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    DRUG:

    ARN22089

    i
    Other names: ARN22089
    Company:
    University of California
    Drug class:
    CDC42 inhibitor
    Related drugs:
    over2years
    Design, Synthesis, In Vitro and In Vivo Characterization of CDC42 GTPase Interaction Inhibitors for the Treatment of Cancer. (PubMed, J Med Chem)
    Recently, we reported the discovery of a novel lead compound, ARN22089, which blocks the interaction of CDC42 GTPases with specific downstream effectors...We discovered and optimized two novel inhibitors (27, ARN25062, and 28, ARN24928), which are optimal back-up/follow-up leads with favorable drug-like properties and in vivo efficacy in PDX tumors. These findings further demonstrate the potential of this class of CDC42/RHOJ inhibitors for cancer treatment, with lead candidates ready for advanced preclinical studies.
    Preclinical • Journal
    |
    BRAF (B-raf proto-oncogene) • CDC42 (Cell Division Cycle 42) • RHOJ (Ras Homolog Family Member J)
    |
    BRAF mutation
    |
    ARN22089
    over3years
    Structure-based design of CDC42 effector interaction inhibitors for the treatment of cancer. (PubMed, Cell Rep)
    ARN22089 selectively blocks CDC42 effector interactions without affecting the binding between closely related GTPases and their downstream effectors. Taken together, we identify a class of therapeutic agents that influence tumor growth by modulating CDC42 signaling in both the tumor cell and its microenvironment.
    Journal
    |
    BRAF (B-raf proto-oncogene)
    |
    BRAF mutation
    |
    ARN22089