Small-molecule positive allosteric modulation of homomeric kainate receptors GluK1-3: development of screening assays and insight into GluK3 structure.
Kainate receptors
X-ray crystallography
calcium-sensitive fluorescence-based assays
electron microscopy
molecular dynamics simulations
Journal
The FEBS journal
ISSN: 1742-4658
Titre abrégé: FEBS J
Pays: England
ID NLM: 101229646
Informations de publication
Date de publication:
25 Dec 2023
25 Dec 2023
Historique:
revised:
20
10
2023
received:
06
07
2023
accepted:
29
11
2023
medline:
25
12
2023
pubmed:
25
12
2023
entrez:
25
12
2023
Statut:
aheadofprint
Résumé
The kainate receptors GluK1-3 (glutamate receptor ionotropic, kainate receptors 1-3) belong to the family of ionotropic glutamate receptors and are essential for fast excitatory neurotransmission in the brain, and are associated with neurological and psychiatric diseases. How these receptors can be modulated by small-molecule agents is not well understood, especially for GluK3. We show that the positive allosteric modulator BPAM344 can be used to establish robust calcium-sensitive fluorescence-based assays to test agonists, antagonists and positive allosteric modulators of GluK1-3. The half maximal effective concentration (EC
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Informations de copyright
This article is protected by copyright. All rights reserved.