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Publikationen

Our doctoral students contributed with their work to several publications and patents. Please find a lists of all publications of our GRK2158 fellows in 2023, 2022, 2021, 2020, 2019, 2018, 2017.

The special issue "Natural product-derived lead structures and modes-of-action against therapy-resistant tumors and microorganisms" in the Journal of Bioorganic & Medicinal Chemistry was edited by the Research Training Group 2158 speaker Holger Gohlke in 2019 and contains numerous contributions of scientists of the Research Training Group 2158.

2024
  • Schmitt, L., Hoppe, J., Cea-Medina, P., Bruch, P.-M., Krings, K. S., Lechtenberg, I., Drießen, D., Peter, C., Bhatia, S., Dietrich, S., Stork, B., Fritz, G., Gohlke, H., Müller, T.J.J., Wesselborg, S. (2024) Novel meriolin derivatives potently inhibit cell cycle progression and transcription in leukemia and lymphoma cells via inhibition of cyclin-dependent kinases (CDKs). Cell Death Discov. 10, 279 https://doi.org/10.1038/s41420-024-02056-6
  • Mazzone, F., Hoeppner, A., Reiners, J., GertzenC.G.W., Applegate, V., Abdullaziz, M.A., Gottstein, J., Degrandi, D., Wesemann, M., Kurz, T., Smits, S.H.J., Pfeffer, K. (2024) 1-Deoxy-d-xylulose 5-phosphate reductoisomerase as target for anti Toxoplasma gondii agents: crystal structure, biochemical characterization and biological evaluation of inhibitors. Biochem J 481 (16): 1075–1096. https://doi.org/10.1042/BCJ20240110
  • Podlesainski, D., Adeniyi, E. T., Gröner, Y., Schulz, F., Krisilia, V., Rehberg, N., Richter, T., Sehr, D., Xie, H., Simons, V. E., Kiffe-Delf, A., Kaschani, F., Ioerger, T. R., Kaiser, M., Kalscheuer, R. (2024) The anti-tubercular callyaerins target the Mycobacterium tuberculosis-specific non-essential membrane protein Rv2113. Cell Chemical Biology 31. https://doi.org/10.1016/j.chembiol.2024.06.002
  • Oikonomou, A., Watrin, T., Valsecchi, L., Scharov, K., Savino, A. M., Schliehe-Diecks, J., Bardini, M., Fazio, G., Bresolin, S., Biondi, A., Borkhardt, A., Bhatia, S., Cazzaniga, G., & Palmi, C. (2024) Synergistic drug interactions of the histone deacetylase inhibitor givinostat (ITF2357) in CRLF2-rearranged pediatric B-cell precursor acute lymphoblastic leukemia identified by high-throughput drug screening. Heliyon, 10(13), e34033. https://doi.org/10.1016/j.heliyon.2024.e34033
  • Mazzone, F., Klischan, M. K. T., Greb, J., Smits, S. H. J., Pietruszka, J., Pfeffer, K. (2024) Synthesis and In vitro evaluation of bichalcones as novel anti-toxoplasma agents. Front. Chem. https://doi.org/10.3389/fchem.2024.1406307
  • Klischan, M. K. T., David, C., Grudzinski, D., Frey, W., Stork, B., Pietruszka, J. (2024) Application of Cyclic Diaryliodonium Salts in the Synthesis of Axially Chiral Natural Product Analogues. Org. Lett. https://doi.org/10.1021/acs.orglett.4c01308 
  • Schmitt, L., Hoppe, J., Cea-Medina, P., Bruch, P-M., Krings, K. S., Lechtenberg, I., Drießen, D., Peter, C., Bhatia, S., Dietrich, S., Stork, B., Fritz, G., Gohlke, H., Müller, T. J. J., Wesselborg, S. (2024) Novel meriolin derivatives potently inhibit cell cycle progression and transcription in leukemia and lymphoma cells via inhibition of cyclin-dependent kinases (CDKs). Cell Death Discov. 10, 279  https://doi.org/10.1038/s41420-024-02056-6
  • Adeniyi, E. T., Kruppa, M., De Benedetti, S., Ludwig, K. C., Krisilia, V., Wassenberg, T. R., Both, M., Schneider, T., Müller, T. J. J., Kalscheuer. R. (2024) Synthesis of Bisindole Alkaloids and Their Mode of Action against Methicillin-Resistant Staphylococcus Aureus. ACS Infect. Dis. 10, 1958–1969 https://doi.org/10.1021/acsinfecdis.3c00657 
  • Schiedlauske, K., Deipenbrock, A., Pflieger, M., Hamacher, A., Hänsel, J., Kassack, M.U., Kurz, T., Teusch, N.E. (2024) Novel Histone Deacetylase (HDAC) Inhibitor Induces Apoptosis and Suppresses Invasion via E-Cadherin Upregulation in Pancreatic Ductal Adenocarcinoma (PDAC). Pharmaceuticals 17, 752. https://doi.org/10.3390/ph17060752
  • Abdullaziz, M. A., Takada, S., Illarionov, B., Pessanha de Carvalho, L., Sakamoto, Y., Höfmann, S., Knak, T., Kiffe-Delf, A. L., Mazzone, F., Pfeffer, K., Kalscheuer, R., Bacher, A., Held, J., Fischer, M., Tanaka, N., & Kurz, T. (2024). Reverse N-Substituted Hydroxamic Acid Derivatives of Fosmidomycin Target a Previously Unknown Subpocket of 1-Deoxy-d-xylulose 5-Phosphate Reductoisomerase (DXR). ACS infectious diseases. 10(5), 1739–1752. https://doi.org/10.1021/acsinfecdis.4c00100   
