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Inhibitors of NF-kappaB signaling: 785 and counting

T D Gilmore1, M Herscovitch

  • 1Biology Department, Boston University, Boston, MA 02215, USA. gilmore@bu.edu

Oncogene
|October 31, 2006
PubMed

Insights

Nuclear factor kappa B (NF-kappaB) signaling regulates key cellular processes. Over 750 inhibitors targeting this pathway, including natural and synthetic compounds, have been identified for potential therapeutic applications.

Area of Science:

  • Molecular Biology
  • Immunology
  • Pharmacology

Background:

  • Nuclear factor kappa B (NF-kappaB) transcription factors are crucial regulators of inflammation, immune responses, cell growth, and apoptosis.
  • The NF-kappaB signaling pathway is frequently dysregulated in chronic inflammatory diseases and cancer, making it a significant therapeutic target.
  • Understanding the molecular intricacies of the NF-kappaB pathway is essential for developing effective modulators.

Purpose of the Study:

  • To review the landscape of identified inhibitors targeting the NF-kappaB signaling pathway.
  • To categorize the diverse range of molecules that modulate NF-kappaB activity.
  • To discuss the therapeutic potential of NF-kappaB inhibitors in various diseases.

Main Methods:

  • Comprehensive literature review of identified NF-kappaB pathway inhibitors.
  • Classification of inhibitors based on their chemical nature (natural/synthetic) and mechanism of action.
  • Analysis of the potential applications of these inhibitors in disease treatment.

Main Results:

  • Over 750 inhibitors of the NF-kappaB pathway have been identified.
  • Inhibitors encompass a wide array of compounds, including antioxidants, peptides, small RNA/DNA, microbial/viral proteins, small molecules, and engineered polypeptides.
  • These inhibitors act at various levels, with some broadly inhibiting NF-kappaB induction and others targeting specific pathways or multiple steps.

Conclusions:

  • NF-kappaB pathway inhibitors represent a promising class of therapeutic agents for cancers, neurodegenerative, and inflammatory diseases.
  • While currently not in clinical use, specific NF-kappaB inhibitors are anticipated for future therapeutic development.
  • The therapeutic benefits of many natural products may be attributed to their NF-kappaB inhibitory properties.

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