Publications

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. 2023, 66, 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. 2024, 67, 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 2024, 14, 2349–2357.

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.

Brands J., Bravo S., Jürgenliemke L., Grätz L., Schihada H., Frechen F., Alenfelder J., Pfeil C., Ohse P. G., Hiratsuka S., Kawakami K., Schmacke L. C., Heycke N., Inoue A., König G., Pfeifer A., Wachten D., Schulte G., Steinmetzer T., Watts V. J., Gomeza J., Simon K., Kostenis E. A molecular mechanism to diversify Ca²⁺ signaling downstream of Gs protein-coupled receptors. Nat Commun. 2024, 15, 7684.

Mühle J., Rodrigues M.J., Alenfelder J., Jürgenliemke L., Guixà-González R., Bacchin A., Andres F., Hennig M., Schihada H., Crüsemann M., König G.M. , Kostenis E., Schertler G., Deupi X. Cyclic peptide inhibitors stabilize Gq/11 heterotrimers. bioRxiv 2024, doi.org/10.1101/2023.10.24.563737.

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. 2023, 66, 13821-13837. 

Jenke, R., Oliinyk, D.m Zenz, T., Körfer, J., Schäker-Hübner, L., Hansen, F. K., Lordick, F., Meier-Rosar, F., Aigner, A., Büch, T. HDAC inhibitors activate lipid peroxidation and ferroptosis in gastric cancer. Biochem. Pharmacol. 2024, 225, 116257.

Scheuerer, S., Motlova, L., Schäker-Hübner, L., Sellmer, A., Feller, F., Ertl, F. J., Koch, P., Hansen, F. K., Barinka, C, Mahboobi, S. Biological and structural investigation of tetrahydro-β-carboline-based selective HDAC6 inhibitors with improved stability. Eur. J. Med. Chem. 2024, 276, 116676.

 Fischle A., Lutsch M., Hübner F., Schäker‑Hübner L., Schürmann L., Hansen F. K., Kalinina S. A. Micro-scale screening of genetically modifed Fusarium fujikuroi strain extends the apicidin family. Nat. Prod. Bioprospect. 2024, 14, 1-20.

Toledano-Pinedo M., Porro-Pérez A., Schäker-Hübner L., Romero F., Dong M., Samadi A., Almendros P., Iriepa I., Bautista-Aguilera O. M., Rodríguez-Fernández M. M., Solana-Manrique C., Sanchis I., Mora-Morell A., Canseco Rodrìguez A., Sànchez-Pérez A. M., Knez D., Gobec S., Bellver-Sanchis A., Pérez B., Dobrydnev A. V.m Artetxe-Zurutuza A., Matheu A., Siwek A., Wolak M., Satała G., Bojarski A. J., Doroz-Płonka A., Handzlik J., Godyń J., Więckowska A., Paricio N., Griñán-Ferré C., Hansen F. K., Marco-Contelles J. Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Diseases. J. Med. Chem. 2024, doi.org/10.1021/acs.jmedchem.4c01367. 

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

Hanke W., Alenfelder J., Liu J., Gutbrod P., Kehraus S., Crüsemann M., Dörmann P., Kostenis E., Scholz M., König G. M. The Bacterial Gq Signal Transduction Inhibitor FR900359 Impairs Soil-Associated Nematodes. J. Chem. Ecol, 2023, 49, 549-569.

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. 2024, 19, 1028–1034.

Huber, M. E., Wurnig, S. L., Moumbock, A. F. A., Toy, L., Kostenis, E., Alonso Bartolomé, A., Szpakowska, M., Chevigné, A., Günther, S., Hansen, F. K., Schiedel, M. Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1. ChemMedChem 2024, DOI: 10.1002/cmdc.202400284.

Lewis, K., Lee, R. E., Brötz-Oesterhelt, H., Hiller, S., Rodnina M. V., Schneider, T., Weingarth, M., Wohlgemuth, I. Sophisticated natural products as antibiotics, Nature 2024, 632, 39-49.