MARK4 Inhibited by AChE Inhibitors, Donepezil and Rivastigmine Tartrate: Insights into Alzheimer's Disease Therapy.
Alzheimer’s disease
MARK4
acetylcholinesterase inhibitors
drug design and discovery
isothermal titration calorimetry
kinase inhibitors
molecular modeling and docking
Journal
Biomolecules
ISSN: 2218-273X
Titre abrégé: Biomolecules
Pays: Switzerland
ID NLM: 101596414
Informations de publication
Date de publication:
20 05 2020
20 05 2020
Historique:
received:
23
04
2020
revised:
15
05
2020
accepted:
17
05
2020
entrez:
24
5
2020
pubmed:
24
5
2020
medline:
7
4
2021
Statut:
epublish
Résumé
Microtubule affinity-regulating kinase (MARK4) plays a key role in Alzheimer's disease (AD) development as its overexpression is directly linked to increased tau phosphorylation. MARK4 is a potential drug target of AD and is thus its structural features are employed in the development of new therapeutic molecules. Donepezil (DP) and rivastigmine tartrate (RT) are acetylcholinesterase (AChE) inhibitors and are used to treat symptomatic patients of mild to moderate AD. In keeping with the therapeutic implications of DP and RT in AD, we performed binding studies of these drugs with the MARK4. Both DP and RT bound to MARK4 with a binding constant (
Identifiants
pubmed: 32443670
pii: biom10050789
doi: 10.3390/biom10050789
pmc: PMC7277793
pii:
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Nootropic Agents
0
Protein Kinase Inhibitors
0
Donepezil
8SSC91326P
MAPK4 protein, human
EC 3.6.4.13
RNA Helicases
EC 3.6.4.13
Rivastigmine
PKI06M3IW0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Science and Engineering Research Board
ID : EMR/2015/002372
Pays : International
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