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Showing 1–3 of 3 results
Advanced filters: Author: Andreas L. Marzinzik Clear advanced filters

  • In this work, Beyer and colleagues have utilized display screening technologies to comprehensively chart RAS proteins “druggability” and in doing so unravel a targetable ligand-induced pocket in RAS opening unprecedented anti-RAS targeted opportunities.

    • Kim S. Beyer
    • Jessica Klein
    • Sauveur-Michel Maira
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-15

  • The selective allosteric ABL1 inhibitor ABL001 (asciminib) represents a new inhibitory mechanism for BCR–ABL1-driven malignancies, and its efficacy and evolving mechanisms of resistance do not overlap with those of other BCR–ABL1 kinase inhibitors.

    • Andrew A. Wylie
    • Joseph Schoepfer
    • William R. Sellers
    Research
    Nature
    Volume: 543, P: 733-737

  • 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