5,076 results found
    1. Cancer Biology

    BRET-based RAS biosensors that show a novel small molecule is an inhibitor of RAS-effector protein-protein interactions

    Nicolas Bery et al.
    A biosensor resource has been developed to monitor the intracellular interactions of RAS family proteins with effector molecules and the effects of inhibitors as an aid to drug development.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Identification of a small molecule inhibitor that stalls splicing at an early step of spliceosome activation

    Anzhalika Sidarovich et al.
    Stalling spliceosome assembly at a novel step before Bact complex formation reveals new insights into the extensive RNP rearrangements and compositional changes that accompany the intricate process of spliceosome activation.
    1. Cell Biology
    2. Immunology and Inflammation

    Small molecule inhibition of Csk alters affinity recognition by T cells

    Boryana N Manz et al.
    The T cell response, especially to weak agonists, is enhanced by acute Csk inhibition.
    1. Cancer Biology

    R-propranolol is a small molecule inhibitor of the SOX18 transcription factor in a rare vascular syndrome and hemangioma

    Jeroen Overman et al.
    Identification of the R(+)-propranolol enantiomer as an inhibitor of the SOX18 transcription factor activity breaks open potential of drug repurposing in vascular diseases.
    1. Cell Biology
    2. Developmental Biology

    Reversal of β cell de-differentiation by a small molecule inhibitor of the TGFβ pathway

    Barak Blum et al.
    Loss of mature β cell identity in diabetes can be prevented and rescued by small molecule inhibitors of the TGFβ pathway.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Structure of the SAS-6 cartwheel hub from Leishmania major

    Mark van Breugel et al.
    The X-ray structure of the SAS-6 cartwheel hub from Leishmania major demonstrates that SAS-6 can be sufficient to determine centriolar cartwheel symmetry.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Inhibition by small-molecule ligands of formation of amyloid fibrils of an immunoglobulin light chain variable domain

    Boris Brumshtein et al.
    Ligands that bind dimers of light chain variable domains inhibit the formation of amyloid fibrils.
    1. Biochemistry and Chemical Biology

    A chemical probe of CARM1 alters epigenetic plasticity against breast cancer cell invasion

    Xiao-Chuan Cai et al.
    A chemical probe was characterized for potency, selectivity, and ability to alter CARM1-dependent epigenetic plasticity against cancer cell invasion.
    1. Cancer Biology

    Renal medullary carcinomas depend upon SMARCB1 loss and are sensitive to proteasome inhibition

    Andrew L Hong et al.
    Faithful models of RMC require SMARCB1 loss for survival, and genetic and small-molecule screens identify inhibition of the ubiquitin-proteasome system (UPS) as a potential therapeutic approach for SMARCB1 deficient cancers.
    1. Biochemistry and Chemical Biology
    2. Developmental Biology

    Pharmacological targeting of the transcription factor SOX18 delays breast cancer in mice

    Jeroen Overman et al.
    A novel molecular strategy to block transcription factor activity using small molecule interference of multiple protein-protein interactions is reported.

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