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Showing 1–4 of 4 results
Advanced filters: Author: Michael A. Prakesch Clear advanced filters

  • The BRCC36 isopeptidase complex (BRISC) is a deubiquitylase that stabilizes interferon receptors, driving inflammation. We discovered ‘BRISC molecular glue’ inhibitors (BLUEs) that selectively inactivate BRISC, promoting interferon receptor ubiquitylation and degradation to dampen immune responses.

    • Francesca Chandler
    • Poli Adi Narayana Reddy
    • Elton Zeqiraj
    ResearchOpen Access
    Nature Structural & Molecular Biology
    Volume: 32, P: 1812-1824

  • A high-throughput small-molecule drug screening platform enabled the detection of compounds targeting the functional interactions of receptor tyrosine kinases and identifies four new EGFR triple-mutant inhibitors.

    • Punit Saraon
    • Jamie Snider
    • Igor Stagljar
    Research
    Nature Chemical Biology
    Volume: 16, P: 577-586

  • A PROTAC termed P4B targeting BRAF V600E mutant has been developed, which displays enhanced inhibitory function in cell lines carrying BRAF mutations that impart resistance to conventional BRAF inhibitors.

    • Ganna Posternak
    • Xiaojing Tang
    • Frank Sicheri
    Research
    Nature Chemical Biology
    Volume: 16, P: 1170-1178

  • Modulation of the unfolded protein response by targeting IRE1 has several potential therapeutic applications. Here, the authors provide a first structural view of inhibitors engaging the RNase-active site of IRE1 that suggests avenues towards the generation of analogues with increased potency and selectivity.

    • Mario Sanches
    • Nicole M. Duffy
    • Frank Sicheri
    Research
    Nature Communications
    Volume: 5, P: 1-16