期刊论文Discovery of a HeliconTM peptide inhibitor of the beta-catenin-TCF interaction with in vivo activity复制

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BH White, Y Si, S Cappucci, Z Li, JD Ramirez…
Cancer …, 2023
aacrjournals.org
Wnt signaling pathway mutations leading to constitutive activation of the driver oncogene β-catenin occur in at least 20% of all human cancers, but β-catenin itself has remained undruggable by traditional modalities. In order to inhibit the activity of β-catenin, we have developed conformationally hyperstabilized α-helical peptides (Helicons) that are cellularly permeable and bind directly to β-catenin in order to block its interaction with TCF family of transcription factors. Starting with a helical peptide derived from phage display, a …