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Targeting Cancer Cells with BET Bromodomain Inhibitors

Yali Xu1, Christopher R Vakoc1

  • 1Cold Spring Harbor Laboratory, Cold Spring Harbor, New York 11724.

Cold Spring Harbor Perspectives in Medicine
|February 19, 2017
PubMed

Insights

Targeting bromodomain and extraterminal (BET) proteins, key transcriptional regulators, shows promise in cancer therapy. BET inhibitors suppress cancer-promoting genes, offering a potential new treatment strategy with tolerable side effects.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Genetics

Background:

  • Cancer cells exhibit unique vulnerabilities to transcriptional regulator targeting.
  • The bromodomain and extraterminal (BET) family of proteins are crucial coactivators in gene expression.
  • BET proteins link acetylated factors to RNA polymerase II activation, playing a role in malignant transformation.

Purpose of the Study:

  • To review the therapeutic effects of targeting BET bromodomains in cancer.
  • To explore the mechanisms and specificity of BET protein function in cancer.
  • To discuss the clinical relevance of BET inhibitors in cancer treatment.

Main Methods:

  • Review of existing literature on BET inhibitors in cancer.
  • Analysis of preclinical (animal) studies on BET inhibition.
  • Examination of clinical trial data (Phase I) for BET inhibitors in human cancer patients.

Main Results:

  • BET inhibitors preferentially suppress the transcription of cancer-promoting genes.
  • Anticancer activity of BET inhibitors observed in various malignant contexts.
  • BET inhibition demonstrates tolerable side effects in normal tissues, supported by clinical trials.

Conclusions:

  • BET bromodomain inhibition represents a significant therapeutic vulnerability in human cancer.
  • BET inhibitors elicit potent anticancer activity, offering a promising new avenue for cancer treatment.
  • Further research into the mechanisms of BET protein function can refine therapeutic strategies.

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