Universität Bonn

Research Training Group RTG 2873 - University of Bonn

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 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.

Imberg L., Siutkina A.I., Erbacher C., Schmidt J., Broekmans D.F., Ovsepyan R.A, Daniliuc C.G., Gonçalves de Oliveira E., Serafim M.S.M., O'Donoghue A.J., Pillaiyar T., Panteleev M.A., Poso A., Kalinina S.A., Bermúdez M., Nekipelov K., Bendas G., Karst U., Kalinin D.V. Pyrazinyl-Substituted Aminoazoles as Covalent Inhibitors of Thrombin: Synthesis, Structure, and Anticoagulant Properties. ACS Pharmacol .Transl. Sci. 2024, 8(1):146-172. doi: 10.1021/acsptsci.4c00515. 

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.

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.

Meringdal J. W., Bade L., Bendas G., Menche D. Diversity Oriented Synthesis of Novel Xanthones Reveal Potent Doxorubicin-Inspired Analogs. ChemMedChem 2024, 19(9):e202400055. doi: 10.1002/cmdc.202400055. Epub 2024 Feb 29.

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(5):2349-2357. doi: 10.1016/j.apsb.2024.03.001. Epub 2024 Mar 6.

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 Jun 13;67(11):8757-8790. doi: 10.1021/acs.jmedchem.4c00053. Epub 2024 May 16.

Mühle J., Alenfelder J., Rodrigues M.J., Jürgenliemke L., Guixà-González R., Grätz L., Andres F., Bacchin A., Hennig M., Schihada H., Crüsemann M., König G.M., Schertler G., Kostenis E., Deupi X.. Cyclic peptide inhibitors function as molecular glues to stabilize Gq/11 heterotrimers. Proc. Natl. Acad. Sci. U S A 2025, 122(19):e2418398122. doi: 10.1073/pnas.2418398122. Epub 2025 May 7.

Feller F., Honin I., Miranda M., Weber H., Henze S., Hanl M., Hansen F. K. Development of the First-in-Class FEM1B-Recruiting Histone Deacetylase Degraders. J .Med. Chem. 2025, doi: 10.1021/acs.jmedchem.4c02569.

Keuler T., Ferber D., Engelhardt J., Steinebach C., Kirsch N., Marleaux M., Weindl G., Geyer M., Gütschow M. Degrading the Key Component of the Inflammasome: Development of an NLRP3 PROTAC. Chem. Commun. 2025, 61, 3001-3004.

Westermann F. G., Okenc A. C. , Granithd P. K. E.,  Marimuthud P.,  Müller C.E., Mansoor S.E. Subtype- specific structural features of the hearing loss–rassociated human P2X2 receptor. PNAS. https://doi.org/10.1073/pnas.2417753122

Hanl M., Feller F., Honin I., Tan K., Miranda M., Schäker-Hübner L., Bückreiß, N., Schiedel M., Gütschow M., Bendas G., Hansen F. K. Target Engagement Studies and Kinetic Live-Cell Degradation Assays Enable the Systematic Characterization of Histone Deacetylase 6 Degraders. ACS Pharmacol. Transl. Sci. 2025, 8, 3074–3089. DOI: 10.1021/acsptsci.5c00247.

Zhai S., Honin I., Schäker-Hübner L., Hanl M., Jacobi L, Dressler F., Pieńkowska D.E., König P., Gerhartz J., Voget R., Bendas G., Gütschow M., Meissner F., Burckhardt B.B., Nowak R.P., Steinebach C., Hansen F. K. Development and Characterization of the First Selective Class IIb Histone Deacetylase Degraders. J. Med. Chem. 202568, 13793–13821. DOI: 10.1021/acs.jmedchem.5c00674.

Sun T., Zhai S., Lepper S., König B., Malenica M., Honin I., Hansen F.K. DCAF16-Based Covalent Molecular Glues for Targeted Protein Degradation of Histone Deacetylases. Archiv der Pharmazie 2025; 358, e70045. DOI: 10.1002/ardp.70045.

Sun T., Zhai S., König B., Honin I., Kponomaizoun C-E., Hansen F. K. Targeted Degradation of Histone Deacetylases via Bypassing E3 Ligase Targeting Chimeras (BYETACs). ACS Med. Chem. Lett. 2025. doi: 10.1021/acsmedchemlett.5c00193.

