Targeting Bet Bromodomains In Hematological Malignancies

Proteins from the BET (Bromodomain and Extra Terminal domain) family regulate gene expression through the control of transcriptional elongation by distant elements known as enhancers. Functional screens and chemical synthesis of BET bromodomain inhibitors have helped uncover the crucial role of BET proteins in the execution of the oncogenic program in numerous malignancies, including MYC-induced lymphomas and acute myeloid leukemias with MLL rearrangements. Here we review the recent advances in the understanding of the role of BET proteins in epigenetic regulation of normal and cancer cells and the wealth of pre-clinicial results of BET bromodomain inhibitors in hematological malignancies.