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BET Bromodomain Proteins as Cancer Therapeutic Targets

Shaokun Shu1, Kornelia Polyak1

  • 1Department of Medical Oncology, Dana-Farber Cancer Institute; Department of Medicine, Brigham and Women's Hospital; and Department of Medicine, Harvard Medical School, Boston, Massachusetts 02215.

Cold Spring Harbor Symposia on Quantitative Biology
|January 8, 2017
PubMed

Insights

BET bromodomain inhibitors show promise for treating cancers by targeting oncogenic transcription factors. However, understanding resistance mechanisms is crucial for effective cancer therapy.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Epigenetic regulators are key targets in cancer therapy.
  • BET bromodomain proteins regulate oncogenic transcription factors like MYC.
  • Inhibiting BET proteins offers a strategy against

Purpose of the Study:

  • Review the role of BET bromodomain proteins in tumorigenesis.
  • Summarize mechanisms of therapeutic response and resistance to BET inhibitors.
  • Focus on BRD4 and breast cancer.

Main Methods:

  • Literature review of epigenetic regulators in cancer.
  • Analysis of BET bromodomain protein function.
  • Examination of clinical development and resistance mechanisms of BET inhibitors.

Main Results:

  • BET bromodomain inhibitors are in clinical trials with promising results.
  • Tumors develop diverse resistance mechanisms to BET inhibitors.
  • BRD4 plays a significant role in breast cancer.

Conclusions:

  • BET bromodomain inhibition is a viable therapeutic strategy for various cancers.
  • Further research into resistance mechanisms is essential for optimizing BET inhibitor efficacy.
  • BRD4 and BET proteins are critical in breast cancer development and treatment.

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