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Showing 1–7 of 7 results
Advanced filters: Author: Klaus Rumpel Clear advanced filters

  • Structural and biochemical characterization of arginine kinase McsB reveals how its phosphagen kinase–like catalytic domain is adapted to target protein substrates while its phosphoarginine-binding domain allosterically controls kinase activity.

    • Marcin J. Suskiewicz
    • Bence Hajdusits
    • Tim Clausen
    Research
    Nature Chemical Biology
    Volume: 15, P: 510-518

  • Antimicrobial resistance is a global health threat and the development of alternative strategies to overcome it is of high interest. Here, the authors report proteolysis targeting chimeras active in bacteria (BacPROTACs) that bind to ClpC1, a component of the mycobacterial protein degradation machinery, and apply them for targeting a range of mycobacterial strains, including antibiotic-resistant ones.

    • Lukas Junk
    • Volker M. Schmiedel
    • Guido Boehmelt
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-15

  • Protein degraders are an emerging drug modality; however, their properties lie beyond typical drug-like space. Here the authors report optimisation via structure-based exit vector and linker design towards the VHL-recruiting PROTAC ACBI2, an orally bioavailable and selective degrader of SMARCA2.

    • Christiane Kofink
    • Nicole Trainor
    • William Farnaby
    ResearchOpen Access
    Nature Communications
    Volume: 13, P: 1-15

  • 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

  • Unpredicted aversive experiences activate DA neurons in dorsal tegmentum; these neurons are important for fear learning. This prediction-error circuit module linking amygdala and dorsal tegmentum enables a solution to an associative learning problem.

    • Florian Groessl
    • Thomas Munsch
    • Wulf Haubensak
    Research
    Nature Neuroscience
    Volume: 21, P: 952-962