^
    2years
    Combined inhibition of BET bromodomain and mTORC1/2 provides therapeutic advantage for rhabdomyosarcoma by switching cell death mechanism. (PubMed, Mol Carcinog)
    Thus, the bromodomain inhibitor RVX-208 significantly augmented the therapeutic effects of the dual mTORC1/2 inhibitors, OSI-027 and PP242, both in vitro and in a human xenograft murine model. While single RVX-208 treatment induces apoptosis and a single mTORC1/2 inhibitor induces macropinocytosis, their combined treatment led to necroptosis-mediated cell death. These data suggest that combined treatment with drugs targeting BRD4 and mTORC1/2 may be an effective therapeutic intervention for drug-resistant RMS.
    Journal
    |
    CCND1 (Cyclin D1) • BRD4 (Bromodomain Containing 4)
    |
    CCND1 expression
    |
    AVTX-006 • torkinib (PP242) • apabetalone (RVX 208)
    over2years
    ABCA1 is associated with the development of acquired chemotherapy resistance and predicts poor ovarian cancer outcome. (PubMed, Cancer Drug Resist)
    Apabetalone treatment reduced ABCA1 protein expression and increased the sensitivity of both parental and carboplatin-resistant ovarian cancer cells to carboplatin. These results suggest that inhibiting ABCA1 transporter may be useful in overcoming acquired chemotherapy resistance and improving outcome for patients with HGSOC.
    Journal
    |
    ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC2 (ATP Binding Cassette Subfamily C Member 2)
    |
    ABCG2 expression
    |
    carboplatin • apabetalone (RVX 208)