  • Tretbar, M., Schliehe-Diecks, J., von Bredow, L., Tan, K., Roatsch, M., Tu, J-W., Kemkes, M., Sönnichsen, M., Schöler, A., Borkhardt, A., Bhatia, S., Hansen, F.K. (2024) Preferential HDAC6 inhibitors derived from HPOB exhibit synergistic antileukemia activity in combination with decitabine. Eur J Med Chem. 272:116447. https://doi.org/10.1016/j.ejmech.2024.116447
  • Schmitt, L., Lechtenberg, I., Drießen, D., Flores-Romero, H., Skowron, M.A., Sekeres, M., Hoppe, J., Krings, K.S., Llewellyn, T.R., Peter, C., Stork, B., Qin, N., Bhatia, S., Nettersheim, D., Fritz, G., García-Sáez, A.J., Müller, T.J.J., Wesselborg, S. (2024) Novel meriolin derivatives activate the mitochondrial apoptosis pathway in the presence of antiapoptotic Bcl-2. Cell Death Discov. 10, 125 https://doi.org/10.1038/s41420-024-01901-y
  • Junk, L., Schmiedel, V.M., Guha, S., Fischel, K., Greb, P., Vill, K., Krisilia, V., van Geelen, L., Rumpel, K., Kaur, P., Krishnamurthy, R.V., Narayanan, S., Shandil, R.K., Singh, M., Kofink, C., Mantoulidis, A., Biber, P., Gmaschitz, G., Kazmaier, U., Meinhart, A., Leodolter, J., Hoi, D., Junker, S., Morreale, F.E., Clausen, T,. Kalscheuer, R., Weinstabl, H., Boehmelt, G. (2024)  Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria. Nat Commun 15, 2005 https://doi.org/10.1038/s41467-024-46218-7
  • Weber, F., Weber, A., Schmitt, L., Lechtenberg, I., Greb, J., Henßen, B., Wesselborg, S., Pietruszka, J. (2024) From the Total Synthesis of Semi-Viriditoxin, Semi-Viriditoxic Acid and Dimeric Naphthopyranones to their Biological Activities in Burkitt B Cell Lymphoma. Chem. Eur J, e202400559.
  • Zhang, H., Dierkes, R. F., Perez-Garcia, P., Costanzi, E., Dittrich, J., Cea, P. A., Gurschke, M., Applegate, V., Partus, K., Schmeisser, C., Pfleger, C., Gohlke, H., Smits, S. H. J., Chow, J., Streit, W. R. (2024) The metagenome-derived esterase PET40 is highly promiscuous and hydrolyses polyethylene terephthalate (PET). FEBS J. 291(1):70-91. doi: 10.1111/febs.16924
  • Amariei, D. A., Haase, M., Klischan, M. K. T., Wäscher, M., Pietruszka, J. (2024) High-Throughput Colorimetric Detection and Quantification of Indoles and Pyrroloindoles for Enzymatic Activity Determination. ChemCatChem e202400052, https://doi.org/10.1002/cctc.202400052
  • Asfaha, Y., Bollmann, L. M., Skerhut, A. J., Fischer, F., Horstick, N., Roth, D., Wecker, M., Mammen, C., Smits, S. H. J., Fluegen, G., Kassack, M. U., Kurz, T. (2024) 5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib. European Journal of Medicinal Chemistry. 263, 115907 https://doi.org/10.1016/j.ejmech.2023.115907
2023
  • Vogt, M., Dienstbier, N., Schliehe-Diecks, J., Scharov, K., Tu, J.-W., Gebing, P., Hogenkamp, J., Bilen, B.-S., Furlan, S., Picard, D., Remke, M., Yasin, L., Bickel, D., Kalia, M., Iacoangeli, A., Lenz, T., Stühler, K., Pandyra, A.A., Hauer, J., Fischer, U., Wagener, R., Borkhardt, A., Bhatia, S. (2023) Co-targeting HSP90 alpha and CDK7 overcomes resistance against HSP90 inhibitors in BCR-ABL1+ leukemia cells. Cell Death Dis. 6;14(12):799. https://doi.org/10.1038/s41419-023-06337-3
  • Klischan, M. K. T., Mazzone, F., Berning, L., Greb, J., Schlamkow, M., Haase, M., Frey, W., Stork, B., Pfeffer, K., Pietruszka, J. (2023) Modular Approach for the Synthesis and Bioactivity Profiling of 8,8′-Biflavones. ACS Omega 8(44):41816–41834. https://doi.org/10.1021/acsomega.3c06503
  • Yakici, N., Kreins, A. Y., Catak, M. C., Babayeva, R., Erman, B., Kenney, H., Gungor, H. E., Cea, P. A., Kawai, T., Bosticardo, M., Delmonte, O. M., Adams, S., Fan, Y. T., Pala, F., Turkyilmaz, A., Howley, E., Worth, A., Kot, H., Sefer, A. P., Kara, A., Bulutoglu, A., Eltan, S. B., Altunbas, M. Y., Bayram, F., Karakus, I. S., Karatay, E., Tekeoglu, S. D., Eser, M., Albayrak, D., Citli, S., Kiykim, A., Karakoc-Aydiner, E., Ozen, A., Ghosh, S., Gohlke, H., Orhan, F., Notarangelo, L. D., Davies, E. G., Baries, S. (2023) Expanding the clinical and immunological phenotypes of PAX1-deficient SCID and CID patients. Clin Immunol. 255, 109757 https://doi.org/10.1016/j.clim.2023.109757
    • Yakici, N., Kreins, A. Y., Catak, M. C., Babayeva, R., Erman, B., Kenney, H., Gungor, H. E., Cea, P. A., Kawai, T., Bosticardo, M., Delmonte, O. M., Adams, S., Fan, Y. T., Pala, F., Turkyilmaz, A., Howley, E., Worth, A., Kot, H., Sefer, A. P., Kara, A., Bulutoglu, A., Eltan, S. B., Altunbas, M. Y., Bayram, F., Karakus, I. S., Karatay, E., Tekeoglu, S. D., Eser, M., Albayrak, D., Citli, S., Kiykim, A., Karakoc-Aydiner, E., Ozen, A., Ghosh, S., Gohlke, H., Orhan, F., Notarangelo, L. D., Davies, E. G., Baries, S. (2023) Corrigendum to "Expanding the clinical and immunological phenotypes of PAX1-deficient SCID and CID patients" [Clinical Immunology 255 (2023) 109757]. Clin Immunol. 256:109799. doi: 10.1016/j.clim.2023.109799. Erratum for: Clin Immunol. 2023, 255:109757.

