4,591 results found
    1. Microbiology and Infectious Disease
    2. Structural Biology and Molecular Biophysics

    Structural basis for potent and broad inhibition of HIV-1 RT by thiophene[3,2-d]pyrimidine non-nucleoside inhibitors

    Yang Yang et al.
    High-resolution structures of HIV-1 RT in complex with two newly developed non-nucleoside inhibitors explain how they retain antiviral activities against drug-resistant RT mutants with considerably reduced susceptibility to rilpivirine.
    1. Neuroscience

    Removal of inhibition uncovers latent movement potential during preparation

    Uday K Jagadisan, Neeraj J Gandhi
    Non-invasive disinhibition of the oculomotor system shows that ongoing preparatory activity in the superior colliculus has movement-generating potential and need not rise to threshold in order to produce a saccade.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    A potent voltage-gated calcium channel inhibitor engineered from a nanobody targeted to auxiliary CaVβ subunits

    Travis J Morgenstern et al.
    A novel engineered protein that uncouples electrical signals from downstream biological responses in excitable cells provides a unique investigative tool with potential therapeutic applications.
    1. Microbiology and Infectious Disease

    TRIM28 promotes HIV-1 latency by SUMOylating CDK9 and inhibiting P-TEFb

    Xiancai Ma et al.
    TRIM28 was found to be a versatile dual-function latency contributor by bridging both suppressive epigenetic modifications and RNAP II transcriptional-pausing, and can be a novel target to develop latency-reversing agents.
    1. Neuroscience

    Dopamine neuron dependent behaviors mediated by glutamate cotransmission

    Susana Mingote et al.
    The conditional reduction of glutaminase in mouse dopamine neurons selectively attenuates glutamate cotransmission at phasic frequencies, revealing the role of dopamine neuron glutamate cotransmission in the attribution of motivational salience.
    1. Human Biology and Medicine

    Metformin inhibits mitochondrial complex I of cancer cells to reduce tumorigenesis

    William W Wheaton et al.
    The anti-diabetic drug metformin, currently in clinical trials as a potential anti-cancer agent, reduces tumor growth by inhibiting mitochondrial complex I of human cancer cells.
    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. Biochemistry and Chemical Biology
    2. Chromosomes and Gene Expression

    Fail-safe control of translation initiation by dissociation of eIF2α phosphorylated ternary complexes

    Martin D Jennings et al.
    Phosphorylated translation initiation factor eIF2, a potent inhibitor of protein synthesis in eukaryotic cells, is also inhibitory to protein synthesis when bound to GTP and initiator tRNA broadening the reach and immediacy of eIF2-mediated control.
    1. Cell Biology

    Kinase-dead ATM protein is highly oncogenic and can be preferentially targeted by Topo-isomerase I inhibitors

    Kenta Yamamoto et al.
    Orphan ATM kinase-domain missense mutations are unexpectedly common and form a potent oncogenic event and a biomarker for Topo-isomerase I inhibitor based therapy.
    1. Cancer Biology
    2. Human Biology and Medicine

    FGF2-FGFR1 signaling regulates release of Leukemia-Protective exosomes from bone marrow stromal cells

    Nathalie Javidi-Sharifi et al.
    Inhibition of FGF2-FGFR1 signaling in bone marrow stroma attenuates secretion of FGF2-laden exosomes and subsequent protection of leukemia cells.

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