Anti-tumor activity of Helicon inhibitors of Β-catenin-TCF interaction in patient-derived xenograft models
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YG Si, M Choi, X Han, B White, Z Wu, E Visness…
Cancer …, 2023
aacrjournals.org
Genetic and epigenetic alterations in the Wnt signaling pathway leading to constitutive activation of the driver oncogene Β-catenin occur in at least 20% of all human cancers. We have developed conformationally hyperstabilized α-helical peptides (Helicons) that bind directly to Β-catenin with picomolar affinity and block its interaction with TCF transcription factors. We describe here the characterization of anti-tumor efficacy, pharmacodynamic biomarkers and mechanism of action using multiple in vivo patient-derived xenograft (PDX) …
