Sven Hennig and colleagues published on covalent bicyclization of quaternary protein complexes

Congratulations to our member Sven Hennig and his colleagues Tom Grossmann (Biomimetic Chemistry) from the Vrije Universiteit Amsterdam and Saskia Neubacher (incircular) for the publications on the covalent bicyclization of quaternary protein complexes in Chem. Great work in which they show not only the successful crosslinking and stabilization of the Pseudomonas fluorescens esterase (Pfe) trimer via the INCYPRO technology, but also solved its crystal structure (PDB ID 8pi1).

Congratulations to Daan and Tassos!

Lately we have noticed that two of our members have something to celebrate!

Daan Swarts has received a NWO Vidi grant for continuing his work on the origin and evolution of RNA silencing pathways. We are looking forward to exciting science that will be funded by this grant. Congratulations, we are looking forward to the science to come! In case young scientist are interested in contributing to this work, according to Twitter positions will open soon.

Also, we congratulate Anastassis (Tassos) Perrakis, who has been elected as a member of EMBO joining leading researchers in the field of life sciences in Europe and beyond.

From the lab: ERC grant

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.

https://onlinelibrary.wiley.com/cms/asset/cea8b02f-4a06-4b65-a926-69b39c2048ca/anie202102082-toc-0001-m.jpg
Development of a bicyclic β-hairpin structure that binds the transcriptional coactivator β-catenin (Wendt et al. Angewandte Chemie, 2021).