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Updated: Dec 7, 2025

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

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Bromodomain inhibitors a decade later: a promise unfulfilled?

Monica M Mita1, Alain C Mita2

  • 1The Samuel Oschin Comprehensive Cancer Institute, Cedars-Sinai Medical Center, Los Angeles, CA, USA.

British Journal of Cancer
|September 29, 2020
PubMed

Insights

Bromodomain inhibitors show promise as cancer drugs but face clinical development hurdles. This review explores challenges and opportunities for advancing these targeted therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Bromodomain inhibitors represent a significant advancement in targeted cancer therapy.
  • Despite promising preclinical data, clinical translation has been challenging.
  • Regulatory approval pathways for these novel agents require careful consideration.

Discussion:

  • Key obstacles include identifying optimal patient populations and managing on-target, off-tumor toxicities.
  • Understanding resistance mechanisms is crucial for sustained therapeutic efficacy.
  • Biomarker development is essential for patient stratification and treatment selection.

Key Insights:

  • Bromodomain inhibitors offer a targeted approach to cancer treatment by modulating epigenetic readers.
  • Clinical efficacy has been limited by dose-limiting toxicities and lack of predictive biomarkers.
  • Overcoming these challenges requires a multidisciplinary approach involving basic science, clinical oncology, and regulatory expertise.

Outlook:

  • Future directions include developing next-generation inhibitors with improved selectivity and safety profiles.
  • Combination strategies with other anticancer agents may enhance therapeutic outcomes.
  • Continued research into bromodomain function in cancer will uncover new therapeutic opportunities.

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