ICG-001, A Novel Small Molecule Regulator of TCF/β-Catenin Masakatsu Transcription

Title: ICG-001, A Novel Small Molecule Regulator of TCF/β-Catenin Masakatsu Transcription

Volume: 1 Issue: 5

Author(s): M. Eguchi, C. Nguyen, S. C. Lee and M. Kahn

Affiliation:

Keywords: peptidomimetics, anti-cancer, wnt pathway, catenin

Abstract: Inherited and somatic mutations in the APC gene, a human tumor-suppressor, occur in a large percentage of colon cancers, leading to elevated levels of nuclear β-Catenin, and to activation of TCF/ β-Catenin-responsive genes including cyclin D1 and c-myc. To identify small molecule antagonists of this pathway, we screened transformed colorectal cells with a secondary structure-templated chemical library, in search of compounds that attenuated a TCF/ β- Catenin-responsive reporter gene. From this library we selected ICG-001 (IC50 = 3 M) as a lead compound. Design and synthesis of the chemical library and some preliminary biological evaluation is described.

Cite this article as:

Eguchi M., Nguyen C., Lee C. S. and Kahn M., ICG-001, A Novel Small Molecule Regulator of TCF/β-Catenin Masakatsu Transcription, Medicinal Chemistry 2005; 1 (5) . https://dx.doi.org/10.2174/1573406054864098