  • Berning, L., Lenz, T., Bergmann, A. K., Poschmann, G., Brass, H. U. C., Schlütermann, D., Friedrich, A., Mendiburo, M. J., David, C., Akgün, S., Pietruszka, J., Stühler, K., Stork, B. (2023) The Golgi stacking protein GRASP55 represents an effector protein of the natural compound Prodigiosin. Cell Commun. Signal. 21(1):275. doi: 10.1186/s12964-023-01275-1
  • Weber, T. M., Leyens, A., Berning, L., Stork, B., Pietruszka, J. (2023) New prodigiosin derivatives - chemoenzymatic synthesis and physiological evaluation. Catal Sci Technol 13: 6165-6184
  • Ganardi, R., Greb, J., Henssen, B., Pietruszka, J. (2023) Atroposelective Total Synthesis of (+)-Isokotanin A via Combined Metal and Enzyme Catalysis. Adv Synth Catal 365(20):3512-3520 https://doi.org/10.1002/adsc.202300698
  • Greb, J., Drennhaus, T., Klischan, M. K. T., Schroeder, Z., Frey, W., Pietruszka, J. (2023) A Common C2-Symmetric 2,2′-Biphenol Building Block and its Application in the Synthesis of (+)-di-epi-Gonytolide A. Chem. Eur. J. 29(34):e202300941, https://doi.org/10.1002/chem.202300941
  • Weber, T. M., Pietruszka, J. (2023) Synthesis of a Water-Soluble Tridentate (Dimethylamino)ethyl Cu(I)/Cu(II)-Ligand. Synthesis 55(14):2128-2133 DOI: 10.1055/a-2034-9427 online available
  • Kruppa, M., Müller, T. J. J. (2023) Masuda Borylation-Suzuki Coupling (MBSC) Sequence: A One-Pot process to access complex (hetero)biaryls. Catalysts 13(2), 359 https://doi.org/10.3390/catal13020350
  • Kruppa, M., Müller, T.J.J. (2023) A Survey on the Synthesis of Variolins, Meridianins, and Meriolins—Naturally Occurring Marine (aza)Indole Alkaloids and Their Semisynthetic Derivatives. Molecules 28, 947. https://doi.org/10.3390/molecules28030947 
  • Hafez, D. E., Dubiel, M., La Spada, G., Catto, M., Reiner-Link, D., Syu, Y.-T., Abdel-Halim, M., Hwang, T.-L., Stark, H., Abadi, A. H. (2023) Novel benzothiazole derivatives as multitargeted-directed ligands for the treatment of Alzheimer’s disease, Journal of Enzyme Inhibition and Medicinal Chemistry, 38:1, DOI: 10.1080/14756366.2023.2175821
  • Łażewska, D., Kaleta, M., Zaręba, P., Godyń, J., Dubiel, M., Honkisz-Orzechowska, E., Doroz-Płonka, A., Więckowska, A., Stark, H., Kieć-Kononowicz, K. (2023) Multitargeting Histamine H3 Receptor Ligands among Acetyl- and Propionyl-Phenoxyalkyl Derivatives. Molecules 28, 2349. https://doi.org/10.3390/molecules28052349 
2022
  • Knak, T., Abdullaziz, M.A., Höfmann, S., Alves Avelar, L.A., Klein, S., Martin, M., Fischer, M., Tanaka, N., Kurz, T. (2022) Over 40 Years of Fosmidomycin Drug Research: A Comprehensive Review and Future Opportunities. Pharmaceuticals  15, 1553. https://doi.org/10.3390/ph15121553 
  • Burmeister, A., Stephan, A., Alves Avelar, L.A., Müller, M.R., Seiwert, A., Höfmann, S., Fischer, F., Torres-Gomez, H., Hoffmann, M.J., Niegisch, G., Bremmer, F., Petzsch, .P, Köhrer, K., Albers, P., Kurz, T., Skowron, M.A., Nettersheim, D. (2022) Establishment and Evaluation of Dual HDAC/BET Inhibitors as Therapeutic Options for Germ Cell Tumors and Other Urological Malignancies. Mol Cancer Ther. 21(11):1674-1688. doi: 10.1158/1535-7163.MCT-22-0207
  • Chu, K. B., Lee, H. A., Pflieger, M., Fischer, F., Asfaha, Y., Alves Avelar, L. A., Skerhut, A., Kassack, M. U., Hansen, F. K., Schöler, A., Kurz, T., Kim, M. J., Moon, E. K., Quan, F. S. (2022) Antiproliferation and Antiencystation Effect of Class II Histone Deacetylase Inhibitors on Acanthamoeba castellanii. ACS Infect Dis. 8(2):271-279. doi: 10.1021/acsinfecdis.1c00390
  • Eissa, N., Venkatachalam, K., Jayaprakash, P., Falkenstein, M., Dubiel, M., Frank, A., Reiner-Link, D., Stark, H., Sadek, B. (2022) The Multi-Targeting Ligand ST-2223 with Histamine H3 Receptor and Dopamine D2/D3 Receptor Antagonist Properties Mitigates Autism-Like Repetitive Behaviors and Brain Oxidative Stress in Mice. Int. J. Mol. Sci. 2021, 22, 1947. doi.org/10.3390/ijms22041947
  • Venkatachalam, K., Zhong, S., Dubiel, M., Satała, G., Sadek, B., Stark, H. (2022) The Novel Pimavanserin Derivative ST-2300 with Histamine H3 Receptor Affinity Shows Reduced 5-HT2A Binding, but Maintains Antidepressant- and Anxiolytic-like Properties in Mice. Biomolecules, 12, 683. https://doi.org/10.3390/biom12050683
  • von Bredow, L., Schäfer, T.M., Hogenkamp, J., Tretbar, M., Stopper, D., Kraft, F.B., Schliehe-Diecks, J., Schöler, A., Borkhardt, A., Bhatia, S., Held, J., Hansen, F.K. (2022) Synthesis, Antiplasmodial, and Antileukemia Activity of Dihydroartemisinin-HDAC Inhibitor Hybrids as Multitarget Drugs. Pharmaceuticals (Basel). 15(3):333. doi: 10.3390/ph15030333
  • Reßing, N., Schliehe-Diecks, J., Watson, P. R., Sönnichsen, M., Cragin, A. D., Schöler, A., Yang, J., Schäker-Hübner, L., Borkhardt, A., Christianson, D. W., Bhatia, S., Hansen, F K. (2022) Development of fluorinated peptoid-based histone deacetylase (HDAC) inhibitors for therapy-resistant acute leukemia. J Med Chem https://doi.org/10.1021/acs.jmedchem.2c01418
  • Sinatra, L., Yang, J., Schliehe-Diecks, J., Dienstbier, N., Vogt, M., Gebing, P., Bachmann, L. M., Sönnichsen, M., Lenz, T., Stühler, K., Schöler, A., Borkhardt, A., Bhatia, S., Hansen, F. K. (2022) Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with antileukemic activity. J Med Chem https://doi.org/10.1021/acs.jmedchem.2c01659
