TACTIC  Publications

 

 

  1. Scholes NS, Bertoni M, Comajuncosa-Creus A, Kladnik K, Guo X, Frommelt F, Hinterndorfer M, Razumkov H, Prokofeva P, Schwalm MP, Born F, Roehm S, Imrichova H, Santini BL, Barone E, Schatz C, Munoz IOM, Lechner S, Rukavina A, Serrano I, Abele M, Koren A, Kubicek S, Knapp S, Gray NS, Superti-Furga G, Kuster B, Shi Y, Aloy P, and Winter GE (2026). Inhibitors supercharge kinase turnover through native proteolytic circuits. Nature 649: 1032-1041.PubMed
  2. Androulidaki A, Liu F, Bebber CM, Kisis I, Sakthivelu V, Hunold P, Koerner L, Dahlhaus A, Yapici FI, Grimm C, Pacholewska A, Tishina S, Doskotz F, Torres Fernandez LA, Stroh J, Abdallah AT, Beck J, Mulalic L, Schmitt A, Grull H, Persigehl T, Quaas A, Peifer M, Bragelmann J, Reinhardt HC, Nieper P, Hansel-Hertsch R, Thomas RK, George J, Schweiger MR, Pasparakis M, Beleggia F, and von Karstedt S (2025). Lack of caspase 8 directs neuronal progenitor-like reprogramming and small cell lung cancer progression. Nat Commun 16: 11280.PubMed
  3. Wang X, Sun J, Ahmad S, Yang D, Li F, Chan UH, Zeng H, Simoben CV, Green SR, Silva M, 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, Owen DR, 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 (E-ASMS). Nat Commun 17: 651.Pubmed
  4. Dampmann M, von Tresckow B, Reinhardt HC, Kuppers R, and von Tresckow J (2025). Insights into the pathogenesis and biology of chronic lymphocytic leukemia through analysis of its B-cell receptor. Leuk Lymphoma 66: 1778-1787.PubMed
  5. Castelli S, Wilson WV, Uslu U, Finck AV, Rommel PC, Assenmacher CA, Atoche SJ, Siurala M, Aznar MA, Young RM, and June CH (2026). IL-9 signaling redirects CAR T cell fate toward CD8(+) memory and CD4(+) cycling states, enhancing antitumor efficacy. Immunity 59: 195-212 e11.PubMed
  6. Mitrovic M, Greco FA, Garcia YC, Lucic A, Hoffmann L, Chander R, Schonfeld J, Liebisch N, Sivashanmugam SA, Schwalm MP, Egner M, Lewandowski M, Merk D, Morasch V, Wolf E, Muller S, Hanke T, Proschak E, Hiesinger K, and Knapp S (2026). Click. Screen. Degrade. A Miniaturized D2B Workflow for Rapid PROTAC Discovery. J Med Chem.PubMed
  7. Hesterberg RS, Davis JT, Handoo KJ, Elmarsafawi AG, Augello AC, Cheng CH, Atkins R, Lee DH, Yang C, Yao J, Patel KR, Mediavilla-Varela M, Pinilla-Ibarz J, Soto-Palma C, Locke FL, Song X, Wang X, Berglund AE, Rodriguez PC, Knittel G, Flumann R, Reinhardt HC, Shaw TI, Yu X, Niedernhofer LJ, and Cleveland JL (2025). Lymphoma accelerates T cell and tissue aging. Cancer Cell 43: 1917-1936 e8.PubMed
  8. O'Hanlon JA, Gutsche K, Muller JE, Ranjan Prusty N, Mirza A, Roumeliotis TI, Yang H, Stubbs M, Hallett ST, Eing L, McAndrew PC, Choudhary JS, Le Bihan YV, Caldwell J, van Montfort RLM, Workman P, Wolf E, Newton GK, and Evans LE (2026). Unhooking the Hook: Optimization of the Aurora A Targeting PROTAC JB170 to CCT400028, an In Vitro Degrader Chemical Probe. J Med Chem 69: 1552-1567.PubMed
  9. Kameri E, Jepsen VH, Stachura P, Ruchel N, Bhave R, Benitez L, Crispi F, Gratacos E, Dragano N, Janssen S, Borkhardt A, Pandyra A, Kogler G, and Fischer U (2024). A gut instinct for childhood leukemia prevention: microbiome-targeting recommendations aimed at parents and caregivers. Front Public Health 12: 1445113.PubMed
  10. Kirschner T, Rodriguez J, Moreira EG, Niggenaber J, Warmuth JD, Verli H, Muller MP, and Rauh D (2025). Targeting KRAS(G13C) with cyclic linker based inhibitors to explore warhead orientation. Sci Rep 15: 38213.PubMed
  11. Zhang R, Huetzen MA, Binici A, Martin-Gago P, Gasper R, Rudashevskaya E, Liu J, Nagaraju C, Reckzeh ES, Stuedle AST, Hopff AS, Mesaros A, Unger A, Thelen M, Janning P, Reinhardt HC, Ziegler S, Jachimowicz RD, and Waldmann H (2026). Targeting a Glutamic Acid in PDEdelta with Fluoromethyl-Aryl Electrophiles Impairs K-Ras Signaling. J Med Chem 69: 964-981.PubMed
  12. Hoffmann L, Lenz C, Farges F, Kimani SW, Dopfer J, Keller S, Schwalm MP, Holzmann H, Kraemer A, Dong A, Li F, Chau I, Halabelian L, Gstaiger M, Muller S, Knapp S, and Nemec V (2025). Discovery of an exquisitely selective WDR5 chemical probe accelerated by a high-quality DEL-ML Hit. RSC Chem Biol 6: 1585-1594.PubMed
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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.
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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
  27. 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
  28. Muller S, Sanfelice D, and Workman P (2025). Probing cancer with small-molecule tools-Progress and challenges. Cancer Cell 43: 323-327.PubMed
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. 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
  36. 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
  37. 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
  38. 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
  39. 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
  40. 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
  41. 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
  42. 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
  43. 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