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A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]

Katayoon H Emami1, Cu Nguyen, Hong Ma

  • 1Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122, USA.

Proceedings of the National Academy of Sciences of the United States of America
|August 18, 2004
PubMed

Insights

A novel compound, ICG-001, targets beta-catenin signaling by binding to cyclic AMP response element-binding protein. This colon cancer drug selectively kills cancer cells while sparing normal cells, showing promise in preclinical models.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Mutations in adenomatous polyposis coli (APC) are common in colon cancer, activating beta-catenin-responsive genes.
  • This aberrant signaling pathway drives tumor growth and proliferation.

Purpose of the Study:

  • To identify small molecule antagonists targeting the beta-catenin pathway.
  • To discover compounds that selectively inhibit cancer cell growth.

Main Methods:

  • Screening a chemical library against a beta-catenin-responsive reporter in colorectal cancer cells.
  • Identifying ICG-001 and characterizing its mechanism of action.
  • Evaluating ICG-001 efficacy in vitro and in vivo (Min mouse and xenograft models).

Main Results:

  • ICG-001 was identified as a specific inhibitor of beta-catenin/T cell factor signaling.
  • ICG-001 selectively induces apoptosis in transformed colon cells, not normal cells.
  • The compound demonstrated efficacy in reducing tumor growth in preclinical cancer models.

Conclusions:

  • ICG-001 represents a promising therapeutic agent for colon cancer.
  • Targeting the beta-catenin pathway with specific inhibitors like ICG-001 offers a selective approach to cancer treatment.

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