4,045 results found
    1. Biochemistry and Chemical Biology
    2. Chromosomes and Gene Expression

    Compensatory induction of MYC expression by sustained CDK9 inhibition via a BRD4-dependent mechanism

    Huasong Lu et al.
    A new potent and selective CDK9 inhibitor induces the expression of the proto-oncogene MYC via a mechanism that depends on the bromodomain protein BRD4.
    1. Neuroscience

    Precise excitation-inhibition balance controls gain and timing in the hippocampus

    Aanchal Bhatia et al.
    Delayed inhibition precisely balances excitation from arbitrary combinations of CA3 neurons and controls the gain of CA1 output by reducing inhibitory delay with increasing excitation.
    1. Cancer Biology

    Synergistic interactions with PI3K inhibition that induce apoptosis

    Yaara Zwang et al.
    A geneome-scale shRNA screen identifies five genes whose suppression promotes cell death upon PI3K inhibition both in vitro and in vivo, thus suggesting potential combination therapies involving PI3K inhibition.
    1. Structural Biology and Molecular Biophysics

    BK channel inhibition by strong extracellular acidification

    Yu Zhou et al.
    Analysis of iconic and gating currents of wild type and mutated BK channels reveals a strong inhibition of this channel by extracellular acidification and elucidates the underlying mechanism that is potentially applicable to other voltage-dependent cation channels.
    1. Neuroscience

    Inhibition gates supralinear Ca2+ signaling in Purkinje cell dendrites during practiced movements

    Michael A Gaffield et al.
    In behaving mice, inhibition from molecular layer interneurons attenuates excitation of Purkinje cells by parallel fibers and suppresses their ability to enhance climbing fiber-triggered dendritic Ca2+ responses.
    1. Microbiology and Infectious Disease

    A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency

    Manabu Aoki et al.
    GRL-142 is an HIV protease inhibitor with a unique structure and atto-to-picomolar potency against a wide range of HIV strains.
    1. Neuroscience

    Inhibition in the auditory brainstem enhances signal representation and regulates gain in complex acoustic environments

    Christian Keine et al.
    Inhibition in the brainstem has further roles beyond temporal sharpening and improves reproduction for a multitude of sounds.
    1. Cancer Biology
    2. Cell Biology

    Inhibitor of ppGalNAc-T3-mediated O-glycosylation blocks cancer cell invasiveness and lowers FGF23 levels

    Lina Song, Adam D Linstedt
    The first inhibitor identified against an iso-enzyme that initiates O-glycosylation in the Golgi complex promises new therapeutic approaches for cancer and chronic kidney disease.
    1. Structural Biology and Molecular Biophysics
    2. Neuroscience

    Cooperative and acute inhibition by multiple C-terminal motifs of L-type Ca2+ channels

    Nan Liu et al.
    C-terminus mediated inhibition is one emerging modality of intervention for L-type Ca2+ channels, which coordinate multiple motifs to acutely tune Ca2+ current and Ca2+ influx down to the lower limits preset by end-stage Ca2+-dependent inactivation.
    1. Biochemistry and Chemical Biology
    2. Microbiology and Infectious Disease

    Transcription inhibition by the depsipeptide antibiotic salinamide A

    David Degen et al.
    Salinamide A exerts antibacterial activity by binding to the bridge-helix cap of bacterial RNA polymerase and allosterically inhibiting nucleotide addition

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