Zhai S., Willemsen N., Sun T., Malenica M., Deng S., Geyer M., Hansen F. K. Targeted Histone Deacetylase Degradation via Chemical Induced Proximity by Direct Recruitment of the CUL4 Complex Adaptor Protein DDB1. ACS Med. Chem. Lett. 2025, 16, 2070–2077. DOI: 10.1021/acsmedchemlett.5c00506.

Feller F., Weber H., Miranda M., Honin I., Hanl M., Hansen F. K. Replacing a Cereblon Ligand by a DDB1 and CUL4 Associated Factor 11 (DCAF11) Recruiter Converts a Selective Histone Deacetylase 6 PROTAC into a Pan-Degrader. ChemMedChem 2025, 20:e202500035. doi: 10.1002/cmdc.202500035.

Feller F., Honin I., Miranda M., Weber H., Henze S., Hanl M., Hansen F. K. Development of the First-in-Class FEM1B-Recruiting Histone Deacetylase Degraders. J. Med. Chem. 2025,68,1824–43. doi: 10.1021/acs.jmedchem.4c02569.

Bhattarai K., Majer T., Haussmann M., Schollmeyer D., Oni F.E., Höfte M., Voget R., Gütschow M., Ruetalo N., Schindler M., Straetener J., Wannenwetsch T., Brötz-Oesterhelt H., Karongo R., Lämmerhofer M., Hennessy R.C., Muletz-Wolz C.R., Gross H. Salamandamide Lipodipeptides are Biosynthetic Intermediate Shunt Products of the Nonamodular Nonribosomal Peptide Assembly Lines of the Viscosin Family. J. Nat. Prod. 2025, 88, 1012-1022. 

Sugrue I., Ade C., O'Connor P. M., Daniel J.M., Innocenti P., Kirsch N., Martin N.I,  Weindl G., Hill C., Schneider T., Paul Ross R. Trans-kingdom conservation of mechanism between bacterial actifensin and eukaryotic defensins. NPJ Antimicrob. Resist. 2025, 3(1):66. doi: 10.1038/s44259-025-00135-x. PMID: 40695989.

Honin I., Sun T., Setia N., Schäker-Hübner L., Hansen F. K. Ortho-Hydroxyanilides: Slow-Acting, Selective Histone Deacetylase 1/2 Inhibitors Suitable for Photocaging Applications. ACS Pharmacol. Transl. Sci. 2025, 8, 4385–4398. DOI: 10.1021/acsptsci.5c00562.

Nekipelov K., Nahain A.A., Otto S., Xu Y., Li J.P., Letunica N., Collett S., Attard C, Monagle P., Vamvounis G., Tsanaktsidis J., Ferro V., Bendas G. A Novel Series of Synthetic Heparin-Mimetics-Itaconic Acid-Containing Copolymers for Targeting Tumor Cell Coagulability and Metastasis. Macromol. Biosci. 2025, 25(7):e2400633. doi: 10.1002/mabi.202400633.

Wittenburg S., Zuleeg M. R., Peter K., Lemnitzer P., Voget R., Bricelj A., Gobec M., Dierlamm  N., Braun M. B., Geiger T. M., Heim C., StakemeierA., Wagner K. G., Nowak R. P., Hartmann M. D., Sosič I., Gütschow M., Krönke J., Steinebach C. Enhancing Solubility in VHL-Based PROTACs: Optimized USP7 Degraders for Improved Developability; J. Med. Chem. 2025, 68, 15711-15737.

König P., Bade L., Eichhorn J. M., Skalski H., Cinatl J., Michaelis M., Bendas G. Increased efficacy of PARP inhibitors against cisplatin-sensitive and -resistant ovarian cancer cells mediated via ATR and ATM inhibition. Cell Death Discov. 2025; 11, doi: 10.1038/s41420-025-02740-1.

Stopper D., Honin I., Feller F., Hansen F. K. Development of Ethyl-Hydrazide-Based Selective Histone Deacetylase 6 (HDAC6) PROTACs. ACS Med. Chem. Lett. 202516, 487–495. DOI: 10.1021/acsmedchemlett.5c00033.

Guhlke M., Herbst J., Nguyen T. G., Schneider, A., Dickschat J.S. , Menche D. Total Synthesis and Stereochemical Proposal of the Hexaene Framework of Bacillaene. Org. Lett 2025, 27, 2317-2322.

Meringdal J.W., Prangenberg V., Treiber T., Schneider A.J., Honsdorf L., Menche D. Ligand Type Guided Keto-Arylation Enables Modular Total Synthesis of Polycyclic CBS Xanthones. Angew. Chem. Int. Ed. Engl. 2025 Jul 22:e202513532. doi: 10.1002/anie.202513532. Online ahead of print.

