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 …

[HTML][HTML] Phylogenetic conservation of protein–lipid motifs in pentameric ligand-gated ion channels

FJ Barrantes - Biochimica et Biophysica Acta (BBA)-Biomembranes, 2015 - Elsevier
Using the crosstalk between the nicotinic acetylcholine receptor (nAChR) and its lipid
microenvironment as a paradigm, this short overview analyzes the occurrence of structural …

Grp94 protein delivers γ-aminobutyric acid type A (GABAA) receptors to Hrd1 protein-mediated endoplasmic reticulum-associated degradation

XJ Di, YJ Wang, DY Han, YL Fu, AS Duerfeldt… - Journal of Biological …, 2016 - ASBMB
Proteostasis maintenance of γ-aminobutyric acid type A (GABA A) receptors dictates their
function in controlling neuronal inhibition in mammalian central nervous systems. However …

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 …

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 …

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 …

Combining valosin-containing protein (VCP) inhibition and suberanilohydroxamic acid (SAHA) treatment additively enhances the folding, trafficking, and function of …

DY Han, XJ Di, YL Fu, TW Mu - Journal of Biological Chemistry, 2015 - ASBMB
GABA A receptors are the primary inhibitory ion channels in the mammalian central nervous
system. The A322D mutation in the α1 subunit results in its excessive endoplasmic reticulum …

Escherichia coli Protein Expression System for Acetylcholine Binding Proteins (AChBPs)

N Abraham, B Paul, L Ragnarsson, RJ Lewis - PLoS One, 2016 - journals.plos.org
Nicotinic acetylcholine receptors (nAChR) are ligand gated ion channels, identified as
therapeutic targets for a range of human diseases. Drug design for nAChR related disorders …

The development of novel polypharmacological agents targeting the multiple binding sites of nicotinic acetylcholine receptors

M Reyes-Parada… - Expert Opinion on Drug …, 2016 - Taylor & Francis
Introduction: Polypharmacology, which refers to the ability of a molecule to simultaneously
interact with multiple target proteins, is shifting the drug discovery process from a 'one-drug …

Solution NMR studies of anesthetic interactions with ion channels

V Bondarenko, M Wells, Y Xu, P Tang - Methods in enzymology, 2018 - Elsevier
NMR spectroscopy is one of the major tools to provide atomic resolution protein structural
information. It has been used to elucidate the molecular details of interactions between …