Publikationen 2024
Weitere Informationen zu den Publikationen der AG Prof. Sippl finden sie hier:
Jungwirth J, Mieland AO, Piée-Staffa A, Heimburg T, Brenner W, Ehrhardt C, Sippl W, Henke A, Krämer OH. Pharmacologically induced proteolysis of histone deacetylase-6 attenuates influenza virus replication despite limited anti-tumor effects. Life Sci. 2025 Jan 13:123401. doi:10.1016/j.lfs.2025.123401.
Çelik C, İdiş ÖD, Özhan Y, Tirpanlar D, Unal N, Gungor B, Aru B, Gurdal EE, Sippl W, Sipahi H, Kırmızıbekmez H. Isolation of anti-inflammatory and cytotoxic secondary metabolites from Valeriana phu and evaluation of their mechanisms of action. Fitoterapia. 2025 Jan 6:181:106377. doi:10.1016/j.fitote.2025.106377 .
Waitman KB, Martin HJ, Carlos JAEG, Braga RC, Souza VAM, Melo-Filho CC, Hilscher S, Toledo MFZJ, Tavares MT, Costa-Lotufo LV, Machado-Neto JA, Schutkowski M, Sippl W, Kronenberger T, Alves VM, Parise-Filho R, Muratov EN.Dona Flor and her two husbands: Discovery of novel HDAC6/AKT2 inhibitors for myeloid cancer treatment. bioRxiv [Preprint]. 2024 Dec 5:2024.11.30.626092. doi:10.1101/2024.11.30.626092.
C. Vorreiter, D. Robaa, W. Sippl. Predicting Fragment Binding Modes Using Customized Lennard-Jones Potentials in Short Molecular Dynamics Simulations. Computational and Structural Biotechnology Journal, 27, 2025, 102-116 doi.org/10.1016/j.csbj.2024.12.017
A. Baumann , N. Papenkordt, D. Robaa, P.D. Szigetvari, A. Vogelmann, F. Bracher, W. Sippl, M. Jung, J. Haavik. Aromatic amino acid hydroxylases as off-targets of histone deacetylase inhibitors. ACS Chem Neurosci. 2024;15(22):4143-4155. doi:10.1021/acschemneuro.4c00346
M. Zmyslia, M.J. Capper, M. Grimmeisen, K. Sartory, B. Deuringer, M. Abdelsalam, K. Shen, M. Jung, W. Sippl, H.G. Koch, L. Kaul, R. Süss, J. Köhnke, C. Jessen-Trefzer C. A Nanoengineered Tandem Nitroreductase: Designing a Robust Prodrug-Activating Nanoreactor. RSC Chem Biol. 2024;6(1):21-35. doi:10.1039/d4cb00127c
H. S. Ibrahim, M. Guo, S. Hilscher, F. Erdmann, M. Schmidt, M. Schutkowski, C. Sheng, and W. Sippl. Probing Class I histone deacetylases (HDAC) with proteolysis targeting chimera (PROTAC) for the development of highly potent and selective degraders. Bioorg Chem. 2024;153:107887. doi:10.1016/j.bioorg.2024.107887 .
M. Halilovic, M. Abdelsalam, J. Zabkiewicz, M. Lazenby, C. Alvares, M. Schmidt, W. Brenner, S. Najafi, I. Oehme, C. Hieber, Y. Zeyn, M. Bros, W. Sippl, O. H. Krämer Selective degradation of mutant FMS-like tyrosine kinase-3 requires a depletion of heat shock proteins by BIM. Leukemia. 2024;38(12):2561-2572. doi:10.1038/s41375-024-02405-5 .
S. Mielniczuk, K. Hoff, F. Baselious, Y. Li, J. Haupenthal, A. M. Kany, M. Riedner, H. Rohde, K. Rox, A. K. H. Hirsch, I. Krimm, W. Sippl, and R. Holl. Development of fragment-based inhibitors of the bacterial deacetylase LpxCwith low nM activity. J Med Chem. 2024;67(19):17363-17391. doi:10.1021/acs.jmedchem.4c01262
F. Berluti, F. Baselious, S. Hagemann, S. Hilscher, M. Schmidt, S. Hüttelmaier, M. Schutkowski, W. Sippl and H. S. Ibrahim. Development of new pyrazoles as class I HDAC inhibitors: synthesis, molecular modelling and biological characterisation in leukaemia cells. Arch Pharm (Weinheim). 2024;357(11):e2400437. doi:10.1002/ardp.202400437
A. Erdogan, Y. Ozhan, H. Sipahi, E.E. Gurdal, W. Sippl W, M. Koksal. iNOS/PGE2 Inhibitors as a novel template for analgesic/anti-inflammatory activity: Design, synthesis, in vitro biological activity and docking studies. Arch Pharm (Weinheim). 2024;357(12):e2400238. doi:10.1002/ardp.202400238
F. Baselious, S. Hilscher, S. Hagemann, S. Tripathe, D. Robaa, C. Barinka, S. Hüttelmaier, M. Schutkowski, W. Sippl. Utilization of an Optimized AlphaFold Protein Model for Structure-Based Design of a Selective HDAC11 Inhibitor with Anti-neuroblastoma Activity. Arch Pharm (Weinheim). 2024;357(10):e2400486. doi:10.1002/ardp.202400486
M. Gekle, R. Eckenstaler, H. Braun, A. Olgac, D. Robaa, S. Mildenberger, V. Dubourg, B. Schreier, W. Sippl, R. Benndorf. Direct GPCR-EGFR interaction enables synergistic membrane-to-nucleus information transfer. Cell Mol Life Sci. 2024;81(1):272. doi:10.1007/s00018-024-05281-5 .
