Targeting HIF-1α

    Mechanism Comment
    Inhibitors of HIF-1a protein translation
    Wortmannin PI3K inhibitors PI3K pathway plays a major role in upregulation of HIF-1 in ∼70% of cancer cells
    LY294002
    Camptothecin Topoisomerase I and II inhibitors Inhibition of topoisomerase I activity associated with HIF-1-dependent gene expression
    Topotecan
    2-Methoxyestradiol (2ME2) Microtubule disrupting agents 2ME2 is a naturally occurring estrogen metabolite and causes mitotic arrest in cancer cells via microtubule depolymerization and inhibition of downstream HIF-1 translation
    Inhibitors of HIF-1a protein degradation
    Geldanamycin Hsp90 inhibitors Hsp90 interacts with HIF-1a and is required for HIF-1a protein stability
    Vorinostat
    Other topics in Molecular Targets and Pathways