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Targeting BET bromodomains for cancer treatment

Marie Jung1,2, Kathy A Gelato1, Amaury Fernández-Montalván1

  • 1Global Drug Discovery, Bayer Pharma AG, D-13353 Berlin, Germany.

Epigenomics
|June 17, 2015
PubMed

Insights

Bromodomain and extraterminal (BET) proteins, particularly BRD4, are key targets in cancer therapy. BET inhibitors show promise in treating leukemia and lymphoma, with ongoing clinical studies reporting encouraging efficacy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The bromodomain and extraterminal (BET) protein family is a novel target in cancer research.
  • BRD4, a key BET protein, plays a crucial role in the transcription of genes vital for cell cycle and apoptosis, such as c-Myc and BCL2.
  • Dysregulation of BRD4 is implicated in various hematological and solid tumors.

Purpose of the Study:

  • To discuss the biological functions of BRD4 and its interaction partners.
  • To review the involvement of BRD4 in different cancer types.
  • To summarize the current landscape of BET bromodomain inhibitors for cancer treatment.

Main Methods:

  • Literature review of BRD4 biology and function.
  • Analysis of preclinical cancer models treated with BET inhibitors.
  • Summary of clinical trial data for BET inhibitors in leukemia and lymphoma.

Main Results:

  • BRD4's role in transcriptional regulation is critical for cancer cell proliferation and survival.
  • Preclinical studies demonstrate significant antitumor activity of BET inhibitors.
  • Early clinical trials in leukemia and lymphoma show promising efficacy signals.

Conclusions:

  • BRD4 is a validated therapeutic target in oncology.
  • BET inhibitors represent a promising class of anti-cancer drugs.
  • Further clinical development of BET inhibitors is warranted for various malignancies.
Keywords:
BET inhibitorBRD4bromodomainc-Mycchromatintranscription control

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