318-323.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
voriconazole binds with high affinity to CYP46A1 in vitro and efficiently inhibits CYP46A1-catalyzed cholesterol hydroxylations in the reconstituted system Homo sapiens
voriconazole voriconazole-induced visual disturbances related to an interaction between the drug and retinal CYP46A1 Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Homo sapiens
-
neural retina
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cholesterol + [reduced NADPH-hemoprotein reductase] + H+ + O2
-
Mus musculus (24S)-24-hydroxycholesterol + [oxidized NADPH-hemoprotein reductase] + H2O
-
?
cholesterol + [reduced NADPH-hemoprotein reductase] + H+ + O2
-
Homo sapiens (24S)-24-hydroxycholesterol + [oxidized NADPH-hemoprotein reductase] + H2O
-
?

Synonyms

Synonyms Comment Organism
cholesterol 24S-hydroxylase
-
Mus musculus
cholesterol 24S-hydroxylase
-
Homo sapiens
CYP46A1
-
Mus musculus
CYP46A1
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Mus musculus
NADPH
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000011
-
voriconazole
-
Homo sapiens

General Information

General Information Comment Organism
physiological function visual disturbances in CYP46A1 gene knockout mice Mus musculus