Targeting BET Bromodomains in Cancer

Cancer is frequently dependent on aberrant gene expression programs that might be vulnerable to targeting with novel therapeutics. Bromodomain and extraterminal domain (BET) proteins are powerful transcriptional coregulators often found as part of oncogenic programs. The bromodomain functionality BET highly druggable, several product candidates in clinical testing. While initial data created doubt about their benefit for cancer patients, more encouraging recently reported myelofibrosis patients may promote additional applications inhibitors oncology monotherapy combination other therapeutic agents. Moreover, a growing number approaches optimize the window by tinkering property profiles provide opportunities. This review provides an update status ongoing activities exploit inhibition mechanism therapy.