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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.
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Philipp Flury,Julian Breidenbach,Nadine Krueger,Rabea Voget,Laura Schaekel, Yaoyao Si,Vesa Krasniqi, Sara Calistri, Matthias Olfert,Katharina Sylvester,Cheila Rocha, Raphael Ditzinger,
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCEno. 4 (2024): 1195-1196
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Neuro-Oncologyno. Supplement_4 (2024): 0-0
Johannes Sievers,Rabea Voget, Feiteng Lu, Kathleen M Garchitorena,Yuen Lam Dora Ng,Cindy H Chau,Christian Steinebach,William D Figg,Jan Krönke,Michael Gütschow
Bioorganic & medicinal chemistry letters (2024): 129858-129858
Julian Breidenbach,Rabea Voget, Yaoyao Si, Alexandra Hingst,Tobias Claff,Katharina Sylvester,Valentina Wolf,Vesa Krasniqi, Abibe Useini,Norbert Straeter,Yukino Ogura,Atsushi Kawaguchi,
JOURNAL OF MEDICINAL CHEMISTRYno. 11 (2024): 8757-8790
Philipp Flury,Julian Breidenbach,Nadine Krüger,Rabea Voget,Laura Schäkel, Yaoyao Si,Vesa Krasniqi, Sara Calistri, Matthias Olfert,Katharina Sylvester,Cheila Rocha, Raphael Ditzinger,
ACS pharmacology & translational scienceno. 2 (2024): 493-514
PHARMACEUTICSno. 1 (2024)
Philipp Flury,Julian Breidenbach,Nadine Krüger,Rabea Voget,Laura Schäkel, Yaoyao Si,Vesa Krasniqi, Sara Calistri, Matthias Olfert,Katharina Sylvester,Cheila Rocha, Raphael Ditzinger,
ACS pharmacology & translational scienceno. 4 (2024): 1195-1196
Yuki Yamauchi,Sho Konno,Noriko Omura, Narumi Yoshioka, Alexandra Hingst,Michael Gütschow,Christa E Müller,Akihiro Taguchi,Atsuhiko Taniguchi,Atsushi Kawaguchi,Yoshio Hayashi
Blaire E Barton, Matthew K Collins,Cindy H Chau,Hyoyoung Choo-Wosoba,David J Venzon,Christian Steinebach, Kathleen M Garchitorena, Bhruga Shah, Eric L Sarin,Michael Gütschow,William D Figg
Biomoleculesno. 6 (2024)
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