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Cholesterol Hydroxylating Cytochrome P450 46A1: From Mechanisms of Action to Clinical Applications
Cholesterol, an essential component of the brain, and its local metabolism are involved in many neurodegenerative diseases. The blood-brain barrier is impermeable to cholesterol; hence, cholesterol homeostasis in the central nervous system represents a ...
Irina A. Pikuleva, Nathalie Cartier
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The manipulation of cholesterol and its metabolites has been hypothesized to be therapeutically beneficial for mood disorders, neurodegenerative disorders, and epilepsies.
Michael Popiolek +7 more
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Polymorphism of the cholesterol-24S-hydroxylase (CYP46A1) gene is thought to be a risk factor for Alzheimer’s disease (AD). A single nucleotide polymorphism (T/C) in intron 2, rs754203, has been confirmed to be implicated in AD.
Yang Chen +9 more
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Objective Compromised brain cholesterol turnover and altered regulation of brain cholesterol metabolism have been allied with some neurodegenerative diseases, including Huntington’s disease (HD). Following our previous studies in HD, in this study we aim
Clévio Nóbrega +12 more
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BackgroundAbnormal cholesterol metabolism is common in type 2 diabetes mellitus (T2DM) and causes dementia. Cholesterol 24S-hydroxylase (CYP46A1) converts cholesterol into 24S-hydroxycholesterol (24-OHC) and maintains cholesterol homeostasis in the brain.
Jijing Shi +14 more
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Identification of the regulatory mechanisms and factors involved in the brain-specific expression of CYP46A1 [PDF]
Tese de doutoramento, Farmácia (Biologia Celular e Molecular), Universidade de Lisboa, Faculdade de Farmácia, 2011Cholesterol has a crucial role in central nervous system physiology and cell signaling, and many studies correlate alterations in brain ...
Silva, Inês Milagre da, 1980-
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In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds
Cytochrome P450 46A1 (CYP46A1) is a central nervous system-specific enzyme, which catalyzes cholesterol 24-hydroxylation. Currently CYP46A1 is being evaluated in a clinical trial for activation by small doses of the anti-HIV drug efavirenz.
Irina A. Pikuleva (163019) +4 more
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Tese de doutoramento, Farmácia (Biologia Celular e Molecular), Universidade de Lisboa, Faculdade de Farmácia, 2016Cholesterol is an essential molecule in central nervous system physiology and cell signalling, with a wide range of roles, such as being an ...
Moutinho, Miguel Alves da Silva de Carvalho, 1986-
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CYP46A1 is a CNS-specific enzyme, which eliminates cholesterol from the brain and retina by metabolism to 24-hydroxycholesterol, thus contributing to cholesterol homeostasis in both organs.
Nicole El-Darzi +5 more
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Cholesterol 24S-hydroxylase (CYP46A1) is of key importance for cholesterol homeostasis in the brain. This enzyme seems to be resistant toward most regulatory factors and at present no drug effects on its activity have been described.
Marjan Shafaati +8 more
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