Emerging molecular mechanisms of signal transduction in pentameric ligand-gated ion channels

Á Nemecz, MS Prevost, A Menny, PJ Corringer - Neuron, 2016 - cell.com
Nicotinic acetylcholine, serotonin type 3, γ-amminobutyric acid type A, and glycine receptors
are major players of human neuronal communication. They belong to the family of …

Protein oligomer engineering: a new frontier for studying protein structure, function, and toxicity

C Liu, J Luo - Angewandte Chemie, 2023 - Wiley Online Library
Prevalent in nature, protein oligomers play critical roles both physiologically and
pathologically. The multimeric nature and conformational transiency of protein oligomers …

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 …

Orthosteric and allosteric potentiation of heteromeric neuronal nicotinic acetylcholine receptors

J Wang, J Lindstrom - British journal of pharmacology, 2018 - Wiley Online Library
Heteromeric nicotinic ACh receptors (nAChRs) were thought to have two orthodox agonist‐
binding sites at two α/β subunit interfaces. Highly selective ligands are hard to develop by …

[HTML][HTML] Potentiation and allosteric agonist activation of α7 nicotinic acetylcholine receptors: binding sites and hypotheses

VR Sanders, NS Millar - Pharmacological Research, 2023 - Elsevier
Considerable progress has been made in recent years towards the identification and
characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors …

[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 …

Allosteric and hyperekplexic mutant phenotypes investigated on an α1 glycine receptor transmembrane structure

G Moraga-Cid, L Sauguet, C Huon… - Proceedings of the …, 2015 - National Acad Sciences
The glycine receptor (GlyR) is a pentameric ligand-gated ion channel (pLGIC) mediating
inhibitory transmission in the nervous system. Its transmembrane domain (TMD) is the target …

Electrically silent mutants unravel the mechanism of binding− gating coupling in Cys-loop receptors

NE Godellas, GD Cymes, C Grosman - Science Advances, 2024 - science.org
The transduction of extracellular chemical signals into intracellular events relies on the
communication between neighboring domains of membrane receptors. In the particular case …

Conformational changes underlying desensitization of the pentameric ligand-gated ion channel ELIC

MN Kinde, Q Chen, MJ Lawless, DD Mowrey, J Xu… - Structure, 2015 - cell.com
Structural rearrangements underlying functional transitions of pentameric ligand-gated ion
channels (pLGICs) are not fully understood. Using 19 F nuclear magnetic resonance and …

The M4 transmembrane α-helix contributes differently to both the maturation and function of two prokaryotic pentameric ligand-gated ion channels

CM Hénault, PF Juranka, JE Baenziger - Journal of Biological Chemistry, 2015 - ASBMB
The role of the outermost transmembrane α-helix in both the maturation and function of the
prokaryotic pentameric ligand-gated ion channels, GLIC and ELIC, was examined by Ala …