B03
Project Area B - Chemical Biology
Prof. Dr. Stefan Knapp
Pharmaceutical Chemistry
Goethe-University Germany, Frankfurt am Main
Phone: +49 170 3682 052
Email
Development of selective inhibitors and PROTACs for key signalling molecules regulating cell state transition and the cell cycle
Chemical tools, highly potent and selective chemical probes as well as molecules that lead to rapid and selective degradation of target proteins such as PROTACs (PROteolysis TArgeting Chimeras) are therefore versatile tools for cell based or in vivo studies on cell states that allow selective targeting of endogenous proteins in a time controlled manner. Our laboratory has a long standing interest in developing selective chemical tool compounds in particular targeting signalling molecules including protein kinases as well as modulators of epigenetic processes. One of the main contributions to this CRC will be therefore providing chemical probe collections tailored to studies on cell state transitions investigated by CRC groups and to develop new chemical probes and PROTACs for targets of high priority within this CRC. Projects that have been identified in the initial phase of this project comprise tailored probe sets for mitotic kinases and epigenetic modulators such as inhibitors of lysine methyltransferases, lysine deacetylases as well as bromodomains.
Project Members
Martin Schwalm
Janik Weckesser
Publications
-
Toward effective Atg8-based ATTECs : Approaches and perspectivesIn: Journal of Cellular Biochemistry (2023) in pressOnline Full Text: dx.doi.org/ (Open Access)
-
Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimizationIn: Cell Chemical Biology Vol. 30 (2023) Nr. 7, pp. 753 - 765.e8Online Full Text: dx.doi.org/ Online Full Text (Open Access)
-
A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing ProteinsIn: Frontiers in Cell and Developmental Biology Vol. 10 (2022) 886537Online Full Text: dx.doi.org/ (Open Access)
-
Novel, highly potent PROTACs targeting AURORA-A kinaseIn: Current Research in Chemical Biology Vol. 2 (2022) 100032Online Full Text: dx.doi.org/ (Open Access)
-
PROTAC degraders as chemical probes for studying target biology and target validationIn: Chemical Society Reviews Vol. 51 (2022) Nr. 18, pp. 7971 - 7993Online Full Text: dx.doi.org/