3,468 results found
    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. 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. 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. 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. 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

    Ret function in muscle stem cells points to tyrosine kinase inhibitor therapy for facioscapulohumeral muscular dystrophy

    Louise A Moyle et al.
    Rescue of DUX4-induced muscle pathology by the RET inhibitor Sunitinib reveals the therapeutic potential for treatment of Facioscapulohumeral muscular dystrophy using tyrosine kinase inhibitors.
    1. Cell Biology
    2. Cancer Biology

    A kinase-independent function of AKT promotes cancer cell survival

    Igor Vivanco et al.
    The oncogenic potential of the serine threonine kinase AKT is not exclusively dependent on catalytic activity, but also involves the non-catalytic function of the pleckstrin homology domain.
    1. Structural Biology and Molecular Biophysics

    Differential impact of BTK active site inhibitors on the conformational state of full-length BTK

    Raji E Joseph et al.
    The first-in-class kinase inhibitor, Ibrutinib, destabilizes its autoinhibited Bruton’s tyrosine kinase (BTK) target, and a remote resistance mutation causes global structural changes that activate BTK catalytic activity.
    1. Cancer Biology

    MARCH5 mediates NOXA-dependent MCL1 degradation driven by kinase inhibitors and integrated stress response activation

    Seiji Arai et al.
    MARCH5 mediates a pathway driving MCL1 degradation in response to cellular stress, which sensitizes to BH3 mimetic drugs targeting BCLXL and provides a broadly effective therapeutic strategy for solid tumors.

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