Publications 2024
Further information concerning the publications from the Sippl group can be found here:
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 Nov 10. 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 Nov 4. 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 Oct 12;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 Sep 17. 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 Sep 20. 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 Sep 18: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 Sep 20: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 Jul 12: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 Jun 20;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 Jun 17: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. JCIM, 2024 May 21. 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 7. 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 May 20;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 Mar 22. 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 Apr 16. 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. 20 (1), 30-39, 2024. doi:10.2174/1573406419666230622121512.