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Showing 1–5 of 5 results
Advanced filters: Author: Trupta Purohit Clear advanced filters

  • The histone methyltransferase ASH1L plays a role in various diseases, including cancer, and has been validated as a therapeutic target; however, no inhibitors of ASH1L have been reported. Here the authors present small molecule inhibitors of ASH1L and demonstrate their on-target activity in leukemia cells and a mouse model of leukemia.

    • David S. Rogawski
    • Jing Deng
    • Jolanta Grembecka
    ResearchOpen Access
    Nature Communications
    Volume: 12, P: 1-14

  • Fragment screening and medicinal chemistry optimization led to development of a small-molecule inhibitor of RING1B–BMI1 E3 ligase, blocking the H2A ubiquitination activity of the Polycomb repressive complex 1 and inducing differentiation in leukemia cells.

    • Shirish Shukla
    • Weijiang Ying
    • Tomasz Cierpicki
    Research
    Nature Chemical Biology
    Volume: 17, P: 784-793

  • An irreversible small-molecule inhibitor of histone methyltransferase NSD1 is developed, which binds covalently to the C2062 residue in the catalytic SET domain and represses H3K36 dimethylation and target gene expression in leukemia cells.

    • Huang Huang
    • Christina A. Howard
    • Tomasz Cierpicki
    Research
    Nature Chemical Biology
    Volume: 16, P: 1403-1410

  • MLL fusion genes often encode leukemogenic proteins that depend on interaction with menin, a component of the MLL SET1-like histone methyltransferase complex. MI-2 and MI-3 are the first small molecules that can block menin–MLL fusion protein interaction and their oncogenic effects in cells.

    • Jolanta Grembecka
    • Shihan He
    • Tomasz Cierpicki
    Research
    Nature Chemical Biology
    Volume: 8, P: 277-284