© Knapp

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

Publications

    Journal articles

  • Schwalm, Martin P.; Knapp, Stefan; Rogov, Vladimir V.
    Toward effective Atg8-based ATTECs : Approaches and perspectives
    In: Journal of Cellular Biochemistry (2023) in press
  • Schwalm, Martin P.; Krämer, Andreas; Dölle, Anja; Weckesser, Janik; Yu, Xufen; Jin, Jian; Saxena, Krishna; Knapp, Stefan
    Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization
    In: Cell Chemical Biology Vol. 30 (2023) Nr. 7, pp. 753 - 765.e8
  • Schwalm, Martin P.; Berger, Lena M.; Meuter, Maximilian N.; Vasta, James D.; Corona, Cesear R.; Röhm, Sandra; Berger, Benedict-Tilman; Farges, Frederic; Beinert, Sebastian M.; Preuss, Franziska; Morasch, Viktoria; Rogov, Vladimir V.; Mathea, Sebastian; Saxena, Krishna; Robers, Matthew B.; Müller, Susanne; Knapp, Stefan
    A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins
    In: Frontiers in Cell and Developmental Biology Vol. 10 (2022) 886537
  • Bozilovic, Jelena; Eing, Lorenz; Berger, Benedict-Tilman; Adhikari, Bikash; Weckesser, Janik; Berner, Nicola B.; Wilhelm, Stephanie; Kuster, Bernhard; Wolf, Elmar; Knapp, Stefan
    Novel, highly potent PROTACs targeting AURORA-A kinase
    In: Current Research in Chemical Biology Vol. 2 (2022) 100032
  • Němec, Václav; Schwalm, Martin P.; Müller, Susanne; Knapp, Stefan
    PROTAC degraders as chemical probes for studying target biology and target validation
    In: Chemical Society Reviews Vol. 51 (2022) Nr. 18, pp. 7971 - 7993