Uncommon Features of a Novel γ-Proteobacterial Pentameric Ligand-Gated Ion Channel Revealed by its Crystal Structure
Sign Up to like & getrecommendations! Published in 2017 at "Biophysical Journal"
DOI: 10.1016/j.bpj.2016.11.1739
Abstract: Pentameric ligand-gated ion channels (pLGICs) control synaptic neurotransmission in higher eukaryotes via an allosteric mechanism, where agonist binding in the extra-cellular domain triggers the opening of an ion-conducting pore in the transmembrane domain. Here we… read more here.
Keywords: gated ion; pentameric ligand; ion; ligand gated ... See more keywords
A chimeric prokaryotic-eukaryotic pentameric ligand gated ion channel reveals interactions between the extracellular and transmembrane domains shape neurosteroid modulation
Sign Up to like & getrecommendations! Published in 2017 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2017.08.007
Abstract: Pentameric ligand-gated ion channels (pLGICs) are the targets of several clinical and endogenous allosteric modulators including anesthetics and neurosteroids. Molecular mechanisms underlying allosteric drug modulation are poorly understood. Here, we constructed a chimeric pLGIC by… read more here.
Keywords: modulation; gated ion; pentameric ligand; ligand gated ... See more keywords
Drug Development in Channelopathies: Allosteric Modulation of Ligand-Gated and Voltage-Gated Ion Channels.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01304
Abstract: Ion channels have been characterized as promising drug targets for treatment of numerous human diseases. Functions of ion channels can be fine-tuned by allosteric modulators, which interact with channels and modulate their activities by binding… read more here.
Keywords: gated voltage; ion channels; gated ion; ion ... See more keywords
Insect RDL Receptor Models for Virtual Screening: Impact of the Template Conformational State in Pentameric Ligand-Gated Ion Channels
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.1c05465
Abstract: The RDL receptor is one of the most relevant protein targets for insecticide molecules. It belongs to the pentameric ligand-gated ion channel (pLGIC) family. Given that the experimental structures of pLGICs are difficult to obtain,… read more here.
Keywords: performance; ligand gated; pentameric ligand; ligand ... See more keywords
Allosteric potentiation of a ligand-gated ion channel is mediated by access to a deep membrane-facing cavity
Sign Up to like & getrecommendations! Published in 2018 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.1809650115
Abstract: Significance Molecular mechanisms of general anesthetic modulation in pentameric ligand-gated ion channels remain controversial. Here we present molecular simulations and functional data that reveal correlations between dynamic differences in a membrane-accessible cavity and dramatic anesthetic… read more here.
Keywords: gated ion; cavity; ion; ligand gated ... See more keywords
Spider toxins targeting ligand-gated ion channels
Sign Up to like & getrecommendations! Published in 2019 at "Toxin Reviews"
DOI: 10.1080/15569543.2019.1579230
Abstract: Abstract Ligand-gated ion channels (LGIC) are membranous proteins that allow ionic flow across plasma membrane upon ligand binding. The channels are implicated in many physiological and pathological processes. Understanding the functionality of LGIC leads to… read more here.
Keywords: ion channels; gated ion; spider toxins; ligand gated ... See more keywords
Characterizing the voltage fluctuations driven by a cluster of ligand-gated channels.
Sign Up to like & getrecommendations! Published in 2021 at "Physical review. E"
DOI: 10.1103/physreve.103.052401
Abstract: In this paper we present the properties of the voltage fluctuations driven by a cluster of ligand-gated channels. First, the second-order moment of the voltage is expressed in form of the integrated resistance and the… read more here.
Keywords: voltage fluctuations; voltage; fluctuations driven; cluster ligand ... See more keywords
Full mutational mapping of titratable residues helps to identify proton-sensors involved in the control of channel gating in the Gloeobacter violaceus pentameric ligand-gated ion channel
Sign Up to like & getrecommendations! Published in 2017 at "PLoS Biology"
DOI: 10.1371/journal.pbio.2004470
Abstract: The Gloeobacter violaceus ligand-gated ion channel (GLIC) has been extensively studied by X-ray crystallography and other biophysical techniques. This provided key insights into the general gating mechanism of pentameric ligand-gated ion channel (pLGIC) signal transduction.… read more here.
Keywords: channel; ion channel; gated ion; ligand gated ... See more keywords
Un-gating and allosteric modulation of a pentameric ligand-gated ion channel captured by molecular dynamics
Sign Up to like & getrecommendations! Published in 2017 at "PLoS Computational Biology"
DOI: 10.1371/journal.pcbi.1005784
Abstract: Pentameric ligand-gated ion channels (pLGICs) mediate intercellular communication at synapses through the opening of an ion pore in response to the binding of a neurotransmitter. Despite the increasing availability of high-resolution structures of pLGICs, a… read more here.
Keywords: molecular dynamics; gated ion; channel; pentameric ligand ... See more keywords
Pentameric Ligand-Gated Ion Channels as Pharmacological Targets Against Chronic Pain
Sign Up to like & getrecommendations! Published in 2020 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2020.00167
Abstract: Chronic pain is a common detrimental condition that affects around 20% of the world population. The current drugs to treat chronic pain states, especially neuropathic pain, have a limited clinical efficiency and present significant adverse… read more here.
Keywords: ion channels; pentameric ligand; ligand gated; chronic pain ... See more keywords
Recent Insight into Lipid Binding and Lipid Modulation of Pentameric Ligand-Gated Ion Channels
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12060814
Abstract: Pentameric ligand-gated ion channels (pLGICs) play a leading role in synaptic communication, are implicated in a variety of neurological processes, and are important targets for the treatment of neurological and neuromuscular disorders. Endogenous lipids and… read more here.
Keywords: gated ion; ligand gated; pentameric ligand; lipid binding ... See more keywords