TACTIC  Publications

 

  1. Wang G, Seidler NJ, Rohm S, Pan Y, Liang XJ, Haarer L, Berger BT, Sivashanmugam SA, Wydra VR, Forster M, Laufer SA, Chaikuad A, Gehringer M, and Knapp S (2025). Probing the Protein Kinases' Cysteinome by Covalent Fragments. Angew Chem Int Ed Engl 64: e202419736.PubMed
  2. Hunold P, Pizzolato G, Heramvand N, Kaiser L, Barbiera G, van Ray O, Thomas R, George J, Peifer M, and Hansel-Hertsch R (2025). DynaTag for efficient mapping of transcription factors in low-input samples and at single-cell resolution. Nat Commun 16: 6585.Pubmed
  3. Falkenhorst J, Ivanyi P, Schulz T, Hamacher R, Kasper B, Hohenberger P, Deinzer CKW, Pink D, Fletcher BS, Haller V, Optaczy Y, Grunewald S, Rauh D, Marino-Enriquez A, Muhlenberg T, Reichardt P, and Bauer S (2025). Phase 2 trial of ponatinib in patients with metastatic gastrointestinal stromal tumor following failure or intolerance of prior therapy with imatinib (POETIG trial). Clin Cancer Res.PubMed
  4. Hillebrand L, Wang G, Rasch A, Masberg B, Chaikuad A, Kronenberger T, Gunther E, Forster M, Poso A, Lammerhofer M, Laufer SA, Knapp S, and Gehringer M (2025). A twist in the tale: shifting from covalent targeting of a tyrosine in JAK3 to a lysine in MK2. RSC Med Chem.PubMed
  5. Zhubi R, Chaikuad A, Munoz Sosa CJ, Joerger AC, and Knapp S (2025). Structural analysis of TRIM family PRYSPRY domains and its implications for E3-ligand design. J Struct Biol X 12: 100134.PubMed
  6. Schonfeld J, Brunst S, Ciomirtan L, Willmer L, Chromik MA, Kumar A, Froemel T, Liebisch N, Hackspacher A, Ehrler JHM, Wintermeier L, Hesse C, Fiedler J, Heering J, Freitag H, Zardo P, Fieguth HG, Bruggerhoff A, Jakob J, Haupl B, Weizel L, Kaiser A, Schubert-Zsilavecz M, Oellerich T, Fleming I, Schebb NH, Furst R, Kannt A, Knapp S, Proschak E, and Hiesinger K (2025). Structure-Based Design of PROTACS for the Degradation of Soluble Epoxide Hydrolase. J Med Chem 68: 13728-13749.
  7. Mandel S, Hanke T, Prendiville N, Baena-Nuevo M, Berger LM, Farges F, Schwalm MP, Berger BT, Kraemer A, Elson L, Saraswati H, Abdul Azeez KR, Dederer V, Mathea S, Corrionero A, Alfonso P, Keller S, Gstaiger M, Krause DS, Muller S, Rohm S, and Knapp S (2025). Covalent Targeting Leads to the Development of a LIMK1 Isoform-Selective Inhibitor. J Med Chem 68: 15026-15049.PubMed
  8. Munick P, Strubel A, Balourdas DI, Funk JS, Mernberger M, Osterburg C, Dreier B, Schaefer JV, Tuppi M, Yuksel B, Schafer B, Knapp S, Pluckthun A, Stiewe T, Joerger AC, and Dotsch V (2025). DARPin-induced reactivation of p53 in HPV-positive cells. Nat Struct Mol Biol 32: 790-801.PubMed
  9. Serafim RAM and Gehringer M (2025). High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024. ACS Pharmacol Transl Sci 8: 2401-2414.PubMed
  10. Tivon B, Wiese J, Muller MP, Gabizon R, Rauh D, and London N (2025). Computational Design of Lysine Targeting Covalent Binders Using Rosetta. J Chem Inf Model.PubMed
  11. Galvez BPJ, Woelffing P, Schwarz M, Ebner S, Rudalska R, Masberg B, Esposito A, Rashidian A, Schevchenko E, Smutna L, Pavek P, Kublbeck J, Kronenberger T, Zender L, Lammerhofer M, Dauch D, and Laufer SA (2025). Uncovering alpha-Selectivity for Liver X Receptor Agonists for Lipotoxic Cancer Therapies. J Med Chem 68: 7180-7196.PubMed
