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Showing 1–5 of 5 results
Advanced filters: Author: Marko Cigler Clear advanced filters

  • Covalent inhibitors are powerful entities in drug discovery. Now the amino acid selectivity and reactivity of a diverse electrophile library have been assessed proteome-wide using an unbiased workflow. This comparative analysis and the probes described could help guide the discovery and design of covalent ligands targeting residues beyond cysteine.

    • Patrick R. A. Zanon
    • Fengchao Yu
    • Stephan M. Hacker
    ResearchOpen Access
    Nature Chemistry
    Volume: 17, P: 1712-1721

  • Targeted protein degradation (TPD) has emerged as a new paradigm for modulating protein activity. Here, the authors develop bifunctional degraders combining a putative ligand of the autophagy-related LC3 protein with different protein targets, which direct proteins of interest to the proteasome by covalently targeting the DCAF11 E3 ligase substrate receptor.

    • Gang Xue
    • Jianing Xie
    • Herbert Waldmann
    ResearchOpen Access
    Nature Communications
    Volume: 14, P: 1-13

  • Detailed analysis of the structure–activity relationship for cyclin K degraders reveals diverse compounds that acquire glue activity through simultaneous binding to the CDK12 kinase pocket and engagement of several key DDB1 interfacial residues.

    • Zuzanna Kozicka
    • Dakota J. Suchyta
    • Nicolas H. Thomä
    ResearchOpen Access
    Nature Chemical Biology
    Volume: 20, P: 93-102