Journal
MEDICINAL CHEMISTRY
Volume 1, Issue 5, Pages 467-472Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1573406054864098
Keywords
Peptidomimetics; Anti-cancer; Wnt Pathway; beta-Catenin
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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 mu M) as a lead compound. Design and synthesis of the chemical library and some preliminary biological evaluation is described.
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