Zobrazeno 1 - 10
of 133
pro vyhledávání: '"Irina A, Pikuleva"'
Publikováno v:
Journal of Lipid Research, Vol 65, Iss 6, Pp 100555- (2024)
Cytochrome P450 46A1 (CYP46A1) is the CNS-specific cholesterol 24-hydroxylase that controls cholesterol elimination and turnover in the brain. In mouse models, pharmacologic CYP46A1 activation with low-dose efavirenz or by gene therapy mitigates the
Externí odkaz:
https://doaj.org/article/c33367ff731c493e950729642ca5ebf6
Publikováno v:
International Journal of Molecular Sciences, Vol 25, Iss 4, p 2242 (2024)
High dose (S)-efavirenz (EFV) inhibits the HIV reverse transcriptase enzyme and is used to lower HIV load. Low-dose EFV allosterically activates CYP46A1, the key enzyme for cholesterol elimination from the brain, and is investigated as a potential tr
Externí odkaz:
https://doaj.org/article/0e025f04b49b4cb1915f39df4ec6ebca
Autor:
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
Publikováno v:
Alzheimer’s Research & Therapy, Vol 14, Iss 1, Pp 1-10 (2022)
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 efavi
Externí odkaz:
https://doaj.org/article/be51f0c921904c6eb9b8ba7aa6a50ed7
Publikováno v:
Journal of Lipid Research, Vol 64, Iss 7, Pp 100401- (2023)
The retina and brain are separated from the systemic circulation by the anatomical barriers, which are permeable (the outer blood-retinal barrier) and impermeable (the blood-brain and inner blood-retina barriers) to cholesterol. Herein we investigate
Externí odkaz:
https://doaj.org/article/5dec79429d9b43af9231e30c0cf209b6
Autor:
Nicole El-Darzi, Natalia Mast, Sandra S. Hammer, Tim F. Dorweiler, Julia V. Busik, Irina A. Pikuleva
Publikováno v:
Journal of Lipid Research, Vol 64, Iss 2, Pp 100323- (2023)
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. 2-Hydroxypropyl-β-cyclodextrin (HPCD), a Food and Drug Admi
Externí odkaz:
https://doaj.org/article/416b987dee114e0eaef22c32059e6f1f
Autor:
Irina A. Pikuleva
Publikováno v:
Exploration of Neuroprotective Therapy, Vol 1, Iss 3, Pp 159-172 (2021)
The brain cholesterol content is determined by the balance between the pathways of in situ biosynthesis and cholesterol elimination via 24-hydroxylation catalyzed by cytochrome P450 46A1 (CYP46A1). Both pathways are tightly coupled and determine the
Externí odkaz:
https://doaj.org/article/d673606794db4f0683a86efd1eb387ca
Autor:
Nicole El-Darzi, Natalia Mast, David A. Buchner, Aicha Saadane, Brian Dailey, Georgios Trichonas, Irina A. Pikuleva
Publikováno v:
Frontiers in Pharmacology, Vol 13 (2022)
A small dose of the anti-HIV drug efavirenz (EFV) was previously discovered to activate CYP46A1, a cholesterol-eliminating enzyme in the brain, and mitigate some of the manifestation of Alzheimer’s disease in 5XFAD mice. Herein, we investigated the
Externí odkaz:
https://doaj.org/article/ed746dc3793c44e1a259e662f90f526e
Publikováno v:
Frontiers in Aging Neuroscience, Vol 14 (2022)
Externí odkaz:
https://doaj.org/article/eb9e020a4e4e469a981b8dbd84c50e4d
Autor:
Irina A. Pikuleva, Nathalie Cartier
Publikováno v:
Frontiers in Aging Neuroscience, Vol 13 (2021)
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
Externí odkaz:
https://doaj.org/article/782f336f32774b2d824aeea6c27b3843
Publikováno v:
International Journal of Molecular Sciences, Vol 23, Iss 14, p 7669 (2022)
Efavirenz (EFV), an FDA-approved anti-HIV drug, has off-target binding to CYP46A1, the CNS enzyme which converts cholesterol to 24-hydroxycholesterol. At small doses, EFV allosterically activates CYP46A1 in mice and humans and mitigates some of the A
Externí odkaz:
https://doaj.org/article/9f42264c85ff4d2eb13d6d7f59d56007