552 results found
    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

    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. Structural Biology and Molecular Biophysics

    The molecular basis for an allosteric inhibition of K+-flux gating in K2P channels

    Susanne Rinné et al.
    A combined systematic alanine scanning and molecular modelling approach reveals the molecular basis for an allosteric inhibition mechanism of K+-flux gating in K2P channels.
    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

    Differential impact of BTK active site inhibitors on the conformational state of full-length BTK

    Raji E Joseph et al.
    The first-in-class kinase inhibitor, Ibrutinib, destabilizes its autoinhibited Bruton’s tyrosine kinase (BTK) target, and a remote resistance mutation causes global structural changes that activate BTK catalytic activity.
    1. Biochemistry and Chemical Biology

    De novo macrocyclic peptides dissect energy coupling of a heterodimeric ABC transporter by multimode allosteric inhibition

    Erich Stefan et al.
    By random nonstandard peptide integrated discovery, combinatorial macrocyclic peptides were leavaged that target a heterodimeric ABC transport complex and explore fundamental principles of the substrate translocation cycle.
    1. Biochemistry and Chemical Biology

    An allosteric Sec61 inhibitor traps nascent transmembrane helices at the lateral gate

    Andrew L MacKinnon et al.
    A small molecule, cotransin, blocks transmembrane domains form integrating into cell membranes by allosterically ‘locking’ the lateral gate of the Sec61 translocation channel.
    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. Biochemistry and Chemical Biology
    2. Cell Biology

    Permeant fluorescent probes visualize the activation of SARM1 and uncover an anti-neurodegenerative drug candidate

    Wan Hua Li et al.
    The first-in-class cell-permeant fluorescent probe provides direct and visual evidence of SARM1 activation in axonal degeneration and identified the first covalent, allosteric inhibitor of SARM1 acting on the NAD-binding pocket in the ARM domain.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Allosteric inhibition of a stem cell RNA-binding protein by an intermediary metabolite

    Carina C Clingman et al.
    The RNA-binding protein MSI1, which is required for stem cell and cancer cell proliferation in the brain and epithelial tissues, also directly senses the concentration of long non-esterified omega-9 fatty acids.

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