We (Sven Hennig and his team) are very excited to be part of Tom Grossmann’s project of fighting colorectal cancer using peptidomimetics. Tom just received an ERC PoC grant which is accelerating the kick-off for this endeavor. Together we have identified a family of peptidomimetic agents that bind beta-catenin and inhibit its interaction with the TCF/LEF transcription factors . For the first time, it was possible to obtain a crystal structure of a synthetic molecule bound to a therapeutically very attractive site on beta-catenin. In addition, we have confirmed cellular activity of these inhibitors verifying selective inhibition of the Wnt signalling pathway (Wendt et al. Angewandte Chemie, 2021, https://doi.org/10.1002/anie.202102082). These findings provide the ideal starting point for the development of novel therapeutics for Wnt-dependent cancers, in particular for CRC. Press: https://www.eurekalert.org/news-releases/767299.
proCOLON: ERC Proof-of-Concept granted to investigate first-in-class beta-catenin inhibitors as treatment for colorectal cancer.