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Schmalz lab - Institute for Organic Chemistry

CHEMICAL SYNTHESIS OF SMALL MOLECULES TO MODULATE PROTEIN-PROTEIN INTERACTIONS AND PROTEIN RELOCALIZATION EVENTS.

Small molecules that compete with native protein-protein interaction interfaces offer new options to modulate functional protein networks (including protein localization). This project aims at the design and chemical synthesis of small molecules, which selectively influence the cellular localization of certain proteins by competing with their natural (protein) binding partners. As the core competence of the group lies in the field of synthetic organic chemistry, the project requires intense cooperation with groups from the biological sciences (structural biology, protein biochemistry, cellular assays, etc.), thus providing a truly interdisciplinary project.

Pascal Engelhardt

PhD student since October 2020

RTG Board Member

EMail: pengelh2[at]smail.uni-koeln.de

"I am an organic chemist from Freiburg working as part of my PhD in Cologne on the development of chemical building blocks for functional biomolecules, which may be used to investigate protein relocalization or to inhibit pathological pathways such as viral infections or breast cancer metastasis. Due to my background in synthetic (bio-)organic chemistry my main fields of interest are organic synthesis, medicinal chemistry and chemical biology with a strong focus on the development of novel therapeutic strategies and molecular drug design."

Publications:

  • Synthetic α-Helical Peptides as Potential Inhibitors of the ACE2 SARS-CoV-2 Interaction. Engelhardt, P..M., Rueda, S..F., Drexelius, M., Neudörfl, J., Lauster, D., Hackenberger, C..P.R., Kühne, R., Neundorf, I. and Schmalz, H. (2022), Chembiochem. 2022 Jul 4:e202200372. doi: 10.1002/cbic.202200372. Online ahead of print. PMID: 35785462

Judith Bruns

PhD student April 2017 - February 2021

PhD Thesis: "Research on the synthesis of novel proline-derived secondary structure mimetics as potential EVH1 respectively SH3 inhibitors"

Publications

  • Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells. Barone M, Müller M, Chiha S, Ren J, Albat D, Soicke A, Dohmen S, Klein M, Bruns J, van Dinther M, Opitz R, Lindemann P, Beerbaum M, Motzny K, Roske Y, Schmieder P, Volkmer R, Nazaré M, Heinemann U, Oschkinat H, Ten Dijke P, Schmalz HG, Kühne R. Proc Natl Acad Sci U S A. 2020 Nov 24;117(47):29684-29690. doi: 10.1073/pnas.2007213117. Epub 2020 Nov 12. PMID: 33184177