  12. Edmonds AK, Balourdas DI, Marsh GP, Felix R, Brasher B, Cooper J, Graber-Feesl C, Kollareddy M, Malik K, Stewart H, Chevassut TJT, Lineham E, Morley S, Fedorov O, Bennett J, Rajasekaran MB, Ojeda S, Harrison DA, Ott CJ, Joerger AC, Maple HJ, and Spencer J (2025). Structure-Guided Design of ISOX-DUAL-Based Degraders Targeting BRD4 and CBP/EP300: A Case of Degrader Collapse. J Med Chem 68: 9638-9660.PubMed
  13. Wagner K, Keiten-Schmitz J, Adhikari B, Patra U, Husnjak K, McNicoll F, Dormann D, Muller-McNicoll M, Tascher G, Wolf E, and Muller S (2025). Induced proximity to PML protects TDP-43 from aggregation via SUMO-ubiquitin networks. Nat Chem Biol.PubMed
  14. Zhao B, Fang R, Schurmann H, Hemmer EJ, Mayer GL, Trajkovic-Arsic M, Althoff K, Yang J, Godfrey L, Liffers ST, Savvatakis K, Dorsch M, Gruner BM, Hahn S, Remke M, Lueong SS, and Siveke JT (2025). PLK1 blockade enhances the anti-tumor effect of MAPK inhibition in pancreatic ductal adenocarcinoma. Cell Rep 44: 115541.PubMed
  15. Maciel EVS, Eisert J, Dederer V, Berwanger A, Knapp S, Empting M, Mathea S, Jensen H, and Lermyte F (2025). Native Flow-Induced Dispersion Analysis - Mass Spectrometry Enables Automated, Multiplexed Ligand Screening from Conventional, Nonvolatile Buffers. Anal Chem.PubMed
  16. Muller S, Sanfelice D, and Workman P (2025). Probing cancer with small-molecule tools-Progress and challenges. Cancer Cell 43: 323-327.PubMed
  17. Willems S, Maksumic L, Niggenaber J, Lin TC, Schulz T, Weisner J, Sievers S, Muller MP, Summerer D, and Rauh D (2025). Advancing TET Inhibitor Development: From Structural Insights to Biological Evaluation. ACS Med Chem Lett 16: 804-810.PubMed
  18. Eisert J, Maciel EVS, Dederer V, Berwanger A, Bailey HJ, Dikic I, Knapp S, Empting M, Mathea S, Jensen H, and Lermyte F (2025). Native Taylor/Non-Taylor Dispersion-Mass Spectrometry (TNT-MS) Allows Rapid Protein Desalting and Multiplexed, Label-Free Ligand Screening. Small Methods: e2500658.PubMed
  19. Mandel S, Hanke T, Mathea S, Chatterjee D, Saraswati H, Berger BT, Schwalm MP, Yamamoto S, Tawada M, Takagi T, Ahmed M, Rohm S, Corrionero A, Alfonso P, Baena M, Elson L, Menge A, Kramer A, Pereira R, Muller S, Krause DS, and Knapp S (2025). Repurposing of the RIPK1-Selective Benzo[1,4]oxazepin-4-one Scaffold for the Development of a Type III LIMK1/2 Inhibitor. ACS Chem Biol.PubMed
  20. Wang X, Sun J, Ahmad S, Yang D, Li F, Chan UH, Zeng H, Simoben CV, Houliston S, Dong A, Bolotokova A, Gibson E, Kutera M, Ghiabi P, Kondratov I, Matviyuk T, Chuprina A, Mavridi D, Lenz C, Joerger AC, Brown BD, Heath RB, Yue WW, Robbie LK, Beyett TS, Muller S, Knapp S, Harding R, Schapira M, Brown PJ, Santhakumar V, Ackloo S, Arrowsmith CH, Edwards AM, Peng H, and Halabelian L (2025). Enantioselective Protein Affinity Selection Mass Spectrometry (EAS-MS). bioRxiv.PUbMed
  21. Funk JS, Klimovich M, Drangenstein D, Pielhoop O, Hunold P, Borowek A, Noeparast M, Pavlakis E, Neumann M, Balourdas DI, Kochhan K, Merle N, Bullwinkel I, Wanzel M, Elmshauser S, Teply-Szymanski J, Nist A, Procida T, Bartkuhn M, Humpert K, Mernberger M, Savai R, Soussi T, Joerger AC, and Stiewe T (2025). Deep CRISPR mutagenesis characterizes the functional diversity of TP53 mutations. Nat Genet 57: 140-153.PubMed
