4,170 results found
    1. Neuroscience

    The switch-like expression of heme-regulated kinase 1 mediates neuronal proteostasis following proteasome inhibition

    Beatriz Alvarez-Castelao et al.
    In neurons, inhibition of the proteasome results in feedback inhibition of protein synthesis, mediated by heme-regulated kinase 1, which is optimized to act as both a sensor and an effector.
    1. Cancer Biology
    2. Cell Biology

    The CUL5 ubiquitin ligase complex mediates resistance to CDK9 and MCL1 inhibitors in lung cancer cells

    Shaheen Kabir et al.
    Targeting the CRL5 ubiquitin ligase complex in combination with CDK9 or MCL1 inhibition could combat innate and acquired resistance of cancer cells to MCL1-targeting therapeutics.
    1. Structural Biology and Molecular Biophysics

    Multi-state recognition pathway of the intrinsically disordered protein kinase inhibitor by protein kinase A

    Cristina Olivieri et al.
    A combination of NMR, fluorescence, and molecular dynamics simulations reveals the recognition mechanism for the intrinsically disordered regulator of protein kinase A, highlighting the enzyme's nuclear export process.
    1. Chromosomes and Gene Expression

    Multiple kinases inhibit origin licensing and helicase activation to ensure reductive cell division during meiosis

    David V Phizicky et al.
    Meiotic cells inhibit two distinct steps of replisome assembly with multiple kinases to prevent DNA replication between Meiosis I and Meiosis II.
    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. Medicine

    Anti-fibrotic activity of a rho-kinase inhibitor restores outflow function and intraocular pressure homeostasis

    Guorong Li et al.
    An FDA-approved, rho-associated kinase inhibitor reverses fibrosis in the conventional outflow pathway of a mouse model of glaucoma and reverses ocular hypertension in patients with steroid glaucoma.
    1. Immunology and Inflammation

    Inhibition of ErbB kinase signalling promotes resolution of neutrophilic inflammation

    Atiqur Rahman et al.
    Targeting ErbB receptor tyrosine kinases modifies neutrophil survival and inflammation across multiple species, and reveals a new use for ErbB therapeutics in resolving inflammatory disease.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Disease-related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors

    Manoj K Rathinaswamy et al.
    The c-terminus of PI3K plays a key role in regulating kinase activity, with c-terminal disease-linked mutations leading to either activation or inhibition, which reveal a path to specific inhibitors.
    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.

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