825 results found
    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. 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. Structural Biology and Molecular Biophysics

    Activation of a nucleotide-dependent RCK domain requires binding of a cation cofactor to a conserved site

    Celso M Teixeira-Duarte et al.
    Cations are essential cofactors in the ATP activation mechanism of the KtrAB cation channel and appear to be cofactors of many other nucleotide-dependent RCK domains.
    1. Immunology and Inflammation

    MicroRNA-122 supports robust innate immunity in hepatocytes by targeting the RTKs/STAT3 signaling pathway

    Hui Xu et al.
    The liver-specific miRNA microRNA-122 plays a previously unknown role in hepatocyte intrinsic innate immunity by targeting the RTKs/STAT3 signaling pathway.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Autoinhibition of Bruton's tyrosine kinase (Btk) and activation by soluble inositol hexakisphosphate

    Qi Wang et al.
    A key B-cell tyrosine kinase that adopts an autoinhibited conformation, and can be activated by either membrane recruitment or soluble inositol hexakisphosphates in solution.
    1. Structural Biology and Molecular Biophysics

    Activation of the archaeal ion channel MthK is exquisitely regulated by temperature

    Yihao Jiang et al.
    Temperature-sensitivity of archaebacterial potassium channel MthK is regulated by RCK domain via alteration of allosteric coupling.
    1. Structural Biology and Molecular Biophysics

    Symmetry transitions during gating of the TRPV2 ion channel in lipid membranes

    Lejla Zubcevic et al.
    Ligand-induced two-fold symmetric arrangement in TRPV2 is observed in the native-like nanodisc-reconstituted condition using cryo-electron microscopy.
    1. Evolutionary Biology

    Birds land reliably on complex surfaces by adapting their foot-surface interactions upon contact

    William RT Roderick et al.
    When landing, Pacific parrotlets exhibit stereotyped leg and wing dynamics regardless of perch diameter and texture, but foot and claw kinematics become surface-specific upon touchdown to successfully grasp the perch.
    1. Cell Biology
    2. Genetics and Genomics

    Manipulation of the human tRNA pool reveals distinct tRNA sets that act in cellular proliferation or cell cycle arrest

    Noa Aharon-Hefetz et al.
    Systematic CRISPR-based editing of tRNA genes revealed that different human cells that span a range of growth rates and different modes of proliferation states require diverse tRNA sets.
    1. Cell Biology

    FAM150A and FAM150B are activating ligands for anaplastic lymphoma kinase

    Jikui Guan et al.
    The secreted molecules FAM150A and FAM150B bind to the ALK RTK extracellular domain, potently activating the receptor activation and driving downstream signaling events.

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