375 results found
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Ligand modulation of sidechain dynamics in a wild-type human GPCR

    Lindsay D Clark et al.
    Generation of a highly deuterated 13C-methyl labeled wild-type GPCR sample is used to facilitate characterization of the molecular environments and fast ps-ns dynamics of sidechains when the receptor is bound to ligands of different efficacy.
    1. Neuroscience

    Cortical astrocytes independently regulate sleep depth and duration via separate GPCR pathways

    Trisha V Vaidyanathan et al.
    Cortical astrocytes play key roles in NREM sleep by regulating sleep depth and duration through separate GPCR pathways, and differentially control neuronal slow-wave activity in local and remote cortical circuits.
    1. Neuroscience

    Antinociceptive modulation by the adhesion GPCR CIRL promotes mechanosensory signal discrimination

    Sven Dannhäuser et al.
    An interdisciplinary approach uncovers a new antinociceptive molecular mechanism and shows that the adhesion GPCR CIRL adjusts the sensation of gentle touch and noxious mechanical insult in opposite directions.
    1. Developmental Biology
    2. Neuroscience

    The adhesion-GPCR BAI1 shapes dendritic arbors via Bcr-mediated RhoA activation causing late growth arrest

    Joseph G Duman et al.
    The adhesion-GPCR BAI1 shapes dendritic arbors in the hippocampus by associating with Bcr late in development and stimulating its RhoA-GEF activity, resulting in dendritic growth arrest.
    1. Cell Biology
    2. Structural Biology and Molecular Biophysics

    Near-atomic structures of the BBSome reveal the basis for BBSome activation and binding to GPCR cargoes

    Shuang Yang et al.
    Membrane recruitment of BBSome is coupled to a conformational change, and interaction of the BBSome with GPCR cargoes depends on the GPCRs releasing their amphipathic helix 8 from the membrane.
    1. Cell Biology
    2. Neuroscience

    Latrophilin GPCR signaling mediates synapse formation

    Richard Sando, Thomas C Südhof
    Spatial restriction of GPCR signaling at nascent synapses by adhesion complexes drives excitatory synapse formation and specificity in the hippocampus.
    1. Cell Biology

    Conformational specificity of opioid receptors is determined by subcellular location irrespective of agonist

    Stephanie E Crilly et al.
    A GPCR activated by the same agonist engages different conformational biosensors at different subcellular locations, suggesting that location-based conformations drive spatial encoding of signaling.
    1. Cell Biology

    G protein-regulated endocytic trafficking of adenylyl cyclase type 9

    André M Lazar et al.
    An adenylyl cyclase isoform is shown to dynamically traffic to endosomes after activation by G protein in mammalian cells, contributing to cellular cAMP signaling by internalized GPCRs.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Agonist-selective recruitment of engineered protein probes and of GRK2 by opioid receptors in living cells

    Miriam Stoeber et al.
    Chemically distinct opioid ligands promote selective protein recruitment by opioid receptors in intact cells.
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Computational design of thermostabilizing point mutations for G protein-coupled receptors

    Petr Popov et al.
    A comprehensive approach to prediction of stabilizing mutations in G-protein coupled receptors yields high hit rate and crystal structures of 5HT2C in both active and inactive states.

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