Acetylcholinesterase Inhibition Assays for High-Throughput Screening.
AChE inhibitors
Acetylcholinesterase (AChE)
Cell-based AChE inhibition assay
Enzyme-based AChE inhibition assay
High-throughput screening
Liver microsomes
Pesticides
Journal
Methods in molecular biology (Clifton, N.J.)
ISSN: 1940-6029
Titre abrégé: Methods Mol Biol
Pays: United States
ID NLM: 9214969
Informations de publication
Date de publication:
2022
2022
Historique:
entrez:
16
3
2022
pubmed:
17
3
2022
medline:
19
3
2022
Statut:
ppublish
Résumé
Acetylcholinesterase (AChE) hydrolyzes acetylcholine (ACh), a vital neurotransmitter that regulates muscle movement and brain function, including memory, attention, and learning. Inhibition of AChE activity can cause a variety of adverse health effects and toxicity. Identifying AChE inhibitors quickly and efficiently warrants developing AChE inhibition assays in a quantitative, high-throughput screening (qHTS) platform. In this chapter, protocols for multiple homogenous AChE inhibition assays used in a qHTS system are provided. These AChE inhibition assays include a (1) human neuroblastoma (SH-SY5Y) cell-based assay with fluorescence or colorimetric detection; (2) human recombinant AChE with fluorescence or colorimetric detection; and (3) combination of human recombinant AChE and liver microsomes with colorimetric detection, which enables detection of test compounds requiring metabolic activation to become AChE inhibitors. Together, these AChE assays can help identify, prioritize, and predict chemical hazards in large compound libraries using qHTS systems.
Identifiants
pubmed: 35294755
doi: 10.1007/978-1-0716-2213-1_6
pmc: PMC9440486
mid: NIHMS1831756
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Acetylcholinesterase
EC 3.1.1.7
Types de publication
Journal Article
Research Support, N.I.H., Intramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
47-58Subventions
Organisme : Intramural NIH HHS
ID : ZIA TR000038
Pays : United States
Informations de copyright
© 2022. This is a U.S. government work and not under copyright protection in the U.S.; foreign copyright protection may apply.
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