Stereoisomers of Schisandrin B Are Potent ATP Competitive GSK-3β Inhibitors with Neuroprotective Effects against Alzheimer's Disease: Stereochemistry and Biological Activity.
Adenosine Triphosphate
/ metabolism
Alzheimer Disease
/ enzymology
Animals
Cell Line, Tumor
Cell Survival
/ drug effects
Cyclooctanes
/ isolation & purification
Enzyme Inhibitors
/ isolation & purification
Glycogen Synthase Kinase 3 beta
/ antagonists & inhibitors
Hippocampus
/ drug effects
Humans
Lignans
/ isolation & purification
Male
Mice
Mice, Inbred ICR
Molecular Docking Simulation
/ methods
Neuroprotective Agents
/ isolation & purification
Polycyclic Compounds
/ isolation & purification
Stereoisomerism
Treatment Outcome
Alzheimer’s disease
GSK-3β inhibitors
SH-SY5Y cells
Schisandrin B
stereoisomers
Journal
ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337
Informations de publication
Date de publication:
20 02 2019
20 02 2019
Historique:
pubmed:
27
6
2018
medline:
27
2
2020
entrez:
27
6
2018
Statut:
ppublish
Résumé
Glycogen synthase kinase-3β (GSK-3β) is a key enzyme in hyperphosphorylation of tau proteins and is a promising therapeutic target in Alzheimer's disease (AD). Here, we reported, for the first time, that the stereoisomers of Schisandrin B (Sch B), (+)-1, (-)-1, (+)-2, and (-)-2, were potent GSK-3β inhibitors. They were demonstrated to selectively target GSK-3β in an orthosteric binding mode, with IC
Identifiants
pubmed: 29944335
doi: 10.1021/acschemneuro.8b00252
doi:
Substances chimiques
Cyclooctanes
0
Enzyme Inhibitors
0
Lignans
0
Neuroprotective Agents
0
Polycyclic Compounds
0
schizandrin B
02XA4X3KZW
Adenosine Triphosphate
8L70Q75FXE
Glycogen Synthase Kinase 3 beta
EC 2.7.11.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM