BIGS-DrugS-DoktorandInnen und  ihre BetreuerInnen haben ihre Forschungsergebnisse erfolgreich veröffentlicht. Herzlichen Glückwunsch!

Al Hamwi G, Alnouri MW, Verdonck S, Leonczak P, Chaki S, Frischbutter S, Kolkhir P, Michaela Matthey M, Kopp C, Bednarski M, Riedel YK, Marx D, Clemens S, Namasivayam V, Gattner S, Thimm D, Sylvester K, Wolf K. Kremer AE, De Jonghe S, Wenzel D, Kotańska M, Ali H, Herdewijn P, Müller CE. Subnanomolar MAS-related G protein-coupled receptor-X2/B2 antagonists with efficacy in human mast cells and disease models; Signal Transduction and Targeted Therapy. DOI: 10.1038/s41392-025-02209-8

Bhattarai K, Majer T, Haussmann M, Schollmeyer D, Oni FE, Höfte M, Voget R, Gütschow M, Ruetalo N, Schindler M, Straetener J, Wannenwetsch T, Brötz-Oesterhelt H, Karongo R, Lämmerhofer M, Hennessy RC, Muletz-Wolz CR, 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. 

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.

Perzolli A, Steinebach C, Krönke J, Gütschow M, Zwaan CM, Barneh F, Heidenreich O.; PROTAC-Mediated GSPT1 Degradation Impairs the Expression of Fusion Genes in Acute Myeloid Leukemia; Cancers, 2025, 17, 211.

Flury P, Krüger N, Sylvester K, Breidenbach J, Al Hamwi G, Qiao J, Chen Y, Rocha C, Serafim MSM, Barbosa da Silva E, Pöhlmann S, Poso A, Kronenberger T, Rox K, O'Donoghue AJ, Yang S, Sträter N, Gütschow M, Laufer SA, Müller CE, 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.

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

Stopper D, Buntrock S, Tan K, Carvalho LP de, Schäker-Hübner L, Held J, Kassack MU, Hansen FK. 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.

Holze J, Lauber F, Soler S, Kostenis E, Weindl G. Label-free biosensor assay decodes the dynamics of Toll-like receptor signaling; Nat com. 15,  9554 (2024)

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

Seidinger A, Roberts R, Bai Y, Müller M, Pfeil E, Matthey M, Rieck S, Alenfelder J, König GM, Pfeifer A, Kostenis E, Klinke A, Fleischmann BK, Wenzel D. Pharmacological Gq inhibition induces strong pulmonary vasorelaxation and reverses pulmonary hypertension. EMBO Mol. Med. 20246(8):1930-1956. doi: 10.1038/s44321-024-00096-0.

Hanke W, Alenfelder J, Liu J, Gutbrod P, Kehraus S, Crüsemann M, Dörmann P, Kostenis E, Scholz M, König GM; The Bacterial Gq Signal Transduction Inhibitor FR900359 Impairs Soil-Associated Nematodes; J. Chem. Ecol, 2023, 49(9-10):549-569, doi:10.1007/s10886-023-01442-1.

Kostenis E, Jürgenliemke L, Alenfelder J; G protein-mediated signal transduction: a molecular choreography of G protein activation after GTP  binding. Signal. Transduct. Target. Ther. 2024, 9(1), 188.

Brands J, Bravo S, Jürgenliemke L, Grätz L, Schihada H, Frechen F, Alenfelder J, Pfeil C, Ohse PG, Hiratsuka S, Kawakami K, Schmacke LC, Heycke  N, Inoue A, König G, Pfeifer A, Wachten D, Schulte G, Steinmetzer T, Watts  VJ, Gomeza J, Simon K, Kostenis E;  A molecular mechanism to diversify Ca2+  signaling downstream of Gs protein-coupled receptors; Nat Commun. 2024 Sep 3;15(1):7684. doi: 10.1038/s41467-024-51991-6. PMID: 39227390.

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 CE, Gütschow M; Macrocyclic Azapeptide Nitriles: Structure-Based Discovery of Potent SARS-CoV-2 Main Protease Inhibitors as Antiviral Drugs; J. Med. Chem. 2024, 67, 8757-8790

Bricelj A, Ng YLD, Gobec M, Kuchta R, Hu W, Javornik Š, Rožič M, Gütschow M, Zheng G, Krönke J, Steinebach C, Sosič I; Design, Synthesis, and Evaluation of BCL-2 Targeting PROTACs; Chem. Eur. J. 2024, e202400430.

Barton BE, Collins MK, Chau CH, Choo-Wosoba H, Venzon DJ, Steinebach C, Garchitorena KM, Shah B, Sarin EL, Gütschow M, Figg WD; Preclinical Evaluation of a Novel Series of Polyfluorinated Thalidomide Analogs in Drug Resistant Multiple Myeloma; Biomolecules, 2024, 14, 725.

Sievers J, Voget R, Lu F, Garchitorena KM, Ng YLD, Chau CH, Steinebach C, Figg WD, Krönke J, Gütschow M; Revisiting the Antiangiogenic Mechanisms of Fluorinated Thalidomide Derivatives; Bioorg. Med. Chem. Lett. 2024, 110, 129858.

Günther M, Schuler M, Hentschel L, Salm H, Schmitz MT, Jaehde U; Medication Risks and Their Association with Patient-Reported Outcomes in Inpatients with Cancer. Cancers

Meringdal JW, Bade L, Bendas G, Menche D; Diversity Oriented Synthesis of Novel Xanthones Reveal Potent Doxorubicin-Inspired Analogs. ChemMedChem 2024:e202400055. doi: 10.1002/cmdc.202400055.

