425 results found
    1. Biochemistry and Chemical Biology
    2. Immunology and Inflammation

    The allosteric activation of cGAS underpins its dynamic signaling landscape

    Richard M Hooy, Jungsan Sohn
    Rigorous biophysical studies reconcile several conflicting views on how cGAS is activated, and present a new unifying allosteric activation mechanism.
    1. Structural Biology and Molecular Biophysics
    2. Cell Biology

    A mutation uncouples the tubulin conformational and GTPase cycles, revealing allosteric control of microtubule dynamics

    Elisabeth A Geyer et al.
    A buried mutation in αβ-tubulin reveals an allosteric response to GDP in the lattice that dictates microtubule catastrophe and shrinking.
    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. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Tuning site-specific dynamics to drive allosteric activation in a pneumococcal zinc uptake regulator

    Daiana A Capdevila et al.
    Internal dynamics play a crucial functional role in MarR (multiple antibiotic resistance repressor) proteins and their role reconciles the distinct allosteric mechanisms proposed previously.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    3.3-Å resolution cryo-EM structure of human ribonucleotide reductase with substrate and allosteric regulators bound

    Edward J Brignole et al.
    Cryo-electron microscopy structures of human ribonucleotide reductase reveal molecular details of substrate selection and allosteric inhibition through assembly of its large subunit into a ring that excludes its small subunit.
    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.
    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. 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

    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. 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.

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