Small-molecule antagonists of the oncogenic Tcf/β-catenin protein complex

By M. Lepourcelet, Y. Chen, Huisheng Wang, P. Crews, F. Petersen, C. Bruseo, A. Wood, R. Shivdasani. 2004

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Intrinsically disordered proteins in human diseases: introducing the D2 concept. (2008, background): “Small molecules from a natural-product library were screened, and a few inhibitors were found (85).”
Wnt signalling and its impact on development and cancer (2008, background): “In 2004, a high-throughput screening method to search for low-molecular-weight antagonists that target the interaction between β-catenin and TCF4 was reported, and fungal derivatives were found that suppress the transcriptional activity of β-cateni”
Wnt signaling in the intestinal epithelium: from endoderm to cancer. (2005, result): “Yet, some promising results have recently been reported by Shivdasani and colleagues (Lepourcelet et al. 2004).”
Wnt/β-catenin signaling and disease. (2012, unknown): “Indeed, though several compounds, such as PKF115-854 and CGP049090, have been suggested to target Wnt signaling at this level (Lepourcelet et al., 2004), their specificity and efficacy remain to be”
Tumour-initiating cells: challenges and opportunities for anticancer drug discovery (2009, background): “Small-molecule antagonists of the oncogenic transcription factor TCF–β-catenin protein complex have been reporte”
WNT and β-catenin signalling: diseases and therapies (2004, background): “Candidate approaches include small-molecule inhibitors that block interaction of β-catenin with TC”