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Showing 1–3 of 3 results
Advanced filters: Author: Judit Debreczeni Clear advanced filters

  • Mutant RAS family members occur in a wide range of tumour types, and there is a great interest in identifying isoform-specific inhibitors. Here, the authors characterise two designed ankyrin repeat proteins (DARPins) that specifically inhibit the KRAS isoform by binding to the region around the KRAS-specific residue histidine 95 and show that they affect KRAS/effector interactions in different ways.

    • Nicolas Bery
    • Sandrine Legg
    • Terence H. Rabbitts
    ResearchOpen Access
    Nature Communications
    Volume: 10, P: 1-11

  • Ras is mutated in many cancers, but so far no drug targeting Ras is in clinical use despite great efforts. Here the authors structurally and functionally characterize a DARPin that potently inhibits the nucleotide exchange of Ras, which might facilitate the development of Ras-targeted therapies.

    • Sandrine Guillard
    • Paulina Kolasinska-Zwierz
    • Ralph Minter
    ResearchOpen Access
    Nature Communications
    Volume: 8, P: 1-11

  • Structural, enzymatic and cellular target engagement studies reveal the mechanism of action by N-hydroxyurea small molecule inhibitors of the DNA repair enzyme, human flap endonuclease-1 (FEN1) that prevent cleavage of DNA flaps in cancer cells.

    • Jack C Exell
    • Mark J Thompson
    • Jane A Grasby
    Research
    Nature Chemical Biology
    Volume: 12, P: 815-821