128 results found
    1. Structural Biology and Molecular Biophysics

    Sterol derivative binding to the orthosteric site causes conformational changes in an invertebrate Cys-loop receptor

    Steven De Gieter, Casey I Gallagher ... Rouslan G Efremov
    Cryo-EM structures of Cys-loop receptor Alpo4 from the thermophilic worm Alvinella pompejana show that a sterol derivative CHAPS binds in and outside of its orthosteric binding site and induces a quaternary twist.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Hsp47 promotes biogenesis of multi-subunit neuroreceptors in the endoplasmic reticulum

    Ya-Juan Wang, Xiao-Jing Di ... Ting-Wei Mu
    Hsp47 positively regulates the functional surface expression of endogenous GABAA receptors and plays a critical and general role in the maturation of Cys-loop neuroreceptors.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    Cryo-EM structure of the benzodiazepine-sensitive α1β1γ2S tri-heteromeric GABAA receptor in complex with GABA

    Swastik Phulera, Hongtao Zhu ... Eric Gouaux
    Structure of the triheteromeric α1β1γ2S GABAA receptor in complex with GABA illuminates the principles of receptor assembly and agonist binding.
    1. Structural Biology and Molecular Biophysics

    Crystal structure and dynamics of a lipid-induced potential desensitized-state of a pentameric ligand-gated channel

    Sandip Basak, Nicolaus Schmandt ... Sudha Chakrapani
    Polyunsaturated fatty acids enhance desensitization in pentameric ligand-gated ion channels.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

    Marijke Brams, Cedric Govaerts ... Chris Ulens
    Development of nanobodies against a model pentameric ligand-gated ion channel demonstrates they can be functionally active as negative or positive allosteric modulators and offers opportunities for future drug development.
    1. Biochemistry and Chemical Biology

    Mapping the molecular motions of 5-HT3 serotonin-gated channel by voltage-clamp fluorometry

    Laurie Peverini, Sophie Shi ... Pierre-Jean Corringer
    Conformational motions elicited by antagonists, partial agonists, and agonists in serotonin-gated ion channels 5-HT3AR progressively spread from the extracellular to the transmembrane domain.
    1. Biochemistry and Chemical Biology

    Collagen induces activation of DDR1 through lateral dimer association and phosphorylation between dimers

    Victoria Juskaite, David S Corcoran, Birgit Leitinger
    Ligand binding induces DDR1 kinase activity through recruitment of DDR1 receptors into signalling clusters in which phosphorylation occurs across different dimers.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Structural basis of death domain signaling in the p75 neurotrophin receptor

    Zhi Lin, Jason Y Tann ... Carlos F Ibanez
    Structures of the death domain of the p75 neurotrophin receptor in complex with downstream effectors show how competitive protein-protein interactions orchestrate the hierarchical activation of downstream pathways in non-catalytic receptors.
    1. Structural Biology and Molecular Biophysics
    2. Neuroscience

    Identification of a pre-active conformation of a pentameric channel receptor

    Anaïs Menny, Solène N Lefebvre ... Pierre-Jean Corringer
    Allosteric reorganizations of a bacterial channel receptor are mapped along the protein structure, using the site-directed bimane quenching fluorescence technique, through parallel real-time conformational and electrophysiological recordings.
    1. Cell Biology
    2. Neuroscience

    CRELD1 is an evolutionarily-conserved maturational enhancer of ionotropic acetylcholine receptors

    Manuela D'Alessandro, Magali Richard ... Jean-Louis Bessereau
    The protein disulphide isomerase CRELD1 controls the biosynthesis of nicotinic acetylcholine receptors in nematode and mouse muscle.

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