Targeting Epigenetics in Cancer

    • Histone acetylation occurs on lysine residues on the histone tail and is associated with transcription activation. It is catalyzed by competing enzymes such as histone lysine acetyltransferases (HATs) and histone deacetylases (HDACs).
      • HDAC inhibitors induce reexpression of tumor suppressors such as p21, p53, and NF-kB. Vorinostat, belinostat, and romidepsin are FDA-approved HDAC inhibitors for T-cell lymphoma. Panobinostat is another FDA-approved HDAC inhibitor in treating multiple myeloma.
      • Bromodomain and extraterminal proteins (BET) is a subfamily of bromodomains, which are histone acetylation readers. BET is a key player in transcriptional elongation and cell antitumor effects in NUT-midline carcinoma and hematologic malignancies in clinical trials.
    Other topics in Molecular Targets and Pathways