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Showing 1–3 of 3 results
Advanced filters: Author: Simona Cotesta Clear advanced filters

  • High-resolution crystal structures of the rat succinate receptor SUCNR1 in an inactive confirmation, and the humanized rat SUCNR1 bound to an antagonist, provide insights into the structure of these receptors and the species selectivity of antagonist binding.

    • Matthias Haffke
    • Dominique Fehlmann
    • Veli-Pekka Jaakola
    Research
    Nature
    Volume: 574, P: 581-585

  • A chemical screen identified BET bromodomain inhibitors as promoters of keratinocyte regenerative function and skin wound healing. Specifically, low-dose transient treatment with BET inhibitors imposes an activated, migratory state in keratinocytes.

    • Gabi Schutzius
    • Christian Kolter
    • Susan Kirkland
    Research
    Nature Chemical Biology
    Volume: 17, P: 280-290

  • Although FPPS is a potential anti-cancer target, the high bone affinity of nitrogen-containing bisphosphonates, FPPS inhibitors used clinically to treat bone disease, has prevented their development as cancer therapeutics. Using fragment-based drug discovery, non-bisphosphonate inhibitors were discovered that bind in a previously undescribed allosteric pocket.

    • Wolfgang Jahnke
    • Jean-Michel Rondeau
    • Jonathan R Green
    Research
    Nature Chemical Biology
    Volume: 6, P: 660-666