Results 1 to 10 of about 132 (109)

Anticonvulsive properties of soticlestat, a novel cholesterol 24‐hydroxylase inhibitor [PDF]

Epilepsia, 2022
AbstractObjectiveThe formation of 24S‐hydroxycholesterol is a brain‐specific mechanism of cholesterol catabolism catalyzed by cholesterol 24‐hydroxylase (CYP46A1, also known as CH24H). CH24H has been implicated in various biological mechanisms, whereas pharmacological lowering of 24S‐hydroxycholesterol has not been fully studied. Soticlestat is a novel
Toshiya Nishi, Cameron S Metcalf, Shinji Fujimoto   +2 more
exaly   +16 more sources

Cholesterol 24-hydroxylase is a novel pharmacological target for anti-ictogenic and disease modification effects in epilepsy

Neurobiology of Disease, 2022
Therapies for epilepsy mainly provide symptomatic control of seizures since most of the available drugs do not target disease mechanisms. Moreover, about one-third of patients fail to achieve seizure control.
Alessia Salamone, Gaetano Terrone, Rossella Di Sapia, Silvia Balosso, Teresa Ravizza, Luca Beltrame, Ilaria Craparotta, Laura Mannarino, Sara Raimondi Cominesi, Massimo Rizzi, Alberto Pauletti, Sergio Marchini, Luca Porcu, Till S. Zimmer, Eleonora Aronica, Matthew During, Brett Abrahams, Shinichi Kondo, Toshiya Nishi, Annamaria Vezzani   +19 more
doaj   +6 more sources

The antifungal drug voriconazole is an efficient inhibitor of brain cholesterol 24S-hydroxylase in vitro and in vivo [PDF]

Journal of Lipid Research, 2010
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, Natalia Mast, Olof Beck, Rima Nayef, Gun Young Heo, Linda Björkhem-Bergman, Dieter Lütjohann, Ingemar Björkhem, Irina A. Pikuleva   +8 more
doaj   +3 more sources

The cholesterol 24-hydroxylase CYP46A1 promotes α-synuclein pathology in Parkinson's disease.

PLoS Biology
Parkinson's disease (PD) is a neurodegenerative disease characterized by the death of dopaminergic neurons in the substantia nigra and the formation of Lewy bodies that are composed of aggregated α-synuclein (α-Syn).
Lijun Dai, Jiannan Wang, Lanxia Meng, Xingyu Zhang, Tingting Xiao, Min Deng, Guiqin Chen, Jing Xiong, Wei Ke, Zhengyuan Hong, Lihong Bu, Zhentao Zhang   +11 more
doaj   +3 more sources

Characterization of soticlestat, a novel cholesterol 24-hydroxylase inhibitor, in acute and chronic neurodegeneration models

Neuroscience Research
We investigated whether soticlestat (TAK-935), a newly discovered cholesterol 24-hydroxylase (CH24H) inhibitor now in phase 3 clinical trials for Dravet and Lennox-Gastaut syndromes, has effects on neurodegeneration in both chronic and acute animal ...
Shigeo Hasegawa, Sayuri Watanabe, Shinji Fujimoto, Shinichi Kondo, Toshiya Nishi   +4 more
doaj   +3 more sources

Altered Cholesterol Homeostasis in Huntington’s Disease

Frontiers in Aging Neuroscience, 2022
Huntington’s disease (HD) is an autosomal dominant genetic disorder caused by an expansion of the CAG repeat in the first exon of Huntingtin’s gene.
Radhia Kacher, Radhia Kacher, Coline Mounier, Coline Mounier, Coline Mounier, Jocelyne Caboche, Jocelyne Caboche, Jocelyne Caboche, Sandrine Betuing, Sandrine Betuing, Sandrine Betuing   +10 more
doaj   +1 more source

Cholesterol 24-Hydroxylase: An Enzyme of Cholesterol Turnover in the Brain [PDF]

Annual Review of Biochemistry, 2009
Cholesterol 24-hydroxylase is a highly conserved cytochrome P450 that is responsible for the majority of cholesterol turnover in the vertebrate central nervous system. The enzyme is expressed in neurons, including hippocampal and cortical neurons that are important for learning and memory formation. Disruption of the cholesterol 24-hydroxylase gene in
David W, Russell, Rebekkah W, Halford, Denise M O, Ramirez, Rahul, Shah, Tiina, Kotti   +4 more
openaire   +2 more sources

Distribution of cholesterol 24-hydroxylase in the monkey brain [PDF]

Neuroscience Bulletin, 2010
Cholesterol 24-hydroxylase catalyzes the conversion of cholesterol to 24-hydroxycholesterol, which is a major pathway for cholesterol elimination from the brain, since 24-hydroxycholesterol can readily cross the blood brain barrier. The present study aimed to elucidate the distribution of cholesterol 24-hydroxylase in the monkey brain.The distribution ...
Xin, He, Wei-Yi, Ong, Qian, Hua
openaire   +2 more sources

cDNA cloning of cholesterol 24-hydroxylase, a mediator of cholesterol homeostasis in the brain [PDF]

Proceedings of the National Academy of Sciences, 1999
The turnover of cholesterol in the brain is thought to occur via conversion of excess cholesterol into 24S-hydroxycholesterol, an oxysterol that is readily secreted from the central nervous system into the plasma. To gain molecular insight into this pathway of cholesterol metabolism, we used expression cloning to isolate cDNAs that encode ...
E G, Lund, J M, Guileyardo, D W, Russell
openaire   +2 more sources

Cholesterol and ocular pathologies: focus on the role of cholesterol-24S-hydroxylase in cholesterol homeostasis [PDF]

OCL, 2015
The retina is responsible for coding the light stimulus into a nervous signal that is transferred to the brain via the optic nerve. The retina is formed by the association of the neurosensory retina and the retinal pigment epithelium that is supported by Bruch’s membrane.
Fourgeux, Cynthia, Martine, Lucy, Gambert-Nicot, Ségolène, Bron, Alain, Creuzot Garcher, Catherine, Brétillon, Lionel   +5 more
openaire   +5 more sources