Mühle J., Alenfelder J., Rodrigues M. J., Jürgenliemke L., Guixà-González R., Grätz L., Andres F., Bacchin A., Hennig M., Schihada H., Crüsemann M., König G. M., Schertler G., Kostenis E., Deupi X.. Cyclic peptide inhibitors function as molecular glues to stabilize Gq/11 heterotrimers. Proc. Natl. Acad. Sci. U S A 2025, 122(19):e2418398122. doi: 10.1073/pnas.2418398122. Epub 2025 May 7.

Schönenbroicher M., Seul M., Morgenschweis S., Heppner F., Menche D. Stereoselective Synthesis of Elaborate Fragments of Vancoresmycin and Amycomycin Enable Full Stereochemical Assignment. Org. Lett. 2026, 28, 3814-3819.

Torres-Püschel D., Zimmer L., Kehraus S., Abdelrahman A. A., Schneider T., Müller A., Carlier A., Crüsemann M. Paenidepsins are a Family of Lipopeptides from Paenibacillus. J Nat Prod. 2026, 89, 966 -979. 

Honin I., Novakova Z., Feller F., Schneider S., Schäker-Hübner L., Barinka C., Hansen, F. K. Cellular Target Engagement and Dissociation Kinetics of Class I-Selective Histone Deacetylase (HDAC) Inhibitors. Int. J. Mol. Sci. 2026, 27, 3036. DOI: 10.3390/ijms27073036.

Zhai S., Kemkes M., Kponomaizoun C.-E., Gerhartz J., Feller F., Tu J.-W., Pieńkowska D. E., Schliehe-Diecks J., Dressel I., Gütschow M., Nowak R. P., Steinebach C., Bhatia S., Hansen F. K. Discovery of Histone Deacetylase 8-Specific Proteolysis-Targeting Chimeras with Anticancer Activity against Hematological Malignancies. J. Med. Chem. 2026, 69, 918–943. DOI: 10.1021/acs.jmedchem.5c00939.

Nekipelov K., Otto S., Henseler M., Vidal-Y-Sy S., Al Nahain A., Gorzelanny C., Ferro V., Bendas G. Comparing Heparin and Heparin Mimetics in Targeting Immunomodulatory Proteins from Platelets to Activate T Cell-Dependent Immune Response in Oncology. ACS Pharmacol Transl Sci. 20269, 954-965. doi: 10.1021/acsptsci.5c00722

Nekipelov K., Ferro V., Bendas G. Fully Synthetic Non-Carbohydrate Heparin Mimetics-Perspectives for Therapeutic Anticoagulation and Beyond? Arch Pharm (Weinheim) 2026, 359(4):e70239. doi: 10.1002/ardp.70239

RTG2873 PostDocs

Lopez V., Schuh H.J.M., Mirza S., Vaaßen V.J., Schmidt M.S., Sylvester K., Idris R.M., Renn C., Schäkel L., Pelletier J., Sévigny J., Naggi A., Scheffler B., Lee S-Y., Bendas G., Müller C.E.. Heparins are potent inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase-1 (NPP1) – a promising target for the immunotherapy of cancer. Front. Immunol. 2023, 14, 1173634; https://doi.org/10.3389/fimmu.2023.1173634 

Mahardhika A. B., Ressemann A., Kremers S. E., Gregório Castanheira M.S., Schoeder C. T., Müller C. E., Pillaiyar T. Design, synthesis, and structure-activity relationships of diindolylmethane derivatives as cannabinoid CB2 receptor agonists. Arch. Pharm. (Weinheim). 2023, 356(3):e2200493. doi: 10.1002/ardp.202200493. Epub 2022 Nov 27.

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. 

Claff T., Schlegel J. G., Voss J.H., Vaaßen V. J., Weiße R.H., Cheng R.K.Y., Markovic-Mueller S., Bucher D., Sträter N., Müller C. E. Crystal structure of adenosine A2A receptor in complex with clinical candidate Etrumadenant reveals unprecedented antagonist interaction. Commun Chem. 2023, 6(1):106. doi: 10.1038/s42004-023-00894-6.    

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.

Claff T., Mahardhika A.B., Vaaßen V. J., Schlegel J.G., Vielmuth C., Weiße R.H., Sträter N., Müller C. E. Structural Insights into Partial Activation of the Prototypic G Protein-Coupled Adenosine A2A Receptor. ACS Pharmacol. Transl. Sci. 20247(5):1415-1425. doi: 10.1021/acsptsci.4c00051. eCollection 2024 May 10.

