Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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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

Affiliation: Institute for Chemical Genomics, 600 Broadway, Suite 580, Seattle, WA 98122, USA.

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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Article Details

VOLUME: 1
ISSUE: 5
Page: [467 - 472]
Pages: 6
DOI: 10.2174/1573406054864098