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Showing 1–5 of 5 results
Advanced filters: Author: Jark Böttcher Clear advanced filters

  • Citizen science taps the efforts of non-experts. Here, authors describe Drugit, an extension of the crowdsourcing game Foldit, and its use in designing a non-peptide binder of Von Hippel Lindau E3 ligase for use with proteolysis targeting chimeras.

    • Thomas Scott
    • Christian Alan Paul Smethurst
    • Rocco Moretti
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-11

  • A chemical probe BI-9321 for the PWWP1 domain of NSD3 and its inactive analog were identified. BI-9321 binds to the methyl-lysine binding site, reduces the association of NSD3 with chromatin and inhibits proliferation of acute myeloid leukemia cells.

    • Jark Böttcher
    • David Dilworth
    • Darryl B. McConnell
    Research
    Nature Chemical Biology
    Volume: 15, P: 822-829

  • A non-covalent inhibitor that binds preferentially to the inactive state of KRAS while sparing NRAS and HRAS is reported, indicating that most KRAS oncoproteins cycle between an active state and an inactive state in cancer cells.

    • Dongsung Kim
    • Lorenz Herdeis
    • Piro Lito
    ResearchOpen Access
    Nature
    Volume: 619, P: 160-166

  • The full-length structure of HUWE1 reveals the bipartite organization of a giant E3 ubiquitin ligase, comprising a catalytic HECT domain and a large, ring-shaped scaffold that provides docking sites for various substrates and regulates E3 activity.

    • Daniel B. Grabarczyk
    • Olga A. Petrova
    • Tim Clausen
    Research
    Nature Chemical Biology
    Volume: 17, P: 1084-1092

  • Six WWE domain-containing proteins also contain domains with E3 ubiquitin ligase activity. We report structures, biophysical and biochemical assays for the discovery of novel WWE domain binders and their respective application.

    • Lena Münzker
    • Serah W. Kimani
    • Jark Böttcher
    ResearchOpen Access
    Communications Biology
    Volume: 7, P: 1-15