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

[ Vol. 1 , Issue. 5 ]

Author(s):

M. Eguchi, C. Nguyen, S. C. Lee and M. Kahn   Pages 467 - 472 ( 6 )

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

Affiliation:

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



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