  • Stuhldreier, F., Schmitt, L., Lenz, T., Hinxlage, I., Zimmermann, M., Wollnitzke, P., Schliehe-Diecks, J., Liu, Y., Jäger, P., Geyh, S., Teusch, N., Peter, C., Bhatia, S., Haas, R., Levkau, B., Reichert, A.S., Stühler, K., Proksch, P., Stork, B., Wesselborg, S. (2022) The mycotoxin viriditoxin induces leukemia- and lymphomaspecific apoptosis by targeting mitochondrial metabolism. Cell Death Dis 13, 938 (2022). https://doi.org/10.1038/s41419-022-05356-w 
  • Erenburg, I.N., Hänsch, S., Chacko, F.M., Hamacher, A., Wintgens, S., Stuhldreier, F., Poschmann, G., Spitz, O., Stühler, K., Wesselborg, S., Hegemann, J.H., Smits, S.H.J., Weidtkamp-Peters, S., Schmitt, L. (2022) Heterologously secreted MbxA from Moraxella bovis induces a membrane blebbing response of the human host cell. SciRep 12:17825 https://doi.org/10.1038/s41598-022-22480-x
  • Reimche, I., Yu, H., Ariantari, N.P., Liu, Z., Merkens, K., Rotfuß, S., Peter, K., Jungwirth, U., Bauer, N., Kiefer, F., Neudörfl, J.-M., Schmalz, H.-G., Proksch, P., Teusch, N. (2022) Phenanthroindolizidine alkaloids isolated from Tylophora ovata as potent inhibitors of inflammation, spheroid growth, and invasion of triple-negative breast cancer. Int. J. Mol. Sci. 23, 10319. https://doi.org/10.3390/ijms231810319  
  • Mazzone, F., Simons, V. E., van Geelen, L., Frank, M., Mandi, A., Kurtán, T., Pfeffer, K., Kalscheuer, R. (2022) In vitro biological activity of natural products from the endophytic fungus Paraboeremia selaginellae against Toxoplasma gondii. Antibiotics 11(9), 1176 https://doi.org/10.3390/antibiotics11091176
  • Berger, A., Knak, T., Kiffe-Delf, A.-L., Mudrovcic, K., Singh, V., Njoroge, M., Burckhardt, B. B., Gopalswamy, M., Lungerich, B., Ackermann, L., Gohlke, H., Chibale, K., Kalscheuer, R., Kurz, T. (2022) Total synthesis of the antimycobacterial natural product chlorflavonin and analogs via a late-stage ruthenium(II)-catalyzed ortho-C(sp²)-H-hydroxylation.  Pharmaceuticals 15(8), 984; https://doi.org/10.3390/ph15080984 
  • Gopalswamy, M., Kroeger, T., Bickel, D., Frieg, B., Akter, S., Schott-Verdugo, S., Viegas, Al., Pauly, T., Mayer, M., Przibilla, J., Reiners, J., Nagel-Steger, L., Smits, S. H. J., Groth, G., Etzkorn, M., Gohlke, G. (2022) Biophysical and pharmacokinetic characterization of a small-molecule inhibitor of RUNX1/ETO tetramerization with anti-leukemic effects. Sci Rep 12, 14158 https://doi.org/10.1038/s41598-022-17913-6
  • Cox, J., Esser, L.M., Jüdt, M., Schmitz, K., Reiffert, K., Grimmler, M., Stork, B., Wesselborg, S., Peter, C. (2022) NF90/NFAR (nuclear factors associated with dsRNA) - a new methylation substrate of the PRMT5-WD45-RioK1 complex. Biol Chem. doi.org/10.1515/hsz-2022-0136
  • Bhatia, S., Spanier, L., Bickel, D., Dienstbier, N., Woloschin, V., Vogt, M., Pols, H., Lungerich, B., Reiners, J., Aghaallaei, N., Diedrich, D., Frieg, B., Schliehe-Diecks, J., Bopp, B., Lang, F., Gopalswamy, M., Loschwitz, J., Bajohgli, B., Skokowa, J., Borkhardt, A., Hauer, J., Hansen, F.K., Smits, S.H.J., Jose, J., Gohlke, H., Kurz, T. (2022) Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization. ACS Cent Sci. 8(5):636-655. https://doi.org/10.1021/acscentsci.2c00013
  • Aengenvoort, J., Sekeres, M., Proksch, P., Fritz, G. (2022) Targeting Mechanisms of the DNA Damage Response (DDR) and DNA Repair by Natural Compounds to Improve cAT-Triggered Tumor Cell Death. Molecules  27, 3567. https://doi.org/10.3390/molecules27113567
  • Mastromarino, M., Niso, M., Abate, C., Proschak, E., Dubiel, M., Stark, H., Castro, M., Lacivita, E., Leopoldo, M. (2022) Design and Synthesis of Arylpiperazine Serotonergic/Dopaminergic Ligands with Neuroprotective Properties. Molecules 27(4), 1297; doi.org/10.3390/molecules27041297
  • Elek, M., Dubiel, M., Mayer, L., Zivkovic, A., Müller, T. J. J., Stark, H. (2022) BOPPY-based novel fluorescent dopamine D2 and D3 receptor ligands. Bioorg Med Chem Lett 59:128573 doi.org/10.1016/j.bmcl.2022.128573
  • Kruppa, M., Sommer, G. A., Müller, T. J. J. (2022) Concise syntheses of marine (bis)indole alkaloids meridianin C, D, F, and G and scalaridine A via one-pot Masuda borylation-Suzuki coupling sequence. Molecules 27, 2233 https://doi.org/10.3390/molecules27072233
  • Yang, X., Ali, S., Zhao, M., Richter, L., Schäfer, V., Schliehe-Diecks, J., Frank, M., Qi, J., Larsen, P. K., Skerra, J., Islam, H., Wachtmeister, T., Alter, C., Huang, A., Bhatia, S., Koehrer, K., Kirschning, C., Weighardt, H., Kalinke, U., Kalscheuer, R., Uhrberg, M., Scheu, S. (2022) The mycotoxin Beauvericin exhibits immunostimulatory effects on dendritic cells via activating the TLR4 signaling pathway. Frontiers in Immunology https://doi.org/10.3389/fimmu.2022.856230
  • Gottstein, J., Zaschke-Kriesche, J., Unsleber, S., Voitsekhovskaiab, I., Kulik, A., Behrmann, L. V., Overbeck, N., Stühler, K., Stegmann, E., Smits, S. H. (2022) New insights into the resistance mechanism for the BceAB-type transporter SaNsrFP. SciRep 12, 4232. https://doi.org/10.1038/s41598-022-08095-2
2021
  • Fischer, F., Avelar, L. A. A., Murray, L., Kurz, T. (2021) Designing HDAC-PROTACs: lessons learned so far. Future Medicinal Chemistry Preprint, https://doi.org/10.4155/fmc-2021-0206

