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Research results

BIGS DrugS PhD students and their supervisors have successfully published their research results.

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2026

Behrmann LV, Harbig TA, Hörauf A, Nieselt K, Pfarr KM. Improved RNA preparation for RNA-seq of the intracellular bacterium Wolbachia wAlbB; Front.  Microbiol. Volume 16 - 2025.

Hafels M., Mattusch A., Wagner K.G., Steffens K.E. Tricalcium Citrate Tetrahydrate TB as Filler in Direct Compression of Minitablets. AAPS PharmSciTech 27, 104 (2026).

 Hafels M., Maslennikow D., Mattusch A., Wagner K.G., Steffens K.E. Overcoming formulation challenges of a moisture-sensitive API using tricalcium citrate TB and anhydrous trimagnesium citrate in direct compression. Eur J Pharm Sci. 2026;227:107666.

Stakemeier A., Mild L., Sievers J., Kalasová J., Steffens K.E., Kuentz M., Steinebach C., Wagner K.G. From prediction to performance: In silico-supported formulation of amorphous solid dispersions for PROTAC NX-2127. Int J Pharm X. 2026 Sep 10;12:100663.

Mild L., Stakemeier A., Nguyen Thi M.N., Wagner K.G. Unlocking the potential of alkaline polymethacrylates via ionic crosslinking in amorphous solid dispersions. Int J Pharm X. 2026 Apr 1;11:100531.

Bi C., Schwermer F., Schäkel L., Mirza S., Baburi H., Riziki P., Schmies C.C., Winzer R., Idris R., Rolshoven G., Schilling J., Luckenbach L., Pelletier J., Brusoni L.S., Al Hroub H., Al Hamwi G., Lopez V., Ahmadsay A., Raulien L., Sylvester K., Sévigny J., Tolosa E., Guse A.H., Müller C.E. Nucleotide-Derived Competitive Inhibitors of Ectonucleotidase CD39─A Promising Extracellular Target for Immunotherapy of Cancer. J Med Chem. 2026 May 14;69(9):10828-10864.

Bi C., Schwermer F., Tang L., Müller C.E., Liu W. Inhibitors of Ectonucleotidase CD39 for Immunotherapy of Cancer and Infections─Recent Developments and Future Perspectives. J Med Chem. 2026 May 14;69(9):9874-9890.

2025

Nagel J., Namasivayam V., Weinhausen S., Sierra-Marquez J., Baqi Y., Al Musawi H.A.M., Abdelrahman A., Vaaßen V.J., Schlegel J.G., Taplick L., Torp J., Kubick J., Maertens B., Geyer M., Claff T., Nicke A., Hagelueken G., Müller C.E. Discovery of an allosteric binding site for anthraquinones at the human P2X4 receptor; Nature Communications; 16, Article number: 10367

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. 

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. 

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.

Sugrue I., Ade C., O'Connor P.M., Daniel J.M., Innocenti P., Kirsch N., Martin N.I., Weindl G., Hill C., Schneider T., Ross R.P. Trans-kingdom conservation of mechanism between bacterial actifensin and eukaryotic defensins. NPJ Antimicrob. Resist. 2025 Jul 22;3(1):66. 

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. 

Wittenburg S.,  Zuleeg M.R., Peter K., Lemnitzer P., Voget R., Bricelj A., Gobec M., Dierlamm N., Braun M.B., Geige T.M., Heim C., Stakemeier A., 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.

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. 

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 8:136-145.

Matziol T., Talagayev V., Slokan T., Strašek Benedik N., Holze J., Sova M., Wolber G., Weindl, G. Discovery of Novel Isoxazole-Based Small-Molecule Toll-Like Receptor 8 Antagonists. J Med Chem 68:4888-4907.

Bockstiegel J., Engelhardt J., Schuchardt M., Tölle M., Weindl G. The vasoconstrictor adenosine 5′-tetraphosphate is a danger signal that induces IL-1β. Mol Med 31:72.

Breuer C., Küppers J., Schulz-Fincke A.C., Heilos A., Lemke C., Spiwokowá P., Schmitz J., Cremer L., Frigolé-Vivas M., 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.

Zhai S., Kemkes M., Kponomaizoun C.E., Feller F., Tu J-W., Pieńkowska D.E., Gerhartz J., Schliehe-Diecks J., Gütschow M., Nowak R.P., Steinebach C., Bhatia S., Hansen F.K. Discovery of histone deacetylase 8 (HDAC8)-specific proteolysis-targeting chimeras with anti-cancer activity against hematological malignancies. ChemRxiv 2025. 

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., Nowak R.P., Steinebach C., Hansen F.K. Development and characterization of the first selective class IIb histone deacetylase degraders. ChemRxiv 2025. 

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. 

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. 

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. 

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. 

Hanl M., Feller F., Honin I., Tan K., Schaeker-Huebner L., Bueckreiss N., Schiedel M., Guetschow M., Bendas G., Hansen F.K. Target engagement studies and kinetic live-cell degradation assays enable the systematic characterization of HDAC6 PROTACs at endogenous protein expression levels. bioRxiv 2025. 

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 Selective Histone Deacetylase 6 PROTAC into a Pan-Degrader. ChemMedChem 2025:e202500035. 

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

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. 

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 C.M., 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 M.S.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.

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. 

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. 


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