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, 67, 16533-55. 

Toledano-Pinedo M., Diez-Iriepa D., Porro-Pérez A., Schäker-Hübner L., Hanl M. Samadi A., Almendros P., Iriepa I., Rodríguez-Fernández M. M., Griñán-Ferré C., Siwek A., Wolak M., Satała G., Bojarski A. J., Doroż-Płonka A., Handzlik J., Godyń J., Knez D., Gobec S., Więckowska A., Hansen F. K., Marco-Contelles J. Contilistat, a New Multitarget Small Polyfunctionalized Indole Derivative. Synlett 2024, doi: 10.1055/s-0043-1775419.

Kraft F. B., Biermann L., Schäker-Hübner L., Hanl M., Hamacher A., Kassack M. U., Hansen F. K. Hydrazide-Based Class I Selective HDAC Inhibitors Completely Reverse Chemoresistance Synergistically in Platinum-Resistant Solid Cancer Cells J. Med. Chem. 2024, doi: 10.1021/acs.jmedchem.4c01817. 

Bollmann L. M., Lange F., Hamacher A., Biermann L., Schäker-Hübner L., Hansen F. K., Kassack M. U. Triple Combination of Entinostat, a Bromodomain Inhibitor, and Cisplatin Is a Promising Treatment Option for Bladder Cancer. Cancers 2024, 16, 3374. 

Stopper D., Buntrock S., Tan K., Carvalho L. P. de, Schäker-Hübner L., Held J., Kassack M. U., Hansen F. K. Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors. Eur. J. Med. Chem. 2025, 281, 117045. DOI: 10.1016/j.ejmech.2024.117045.

Artetxe-Zurutuza A., Iturrioz-Rodriguez N., Elizazu J., Toledano-Pinedo M., Porro-Pérez A, Goñi I. de, Elua-Pinin A., Schäker-Hübner L., Azkargorta M., Elortza F., Iriepa I., Lòpez-Muñoz F., Moncho-Amor V., Hansen F. K., Sampron N, Marco-Contelles J. L., Matheu A. Generation and validation of a novel multitarget small molecule in glioblastoma. Cell Death Dis. 2025, 16(1):250. doi: 10.1038/s41419-025-07569-1.

Schäker-Hübner L., Toledano-Pinedo M., Eimermacher S., Krasniqi V., Porro-Pérez A., Tan K., Horn G., Stegen P., Elsinghorst P. W., Wille T., Pietsch M., Gütschow M., Marco-Contelles J., Hansen F. K. Contilisant-Belinostat Hybrids: Polyfunctionalized Indole Derivatives as Multineurotarget Drugs for the Potential Treatment of Alzheimer's Disease. ACS Pharmacol. Transl. Sci. 2025, 8(3):831–40. doi: 10.1021/acsptsci.4c00709.

Stopper D., Biermann L., Watson P. R., Li J,. König B., Gaynes M. N., Pessanha de Carvalho L., Klose J., Hanl M., Hamacher A., Schäker-Hübner L., Ramsbeck D., Held J., Christianson D.W., Kassack M.U., Hansen F. K. Exploring Alternative Zinc-Binding Groups in Histone Deacetylase (HDAC) Inhibitors Uncovers DS-103 as a Potent Ethylhydrazide-Based HDAC Inhibitor with Chemosensitizing Properties. J. Med. Chem. 2025, 68(4):4426–52. doi: 10.1021/acs.jmedchem.4c02373.

Wurnig S. L., Hanl M., Geiger T. M., Zhai S., Dressel I., Pieńkowska D. E., Nowak R.P., Hansen F. K.  Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC6. RSC Med. Chem. 2025, 2452–2459. DOI: 10.1039/d4md00972j.

Lewash M., Kostenis E., Müller C. E. GPR17 - orphan G protein-coupled receptor with therapeutic potential. Trends Pharmacol. Sci. 2025 Jul;46(7):610-628. doi: 10.1016/j.tips.2025.05.001. Epub 2025 Jun 20.

Barone S., Bello I., Filocamo G., Cerchia C., Guadagni A., Brunetti M., Cosentino E., Hanl M., König B., Esposito C., Schäker-Hübner L., Summa V., Panza E., Hansen F. K., Brindisi M. Fine-tuning the combination of novel spirocyclic capping moieties and heterocyclic zinc binding groups for selective HDAC6 inhibition: design, synthesis, kinetic and biological studies. Eur. J. Med. Chem. 2026, 118806. DOI: 10.1016/j.ejmech.2026.118806.

