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

    Allosteric modulation in monomers and oligomers of a G protein-coupled receptor

    Rabindra V Shivnaraine et al.
    Allosteric modulation in the M2 muscarinic receptor derives from a mix of interactions within and between the protomers of an oligomer.
    1. Neuroscience

    Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

    Joan Font et al.
    Localized drug photoactivation provides light-mediated analgesia in behaving mice.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    An NMDAR positive and negative allosteric modulator series share a binding site and are interconverted by methyl groups

    Riley Perszyk et al.
    A series of novel compounds selective for N-methyl-D-aspartate-type glutamate receptor includes positive and negative allosteric modulators that act at the same site, show use-dependence, increase agonist potency, and have differential activity based on the agonist concentration.
    1. Structural Biology and Molecular Biophysics

    Voltage-dependent dynamics of the BK channel cytosolic gating ring are coupled to the membrane-embedded voltage sensor

    Pablo Miranda et al.
    Allosteric modulation of BK channels, vital for the physiology of nerve, muscle and endocrine cells, is determined by direct coupling between gating ring RCK1 domains and the voltage sensor function.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    Conformational dynamics between transmembrane domains and allosteric modulation of a metabotropic glutamate receptor

    Vanessa A Gutzeit et al.
    Single molecule subunit counting, FRET and electrophysiology experiments reveal that metabotropic glutamate receptor subunits interact and rearrange at the level of the transmembrane domains in response to allosteric modulators.
    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 et al.
    Polyunsaturated fatty acids enhance desensitization in pentameric ligand-gated ion channels.
    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
    2. Structural Biology and Molecular Biophysics

    Pharmacology: A Swiss army knife for targeting receptors

    Johansen B Amin, Lonnie P Wollmuth
    A compound can change the activity of NMDA receptors in some regions of a synapse without affecting those in other regions.
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    1. Structural Biology and Molecular Biophysics

    Structural Biology: NMR illuminates the pathways to ALS

    Tao Xie, Charalampos G Kalodimos
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