  • Eissa, N., Venkatachalam, K., Jayaprakash, P., Falkenstein, M., Dubiel, M., Frank, A., Reiner-Link, D., Stark, H., Sadek, B. (2021) The Multi-Targeting Ligand ST-2223 with Histamine H3 Receptor and Dopamine D2/D3 Receptor Antagonist Properties Mitigates Autism-Like Repetitive Behaviors and Brain Oxidative Stress in Mice. Int. J. Mol. Sci. 22, 1947. https://doi.org/10.3390/ijms22041947  

  • Staszewski, M., Nelic, D., Jończyk, J., Dubiel, M., Frank, A., Stark, H., Bajda, M., Jakubik, J., Walczyński, K. (2021) ACS Chemical Neuroscience 12 (13), 2503-2519, DOI: 10.1021/acschemneuro.1c00237

  • Wu, W., Wang, X., Sun, Y., Berleth, N., Deitersen, J., Schlütermann, D., Stuhldreier, F., Cox, J., Wallot-Hieke, N., Mendiburo, M. J., Cox, J., Peter, C., Bergmann, A. K., Stork, B. (2021) TNF-induced necroptosis initiates early autophagy events via RIPK3-dependent AMPK activation, but inhibits late autophagy. Autophagy DOI: 10.1080/15548627.2021.1899667

  • Deitersen, J., Berning, L., Stuhldreier, F., Ceccacci, S., Schlütermann, D., Friedrich, A., Wu, W., Sun, Y., Böhler, P., Berleth, N., Mendiburo, M. J., Seggewiß, S., Anand, R., Reichert, A. S., Monti, M. C., Proksch, P., Stork, B. (2021) High-throughput screening for natural compound-based autophagy modulators reveals novel chemotherapeutic mode of action for arzanol. Cell Death Dis. 12(6):560. DOI: 10.1038/s41419-021-03830-5

  • Schmitz, K., Cox, J., Esser, L. M., Voss, M., Sander, K., Löffler, A., Hillebrand, F., Erkelenz, S., Schaal, H., Kähne, T., Klinker, S., Zhang, T., Nagel-Steger, L., Willbold, D., Seggewiß, S., Schlütermann, D., Stork, B., Grimmler, M., Wesselborg, S., Peter, C. (2021) An essential role of the autophagy activating kinase ULK1 in snRNP biogenesis. Nucleic Acids Res. 49(11):6437-6455 DOI: 10.1093/nar/gkab452

