13 results found
    1. Cell Biology
    2. Physics of Living Systems

    A high-throughput platform for single-molecule tracking identifies drug interaction and cellular mechanisms

    David Trombley McSwiggen, Helen Liu ... Hilary P Beck
    Single-molecule tracking at scale, analyzing millions of cells and thousands of compounds per day, demonstrates that measuring protein motion provides mechanistic insights relevant to drug discovery.
    1. Cell Biology

    Formation of a giant unilocular vacuole via macropinocytosis-like process confers anoikis resistance

    Jeongsik Kim, Dahyun Kim ... Dae-Sik Lim
    Formation of a giant unilocular vacuole through a macropinocytosis-like process in cells with disrupted actin cytoskeleton promotes resistance to anoikis.
    1. Immunology and Inflammation

    Nociceptor Neurons Control Pollution-Mediated Neutrophilic Asthma

    Jo-Chiao Wang, Theo Crosson ... Sebastien Talbot
    Not revised
    Reviewed Preprint v1
    • Valuable
    • Solid
    1. Structural Biology and Molecular Biophysics

    Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors

    Marc Kschonsak, Christine C Jao ... John C Tellis
    Cryogenic electron microscopy enables real-time structure-based drug design to advance the discovery of novel classes of small molecule inhibitors.
    1. Cancer Biology
    2. Chromosomes and Gene Expression

    eRNA profiling uncovers the enhancer landscape of oesophageal adenocarcinoma and reveals new deregulated pathways

    Ibrahim Ahmed, Shen-Hsi Yang ... Andrew D Sharrocks
    eRNAs detected in patient-derived transcriptomic data can delineate potential active enhancer regions in oesophageal adenocarcinoma and uncover genes associated with the cancer phenotype.
    1. Biochemistry and Chemical Biology
    2. Cancer Biology

    Stereospecific lasofoxifene derivatives reveal the interplay between estrogen receptor alpha stability and antagonistic activity in ESR1 mutant breast cancer cells

    David J Hosfield, Sandra Weber ... Sean W Fanning
    Effective antiestrogens engage a new structural interaction to improve therapeutic antagonism in hormone-resistant breast cancer cells expressing Y537S estrogen receptor alpha.
    1. Structural Biology and Molecular Biophysics

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

    Raji E Joseph, Neha Amatya ... Amy Andreotti
    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. Chromosomes and Gene Expression

    Genome-wide alterations of uracil distribution patterns in human DNA upon chemotherapeutic treatments

    Hajnalka L Pálinkás, Angéla Békési ... Beáta G Vértessy
    Human genomic DNA contains uracil in the late replicating, constitutive heterochromatic regions, while treatment with drugs perturbing thymidylate biosynthesis shifts the uracil distribution pattern towards the euchromatin in UNG-inhibited cells.
    1. Cancer Biology

    The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells

    Sean W Fanning, Rinath Jeselsohn ... Geoffrey L Greene
    Bazedoxifene's SERD activities enable it to resist the impact of activating ESR1 mutations in breast cancer.

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