2,985 results found
    1. Biochemistry and Chemical Biology

    Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

    Rajendra Uprety et al.
    The structure-based design established a new approach to control pathway-selective activation of opioid receptors, resulting in new dual MOR/KOR G-protein biased agonist analgesics with attenuated liabilities.
    1. Structural Biology and Molecular Biophysics

    De novo design of a homo-trimeric amantadine-binding protein

    Jooyoung Park et al.
    The first successful de novo design of a homo-trimeric protein that binds a C3 symmetric small molecule larger than a metal ion is an advance for computational protein design.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Structural basis of nucleoside and nucleoside drug selectivity by concentrative nucleoside transporters

    Zachary Lee Johnson et al.
    Studies of the substrate selectivity of concentrative nucleoside transporters provide proof of principle for structure-based improvement of drug delivery by these transporters.
    1. Cell Biology
    2. Microbiology and Infectious Disease

    Coalescing beneficial host and deleterious antiparasitic actions as an antischistosomal strategy

    John D Chan et al.
    Engagement of both host and parasite signaling pathways proves a novel approach for developing improved anti-parasitic therapies.
    1. Cell Biology
    2. Computational and Systems Biology

    Active machine learning-driven experimentation to determine compound effects on protein patterns

    Armaghan W Naik et al.
    In an investigation into the effects of drugs on proteins, an active machine learning algorithm chose which sets of experiments to perform and was able to learn an accurate model of the effects after doing only a fraction of the experiments.
    1. Neuroscience

    Analysis of the immune response to sciatic nerve injury identifies efferocytosis as a key mechanism of nerve debridement

    Ashley L Kalinski et al.
    In the injured sciatic nerve, blood-derived monocytes and macrophages eat dying leukocytes, thereby contributing to nerve debridement and inflammation resolution, and this correlates with neuronal regeneration.
    1. Biochemistry and Chemical Biology

    The structural determinants of PH domain-mediated regulation of Akt revealed by segmental labeling

    Nam Chu et al.
    NMR and biochemical analysis reveal new insights into how the critical protein kinase Akt is regulated by phosphorylation and is inhibited by an experimental therapeutic.
    1. Chromosomes and Gene Expression
    2. Genetics and Genomics

    Controlling gene activation by enhancers through a drug-inducible topological insulator

    Taro Tsujimura et al.
    A novel synthetic DNA cassette of CTCF-binding sites combined with the drug-controllable induction system of heterochromatin enabled switchable blocking of chromatin conformation and gene-enhancer interaction.
    1. Neuroscience

    A subcortical circuit linking the cerebellum to the basal ganglia engaged in vocal learning

    Ludivine Pidoux et al.
    The cerebellum sends a functional input to the song-related basal ganglia via the thalamus in songbirds that can modify premotor activity, and it participates to song learning in juvenile birds.
    1. Structural Biology and Molecular Biophysics

    Mechanism of pharmacochaperoning in a mammalian KATP channel revealed by cryo-EM

    Gregory M Martin et al.
    Diverse KATP channel inhibitors occupy a common binding pocket and stabilize an interaction between Kir6.2 and SUR1 to allosterically control gating and promote the assembly and trafficking of nascent channels.

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