176 results found
    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. Neuroscience

    Constitutive activation of kappa opioid receptors at ventral tegmental area inhibitory synapses following acute stress

    Abigail M Polter et al.
    Rats exposed to a single stressful event experience days-long constitutive activation of the kappa opioid receptor at inhibitory synapses in part of the brain’s reward system, which increases their drug-seeking behavior.
    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

    Visualizing endogenous opioid receptors in living neurons using ligand-directed chemistry

    Seksiri Arttamangkul et al.
    Opioid sensitive neurons were identified using a traceless affinity labeling strategy to covalently label endogenous mu-opioid receptors with fluorescent compounds in living brain slices from wild type animals.
    1. Biochemistry and Chemical Biology

    Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

    Rajendra Uprety et al.
    The structure-based design established a new approach to control pathway-selective activation of opioid receptors, resulting in new dual MOR/KOR G-protein biased agonist analgesics with attenuated liabilities.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor

    Kathryn E Livingston et al.
    Opioid drug efficacy and allosteric modulation is measured using an active state sensor of the mu-opioid receptor.
    1. Neuroscience

    Alcohol drinking alters stress response to predator odor via BNST kappa opioid receptor signaling in male mice

    Lara S Hwa et al.
    Heavy alcohol drinking primes dynorphin /kappa opioid systems in the bed nucleus of the stria terminalis to alter stress responses in mice.
    1. Neuroscience

    Synapse-specific opioid modulation of thalamo-cortico-striatal circuits

    William T Birdsong et al.
    By differentially modulating the two major excitatory inputs to the striatum, mu- and delta-opioid receptors regulate the balance between thalamic and cortical inputs to the striatum.
    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

    Compartment-specific opioid receptor signaling is selectively modulated by different dynorphin peptides

    Jennifer M Kunselman et al.
    Different dynorphins, which signal similarly from the cell surface, can differentially localize G protein-coupled receptors to specific subcellular compartments and cause divergent receptor fates and distinct spatiotemporal patterns of signaling.

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