  • Schlütermann, D., Berleth, N., Deitersen, J., Wallot-Hieke, N., Friesen, O., Wu, W., Stuhldreier, F., Sun, Y., Berning, L., Friedrich, A., Mendiburo, M. J., Peter, C., Wiek, C., Hanenberg, H., Stefanski, A., Stühler, K., Stork, B. (2021) FIP200 controls the TBK1 activation threshold at SQSTM1/p62-positive condensates. Sci Rep 11(1):13863 doi: 10.1038/s41598-021-92408-4

  • Sun, Y., Berleth, N., Wu, W., Schlütermann, D., Deitersen, J., Stuhldreier, F., Berning, L., Friedrich, A., Akgün, S., Mendiburo, M., J., Wesselborg, S., Conrad, M., Berndt, C., Stork, B. (2021) Fin56-induced ferroptosis is supported by autophagy-mediated GPX4 degradation and functions synergistically with mTOR inhibition to kill bladder cancer cells. Cell Death Dis. 12(11): 1028 doi: 10.1038/s41419-021-04306-2

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  • Schäker-Hübner, L., Warstat, R., Ahlert, H., Mishra, P., Kraft, F.B., Schliehe-Diecks, J., Schöler, A., Borkhardt, A., Breit, B., Bhatia, S., Hügle, M., Günther, S., Hansen, F.K. (2021) 4-Acyl Pyrrole Capped HDAC Inhibitors: A New Scaffold for Hybrid Inhibitors of BET Proteins and Histone Deacetylases as Antileukemia Drug Leads. J Med Chem. https://doi.org/10.1021/acs.jmedchem.1c01119
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  • Merkt, F. K., Mazzone, F., Shaneh Sazzadeh, S., Bonda, L., Hinz, L.K.E., Gruber, I., Buchholz, K., Janiak, C., Pfeffer, K., Müller, T.J.J. (2021) Fluorescent Indolo[3,2‐a]phenazines against Toxoplasma gondii – concise synthesis by Au‐catalyzed cycloisomerization with 1,2‐Silyl migration and ipso‐Iodination‐Suzuki Sequence. Chemistry - A European Journal http://dx.doi.org/10.1002/chem.202101391
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2020
  • Gao, Y., Stuhldreier, F., Schmitt, L., Wesselborg, S., Guo, Z., Zou, K., Mándi, A., Kurtán, T., Liu, Z., Proksch, P. (2020) Induction of New Lactam Derivatives from the Endophytic Fungus Aplosporella javeedii through an OSMAC Approach. Frontiers in Microbiotechnology 11, 600983 DOI:10.3389/fmicb.2020.600983
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  • Fejzagic, A.V., Myllek, S., Hogenkamp, F., Greb, J., Pietruszka, J., Classen, T. (2020) A Fluorescence-Based Assay System for the Determination of Haloperoxidase-Activity Using a Two-Dimensional Calibration Approach. ChemistryOpen 9: 959-966, doi: 10.1002/open.202000184 

  • Furtmann, F., Porta, N., Hoang, D.T., Reiners, J., Schumacher, J., Gottstein, J., Gohlke, H., Smits, S.H.J. (2020) Characterization of the Nucleotide-Binding Domain NsrF from the BceAB-type ABC-Transporter NsrFP from the Human Pathogen Streptococcus agalactiae. SciRep 10, 15208

  • Reßing, N., S Ouml Nnichsen, M., Osko, J., Schöler, A., Schliehe-Diecks, J., Skerhut, A.J., Borkhardt, A., Hauer, J., Kassack, M.U., Christianson, D.W., Bhatia, S., Hansen, F.K. (2020) Multicomponent synthesis, binding mode and structure-activity relationships of selective histone deacetylase 6 (HDAC6) inhibitors with bifurcated capping groups. J Med Chem. 63 (18), 10339-10351 doi: 10.1021/acs.jmedchem.9b01888

  • Mayer, L., Kohlbecher, R., Müller, T.J.J (2020) Concatenating Suzuki Arylation and Buchwald-Hartwig Amination by A Sequentially Pd-catalyzed One-Pot Process – Consecutive Three-Component Synthesis of C,N-Diarylated Heterocycles. Chem. Eur. J.  26, 15130–15134. DOI: 10.1002/chem.202003837
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  • Friedrich, A., Assmann, A.-S., Schumacher, L., van Stuijvenberg, J., Kassack, M.U., Schulz, W.A., Roos, W.P., Hansen, F.K., Pflieger, M., Kurz, T., Fritz, G. (2020) In vitro assessment of the genotoxic hazard of novel hydroxamic acid- and benzamide-type histone deacetylase inhibitors (HDACi). Int J Mol Sci in press

  • Weber, A., Breugst, M., Pietruszka, J. (2020) Experimental and Computational Investigations of the Reaction between α,β-unsaturated Lactones and 1,3-Dienes by Cooperative Lewis-Acid/Brønsted-Acid Catalysis. Angew. Chem. Int. Ed. DOI:10.1002/anie.202008365

