Structure-function Studies of GABA (A) Receptors and Related computer-aided Studies.
GABA (A) receptors
and benzodiazepines
in silico
structure-function
Journal
Journal of molecular neuroscience : MN
ISSN: 1559-1166
Titre abrégé: J Mol Neurosci
Pays: United States
ID NLM: 9002991
Informations de publication
Date de publication:
Oct 2023
Oct 2023
Historique:
received:
03
08
2023
accepted:
12
09
2023
medline:
5
12
2023
pubmed:
26
9
2023
entrez:
26
9
2023
Statut:
ppublish
Résumé
The γ-aminobutyric acid type A receptor (GABA (A) receptor) is a membrane protein activated by the neurotransmitter GABA. Structurally, this major inhibitory neurotransmitter receptor in the human central nervous system is a pentamer that can be built from a selection of 19 subunits consisting of α(1,2,3,4,5 or 6), β (1,2 or 3), γ (1,2 or 3), ρ (1,2 or 3), and δ, π, θ, and ε. This creates several possible pentameric arrangements, which also influence the pharmacological and physiological properties of the receptor. The complexity and heterogeneity of the receptors are further increased by the addition of short and long splice variants in several subunits and the existence of multiple allosteric binding sites and expansive ligands that can bind to the receptors. Therefore, a comprehensive understanding of the structure and function of the receptors is required to gain novel insights into the consequences of receptor dysfunction and subsequent drug development studies. Notably, advancements in computational-aided studies have facilitated the elucidation of residual interactions and exploring energy binding, which may otherwise be challenging to investigate. In this review, we aim to summarize the current understanding of the structure and function of GABA (A) receptors obtained from advancements in computational-aided applications.
Identifiants
pubmed: 37750966
doi: 10.1007/s12031-023-02158-3
pii: 10.1007/s12031-023-02158-3
doi:
Substances chimiques
Receptors, GABA-A
0
Receptors, GABA
0
gamma-Aminobutyric Acid
56-12-2
Types de publication
Review
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
804-817Subventions
Organisme : Short Term Grant, School of Medical Sciences, Universiti Sains Malaysia
ID : 304.PPSP.6315407
Informations de copyright
© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.
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