en
Michael Gütschow
© Uni Bonn
Prof. Dr. Michael Gütschow

Website

Affiliations
  • Pharmazeutisches Institut
  • Faculty of Mathematics and Natural Sciences
Research topics
  • Drug design
  • Enzyme inhibitors
  • PROTACs
  • Activity-based probes
Based on investigations on the biochemistry of the protease-inhibitor interaction and inhibition kinetics, we are designing and synthesizing tailored inhibitors for therapeutically relevant proteases and the main protease of SARS-CoV-2. We equipped synthetic inhibitors with reporter groups to assemble activity-based probes as valuable tool compounds to study target enzymes in a pathophysiological context. Proteolysis targeting chimeras (PROTACs) are bifunctional small molecules, which simultaneously bind a target protein and an E3 ubiquitin ligase. We are developing PROTACs, e.g. for the self-directed ubiquitination of ligases or the degradation of kinases, thus significantly contributing to this pioneering new modality in drug discovery.
Selected publications

C. Lemke, J. Benýšek, D. Brajtenbach, C. Breuer, A. Jílková, M. Horn, M. Buša, L. Ulrychová, A. Illies, K. F. Kubatzky, U. Bartz, M. Mareš, M. Gütschow (2021) An Activity-Based Probe for Cathepsin K Imaging with Excellent Potency and Selectivity; J. Med. Chem. 64:13793-13806.

J. Breidenbach, C. Lemke, T. Pillaiyar, L. Schäkel,§ G. Al Hamwi, M. Diett, R. Gedschold, N. Geiger, V. Lopez, S. Mirza, V. Namasivayam, A. C. Schiedel, K. Sylvester, D. Thimm, C. Vielmuth, L. P. Vu, M. Zyulina, J. Bodem, M. Gütschow, C. E. Müller (2021) Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors; Angew. Chem. Int. Ed. 60:10423-10429.

C. Steinebach, Y. L. D. Ng, I. Sosič, C.-S. Lee, S. Chen, S. Lindner, L. P. Vu, A. Bricelj, R. Haschemi, M. Monschke, E. Steinwarz, K. G. Wagner, G. Bendas, J. Luo, M. Gütschow, J. Krönke (2020) Systematic Exploration of Different E3 Ubiquitin Ligases: An Approach Towards Potent and Selective CDK6 Degraders; Chem. Sci. 11:3474-3486.

Michael Gütschow
© Uni Bonn
Prof. Dr. Michael Gütschow

Website

-