680 results found
    1. Evolutionary Biology
    2. Structural Biology and Molecular Biophysics

    Structurally distributed surface sites tune allosteric regulation

    James W McCormick et al.
    Deep mutational scanning of a synthetic allosteric chimera revealed that a sparse set of mutations on the protein surface improved regulation.
    1. Microbiology and Infectious Disease

    HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors

    Pratibha C Koneru et al.
    Pyridine-based allosteric inhibitors selectively target HIV-1 integrase tetramers and exhibit enhanced antiviral activity against a dolutegravir resistant mutant virus indicating potential clinical benefits for combining these two classes of inhibitors.
    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. Structural Biology and Molecular Biophysics

    An expanded allosteric network in PTP1B by multitemperature crystallography, fragment screening, and covalent tethering

    Daniel A Keedy et al.
    By measuring how multiple conformations shift in response to temperature, a new allosteric binding site is discovered for the phosphatase PTP1B.
    1. Structural Biology and Molecular Biophysics

    Genetically tunable frustration controls allostery in an intrinsically disordered transcription factor

    Jing Li et al.
    Allostery in an intrinsically disordered domain of glucocorticoid receptor is mediated by opposing thermodynamic signals that are directed through the production of different isoforms.
    1. Biochemistry and Chemical Biology

    Identification of an allosteric binding site on the human glycine transporter, GlyT2, for bioactive lipid analgesics

    Shannon N Mostyn et al.
    Identification of how bioactive lipids bind and inhibit glycine transporters has the potential to be exploited in the development of a new class of analgesics for chronic pain.
    1. Structural Biology and Molecular Biophysics

    Allosteric communication in DNA polymerase clamp loaders relies on a critical hydrogen-bonded junction

    Subu Subramanian et al.
    Deep mutagenesis of a clamp-loader complex reveals a critical hydrogen-bonded junction that is important for allosteric communication in oligomeric AAA+ ATPases.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Uncovering an allosteric mode of action for a selective inhibitor of human Bloom syndrome protein

    Xiangrong Chen et al.
    Discovery and characterisation of a novel allosteric inhibitor-binding site in human Bloom syndrome protein.
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Functional cross-talk between allosteric effects of activating and inhibiting ligands underlies PKM2 regulation

    Jamie A Macpherson et al.
    Specific residues within an enzyme integrate allosteric inputs that originate from distinct ligand-binding pockets.
    1. Structural Biology and Molecular Biophysics

    Mechanistic insights into the active site and allosteric communication pathways in human nonmuscle myosin-2C

    Krishna Chinthalapudi et al.
    R788 is part of an allosteric communication pathway that connects the converter at the distal end of the myosin motor domain via the relay helix with switch-2 of the active site.

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