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|Ref Type||Journal Article|
|Authors||Emami KH, Nguyen C, Ma H, Kim DH, Jeong KW, Eguchi M, Moon RT, Teo JL, Kim HY, Moon SH, Ha JR, Kahn M|
|Title||A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected].|
|Journal||Proceedings of the National Academy of Sciences of the United States of America|
|Date||2004 Aug 24|
|Abstract Text||Inherited and somatic mutations in the adenomatous polyposis coli occur in most colon cancers, leading to activation of beta-catenin-responsive genes. To identify small molecule antagonists of this pathway, we challenged transformed colorectal cells with a secondary structure-templated chemical library, looking for compounds that inhibit a beta-catenin-responsive reporter. We identified ICG-001, a small molecule that down-regulates beta-catenin/T cell factor signaling by specifically binding to cyclic AMP response element-binding protein. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells, and is efficacious in the Min mouse and nude mouse xenograft models of colon cancer.|
|Molecular Profile||Treatment Approach|
|Gene Name||Source||Synonyms||Protein Domains||Gene Description||Gene Role|
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|ICG-001||ICG001|ICG 001||CTNNB1 Inhibitor 26||ICG-001 disrupts the interaction of CTNNB1 and c-AMP response element-binding protein, thereby preventing downstream CTNNB1 signaling to promote apoptosis (PMID: 15314234, PMID: 29332125, PMID: 32642722).|
|Gene||Variant||Impact||Protein Effect||Variant Description||Associated with drug Resistance|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|APC inact mut||colon cancer||sensitive||ICG-001||Preclinical||Actionable||In a preclinical study, ICG-001 decreased cell proliferation in colon cancer cell lines and in mouse models carrying APC inactivating mutations (PMID: 15314234).||15314234|