Targeting BET bromodomain proteins in solid tumors
- Oncotarget. 2016 Aug 16;7(33):53997-54009. doi: 10.18632/oncotarget.9804.
- 1. Department of Medicine, University of Michigan Medical Center, Ann Arbor, MI, USA.
- 2. Dana-Farber Cancer Institute and Harvard Medical School, Boston, MA, USA.
- 3. Department of Medicine, Feinberg School of Medicine, Northwestern University, Chicago, IL, USA.
- 4. The Robert H. Lurie Comprehensive Cancer Center of Northwestern University, Chicago, IL, USA.
- 5. Jesse Brown VA Medical Center, Chicago, IL, USA.
There is increasing interest in inhibitors targeting BET (bromodomain and extra-terminal) proteins because of the association between this family of proteins and Cancer progression. BET inhibitors were initially shown to have efficacy in hematologic malignancies; however, a number of studies have now shown that BET inhibitors can also block progression of non-hematologic malignancies. In this Review, we summarize the efficacy of BET inhibitors in select solid tumors; evaluate the role of BET proteins in mediating resistance to current targeted therapies; and consider potential toxicities of BET inhibitors. We also evaluate recently characterized mechanisms of resistance to BET inhibitors; summarize ongoing clinical trials with these inhibitors; and discuss potential future roles of BET inhibitors in patients with solid Tumors.