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. 2005 Sep;1(5):467-72.
doi: 10.2174/1573406054864098.

ICG-001, a novel small molecule regulator of TCF/beta-catenin transcription

Masakatsu Eguchi  1 , Cu Nguyen, Sung Chan Lee, Michael Kahn
Affiliations

ICG-001, a novel small molecule regulator of TCF/beta-catenin transcription

Masakatsu Eguchi et al. Med Chem. 2005 Sep.

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 beta-Catenin, and to activation of TCF/beta-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/beta-Catenin-responsive reporter gene. From this library we selected ICG-001 (IC50=3 microM) as a lead compound. Design and synthesis of the chemical library and some preliminary biological evaluation is described.

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