271 results found
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Conformational dynamics in TRPV1 channels reported by an encoded coumarin amino acid

    Ximena Steinberg et al.
    Single-molecule measurement of conformational dynamics using a genetically encoded fluorescent probe suggests that the selectivity filter region of TRPV1 channels undergoes dynamic motion during agonist activation.
    1. Structural Biology and Molecular Biophysics

    Structure-based characterization of novel TRPV5 inhibitors

    Taylor ET Hughes et al.
    Structure-based virtual screening reveals multiple novel TRPV5 inhibitors that bind and exert their effect from previously unidentified binding sites as characterized by cryo-electron microscopy and electrophysiology.
    1. Biochemistry and Chemical Biology

    Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine

    Qiang Liu et al.
    Identifying and understanding that local anesthetic dyclonine targets TRPV3 channels will help to conceive therapeutic interventions.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    PIP2 depletion promotes TRPV4 channel activity in mouse brain capillary endothelial cells

    Osama F Harraz et al.
    TRPV4 channels in brain capillaries are suppressed by the phosphoinositide PIP2 and activated by receptor agonists implicated in neurovascular coupling.
    1. Neuroscience

    Anti-nociceptive action of peripheral mu-opioid receptors by G-beta-gamma protein-mediated inhibition of TRPM3 channels

    Sandeep Dembla et al.
    Pro-nociceptive and pro-inflammatory TRPM3 (transient receptor potential melastatin 3) channels, expressed in somatosensory neurons, are inhibited by activation of Gαi-coupled receptors, such as µ-opioid receptors, in vitro and in vivo.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    Disease-associated mutations in the human TRPM3 render the channel overactive via two distinct mechanisms

    Siyuan Zhao et al.
    Disease-associated mutants of the TRPM3 ion channel are overactive, and they are inhibited by the antiepileptic medication primidone, offering a potential therapeutic intervention to treat this channelopathy.
    1. Structural Biology and Molecular Biophysics

    Structure of the human lipid-gated cation channel TRPC3

    Chen Fan et al.
    Cryo-EM structure reveals architecture, lipid-binding sites, and ion-conducting pore of the human TRPC3 cation channel.
    1. Structural Biology and Molecular Biophysics

    Symmetry transitions during gating of the TRPV2 ion channel in lipid membranes

    Lejla Zubcevic et al.
    Ligand-induced two-fold symmetric arrangement in TRPV2 is observed in the native-like nanodisc-reconstituted condition using cryo-electron microscopy.
    1. Structural Biology and Molecular Biophysics

    Molecular mechanism of TRPV2 channel modulation by cannabidiol

    Ruth A Pumroy et al.
    Cannabidiol binds to TRPV2 via a previously unidentified, but highly conserved, pocket.
    1. Structural Biology and Molecular Biophysics

    New capsaicin analogs as molecular rulers to define the permissive conformation of the mouse TRPV1 ligand-binding pocket

    Simon Vu et al.
    Novel capsaicin analogs with conserved chemistry but varying sizes were used as molecular rulers to investigate energetics of conformational changes in the ligand-binding pocket and mechanisms of TRPV1 ligand-gating.

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