Universität Bonn

Research Training Group RTG 2873 - University of Bonn

Publications

2023/2024

Publications of RTG 2873 PhD Students

Steinebach C., Bricelj A., Murgai A., Sosič I., Bischof L., Ng Y. L. D., Bischof C., Heim C., Maiwald S., Proj N., Voget R., Feller F., Košmrlj J., Sapozhnikova V., Schmidt A., Zuleeg M. R., Lemmitzer P., Mertins P., Hansen F. K.Gütschow M., Krönke J., Hartmann M. D. Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs. J. Med. Chem. 202366, 14513–14543.

Bockstiegel J., Wurnig S. L., Engelhardt J.,  Enns J.Hansen F. K.Weindl G. Pharmacological inhibition of HDAC6 suppresses NLRP3 inflammasome-mediated IL-1β release. Biochem. Pharmacol. 2023. 215: 115693. doi: 10.1016/j.bcp.2023.115693

Kraft F. B., Enns J., Honin I., Engelhardt J., Scholer A., Smith S. T., Meiler J., Schäker-Hübner L., Weindl G., Hansen F. K. Groebke Blackburn Bienaymé-mediated multi-component synthesis of selective HDAC6 inhibitors with anti-inflammatory properties. Bioorg. Chem. 2024, 143, 107072.

Flury P., Breidenbach J., Krüger N., Voget R., Schäkel L., Si Y., Krasniqi V., Calistri S., Olfert M., Sylvester K., Rocha C., Ditzinger R., Rasch A., Pöhlmann S., Kronenberger T., Poso A., Rox K., Laufer S. A., Müller C. E.Gütschow M., Pillaiyar T. Cathepsin-Targeting SARS-CoV-2 Inhibitors: Design, Synthesis, and Biological Activity. ACS Pharmacol. Transl. Sci. 2024 , 7, 493-514.

Breidenbach J., Voget, R., Si, Y., Hingst, A., Claff, T., Sylvester, K., Wolf, V., Krasniqi, V., Useini, A., Sträter, N., Ogura, Y., Kawaguchi, A., Müller, C. E.Gütschow, M. Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs. J. Med. Chem. 202467, 11, 8757–8790.

Voget, R., Breidenbach, J., Claff, T., Hingst, A., Sylvester, K., Steinebach, C., Vu, L. P., Weiße, R. H., Bartz, U., Sträter, N., Müller, C. E.Gütschow, M. Development of an Active-site Titrant for SARS-CoV-2 Main Protease as an Indispensable Tool for Evaluating Enzyme Kinetics. Acta Pharm. Sin. B 202414, 2349–2357.

Sievers, J., Voget, R., Lu, F., Garchitorena, K. M., Ng, Y. L. D., Chau, C. H., Steinebach, C., Figg, W. D., Krönke, J., Gütschow, M. Revisiting the Antiangiogenic Mechanisms of Fluorinated Thalidomide Derivatives. Bioorg. Med. Chem. Lett. 2024110, 129858.

 

Kostenis E., Jürgenliemke, L., Alenfelder J. G protein-mediated signal transduction: a molecular choreography of G protein activation after GTP binding. Signal Transduction and Targeted Therapy 2024, 9,188.

Associated Postdocs

König B., Watson, P. R. Reßing N., Cragin A. D., Schäker-Hübner L., Christianson D. W., Hansen F. K. Difluoromethyl-1,3,4-oxadiazoles Are Selective, Mechanism-Based, and Essentially Irreversible Inhibitors of Histone Deacetylase 6. J. Med. Chem. 202366, 13821-13837. 

Collaboration of PIs

Sinatra L., Vogelmann A., Friedrich F., Tararina M. A., Neuwirt E., Colcerasa A., König P., Toy L., Yesiloglu T. Z., Hilscher S., Gaitzsch L., Papenkordt N., Zhai S.,  Zhang L., Romier C., Einsle O., Sippl W., Schutkowski M., Gross O., Bendas G., Christianson D. W., Hansen F. K., Jung M., Schiedel M. Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation. J. Med. Chem. 2023, 66, 14787-14814.

Huber M. E., Wurnig S., Toy L., Weiler C., Merten N., Kostenis E.Hansen F. K., Schiedel M. Fluorescent Ligands Enable Target Engagement Studies for the Intracellular Allosteric Binding Site of the Chemokine Receptor CXCR2. J. Med. Chem. 2023, 66, 9916-9933.

Wollnitzke P., Wagner R., Afsar S. Y., Werner M., Geschold R., Müller C. E., Werz O., van Echten-Deckert G., Menche D. Synthesis and biological evaluation of simplified ajudazol derivatives reveal potent 5-lipoxygenase inhibition and considerable apoptotic activity in neuroblastoma cells. Bioorg. Med. Chem. Lett. 2023, doi.org/10.1016/j.bmcl.2023.129464

Yamauchi, Y., Konno, S., Noriko, N., Yoshioka, N., Hingst, A., Gütschow, M.Müller, C. E., Taguchi, A., Taniguchi, A., Kawaguchi, A., Hayashi, Y. Detection of Active SARS-CoV-2 3CL Protease in Infected Cells using Activity-based Probes with a 2,6-Dichlorobenzoyloxymethyl Ketone Reactive Warhead. ACS Chem. Biol. 202419, 1028–1034.


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