4,697 results found
    1. Cancer Biology
    2. Structural Biology and Molecular Biophysics

    Dynamics of human protein kinase Aurora A linked to drug selectivity

    Warintra Pitsawong et al.
    Slow conformational changes after drug binding rationalize selectivity, affinity and long on-target residence time for kinase inhibitors.
    1. Biochemistry and Chemical Biology
    2. Microbiology and Infectious Disease

    The NTP generating activity of pyruvate kinase II is critical for apicoplast maintenance in Plasmodium falciparum

    Russell P Swift et al.
    The pyruvate kinase contained in the apicoplast organelle of malaria parasites makes the nucleotide triphosphates required for several processes including transcription of the organellar genome.
    1. Cell Biology

    Polo-like kinase 1 induces epithelial-to-mesenchymal transition and promotes epithelial cell motility by activating CRAF/ERK signaling

    Jianguo Wu et al.
    Overexpression of PLK1 triggers oncogenic transformation and transcriptional reprogramming of prostate epithelial cells, which stimulates cell migration and invasion.
    1. Neuroscience

    Dysregulated Dscam levels act through Abelson tyrosine kinase to enlarge presynaptic arbors

    Gabriella R Sterne et al.
    Targeting Abelson kinase can be beneficial for treating disorders characterized by dysregulated Down Syndrome Cell Adhesion Molecule signaling.
    1. Structural Biology and Molecular Biophysics
    2. Computational and Systems Biology

    A dynamic mechanism for allosteric activation of Aurora kinase A by activation loop phosphorylation

    Emily F Ruff et al.
    Phosphorylation of Aurora A does not trigger a population shift to the active state as previously thought, but instead switches the kinase on by tuning the structure and dynamics of a dynamically sampled subpopulation.
    1. Cell Biology
    2. Cancer Biology

    MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells

    Yubao Wang et al.
    Maternal embryonic leucine zipper kinase (MELK) is a new anti-cancer target that is highly selective for basal-like breast cancer.
    1. Structural Biology and Molecular Biophysics

    Structure of substrate-bound SMG1-8-9 kinase complex reveals molecular basis for phosphorylation specificity

    Lukas M Langer et al.
    First structural view of a substrate-bound PIKK (PI3K-related-kinase) by cryo-EM explains phosphorylation specificity toward a short amino-acid motif shared across the PIKK family and rationalizes PIKK auto-inhibition by regulatory domain.
    1. Cancer Biology
    2. Cell Biology

    Inhibitor-induced HER2-HER3 heterodimerisation promotes proliferation through a novel dimer interface

    Jeroen Claus et al.
    The clinically approved HER2 inhibitor lapatinib causes HER2 and HER3 kinase domains to dimerise in a non-canonical, symmetric orientation, providing a platform for oligomerisation and predisposing to receptor-driven cell proliferation.
    1. Cell Biology
    2. Developmental Biology

    Control of PNG kinase, a key regulator of mRNA translation, is coupled to meiosis completion at egg activation

    Masatoshi Hara et al.
    The kinase that controls maternal mRNA translation is regulated by phosphorylation of its activating subunit to restrict kinase activity to the developmental window between meiosis completion and early embryogenesis.
    1. Cell Biology

    Salt-inducible kinases mediate nutrient-sensing to link dietary sugar and tumorigenesis in Drosophila

    Susumu Hirabayashi, Ross L Cagan
    The ability of tumors to respond to nutritional signals is mediated by Salt-inducible kinases, which ensure tumor growth under nutrient-rich conditions including obesity.

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