Publications
2023/2024/2025
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.
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 2024, 14, 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. 2024, 110, 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, May 2;19(9):e202400055. doi: 10.1002/cmdc.202400055. Epub 2024 Feb 29.
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 Aug 12; 5(10):1017–34. doi: 10.1039/d4cb00140k. Epub ahead of print. PMID: 39247680; PMCID: PMC11376024.
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 Nov 14;67(21):19365-19394. doi: 10.1021/acs.jmedchem.4c01755. Epub 2024 Nov 1.PMID: 39484825.
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 May 13;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.
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. 2025. 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(7):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.
Stopper D., Honin I., Feller F., Hansen F.K. Development of Ethyl-Hydrazide-Based Selective Histone Deacetylase 6 (HDAC6) PROTACs. ACS Med. Chem. Lett. 2025; 16(3):487–95. doi: 10.1021/acsmedchemlett.5c00033.
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; May 19;20(10):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(2):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 Jul 22;3(1):66. doi: 10.1038/s44259-025-00135-x. PMID: 40695989.
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.
S. Wittenburg, M. R. Zuleeg, K. Peter, P. Lemnitzer, R. Voget, A. Bricelj, M. Gobec, N. Dierlamm, M. B. Braun, T. M. Geiger, C. Heim, A. Stakemeier, K. G. Wagner, R. P. Nowak, M. D. Hartmann, I. Sosič, M. Gütschow, J. Krönke, C. Steinebach. Enhancing Solubility in VHL-Based PROTACs: Optimized USP7 Degraders for Improved Developability; J. Med. Chem. 2025, 68, 15711-15737.
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 Mar;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 Jun 1;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. 2024 Apr 29;7(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.
Kraft F.B., Enns J., Honin I., Engelhardt J., Schöler 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 Feb;143:107072. doi: 10.1016/j.bioorg.2023.107072. Epub 2024 Jan 2.PMID: 38185013.
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, 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 JL, 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. doi: 10.1039/d4md00972j.
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.
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.
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 May;14(5):2349-2357. doi: 10.1016/j.apsb.2024.03.001. Epub 2024 Mar 6.
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.
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.
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 Jan 19;7(2):493-514. doi: 10.1021/acsptsci.3c00313. eCollection 2024 Feb 9.
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.
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.
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 Oct 16;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 Dec 23;8(1):136-145. doi: 10.1021/acsptsci.4c00496. eCollection 2025 Jan 10.PMID: 39816791.
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.
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.
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.
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.
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.
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