[HTML][HTML] The molecular basis of drug selectivity for α5 subunit-containing GABAA receptors
VB Kasaragod, T Malinauskas, AA Wahid… - Nature Structural & …, 2023 - nature.com
Abstract α5 subunit-containing γ-aminobutyric acid type A (GABAA) receptors represent a
promising drug target for neurological and neuropsychiatric disorders. Altered expression …
promising drug target for neurological and neuropsychiatric disorders. Altered expression …
Direct structural insights into GABAA receptor pharmacology
GABA A receptors are pentameric ligand-gated ion channels that mediate most fast
neuronal inhibition in the brain. In addition to their important physiological roles, they are …
neuronal inhibition in the brain. In addition to their important physiological roles, they are …
A structural perspective on GABAA receptor pharmacology
S Scott, AR Aricescu - Current opinion in structural biology, 2019 - Elsevier
Highlights•Several structures of heteromeric αβγ GABA A receptors have recently been
described.•The binding modes of clinically relevant benzodiazepines have been …
described.•The binding modes of clinically relevant benzodiazepines have been …
A benzodiazepine ligand with improved GABAA receptor α5-subunit selectivity driven by interactions with Loop C
X Simeone, F Koniuszewski, M Müllegger… - Molecular …, 2021 - ASPET
The family of GABAA receptors is an important drug target group in the treatment of sleep
disorders, anxiety, epileptic seizures, and many others. The most frequent GABAA receptor …
disorders, anxiety, epileptic seizures, and many others. The most frequent GABAA receptor …
[HTML][HTML] GABAA Receptor Ligands Often Interact with Binding Sites in the Transmembrane Domain and in the Extracellular Domain—Can the Promiscuity Code Be …
MT Iorio, FD Vogel, F Koniuszewski, P Scholze… - International Journal of …, 2020 - mdpi.com
Many allosteric binding sites that modulate gamma aminobutyric acid (GABA) effects have
been described in heteropentameric GABA type A (GABAA) receptors, among them sites for …
been described in heteropentameric GABA type A (GABAA) receptors, among them sites for …
Allosteric modulation of GABAA receptors via multiple drug-binding sites
W Sieghart - Advances in pharmacology, 2015 - Elsevier
GABA A receptors are ligand-gated ion channels composed of five subunits that can be
opened by GABA and be modulated by multiple pharmacologically and clinically important …
opened by GABA and be modulated by multiple pharmacologically and clinically important …
GABAA receptors and the diversity in their structure and pharmacology
Abstract GABA A receptors (GABA A Rs) are a class of ligand-gated ion channels with high
physiological and therapeutic significance. In the brain, these pentameric receptors occur …
physiological and therapeutic significance. In the brain, these pentameric receptors occur …
Insights into the structure and pharmacology of GABAA receptors
CRJ Carter, JL Kozuska, SMJ Dunn - Future medicinal chemistry, 2010 - Taylor & Francis
GABA is the major inhibitory neurotransmitter in the adult mammalian CNS. The ionotropic
GABA type A receptors (GABAARs) belong to the Cys-loop family of receptors. Each …
GABA type A receptors (GABAARs) belong to the Cys-loop family of receptors. Each …
Fishing for allosteric sites on GABAA receptors
RW Olsen, CSS Chang, G Li, HJ Hanchar… - Biochemical …, 2004 - Elsevier
GABAA receptors have structural and functional homology with a super-family of cys-loop
ligand-gated ion channel receptors including the nicotinic acetylcholine receptors. Amino …
ligand-gated ion channel receptors including the nicotinic acetylcholine receptors. Amino …
[HTML][HTML] Molecular tools for GABAA receptors: High affinity ligands for β1-containing subtypes
X Simeone, DCB Siebert, K Bampali, Z Varagic… - Scientific reports, 2017 - nature.com
Abstract γ-Aminobutyric acid type A (GABAA) receptors are pentameric GABA-gated chloride
channels that are, in mammalians, drawn from a repertoire of 19 different genes, namely α1 …
channels that are, in mammalians, drawn from a repertoire of 19 different genes, namely α1 …
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