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

    Structurally distributed surface sites tune allosteric regulation

    James W McCormick, Marielle AX Russo ... Kimberly A Reynolds
    Deep mutational scanning of a synthetic allosteric chimera revealed that a sparse set of mutations on the protein surface improved regulation.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

    Ziva Vuckovic, Jinan Wang ... David M Thal
    Structural biology studies reveal the importance of protein dynamics on understanding molecular mechanisms underlying allosteric modulation of G protein-coupled receptors (GPCR) that offer insights into future GPCR research and drug discovery.
    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, Brendan Kelly ... James W Wells
    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, Zachary B Hill ... James S Fraser
    By measuring how multiple conformations shift in response to temperature, a new allosteric binding site is discovered for the phosphatase PTP1B.
    1. Microbiology and Infectious Disease

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

    Pratibha C Koneru, Ashwanth C Francis ... Mamuka Kvaratskhelia
    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. Structural Biology and Molecular Biophysics

    Enhanced specificity mutations perturb allosteric signaling in CRISPR-Cas9

    Lukasz Nierzwicki, Kyle W East ... Giulia Palermo
    Allostery holds critical role in CRISPR-Cas9 specificity enhancement.
    1. Structural Biology and Molecular Biophysics

    Allosteric modulation of the adenosine A2A receptor by cholesterol

    Shuya Kate Huang, Omar Almurad ... R Scott Prosser
    Cholesterol exhibits transient interaction with A2AR and regulates receptor conformational equilibria through indirect membrane effects.
    1. Structural Biology and Molecular Biophysics

    Genetically tunable frustration controls allostery in an intrinsically disordered transcription factor

    Jing Li, Jordan T White ... Vincent J Hilser
    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. 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, Alina Theisen ... Dimitrios Anastasiou
    Specific residues within an enzyme integrate allosteric inputs that originate from distinct ligand-binding pockets.
    1. Computational and Systems Biology
    2. Structural Biology and Molecular Biophysics

    Deep mutational scanning and machine learning reveal structural and molecular rules governing allosteric hotspots in homologous proteins

    Megan Leander, Zhuang Liu ... Srivatsan Raman
    Deep mutational scanning of homologous proteins shows conservation in allosteric mechanisms but differences in molecular details within the protein family.

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