C. Schneider, J. Hilbert, F. Genevaux, S. Höfer, L. Krauß, F. Schicktanz, C. T. Contreras, S. Jansari, A. Papargyriou, T. Richter, A. M. Alfayomy, C. Falcomatà, C. Schneeweis, F. Orben, R. Öllinger, F. Wegwitz, A. Boshnakovska, P. Rehling, D. Müller, P. Ströbel, V. Ellenrieder, L. Conradi, E. Hessmann, M. Ghadimi, M. Grade, M. Wirth, K. Steiger, R. Rad, B. Kuster, W. Sippl, M. Reichert, D. Saur, G. Schneider. A Novel AMPK Inhibitor Sensitizes Pancreatic Cancer Cells to Ferroptosis Induction. Adv Sci (Weinh). 2024;11(31):e2307695. doi:10.1002/advs.202307695.
C. Vorreiter, D. Robaa, W. Sippl. Exploring Aromatic Cage Flexibility Using Cosolvent MD Simulations – an In-Silico Case Study on Tudor Domains. J Chem Inf Model. 2024;64(11):4553-4569. doi:10.1021/acs.jcim.4c00298
A. Colcerasa, F. Friedrich, J. Melesina, P. Moser, A. Vogelmann, P. Tzortzoglou, E. Neuwirt, M. Sum, L., D. Robaa, Zhang, E. Ramos-Morales, C. Romier, O. Einsle, E. Metzger, R. Schüle, O. Gross, W. Sippl, M. Jung. Structure-activity studies of 1,2,4-oxadiazoles for the inhibition of the NAD+ dependent lysine deacylase Sirtuin 2. J Med Chem. 2024 Jun 27;67(12):10076-10095. doi:10.1021/acs.jmedchem.4c00229 .
A. Soudi, O. Bender, I. Celik, A.A.A. El-Hafeez, R. Dogan, A. Atalay, E.B.Elkaeed, A.A. Alsfouk, E.M.N. Abdelhafez, O.M. Aly, W. Sippl, T.F.S. Ali. Discovery and Anticancer Screening of Novel Oxindole-Based Derivative Bearing Pyridyl Group as Potent and Selective Dual FLT3/CDK2 Kinase Inhibitor. Pharmaceuticals (Basel). 2024;17(5):659. doi:10.3390/ph17050659
A. G. Kansy, R. Ashry, A. M. Mustafa, A. Alfayomy, M.P. Radsak, Y. Zeyn, M. Bros, W. Sippl and O. H. Krämer. Pharmacological degradation of ATR induces antiproliferative DNA replication stress in leukemic cells.Mol Oncol. 2024;18(8):1958-1965. doi:10.1002/1878-0261.13638.
A. M. Alfayomy, R. Ashry, A. Kansy, A.C. Sarnow, F. Erdmann, M. Schmidt, O. H. Krämer, W. Sippl. Design, synthesis, and biological characterization of proteolysis targeting chimera (PROTACs) for the Ataxia telangiectasia and RAD3-related (ATR) kinase. European J Med Chem. 2024, 267:116167. https://doi.org/10.1016/j.ejmech.2024.116167
N. Cheshmazar, M. Hamzeh-Mivehroud, S. Hemmati, H. Abolhasani, F. Heidari, H. N. Charoudeh, M. Zessin, M. Schutkowski, W. Sippl, S. Dastmalchi. Key structural requirements of benzamide derivatives for HDAC inhibition: Design, synthesis and biological evaluation. Future Med Chem. 2024;16(9):859-872. doi:10.4155/fmc-2023-0122
F. Baselious, S. Hilscher, D. Robaa, C. Barinka, M. Schutkowski, W. Sippl. Comparative Structure-Based Virtual Screening Utilizing Optimized AlphaFold Model Identifies Selective HDAC11 Inhibitor. Int. J. Mol. Sci. 2024, 25(2), 1358; doi.org/10.3390/ijms25021358
M. Pannek, Z. Al Halabi, D. Tomaselli, M. Menna, F. Fiorentino, D. Robaa, M. Weyand, M. Puhlmann, S. Tomassi, F. Barreca, M. Tafani, E. Zaganjor, M. Haigis, W. Sippl, D. Rotili, A. Mai, C. Steegborn. Specific Inhibitors of the Mitochondrial Deacylase Sirtuin 4 Endowed with Cellular Activity. J Med Chem. 2024; 67(3):1843-1860. doi:10.1021/acs.jmedchem.3c01496 .
L. Seitz, N. Reiling, C. Vorreiter, W. Sippl, S. Kessler, A. Hilgeroth.Synthesis and Evaluation of Novel Substituted N-Aryl 1,4-Dihydropyridines as An-tituberculostatic Agents. Med Chem. 2024l;20 (1), 30-39. doi:10.2174/1573406419666230622121512.