Zhai S, Schäker-Hübner L, Hanl M, Jacobi L, Pieńkowska DE, Gerhartz J, Voget R, Gütschow, M, Meissner F, Nowak RP, Steinebach C, Hansen FK; Development and characterization of the first selective class IIb histone deacetylase degraders. ChemRxiv 2024. doi: 10.26434/chemrxiv-2024-ngppg.

Stopper D, Carvalho LP de, Souza ML de, Winzeler E, Held J, Hansen FK; Development of Peptoid-Based Heteroaryl-Decorated Histone Deacetylase (HDAC) Inhibitors with Dual-Stage Antiplasmodial Activity. ChemRxiv 2024. doi: 10.26434/chemrxiv-2024-7w3v0.

Scheuerer S, Motlova L, Schäker-Hübner L, Sellmer A, Feller F, Ertl FJ, Koch P, Hansen FK, Barinka C, Mahboobi S; Biological and structural investigation of tetrahydro-β-carboline-based selective HDAC6 inhibitors with improved stability. Eur J Med Chem 2024:116676. doi: 10.1016/j.ejmech.2024.116676.

Kraft FB, Biermann L, Schäker-Hübner L, Hanl M, Hamacher A, Kassack MU, Hansen FK; Hydrazide-based class I HDAC inhibitors with HDAC3 preference completely reverse chemoresistance in a synergistic manner in platinum-resistant solid cancer cells. ChemRxiv 2024. doi: 10.26434/chemrxiv-2024-txxrk.

Huber ME, Wurnig SL, Moumbock AFA, Toy L, Kostenis E, Alonso Bartolomé A, Szpakowska M, Chevigné A, Günther S, Hansen FK, Schiedel M; Development of a NanoBRET Assay Platform to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1. ChemMedChem 2024:e202400284. doi: 10.1002/cmdc.202400284.

Behrmann LV, Meier K, Vollmer J, Chiedo CC, Schiefer A, Hörauf A, Pfarr K; In vitro extracellular replication of Wolbachia endobacteria. Front. Microbiol., 18 July 2024 Sec. Microbial Symbioses, Volume 15 - 2024 | https://doi.org/10.3389/fmicb.2024.1405287 

Löckener I, Behrmann LV,  Reuter J, Schiefer A, Klöckner A, Krannich S, Otten C, Mölleken K, Ichikawa S, Hoerauf A, Schneider T, Pfarr KM, Henrichfreise B; The MraY Inhibitor Muraymycin D2 and Its Derivatives Induce Enlarged Cells in Obligate Intracellular Chlamydia and Wolbachia and Break the Persistence Phenotype in Chlamydia. Antibiotics 2024, 13(5), 421; https://doi.org/10.3390/antibiotics13050421

Holze J, Lauber F, Kostenis E, Weindl G; Label-free biosensor assay decodes the dynamics of Toll-like receptor signaling. bioRxiv 2024.01.18.576268

Meringdal JW, Bade L, Bendas G, Menche D:Diversity Oriented Synthesis of Novel Xanthones Reveal Potent Doxorubicin-Inspired Analogs. ChemMedChem 2024:e202400055. doi: 10.1002/cmdc.202400055.

König B, Hansen FK; 2-(Difluoromethyl)-1,3,4-oxadiazoles: The Future of Selective Histone Deacetylase 6 Modulation? ACS Pharmacol. Transl. Sci. 2024. doi: 10.1021/acsptsci.4c00031.

Voget R, Breidenbach J, Claff T, Hingst A, Sylvester K, Steinebach C, Vu LP,  Weiße R, Bartz U, Sträter N,  Müller CE, Gütschow M; Development of an active-site titrant for SARS-CoV-2 main protease as an indispensable tool for evaluating enzyme kinetics. Acta Pharmaceutica Sinica B 2024; https://doi.org/10.1016/j.apsb.2024.03.001

Reverte-Salisa L, Sissig S, Hildebrand S, Yao X, Zurkovic J, Jaeckstein MY, Heeren J, Lezoualc'h F, Krahmer N, Pfeifer A; EPAC1 enhances brown fat growth and beige adipogenesis, Nat Cell Biol 26, 113–123 (2024). https://doi.org/10.1038/s41556-023-01311-9

Hopp MT, Holze J, Lauber F, Holtkamp L, Rathod DC, Miteva MA, Prestes EB, Geyer M, Manoury B, Merle NS, Roumenina LT, Bozza MT, Weindl G, Imhof D; Insights into the molecular basis and mechanism of heme-triggered TLR4 signalling: The role of heme-binding motifs in TLR4 and MD2. Immunology 171:181-197.

Pachòn-Angona I, Bernard PJ, Simakov A, Maj M, Jozwiak K, Novotna A, Lemke C, Gütschow M, Martin H, Oset-Gasque MJ, Marco-Contelles J, Ismaili L; Design and Synthesis of Multi-Functional Ligands through Hantzsch Reaction: Targeting Ca2+ Channels, Activating Nrf2 and Possessing Cathepsin S Inhibitory and Antioxidant Properties; Pharmaceutics 2024, 16, 121.

Kraft FB, Enns J, Honin I, Engelhardt J, Schöler A, Smith ST, Meiler J, Schäker-Hübner L, Weindl G, Hansen FK; Groebke Blackburn Bienaymé-mediated multi-component synthesis of selective HDAC6 inhibitors with anti-inflammatory properties. Bioorg Chem 2024; 143:107072. doi: 10.1016/j.bioorg.2023.107072.