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Targeting the cancer epigenome: synergistic therapy with bromodomain inhibitors

Mahalakshmi Ramadoss1, Vijayalakshmi Mahadevan2

  • 1Centre for Nanotechnology and Advanced Biomaterials (CeNTAB), School of Chemical & Biotechnology, SASTRA University, Thanjavur, Tamil Nadu, 613401, India.

Drug Discovery Today
|September 26, 2017
PubMed

Insights

Bromodomain and extraterminal (BET) inhibitors show promise in cancer therapy by targeting epigenetic readers. Combinations with other drugs may overcome resistance and improve treatment outcomes.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Epigenetic and genomic changes drive cancer development.
  • Bromodomain (BRD) and extraterminal (BET) inhibitors are effective in clinical cancer studies.
  • BET proteins are epigenetic 'readers' crucial for gene regulation.

Purpose of the Study:

  • To review mechanisms of BET inhibition in cancer.
  • To explore synergistic combinations of BET inhibitors with other cancer drugs.
  • To highlight strategies for overcoming drug resistance and developing novel BET inhibitors.

Main Methods:

  • Literature review of BET inhibitor mechanisms.
  • Analysis of synergistic drug combinations.
  • Discussion of evolving therapeutic strategies.

Main Results:

  • BET inhibitors are effective in various cancers.
  • Combinations with HDACi, HMTi, DNMTi, kinase, Bcl-2, and proteasome inhibitors show potential.
  • Synergistic approaches may overcome drug resistance.

Conclusions:

  • BET inhibitors represent a significant advancement in epigenetic cancer therapy.
  • Combination therapies offer promising strategies to enhance efficacy and combat resistance.
  • Ongoing development of novel BET inhibitors is crucial for future cancer treatment.

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