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
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
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