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 …

Crystal structure of human glycine receptor-α3 bound to antagonist strychnine

X Huang, H Chen, K Michelsen, S Schneider… - Nature, 2015 - nature.com
Neurotransmitter-gated ion channels of the Cys-loop receptor family are essential mediators
of fast neurotransmission throughout the nervous system and are implicated in many …

Crystal structures of a GABAA-receptor chimera reveal new endogenous neurosteroid-binding sites

D Laverty, P Thomas, M Field, OJ Andersen… - Nature structural & …, 2017 - nature.com
Abstract γ-Aminobutyric acid receptors (GABAARs) are vital for controlling excitability in the
brain. This is emphasized by the numerous neuropsychiatric disorders that result from …

Glycine receptor mechanism elucidated by electron cryo-microscopy

J Du, W Lü, S Wu, Y Cheng, E Gouaux - Nature, 2015 - nature.com
The strychnine-sensitive glycine receptor (GlyR) mediates inhibitory synaptic transmission in
the spinal cord and brainstem and is linked to neurological disorders, including autism and …

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 …

Human secreted Ly-6/uPAR related protein-1 (SLURP-1) is a selective allosteric antagonist of α7 nicotinic acetylcholine receptor

EN Lyukmanova, MA Shulepko, D Kudryavtsev… - PLoS …, 2016 - journals.plos.org
SLURP-1 is a secreted toxin-like Ly-6/uPAR protein found in epithelium, sensory neurons
and immune cells. Point mutations in the slurp-1 gene cause the autosomal inflammation …

[HTML][HTML] Elephants in the dark: insights and incongruities in pentameric ligand-gated ion channel models

RJ Howard - Journal of Molecular Biology, 2021 - Elsevier
The superfamily of pentameric ligand-gated ion channels (pLGICs) comprises key players in
electrochemical signal transduction across evolution, including historic model systems for …

Drosophila functional screening of de novo variants in autism uncovers damaging variants and facilitates discovery of rare neurodevelopmental diseases

PC Marcogliese, SL Deal, J Andrews, JM Harnish… - Cell reports, 2022 - cell.com
Individuals with autism spectrum disorder (ASD) exhibit an increased burden of de novo
mutations (DNMs) in a broadening range of genes. While these studies have implicated …

Phosphorylation state–dependent modulation of spinal glycine receptors alleviates inflammatory pain

MA Acuña, GE Yévenes, WT Ralvenius… - The Journal of …, 2016 - Am Soc Clin Investig
Diminished inhibitory neurotransmission in the superficial dorsal horn of the spinal cord is
thought to contribute to chronic pain. In inflammatory pain, reductions in synaptic inhibition …

Positive allosteric modulators of Glycine receptors and their potential use in pain therapies

CI Gallagher, DA Ha, RJ Harvey, RJ Vandenberg… - Pharmacological …, 2022 - Elsevier
Glycine receptors are ligand-gated ion channels that mediate synaptic inhibition throughout
the mammalian spinal cord, brainstem, and higher brain regions. They have recently …