Application | Comment | Organism |
---|---|---|
drug development | generation of imidazo[1,2-a]pyridine analogues that effectively inhibit cholesterol 24-hydroxylase (CYP46A1). They can be used for prophylactic treatment of neurodegenerative disorders, such as Alzheimer's disease and Parkinson's disease | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)[8-(1,3-oxazol-5-yl)-6-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methanone | - |
Homo sapiens | |
(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)[8-(1,3-oxazol-5-yl)-6-(trifluoromethyl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]methanone | - |
Homo sapiens | |
(4-benzyl-4-hydroxypiperidin-1-yl)([2,4'-bipyridin]-3-yl)methanone | - |
Homo sapiens | |
1-[3-(3-oxa-8-azabicyclo[3.2.1]octane-8-carbonyl)-6-(trifluoromethyl)imidazo[1,2-a]pyridin-8-yl]-4H-1,2,4-triazol-1-ium | - |
Homo sapiens | |
2-[5-methyl-1-(pyridine-4-carbonyl)-5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-3-yl]benzonitrile | - |
Homo sapiens | |
8-(1,3-oxazol-5-yl)-N-phenyl-6-(trifluoromethyl)imidazo[1,2-a]pyridine-3-carboxamide | - |
Homo sapiens | |
additional information | generation of a series of imidazo[1,2-a]pyridine analogues that effectively inhibit cholesterol 24-hydroxylase (CYP46A1), synthesis and evaluation, overview | Homo sapiens | |
N-benzyl-8-(1,3-oxazol-5-yl)-6-(trifluoromethyl)imidazo[1,2-a]pyridine-3-carboxamide | - |
Homo sapiens | |
voriconazole | - |
Homo sapiens | |
[6-cyclopropyl-8-(1,3-oxazol-5-yl)imidazo[1,2-a]pyridin-3-yl](3-oxa-8-azabicyclo[3.2.1]octan-8-yl)methanone | - |
Homo sapiens | |
[6-fluoro-8-(1,3-oxazol-5-yl)imidazo[1,2-a]pyridin-3-yl](3-oxa-8-azabicyclo[3.2.1]octan-8-yl)methanone | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
cholesterol + [reduced NADPH-hemoprotein reductase] + O2 | Homo sapiens | - |
(24S)-cholest-5-ene-3beta,24-diol + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9Y6A2 | gene CYP46A1 | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cholesterol + [reduced NADPH-hemoprotein reductase] + O2 | - |
Homo sapiens | (24S)-cholest-5-ene-3beta,24-diol + [oxidized NADPH-hemoprotein reductase] + H2O | - |
? |
Synonyms | Comment | Organism |
---|---|---|
CYP46A1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
malfunction | polymorphisms in the CYP46 gene and CYP46A1 enzyme dysfunction are involved in neurodegenerative disorders, such as Alzheimer's disease and Parkinson's disease. The 24(S)-hydroxycholesterol levels in cerebrospinal fluid are higher in patients with Alzheimer's disease compared to healthy control. CYP46A1 inhibition by voriconazole decreases 24S-hydroxycholesterol levels in the retina and affects cholesterol homeostasis and function in the retina | Homo sapiens |