Novel Curcumin-Diethyl Fumarate Hybrid as a Dualistic GSK-3β Inhibitor/Nrf2 Inducer for the Treatment of Parkinson's Disease.
Curcumin analogues
Diethyl fumarate
Glycogen synthase kinase-3β
Neurodegeneration
Nuclear factor-erythroid related factor 2
Oxidative stress
Parkinson’s disease
Journal
ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337
Informations de publication
Date de publication:
02 09 2020
02 09 2020
Historique:
pubmed:
15
7
2020
medline:
22
6
2021
entrez:
15
7
2020
Statut:
ppublish
Résumé
Common copathogenic factors, including oxidative stress and neuroinflammation, are found to play a vital role in the development of neurodegenerative disorders, including Alzheimer's disease (AD) and Parkinson's disease (PD). Nowadays, owing to the multifactorial character of the diseases, no effective therapies are available, thus underlying the need for new strategies. Overexpression of the enzyme GSK-3β and downregulation of the Nrf2/ARE pathway are responsible for a decrease in antioxidant defense effects. These pieces of evidence underline the usefulness of dual GSK-3β inhibitors/Nrf2 inducers. In this regard, to design a dual modulator, the structures of a curcumin-based analogue, as GSK-3β inhibitor, and a diethyl fumarate fragment, as Nrf2 inducer, were combined. Among the hybrids,
Identifiants
pubmed: 32663009
doi: 10.1021/acschemneuro.0c00363
pmc: PMC8009478
doi:
Substances chimiques
Fumarates
0
NF-E2-Related Factor 2
0
diethyl fumarate
5WBU5A3E8A
Glycogen Synthase Kinase 3 beta
EC 2.7.11.1
Curcumin
IT942ZTH98
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
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