CYP46A1 activation by low-dose efavirenz enhances brain cholesterol metabolism in subjects with early Alzheimer’s disease
Abstract Background Efavirenz is an anti-HIV drug, and cytochrome P450 46A1 (CYP46A1) is a CNS-specific enzyme that metabolizes cholesterol to 24-hydroxycholesterol (24HC). We have previously shown that allosteric CYP46A1 activation by low-dose efavirenz in a transgenic mouse model of Alzheimer’s di...
Main Authors: | Alan J. Lerner, Steven E. Arnold, Erin Maxfield, Aaron Koenig, Maria E. Toth, Brooke Fortin, Natalia Mast, Bianca A. Trombetta, John Denker, Andrew A. Pieper, Curtis Tatsuoka, Sangeetha Raghupathy, Irina A. Pikuleva |
---|---|
Format: | Article |
Language: | English |
Published: |
BMC
2022-12-01
|
Series: | Alzheimer’s Research & Therapy |
Subjects: | |
Online Access: | https://doi.org/10.1186/s13195-022-01151-z |
Similar Items
-
7,8-Dihydroxy Efavirenz Is Not as Effective in CYP46A1 Activation In Vivo as Efavirenz or Its 8,14-Dihydroxy Metabolite
by: Natalia Mast, et al.
Published: (2024-02-01) -
Increased Acetylcholine Levels and Other Brain Effects in 5XFAD Mice after Treatment with 8,14-Dihydroxy Metabolite of Efavirenz
by: Natalia Mast, et al.
Published: (2022-07-01) -
Low-Dose Anti-HIV Drug Efavirenz Mitigates Retinal Vascular Lesions in a Mouse Model of Alzheimer’s Disease
by: Nicole El-Darzi, et al.
Published: (2022-06-01) -
Cholesterol Hydroxylating Cytochrome P450 46A1: From Mechanisms of Action to Clinical Applications
by: Irina A. Pikuleva, et al.
Published: (2021-07-01) -
Effects of CYP46A1 Inhibition on Long-Term-Depression in Hippocampal Slices ex vivo and 24S-Hydroxycholesterol Levels in Mice in vivo
by: Michael Popiolek, et al.
Published: (2020-10-01)