381 results found
    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. 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

    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

    Allosteric mechanism for KCNE1 modulation of KCNQ1 potassium channel activation

    Georg Kuenze et al.
    An integrative structural biology approach provides refined models of the KCNQ1-KCNE1 channel complex, which propose a new mechanism to explain how KCNE1 modulates KCNQ1 channel activation.
    1. Neuroscience
    2. Structural Biology and Molecular Biophysics

    Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

    Marijke Brams et al.
    Development of nanobodies against a model pentameric ligand-gated ion channel demonstrates they can be functionally active as negative or positive allosteric modulators and offers opportunities for future drug development.
    1. Biochemistry and Chemical Biology
    2. Microbiology and Infectious Disease

    Hepatitis B virus core protein allosteric modulators can distort and disrupt intact capsids

    Christopher John Schlicksup et al.
    Small molecule antivirals that drive assembly of HBV capsid protein can also bind to pre-assembled capsids causing them to change morphology or even break, suggesting a complex transduction of binding effects across the capsid.
    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. 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. Structural Biology and Molecular Biophysics

    Site-specific effects of neurosteroids on GABAA receptor activation and desensitization

    Yusuke Sugasawa et al.
    Differential, state-dependent occupancy of three discrete binding sites on α1β3 GABAA receptors determines whether a specific neurosteroid analogue potentiates or inhibits GABA-elicited currents or competitively antagonizes neurosteroid action.

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