[HTML][HTML] Elephants in the dark: insights and incongruities in pentameric ligand-gated ion channel models

RJ Howard - Journal of Molecular Biology, 2021 - Elsevier
The superfamily of pentameric ligand-gated ion channels (pLGICs) comprises key players in
electrochemical signal transduction across evolution, including historic model systems for …

[HTML][HTML] Recent progress on the molecular pharmacology of propofol

P Tang, R Eckenhoff - F1000Research, 2018 - ncbi.nlm.nih.gov
The precise mechanism by which propofol enhances GABAergic transmission remains
unclear, but much progress has been made regarding the underlying structural and dynamic …

Structural basis of neurosteroid anesthetic action on GABAA receptors

Q Chen, MM Wells, P Arjunan, TS Tillman… - Nature …, 2018 - nature.com
Type A γ-aminobutyric acid receptors (GABAARs) are inhibitory pentameric ligand-gated ion
channels in the brain. Many anesthetics and neurosteroids act through binding to the …

Structural basis for a bimodal allosteric mechanism of general anesthetic modulation in pentameric ligand-gated ion channels

Z Fourati, RJ Howard, SA Heusser, H Hu, RR Ruza… - Cell reports, 2018 - cell.com
Ion channel modulation by general anesthetics is a vital pharmacological process with
implications for receptor biophysics and drug development. Functional studies have …

GABAA receptor family: overview on structural characterization

MJ Amundarain, RP Ribeiro, MD Costabel… - Future medicinal …, 2019 - Taylor & Francis
The pentameric γ-aminobutyric acid type A receptors are ion channels activated by ligands,
which intervene in the rapid inhibitory transmission in the mammalian CNS. Due to their rich …

[HTML][HTML] Structural evidence for the binding of monocarboxylates and dicarboxylates at pharmacologically relevant extracellular sites of a pentameric ligand-gated ion …

Z Fourati, L Sauguet, M Delarue - Acta Crystallographica Section D …, 2020 - scripts.iucr.org
GLIC is a bacterial homologue of the pentameric ligand-gated ion channels (pLGICs) that
mediate the fast chemical neurotransmission of nerve signalling in eukaryotes. Because the …

Probing proline residues in the prokaryotic ligand-gated ion channel, ELIC

R Mosesso, DA Dougherty, SCR Lummis - Biochemistry, 2018 - ACS Publications
Erwinia ligand-gated ion channel (ELIC) is a bacterial homologue of vertebrate pentameric
ligand-gated ion channels (pLGICs) and has proven to be a valuable model for …

Alcohol reduces muscle fatigue through atomistic interactions with nicotinic receptors

HR Noori, C Mücksch, V Vengeliene, K Schönig… - Communications …, 2018 - nature.com
Alcohol consumption affects many organs and tissues, including skeletal muscle. However,
the molecular mechanism of ethanol action on skeletal muscle remains unclear. Here, using …

Characterization of a 5-HT3–ELIC Chimera Revealing the Sites of Action of Modulators

KL Price, SCR Lummis - ACS Chemical Neuroscience, 2018 - ACS Publications
Cys-loop receptors are major sites of action for many important therapeutically active
compounds, but the sites of action of those that do not act at the orthosteric binding site or at …

Ketamine Inhibition of the Pentameric Ligand-Gated Ion Channel GLIC

BF Ion, MM Wells, Q Chen, Y Xu, P Tang - Biophysical Journal, 2017 - cell.com
Ketamine inhibits pentameric ligand-gated ion channels (pLGICs), including the bacterial
pLGIC from Gloeobacter violaceus (GLIC). The crystal structure of GLIC shows R-ketamine …