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Showing 1–6 of 6 results
Advanced filters: Author: Petra Janning Clear advanced filters

  • Natural product–inspired compounds are primed to interact with and manipulate biological processes, but obtaining these complex molecules poses synthetic challenges. The development of a 12-step, 1-pot cascade reaction leads to the 'centrocountins', tetrahydroindoloquinolizines that modulate mitosis by targeting the centrosome-associated proteins nucleophosmin and Crm1.

    • Heiko Dückert
    • Verena Pries
    • Herbert Waldmann
    Research
    Nature Chemical Biology
    Volume: 8, P: 179-184

  • In targeted protein degradation, a degrader molecule brings a neosubstrate protein proximal to a hijacked E3 ligase for its ubiquitination. Here, pseudo-natural products derived from (−)-myrtanol—iDegs—are identified to inhibit and induce degradation of the immunomodulatory enzyme indoleamine-2,3-dioxygenase 1 (IDO1) by a distinct mechanism. iDegs prime apo-IDO1 ubiquitination and subsequent degradation using its native proteolytic pathway.

    • Elisabeth Hennes
    • Belén Lucas
    • Herbert Waldmann
    ResearchOpen Access
    Nature Chemistry
    P: 1-12

  • A probe for the ubiquitin-like protein Fubi led to the discovery of dual ubiquitin/Fubi C-terminal hydrolase activity in the deubiquitinase USP16 in addition to USP36, enabling structural characterization of this distinctive Ub/Ubl specificity, and revealed a synergistic role of USP16 in ribosomal protein maturation.

    • Rachel O’Dea
    • Nafizul Kazi
    • Malte Gersch
    ResearchOpen Access
    Nature Chemical Biology
    Volume: 19, P: 1394-1405

  • The deubiquitinase UCHL1 has been linked to cancer invasiveness and neurodegeneration yet its molecular roles have remained poorly defined. Here the authors reveal the structural basis for how UCHL1 can be specifically inhibited and how chemogenomic probes can be used to dissect its functions in living cells.

    • Christian Grethe
    • Mirko Schmidt
    • Malte Gersch
    ResearchOpen Access
    Nature Communications
    Volume: 13, P: 1-17

  • The cholesterol-transfer protein GRAMD1A is identified as the target of the autophagy inhibitors autogramin-1 and autogramin-2. GRAMD1A is found to be required for autophagosome biogenesis.

    • Luca Laraia
    • Alexandra Friese
    • Herbert Waldmann
    Research
    Nature Chemical Biology
    Volume: 15, P: 710-720