Gating of pentameric ligand-gated ion channels: structural insights and ambiguities

JB Corrie, JE Baenziger - Structure, 2013 - cell.com
Pentameric ligand-gated ion channels (pLGICs) mediate fast synaptic communication by
converting chemical signals into an electrical response. Recently solved agonist-bound and …

Advances in NMR methods to map allosteric sites: from models to translation

S Boulton, G Melacini - Chemical Reviews, 2016 - ACS Publications
The last five years have witnessed major developments in the understanding of the allosteric
phenomenon, broadly defined as coupling between remote molecular sites. Such advances …

[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 …

A release of local subunit conformational heterogeneity underlies gating in a muscle nicotinic acetylcholine receptor

MJ Thompson, F Mansoub Bekarkhanechi… - Nature …, 2024 - nature.com
Synaptic receptors respond to neurotransmitters by opening an ion channel across the post-
synaptic membrane to elicit a cellular response. Here we use recent Torpedo acetylcholine …

[HTML][HTML] NMR structures of the human α7 nAChR transmembrane domain and associated anesthetic binding sites

V Bondarenko, DD Mowrey, TS Tillman… - … et Biophysica Acta (BBA …, 2014 - Elsevier
The α7 nicotinic acetylcholine receptor (nAChR), assembled as homomeric pentameric
ligand-gated ion channels, is one of the most abundant nAChR subtypes in the brain …

Seeking structural specificity: direct modulation of pentameric ligand-gated ion channels by alcohols and general anesthetics

RJ Howard, JR Trudell, RA Harris, LA Morrow - Pharmacological reviews, 2014 - Elsevier
Alcohols and other anesthetic agents dramatically alter neurologic function in a wide range
of organisms, yet their molecular sites of action remain poorly characterized. Pentameric …

Insights into distinct modulation of α7 and α7β2 nicotinic acetylcholine receptors by the volatile anesthetic isoflurane

DD Mowrey, Q Liu, V Bondarenko, Q Chen… - Journal of Biological …, 2013 - ASBMB
Nicotinic acetylcholine receptors (nAChRs) are targets of general anesthetics, but functional
sensitivity to anesthetic inhibition varies dramatically among different subtypes of nAChRs …

Role of the cys loop and transmembrane domain in the allosteric modulation of α4β2 nicotinic acetylcholine receptors

C Alcaino, M Musgaard, T Minguez… - Journal of Biological …, 2017 - ASBMB
Allosteric modulators of pentameric ligand-gated ion channels are thought to act on
elements of the pathways that couple agonist binding to channel gating. Using α4β2 …

Multiple binding sites in the nicotinic acetylcholine receptors: An opportunity for polypharmacolgy

P Iturriaga-Vásquez, J Alzate-Morales… - Pharmacological …, 2015 - Elsevier
For decades, the development of selective compounds has been the main goal for chemists
and biologists involved in drug discovery. However, diverse lines of evidence indicate that …

A membrane-embedded pathway delivers general anesthetics to two interacting binding sites in the Gloeobacter violaceus ion channel

MJ Arcario, CG Mayne, E Tajkhorshid - Journal of Biological Chemistry, 2017 - ASBMB
General anesthetics exert their effects on the central nervous system by acting on ion
channels, most notably pentameric ligand-gated ion channels. Although numerous studies …