Cholesterol hydroxylating cytochrome P450 46A1: from mechanisms of action to clinical applications

IA Pikuleva, N Cartier - Frontiers in Aging Neuroscience, 2021 - frontiersin.org
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; …

Efavirenz: history, development and future

B Costa, N Vale - Biomolecules, 2022 - mdpi.com
Efavirenz (Sustiva®) is a first-generation non-nucleoside reverse transcriptase inhibitor
(NNRTI) used to treat human immunodeficiency virus (HIV) type 1 infection or to prevent the …

Prion therapeutics: Lessons from the past

KH Shim, N Sharma, SSA An - Prion, 2022 - Taylor & Francis
Prion diseases are a group of incurable zoonotic neurodegenerative diseases (NDDs) in
humans and other animals caused by the prion proteins. The abnormal folding and …

Peptide aptamer targeting Aβ–PrP–Fyn axis reduces Alzheimer's disease pathologies in 5XFAD transgenic mouse model

T Ali, AN Klein, A Vu, MI Arifin, S Hannaoui… - Cellular and Molecular …, 2023 - Springer
Currently, no effective therapeutics exist for the treatment of incurable neurodegenerative
diseases such as Alzheimer's disease (AD). The cellular prion protein (PrPC) acts as a high …

The normalizing effects of the CYP46A1 activator efavirenz on retinal sterol levels and risk factors for glaucoma in Apoj−/− mice

N El-Darzi, N Mast, Y Li, B Dailey, M Kang… - Cellular and Molecular …, 2023 - Springer
Apolipoprotein J (APOJ) is a multifunctional protein with genetic evidence suggesting an
association between APOJ polymorphisms and Alzheimer's disease as well as exfoliation …

Cellulose ether treatment inhibits amyloid beta aggregation, neuroinflammation and cognitive deficits in transgenic mouse model of Alzheimer's disease

T Ali, AN Klein, K McDonald, L Johansson… - Journal of …, 2023 - Springer
Alzheimer's disease (AD) is an incurable, progressive and devastating neurodegenerative
disease. Pathogenesis of AD is associated with the aggregation and accumulation of …

[HTML][HTML] Targeting cytochrome P450 46A1 and brain cholesterol 24-hydroxylation to treat neurodegenerative diseases

IA Pikuleva - Exploration of neuroprotective therapy, 2021 - ncbi.nlm.nih.gov
The brain cholesterol content is determined by the balance between the pathways of in situ
biosynthesis and cholesterol elimination via 24-hydroxylation catalyzed by CYP46A1 …

Low-dose anti-HIV drug efavirenz mitigates retinal vascular lesions in a mouse model of Alzheimer's disease

N El-Darzi, N Mast, DA Buchner, A Saadane… - Frontiers in …, 2022 - frontiersin.org
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 …

What is the role of lipids in prion conversion and disease?

C Alves Conceição, G Assis de Lemos… - Frontiers in Molecular …, 2023 - frontiersin.org
The molecular cause of transmissible spongiform encephalopathies (TSEs) involves the
conversion of the cellular prion protein (PrPC) into its pathogenic form, called prion scrapie …

Synthesis and anti-prion aggregation activity of acylthiosemicarbazide analogues

DH Kim, J Kim, H Lee, D Lee, SM Im… - Journal of enzyme …, 2023 - Taylor & Francis
Prions are infectious protein particles known to cause prion diseases. The biochemical entity
of the pathogen is the misfolded prion protein (PrPSc) that forms insoluble amyloids to …