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Ref Type Journal Article
PMID (22224445)
Authors Tian W, Han X, Yan M, Xu Y, Duggineni S, Lin N, Luo G, Li YM, Han X, Huang Z, An J
Title Structure-based discovery of a novel inhibitor targeting the β-catenin/Tcf4 interaction.
Journal Vol Issue Date Pages Journal Short Title
Biochemistry 51 2 2012 Jan 17 724-31 Biochemistry
URL
Abstract Text Overactivation or overexpression of β-catenin in the Wnt (wingless) signaling pathway plays an important role in tumorigenesis. Interaction of β-catenin with T-cell factor (Tcf) DNA binding proteins is a key step in the activation of the proliferative genes in response to upstream signals of this Wnt/β-catenin pathway. Recently, we identified a new small molecule inhibitor, named BC21 (C(32)H(36)Cl(2)Cu(2)N(2)O(2)), which effectively inhibits the binding of β-catenin with Tcf4-derived peptide and suppresses β-catenin/Tcf4 driven reporter gene activity. This inhibitor decreases the viability of β-catenin overexpressing HCT116 colon cancer cells that harbor the β-catenin mutation, and more significantly, it inhibits the clonogenic activity of these cells. Down-regulation of c-Myc and cyclin D1 expression, the two important effectors of the Wnt/β-catenin signaling, is confirmed by treating HCT116 cells with BC21. This compound represents a new and modifiable potential anticancer candidate that targets β-catenin/Tcf-4 interaction.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
BC21 BC21 1 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
BC21 CTNNB1 Inhibitor 27 BC21 inhibits the interaction of CTNNB1 with TCF7L2 to block Wnt signaling, which can prevent cell proliferation and induce apoptosis (PMID: 22224445).
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
CTNNB1 mutant colorectal cancer sensitive BC21 Preclinical Actionable In a preclinical study, BC21 inhibited growth and viability of a colorectal cancer cell line with a CTNNB1 mutation and increased beta-catenin expression in culture (PMID: 22224445). 22224445