  22. Bhandare P, Narain A, Hofstetter J, Rummel T, Wenzel J, Schulein-Volk C, Lamer S, Eilers U, Schlosser A, Eilers M, Erhard F, and Wolf E (2025). Phenotypic screens identify SCAF1 as critical activator of RNAPII elongation and global transcription. Nucleic Acids Res 53.PubMed
  23. Schulz T, Gontla R, Teuber A, Beerbaum M, Fletcher BS, Muhlenberg T, Kaitsiotou H, Hardick J, Jeyakumar K, Keul M, Muller MP, Sievers S, Bauer S, and Rauh D (2025). Design, Synthesis, and SAR of Covalent KIT and PDGFRA Inhibitors horizontal line Exploring Their Potential in Targeting GIST. J Med Chem 68: 3238-3259.PubMed
  24. Moyano PM, Kubina T, Paruch SO, Jaroskova A, Novotny J, Skockova V, Ovesna P, Suchankova T, Prokofeva P, Kuster B, Smida M, Chaikuad A, Kramer A, Knapp S, Soucek K, and Paruch K (2025). Thieno[3,2-b]pyridine: Attractive scaffold for highly selective inhibitors of underexplored protein kinases with variable binding mode. Angew Chem Int Ed Engl 64: e202412786.PubMed
  25. Miletic N, Weckesser J, Mosler T, Rathore R, Hoffmann ME, Gehrtz P, Schlesiger S, Hartung IV, Berner N, Wilhelm S, Muller J, Adhikari B, Nemec V, Sivashanmugam SA, Elson L, Holzmann H, Schwalm MP, Hoffmann L, Abdul Azeez KR, Muller S, Kuster B, Wolf E, Dikic I, and Knapp S (2025). Workflow for E3 Ligase Ligand Validation for PROTAC Development. ACS Chem Biol 20: 507-521.PubMed
  26. Haag A, Nemec V, Janovska P, Bartosikova J, Adhikari B, Muller J, Schwalm MP, Cada S, Ohmayer U, Daub H, Kim Y, Born F, Wolf E, Bryja V, and Knapp S (2025). Development and Discovery of a Selective Degrader of Casein Kinases 1 delta/epsilon. J Med Chem 68: 506-530.PubMed
  27. Pieper NM, Schnell J, Bruecher D, Knapp S, and Vogler M (2024). Inhibition of bromodomain and extra-terminal proteins targets constitutively active NFkappaB and STAT signaling in lymphoma and influences the expression of the antiapoptotic proteins BCL2A1 and c-MYC. Cell Commun Signal 22: 415.PubMed
  28. Zhu WF, Franz HM, Kramer A, Duman E, Empel C, Gobel MW, Koenigs RM, Knapp S, Hiesinger K, Proschak E, and Hernandez-Olmos V (2024). Oxadiazolone-Based Aromatic Annulations: A Nitrenoid Precursor for Tricyclic Aminoheterocycles. J Org Chem 89: 15542-15552.PubMed
  29. Vogt M, Dudvarski Stankovic N, Cruz Garcia Y, Hofstetter J, Schneider K, Kuybu F, Hauck T, Adhikari B, Hamann A, Rocca Y, Grysczyk L, Martin B, Gebhardt-Wolf A, Wiegering A, Diefenbacher M, Gasteiger G, Knapp S, Saur D, Eilers M, Rosenfeldt M, Erhard F, Vos SM, and Wolf E (2024). Targeting MYC effector functions in pancreatic cancer by inhibiting the ATPase RUVBL1/2. Gut 73: 1509-1528.PubMed
  30. Kramer A and Knapp S (2024). Elimination of mutant SWI/SNF complexes by protein quality control: new opportunities targeting aggressive rhabdoid tumours. Signal Transduct Target Ther 9: 224.PubMed
  31. Sflakidou E, Adhikari B, Siokatas C, Wolf E, and Sarli V (2024). Development of 2-Aminoadenine-Based Proteolysis-Targeting Chimeras (PROTACs) as Novel Potent Degraders of Monopolar Spindle 1 and Aurora Kinases. ACS Pharmacol Transl Sci 7: 3488-3501.PubMed