Targeting BET bromodomain proteins in solid tumors

Vaibhav Sahai; Amanda J. Redig; Katharine A. Collier; Frank D. Eckerdt; Hidayatullah G. Munshi

doi:10.18632/oncotarget.9804

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Targeting BET bromodomain proteins in solid tumors

Vaibhav Sahai, Amanda J. Redig, Katharine A. Collier, Frank D. Eckerdt and Hidayatullah G. Munshi _

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Oncotarget. 2016; 7:53997-54009. https://doi.org/10.18632/oncotarget.9804

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Abstract

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

Correspondence to:

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

Abstract

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.

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Targeting BET bromodomain proteins in solid tumors

Abstract