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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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

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

Volume 1, Issue 5, 2005

Page: [467 - 472] Pages: 6

DOI: 10.2174/1573406054864098

Price: $65

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.

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


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