2. Academic Validation
  3. A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]

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

  • Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7. doi: 10.1073/pnas.0404875101.
Katayoon H Emami 1,  Cu Nguyen,  Hong Ma,  Dae Hoon Kim,  Kwang Won Jeong,  Masakatsu Eguchi,  Randall T Moon,  Jia-Ling Teo,  Hak Yeop Kim,  Sung Hwan Moon,  Jong Ryul Ha,  Michael Kahn
Affiliations

Affiliation

  • 1 Institute for Chemical Genomics, 600 Broadway, Seattle, WA 98122, USA.
PMID: 15314234 DOI: 10.1073/pnas.0404875101
Abstract

Inherited and somatic mutations in the adenomatous polyposis coli occur in most colon cancers, leading to activation of beta-catenin-responsive genes. To identify small molecule antagonists of this pathway, we challenged transformed colorectal cells with a secondary structure-templated chemical library, looking for compounds that inhibit a beta-catenin-responsive reporter. We identified ICG-001, a small molecule that down-regulates beta-catenin/T cell factor signaling by specifically binding to cyclic AMP response element-binding protein. ICG-001 selectively induces Apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells, and is efficacious in the Min mouse and nude mouse xenograft models of colon Cancer.

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