Schäker-Hübner L., Hansen F. K. Recommended Tool Compounds: Isoform- and Class-Specific Histone Deacetylase Inhibitors. ACS Pharmacol. Transl. Sci. 2026. DOI: 10.1021/acsptsci.5c00619.

Toledano-Pinedo M., Porro-Pérez A., Schäker-Hübner L., Diez-Iriepa D., Iriepa I.; Siwek A.,Wolak M., Satała G., Bojarski A. J., Doroz-Płonka A., Handzlik J., Godyń J., Dallemagne P., Rochais C., Davis A., Since M., Pérez B., Bellver-Sanchis A., Irisarri A., Pallàs M., Solana-Manrique C., López-Muñoz F., Ismaili L., Griñán-Ferré C., Paricio, N., Hansen F. K., Więckowska A., Marco-Contelles J. Polyfunctionalized N-Arylsulfonyl Indoles: Identification of (E)-N-Hydroxy-3-{3-[(5-(3-(piperidin-1-yl)propoxy]-1H-indol-1-yl)sulfonyl]phenyl}acrylamide (MTP150) for the Epigenetic-based Therapy of Parkinson’s Disease. Int. J. Mol. Sci. 2026, 27, 3135. DOI: 10.3390/ijms27073135.

Participating groups

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.

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

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.

Ludwig K. C., Puls J. S., Matos de Opitz C.L., Innocenti P., Daniel J.M., Bornikoel .J, Arts M., Krannich S., Straetener J., Brajtenbach D., Henrichfreise B., Sass P., Mueller A., Martin N. I., Brötz-Oesterhelt H., Kubitscheck U., Grein F., Schneider T. The Dual Mode of Antibacterial Action of the Synthetic Small Molecule DCAP Involves Lipid II Binding. J. Am. Chem. Soc. 2024 Sep 11;146(36):24855-24862. doi: 10.1021/jacs.4.

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. 2024,19;7(2):493-514. doi: 10.1021/acsptsci.3c00313. eCollection 2024 Feb 9.

Oneto A., Hamwi G. A., Schäkel L., Krüger N., Sylvester K., Petry M., Shamleh R. A., Pillaiyar T., Claff T., Schiedel A. C., Sträter N., Gütschow M., Müller C. E. Nonpeptidic Irreversible Inhibitors of SARS-CoV-2 Main Protease with Potent Antiviral Activity. J. Med. Chem. 2024 , 67, 14986-15011.

Dreckmann T. M., Fritz L., Kaiser C. F., Bouhired S. M., Wirtz D. A., Rausch M., Müller A., Schneider T., König G. M., Crüsemann M. Biosynthesis of the corallorazines, a widespread class of antibiotic cyclic lipodipeptides. RCS Chem. Biol. 2024, DOI: 10.1039/d4cb00157e.

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. 2024,19(20):e202400284. doi: 10.1002/cmdc.202400284. Epub 2024 Jul 24.PMID: 38932712.

Engelhardt J., Klawonn A., Dobbelstein A.K., Abdelrahman A., Oldenburg J., Brandenburg K., Müller C.E., Weindl G. Lipopolysaccharide-Neutralizing Peptide Modulates P2X7 Receptor-Mediated Interleukin-1β Release. ACS Pharmacol .Transl. Sci. 2024, 23;8(1):136-145. doi: 10.1021/acsptsci.4c00496. eCollection 2025 Jan 10.PMID: 39816791.

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.

Voitsekhovskaia I., Ho Y.T.C., Klatt C., Müller A., Machell D.L., Tan Y.J., Triesman M., Bingel M., Schittenhelm R.B., Tailhades J., Kulik A., Maier M.E., Otting G., Wohlleben W., Schneider T., Cryle M., Stegmann E. Altering glycopeptide antibiotic biosynthesis through mutasynthesis allows incorporation of fluorinated phenylglycine residues. RSC Chem. Biol. 2024, 5(10):1017–34. doi: 10.1039/d4cb00140k. Epub ahead of print. PMID: 39247680; PMCID: PMC11376024.

Holze J., Lauber F., Soler S., Kostenis E., Weindl G. Label-free biosensor assay decodes the dynamics of Toll-like receptor signaling. Nat. Commun. 2024, 15(1):9554. doi: 10.1038/s41467-024-53770-9.