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  • Mulnaes, D., Porta, N., Clemens, R., Apanasenko, I., Reiners, J., Gremer, L., Neudecker, P., Smits,. S.H.J., Gohlke, H. (2020) TopModel: Template-based protein structure prediction at loq sequence identity using top-down consensus and deep neural networks. JCTC dx.doi.org/10.1021/acs.jctc.9b00825
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  • van Geelen, L., Kaschani, F., Sazzadeh, S.S., Adeniyi, E.T., Meier, D., Proksch, P., Pfeffer, K., Kaiser, M., Ioerger, T.R., Kalscheuer, R. (2020) Natural brominated phenoxyphenols kill persistent and biofilm-incorporated cells of MRSA and other pathogenic bacteria. Appl Microbiol Biotechnol, 104(13):5985-5998 doi: 10.1007/s00253-020-10654-4
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2019
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  • Form, I.C., Bonus, M., Gohlke, H., Lin, W., Daletos, G., Proksch, P. (2019) Xanthone, benzophenone and bianthrone derivatives from the hypersaline lake-derived fungus Aspergillus wentii. Bioorg Med Chem 27(20):115005 (special issue, see below)
  • Porta, N., Zaschke-Kriesche, J., Frieg, B., Gopalswamy, M., Zivkovic, A., Etzkorn, M., Stark, H., Smits, S.H.J., Gohlke, H. (2019) Small-molecule inhibitors of nisin resistance protein NSR from the human pathogen Streptococcus agalactiae. Bioorg Med Chem 27(20):115079 (special issue, see below)
  • Deitersen, J., El-Kashef, D.H., Proksch, P., Stork, B. (2019) Anthraquinones and autophagy – Three rings to rule them all? Bioorg Med Chem 27(20):115042 (special issue, see below)
  • Pflieger, M., Hamacher, A., Öz, T., Horstick-Muche, N., Boesen, B., Schrenk, C., Kassack, M.U., Kurz, T. (2019) Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. Bioorg Med Chem 27:115036 (special issue, see below)
  • Bickel, D., Gohlke, H. (2019) C-terminal modulators of heat shock protein of 90 kDa (HSP90): State of development and modes of action. Bioorg Med Chem 27(21):115080 (special issue, see below)
  • Wang, C., Engelke, L., Bickel, D., Hamacher, A., Frank, M., Proksch, P., Gohlke, H., Kassack, M.U. (2019) The tetrahydroxanthone-dimer phomoxanthone A is a strong inducer of apoptosis in cisplatin-resistant solid cancer cells. Bioorg Med Chem 27(19):115044 (special issue, see below)
  • Frank, A., Meza-Arriagada, F., Salas, C.O., Espinosa-Bustos, C., Stark, H. (2019) Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine H3 receptor. Bioorg Med Chem 27:3194-3200 (special issue, see below)
  • Drießen, D., Stuhldreier, F., Frank, A., Stark, H., Wesselborg, S., Stork, B., Müller, T.J.J. (2019) Novel meriolin derivatives as rapid apoptosis inducers. Bioorg Med Chem 27: 3463-3468 (special issue, see below)
  • Zaschke-Kriesche, J., Reiners, J., Lagedroste, M., Smits, S.H. (2019) Influence of nisin hinge-region variants on lantibiotic immunity and resistance proteins, Bioorg Med Chem 27:3947-3953 (special issue, see below)
  • Mechsner, B., Böse, D., Hogenkamp, F., Ledermann, N., Hartmann, R., Bochinsky, K., Frey, W., Pietruszka, J. (2019) Enantioselective total synthesis of altersolanol A and N. Bioorg Med Chem 27: 2991-2997 (special issue, see below)
  • Zaschke-Kriesche, J., Behrmann, L.V., Reiners, J., Lagedroste, M., Gröner, Y., Kalscheuer, R., Smits, S.H. (2019) Bypassing lantibiotic resistance by an effective nisin derivative, Bioorg Med Chem 27:3454-3462 (special issue, see below)
  • Sachs, J., Döhl, K., Weber, A.,  Bonus, M., Ehlers, F., Fleischer, E., Klinger, A., Gohlke, H., Pietruszka, J., Schmitt, L., Teusch, N. (2019) Novel 3,4-dihydroisocoumarines inhibit human P-gp and BCRP in multidrug resistant tumors and demonstrate substrate inhibition of yeast Pdr5, Front. Pharmacol. 10:400
2018
  • Rehberg, N., Akone, H.S., Loerger, T.R., Erlenkamp, G., Daletos, G., Gohlke, H., Proksch, P., Kalscheuer, R. (2018) Chlorflavonin targets acetohydroxyacid synthase catalytic subunit IlvB1 for synergistic killing of Mycobacterium tuberculosis. ACS Infect. Dis. 4, 123-134.
  • Yu, H., Sperlich, J., Mándi, A., Kurtán, T., Dai, H., Teusch, N., Guo, Z.-Y., Zou, K., Liu, Z., Proksch, P. (2018) Azaphilone derivatives from the fungus Coniella fragariae inhibit NF-κB activation and reduce tumor cell migration. J Nat Prod 81(11):2493-2500
  • Frank, A., Kiss, D.J., Keserü, G.M., Stark, H. (2018) Binding kinetics of cariprazine and aripiprazole at the dopamine D3 receptor. SciRep 8:12509
  • Espinosa-Bustos, C., Frank, A., Arancibia-Opazo, S., Salas, C. O., Fierro, A., Stark, H. (2018) New lead elements for histamine H3 receptor ligands in the pyrrolo[2,3-d]pyrimidine class. Bioorg & Med Chem Lett 28:2890-2893
  • Böhler, P., Stuhldreier, F., Anand, R., Kondadi A.K., Schlütermann, D., Berleth, N., Deitersen, J., Wallot-Hieke, N., Wu, W., Frank, M., Niemann, H., Wesbuer, E., Barbian, A., Luyten, T., Parys, j.B., Weidtkamp-Peters, S., Borchardt, A., Reichert, A., Pena-Blanco, A., Garcia-Saez, A.J., Itskanov, S., van der Bliek, A.M., Proksch, P., Wesselborg, S., Stork, B. (2018) The mycotoxin phomoxanthone A disturbs the form and function of the inner mitochondrial membrane. Cell Death and Disease 9:286 
