Targeting bet bromodomain proteins in solid tumors

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

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

51 Scopus citations

Abstract

There is increasing interest in inhibitors targeting BET (bromodomain and extraterminal) 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.

Original languageEnglish (US)
Pages (from-to)53997-54009
Number of pages13
JournalOncotarget
Volume7
Issue number33
DOIs
StatePublished - Aug 1 2016

Keywords

  • Brain tumors
  • Breast and prostate cancers
  • Gastrointestinal cancers
  • Lung cancers
  • NUT midline carcinoma

ASJC Scopus subject areas

  • Oncology

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