3,506 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. 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. 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. 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.
    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. 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.

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