  • Schlütermann, D., Skowron, M.A., Berleth, N., Böhler, P., Deitersen, J., Stuhldreier, F., Wallot-Hieke, N., Wu, W., Peter, C., Hoffmann, M.J., Niegisch, G., Stork, B. (2018) Targeting urothelial carcinoma cells by combining cisplatin with a specific inhibitor of the autophagy-inducing class III PtdIns3K complex. Urol Oncol. 36(4):160
  • Wallot-Hieke, N., Verma, N., Schlütermann, D., Berleth, N., Deitersen, J., Böhler, P., Stuhldreier, F., Wu, W., Seggewiß, S., Peter, C., Gohlke, H., Mizushima, N., Stork, B. (2018) Systematic analysis of ATG13 domain requirements for autophagy induction. Autophagy 14:743-761
  • Clemens, R., Zaschke-Kriesche, J., Khosa S., Smits S.H.J. (2018) Insight into two ABC transporter families involved in lantibiotic resistance. Front. Mol. Biosci. 4:91 
  • Krüger, K., Geist, K., Stuhldreier, F., Schumacher, L., Blümel, L., Remke, M., Wesselborg, S., Stork, B., Klöcker, N., Bormann, S., Roos, W.P., Honnen, S., Fritz, G. (2018) Multiple DNA damage-dependent and DNA damage-independent stress responses define the outcome of ATR/Chk1 targeting in medulloblastoma cells. Cancer Lett 430:34-46
  • Brückmann, H., Frank, A., Reiner, D., Stark, H. (2018) Pharmakotherapie des Restless-Legs-Syndroms – eine detaillierte Betrachtung. Pharmakon 1/2018
  • Alachkar, A., Lazewska, D., Latacz, G., Frank, A., Siwek, A., Lubelska, A., Honkisz-Orzechowska, E., Handzlik, J., Stark, H., Kiec-Kononowicz, K., Sadek, B. (2018) Studies on Anticonvulsant Effects of Novel Histamine H3R Antagonists in Electrically and Chemically Induced Seizures in Rats. Int J Mol Sci 19:3386
  • Kaletsch, A., Pinkemeil, M., Hoffmann, M.J., Jaguva Vasudevan, A.A., Wang, C., Hansen, F.K., Wiek, C., Hanenberg, H., Gertzen, C., Gohlke, H., Kassack, M.U., Kurz, T., Schulz, W.A., Niegisch, G. (2018) Effects of novel HDAC inhibitors on urothelial carcinoma cells. Clinical Epigenetics 10:100
  • Schipp, C., Schlütermann, D., Hönscheid, A., Nabhani, S., Höll, J., Oommen, P.T., Ginzel, S., Fleckenstein, B., Stork, b., Borkhardt, A., Stepensky, P., Fischer, U. (2018) EBV negative lymphoma and autimmune lymphoproliferative syndorem like phenotype extend the clinical spectrum of primary immunodeficiency caused by STK4 deficiency. Front Immunol 9:2400
2017
  • Reiners, J., Lagedroste, M., Ehlen, K., Leusch, S., Zaschke-Kriesche, J., Smits, S. H. J. (2017) The N-terminal region of nisin is important for the BceAB-Type ABC transporter NsrFP from Streptococcus agalactiae COH1. Frontiers in Microbiology 8: 1643   
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  • Weber, A., Döhl, K., Sachs, J., Nordschild, A.C.M., Schröder, D., Kulik, A., Fischer, T., Schmitt, L., Teusch, N., Pietruszka, J. (2017) Synthesis and cytotoxic activities of goniothalamins and derivatives. Bioorg. Med. Chem., 25: 6115-6125
  • Sperlich, J., Kerr, R., Teusch, N. (2017). The marine natural product pseudopterosin blocks cytokin release of triple-negative breast cancer and monocytic leukemia cells by inhibiting NF-κB signaling. Marine Drugs 15: 262 
  • Mokhlesi, A., Stuhldreier, F., Wex, K.W., Berscheid, A., Hartmann, R., Rehberg, N., Sureechatchaiyan, P., Chaidir, C., Kassack, M.U., Kalscheuer, R., Brötz-Oesterhelt, H., Wesselborg, S., Stork, B., Daletos, G., Proksch, P. (2017) Cyclic cystine-bridged peptides from the marine sponge Clathria basilana induce apoptosis in tumor cells and depolarize the bacterial cytoplasmic membrane. J Nat Prod 80(11):2941-2952
  • Lang, A., Anand, R., Altinoluk-Hambüchen, S., Ezzahoini, H., Stefanski, A., Iram, A., Bergmann, L., Urbach, J., Böhler, P., Hänsel, J., Franke, M., Stühler, K., Krutmann, J., Scheller, J., Stork, B., Reichert, A.S., Piekorz, R.P. (2017) SIRT4 interacts with OPA1 and regulates mitochondrial quality control and mitophagy. Aging (Albany NY) 9(10):2163-2189
  • Liu, Y., Stuhldreier, F., Kurt, T., Mandi, A., Arumugam, S., Lin, W., Stork, B., Wesselborg, S., Weber, H., Henrich, B., Daletos, G., Proksch, P. (2017) Daldinone derivatives from the mangrove-derived endophytic fungus Annulohypoxylon sp. RSC Advances 7, 5381-5393
Patents
  • T. J. J. Müller, G. Sommer, B. O. A. Tasch, R. Kalscheuer, N. Rehberg (2018) Bis-Indole Derivatives for Use in the Treatment of Bacterial Infections, WO2018060367 (A1) - 2018-04-05; EP3301096 (A1) - 2018-04-04.

Special Issue "Natural product-derived lead structures and modes-of-action against therapy-resistant tumors and microorganisms" in Journal of Bioorganic & Medicinal Chemistry

Several scientists of Research Training Group 2158 contributed to this special issue, which is edited by by the Research Training Group 2158 speaker Holger Gohlke, and thus demonstrate the close cooperation of the groups working in the Research Training Group and their work on the field of natural product research (Publications of our doctoral students are listed above).

More information about this issue: https://www.sciencedirect.com/journal/bioorganic-and-medicinal-chemistry/special-issue/10WBM0BS0L1

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