Targeting BET bromodomain proteins in solid tumors
Metrics: PDF 2066 views | HTML 2942 views | ?
Vaibhav Sahai1, Amanda J. Redig2, Katharine A. Collier3, Frank D. Eckerdt4 and Hidayatullah G. Munshi3,4,5
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
Hidayatullah G. Munshi, email:
Keywords: NUT midline carcinoma, breast and prostate cancers, lung cancers, gastrointestinal cancers, brain tumors
Received: April 09, 2016 Accepted: May 29, 2016 Published: June 05, 2016
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.
All site content, except where otherwise noted, is licensed under a Creative Commons Attribution 3.0 License.