96 results found
    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. 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

    Gain of channel function and modified gating properties in TRPM3 mutants causing intellectual disability and epilepsy

    Evelien Van Hoeymissen et al.
    Two mutations in TRPM3 resulting in developmental and epileptic encephalopathies result in a gain-of-channel function, which may lie at the basis of epileptic activity and neurodevelopmental symptoms in the patients.
    1. Immunology and Inflammation
    2. Microbiology and Infectious Disease

    Primate TRIM5 proteins form hexagonal nets on HIV-1 capsids

    Yen-Li Li et al.
    To protect mammals against retroviral infections, TRIM5 restriction factors recognize viral capsids by forming complementary hexagonal nets that can adapt to the patterns of capsid protein subunits on the viral capsid surface.
    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

    Ligand recognition and gating mechanism through three ligand-binding sites of human TRPM2 channel

    Yihe Huang et al.
    High-resolution structures of human TRPM2 in different functional states provided the mechanism underlying ligand recognition, channel activation and inhibition.
    1. Structural Biology and Molecular Biophysics

    Epithelial magnesium transport by TRPM6 is essential for prenatal development and adult survival

    Vladimir Chubanov et al.
    Mice deficient in the TRPM6 channel suffer from impaired prenatal development, shortened lifespan, growth deficit and disturbed energy balance due to a defect in epithelial Mg2+ uptake, thus highlighting a pivotal role of TRPM6 in organismal Mg2+ homeostasis.
    1. Neuroscience

    Upregulation of TRPM3 in nociceptors innervating inflamed tissue

    Marie Mulier et al.
    The expression and function of the cation channel TRPM3 is strongly increased in sensory neurons innervating inflamed tissue, likely contributing to inflammatory hyperalgesia and persistent pain.
    1. Structural Biology and Molecular Biophysics

    Structure of a TRPM2 channel in complex with Ca2+ explains unique gating regulation

    Zhe Zhang et al.
    The 3Å structure and correlated functional analysis of the TRPM2 cation channel from Nematostella vectensis shed light on the molecular mechanisms of TRPM2 regulation by intra- and extracellular Ca2+, and of inactivation of human TRPM2.
    1. Neuroscience

    G protein βγ subunits inhibit TRPM3 ion channels in sensory neurons

    Talisia Quallo et al.
    TRPM3 inhibition is identified as a novel mechanism for G-protein βγ subunit signalling.

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