Boshta N.M., Lewash M., Köse M., Namasivayam V., Sarkar S., Voss J.H., Liedtke A.J., Junker A., Tian M., Stößel A., Rashed M., Mahal A., Merten N., Pegurier C., Hockemeyer J., Kostenis E., Müller C.E. Discovery of Anthranilic Acid Derivatives as Antagonists of the Pro-Inflammatory Orphan G Protein-Coupled Receptor GPR17. J .Med. Chem. 2024, 67(21):19365-19394. doi: 10.1021/acs.jmedchem.4c01755. Epub 2024 Nov 1.PMID: 39484825.

Wurnig S. L., Huber M. E., Weiler C., Baltrukevich H., Merten N., Stötzel I., Steffen T., Chang Y., Klammer R. H. L., Baumjohann D., Kiermaier E., Kolb P., Kostenis E., Schiedel M., Hansen F. K. A Fluorescent Probe Enables the Discovery of Improved Antagonists Targeting the Intracellular Allosteric Site of the Chemokine Receptor CCR7. J. Med. Chem. 2025, 68(4):4308–33. doi: 10.1021/acs.jmedchem.4c02102.

Treiber T., Li W.-S., Bingel M., Müller A., Eckhardt M., Menche D. Total Synthesis of Epicoccolides A and B by Oxidative Skeleton Rearrangement Leads to a Structural Revision and Questions Proposed Biosynthesis. Org. Lett. 2025, 27, 6539−6544.

Flury P., Krüger N., Sylvester K., Breidenbach J., Al Hamwi G., Qiao J., Chen, Y., Rocha C., Sá Magalhães Serafim M., Barbosa da Silva E., Pöhlmann S., Poso A., Kronenberger T., Rox K., O’Donoghue A. J., Yang S., Sträter N., Gütschow M. Laufer S. A., Müller C. E., Pillaiyar T. Design, Synthesis, and Unprecedented Interactions of Covalent Dipeptide-Based Inhibitors of SARS-CoV‑2 Main Protease and Its Variants Displaying Potent Antiviral Activity. J. Med. Chem. 2025, 68, 3626-3652.

Tan K., Rodríguez-Fernández M. M., Keuler T., Hansen F. K., Gütschow M., Weindl G., Marco-Contelles J. Crosstalk between NLRP3 Signaling and Histone Deacetylases in Inflammasome-Driven Diseases. J. Med. Chem. 2026, 69, 102–120. DOI: 10.1021/acs.jmedchem.5c02657. 

Outstanding papers of GRK scientists

Shukla R., Peoples A.J., Ludwig K.C., Maity S., Derks M.G.N., De Benedetti S., Krueger A.M., Vermeulen B.J.A., Harbig T., Lavore F., Kumar R., Honorato R.V., Grein F., Nieselt K., Liu Y., Bonvin A.M.J.J., Baldus M., Kubitscheck U., Breukink E., Achorn C., Nitti A., Schwalen C.J., Spoering A.L., Ling L.L., Hughes D., Lelli M., Roos W.H., Lewis K., Schneider T., Weingarth M. An antibiotic from an uncultured bacterium binds to an immutable target. Cell 2023 Sep 14;186(19):4059-4073.e27. doi: 10.1016/j.cell.2023.07.038. Epub 2023 Aug 22. PMID: 37611581. 

Pietruschka G., Ranzani A.T., Weber A., Patwari T., Pilsl S., Renzl C., Otte D.M., Pyka D., Möglich A., Mayer G. An RNA Motif That Enables Optozyme Control and Light-Dependent Gene Expression in Bacteria and Mammalian Cells. Adv. Sci. (Weinh). 2024 Mar;11(12):e2304519. doi: 10.1002/advs.202304519. Epub 2024 Jan 16.PMID: 38227373. 

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.

Meringdal J.W., Menche D. Suzuki-Miyaura (hetero-)aryl cross-coupling: recent findings and recommendations. Chem. Soc. Rev. 2025 Jun 16;54(12):5746-5765. doi: 10.1039/d4cs01108b. PMID: 40392002.

Breuer C., Küppers J., Schulz-Fincke A. C., Heilos A., Lemke C., Spiwokowá P., Schmitz, J., Cremer L., Frigolé-Vivas N, Lülsdorff M., Mertens M. D., Wichterle F., Apeltauer M., Horn M., Gilberg E., Furtmann N., Bajorath J., Bartz U., Engels B., Mareš M., Gütschow M. Redirecting the Peptide Cleavage Causes Protease Inactivation. Angew. Chem. Int. Ed. 2025, 64, e202506832.


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