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Targeting BET bromodomain proteins in solid tumors

Vaibhav Sahai1, Amanda J Redig2, Katharine A Collier3

  • 1Department of Medicine, University of Michigan Medical Center, Ann Arbor, MI, USA.

Oncotarget
|June 11, 2016
PubMed

Insights

Bromodomain and extra-terminal (BET) inhibitors show promise in treating various cancers, including solid tumors. This review covers their efficacy, resistance mechanisms, and future potential in oncology.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Increasing interest in bromodomain and extra-terminal (BET) protein inhibitors due to their link to cancer progression.
  • Initial efficacy demonstrated in hematologic malignancies, with emerging evidence in solid tumors.
  • BET proteins play a critical role in cancer cell proliferation and survival.

Approach:

  • Reviewing the efficacy of BET inhibitors in various solid tumors.
  • Evaluating the role of BET proteins in acquired resistance to targeted therapies.
  • Assessing potential toxicities and resistance mechanisms associated with BET inhibitors.

Key Points:

  • BET inhibitors demonstrate efficacy beyond hematologic cancers, showing potential in solid tumors.
  • Understanding BET protein function is crucial for overcoming resistance to current cancer treatments.
  • Ongoing clinical trials are exploring novel strategies and combinations involving BET inhibitors.

Conclusions:

  • BET inhibitors represent a promising therapeutic strategy for a range of solid tumors.
  • Further research into resistance mechanisms and toxicity profiles is essential for optimizing clinical use.
  • Future applications of BET inhibitors may expand to include combination therapies and personalized treatment approaches.
Keywords:
NUT midline carcinomabrain tumorsbreast and prostate cancersgastrointestinal cancerslung cancers

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