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Domain-selective targeting of BET proteins in cancer and immunological diseases

Massimo Petretich1, Emmanuel H Demont2, Paola Grandi1

  • 1Cellzome GmbH, Functional Genomics R&D, GlaxoSmithKline, 69117 Heidelberg, Germany.

Current Opinion in Chemical Biology
|August 4, 2020
PubMed

Insights

Cancer and inflammation share common protein targets. Bromodomain and extraterminal domain (BET) inhibitors show promise for treating both cancer and inflammatory diseases by targeting epigenetic mechanisms.

Area of Science:

  • Oncology
  • Immunology
  • Molecular Biology

Background:

  • Cancer and inflammation are intrinsically linked, with chronic inflammation potentially driving tumor development and cancers often inducing inflammation.
  • Epigenetic mechanisms, including those involving bromodomain and extraterminal domain (BET) proteins, are crucial in cancer therapy resistance and immune modulation.
  • BET proteins regulate cell proliferation and inflammatory mediator production, making them key targets for therapeutic intervention.

Purpose of the Study:

  • To review recent pharmacological strategies targeting BET proteins for cancer and inflammatory diseases.
  • To discuss approaches inhibiting single or multiple bromodomains within the BET family.
  • To explore the potential for differentiating clinical efficacy and safety profiles of BET inhibitors.

Main Methods:

  • Review of current literature on BET inhibitors in cancer and inflammatory disease research.
  • Analysis of small molecule inhibitors targeting BET protein family members.
  • Examination of strategies for selective inhibition of specific bromodomains within the BET family.

Main Results:

  • A growing number of small molecules targeting BET protein function have been developed.
  • Inhibiting BET proteins offers a potential therapeutic avenue for both oncological and inflammatory conditions.
  • Targeting specific bromodomains may allow for a better separation of efficacy and safety signals.

Conclusions:

  • BET proteins represent a convergence point for cancer and inflammation, offering shared therapeutic targets.
  • Pharmacological inhibition of BET proteins is a rapidly advancing field with significant therapeutic potential.
  • Selective targeting of BET bromodomains may lead to improved clinical outcomes and reduced toxicity.
Keywords:
BD1BD2BETBromodomainCancerChemical probesInflammationProTACSelectivity

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