Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H).

Animals Brain / drug effects Cholesterol 24-Hydroxylase / antagonists & inhibitors Crystallography, X-Ray Drug Stability Enzyme Inhibitors / chemical synthesis Female Humans Mice, Inbred C57BL Microsomes, Liver / metabolism Molecular Structure Piperidines / chemical synthesis Protein Binding Pyridines / chemical synthesis Structure-Activity Relationship

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
26 08 2021
Historique:
pubmed: 14 8 2021
medline: 16 11 2021
entrez: 13 8 2021
Statut: ppublish

Résumé

Cholesterol 24-hydroxylase (CH24H, CYP46A1), a brain-specific cytochrome P450 (CYP) family enzyme, plays a role in the homeostasis of brain cholesterol by converting cholesterol to 24

Identifiants

DOI: 10.1021/acs.jmedchem.1c00864 PMID: 34387987
pubmed: 34387987
doi: 10.1021/acs.jmedchem.1c00864
doi:

Substances chimiques

Enzyme Inhibitors 0
Piperidines 0
Pyridines 0
soticlestat 1766MU795L
Cholesterol 24-Hydroxylase EC 1.14.14.25

Types de publication

Journal Article Research Support, N.I.H., Extramural

Langues

eng

Sous-ensembles de citation

IM

Pagination

12228-12244

Subventions

Organisme : NIGMS NIH HHS
ID : P30 GM138396
Pays : United States

Auteurs

Tatsuki Koike (T)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
ORCID: 0000-0002-3264-1406

Masato Yoshikawa (M)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
ORCID: 0000-0002-7175-1173

Haruhi Kamisaki Ando (HK)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

William Farnaby (W)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Toshiya Nishi (T)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Etsurou Watanabe (E)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Jason Yano (J)

Takeda California Inc., 9625 Towne Centre Drive, San Diego, California 92121, United States.

Maki Miyamoto (M)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Shigeru Kondo (S)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Tsuyoshi Ishii (T)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

Takanobu Kuroita (T)

Research, Takeda Pharmaceutical Company Ltd., 26-1 Muraoka-Higashi, 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Hémoprotéines › Cytochromes › Cytochrome P-450 enzyme system › Steroid hydroxylases › Cholesterol 24-hydroxylase › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Techniques d'investigation › Techniques de chimie analytique › Cristallographie aux rayons X › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Techniques d'investigation › Stabilité de médicament › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée C57BL › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Microsomes › Microsomes du foie › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pipéridines › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyridines › Discovery of Soticlestat, a Potent and...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery of Soticlestat, a Potent and...