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Our doctoral students contributed with their work to several publications and patents. Please find a lists of all publications of our GRK2158 fellows in 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.

  • Ganardi, R., Greb, J., Henssen, B., Pietruszka, J. (2023) Atroposelective Total Synthesis of (+)-Isokotanin A via Combined Metal and Enzyme Catalysis. Adv Synth Catal 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., 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 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 
  • 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 
  • Eissa, N., Venkatachalam, K., Jayaprakash, P., Falkenstein, M., Dubiel, M., Frank, A., Reiner-Link, D., Stark, H., Sadek, B. 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
  • 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 vitra 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
  • 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

  • Selg, C., Schöler, A., Schliehe-Diecks, J., Hanl, M., Sinatra, L., Borkhardt, A., Sarosi M.B., Bhatia, S., Hey-Hawkins, E., Hansen, F.K. (2021) Borinostats: solid-phase synthesis of carborane-capped histone deacetylase inhibitors with a tailor-made selectivity profile. Chemical Science 12, 11873-11881, https://doi.org/10.1039/D1SC02268G

  • 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
  • Gottstein, J., Klose, H., Knospe, C.V., Reiners, J., Smits, S.H., Schmitt, L. (2021) Lantibiotika – hoffnungsvolle Alternative gegen Antibiotikaresistenz? Biospektrum in press
  • Fischer, F. & Alves Avelar, L.A. (2021) A short overview of resistance to approved histone deacetylase inhibitors. Future Med. Chem. 13(14): 1153-1155 https://doi.org/10.4155/fmc-2021-0102
  • Taki, A.C., Jabbar, A., Kurz, T., Lungerich, B., Ma, G., Byrne, J.J., Pflieger, M., Asfaha, Y., Fischer, F., Chang, B.C.H., Sleebs, B.E., Gasser, R.B. (2021) Three small molecule entities (MPK18, MPK334 and YAK308) with activity against Haemonchus contortus In Vitro. Molecules 26, 2819. https://doi.org/10.3390/molecules26092819 
  • 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
  • Avelar, L.A.A., Schrenk, C., Sönnichsen, M., Hamacher, A., Hansen, F.K., Schliehe-Diecks, J., Borkhardt, A., Bhatia, S., Kassack, M.U. and Kurz, T (2021). Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. Eur. J. Med. Chem. 211, 113095 https://doi.org/10.1016/j.ejmech.2020.113095
  • Pflieger, M., Sönnichsen, M., Horstick-Muche, N., Yang, J., Schliehe-Diecks, J., Schöler, A., Borkhardt, A., Hamacher, A., Kassack, M.U., Hansen, F.K., Bhatia, S., Kurz, T. (2021) Oxa Analogues of Nexturastat A Demonstrate Improved HDAC6 Selectivity and Superior Antileukaemia Activity. Chem Med Chem 16:1799-1804 https://doi.org/10.1002/cmdc.202001011
  • Berning, L., Schlütermann, D., Friedrich, A., Berleth, N., Sun, Y., Wu, W., Mendiburo, M.J., Deitersen, J., Brass, H.U.C., Skowron, M.A., Hoffmann, M.J., Niegisch, G., Pietruszka, J., Stork, B. (2021) Prodigiosin Sensitizes Sensitive and Resistant Urothelial Carcinoma Cells to Cisplatin Treatment. Molecules  26, 1294. https://doi.org/10.3390/molecules26051294
  • Maaß, S., Bartel, J., Mücke, P.A., Schlüter, R., Sura, T., Zaschke-Kriesche, J., Smits, S.H.J., Becher, D. (2021) Proteomic Adaptation of Clostridioides difficile to Treatment with the Antimicrobial Peptide Nisin. Cells 10(2), 372; https://doi.org/10.3390/cells10020372
  • Schmitt, L., Hinxlage, I., Cea, P.A., Gohlke, H., Wesselborg, S. (2021) 40 years of research on polybrominated diphenyl ethers (PBDEs) – A historical overview and newest data of a promising anticancer drug. Molecules 26, 995. https://doi.org/10.3390/molecules26040995
  • 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
  • Smits, S.H.J., Schmitt, L., Beis, K. (2020) Self-immunity to antibacterial peptides by ABC transporters. FEBS Letters 594, 3920-3942
  • Rehberg, N., Sommer, G.A., Drießen, D., Kruppa, M., Adeniyi, E.T., Chen, S., Wang, L., Wolf, K., Tasch, B.O.A., Ioerger, T.R., Zhu, K., Müller, T.J.J., Kalscheuer, R. (2020) Nature-inspired (di)azine-bridged bisindole alkaloids with potent antibacterial in vitro and in vivo efficacy against Methicillin-resistant Staphylococcus aureus.  J Med Chem 63(21), 12623-12641 DOI:10.1021/acs.jmedchem.0c00826
  • Dorst, A., Berg, R., Gerzten, C.G.W., Schäfle, D., Zerbe, K., Gwerder, M., Schnell, S.D., Sander, P., Gohlke, H., Gademann, K. (2020) Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, 2 Synthesis, and Biological Evaluation. ACS Med Chem Lett dx.doi.org/10.1021/acsmedchemlett.0c00381
  • Reiners, J., Lagedroste, M., Gottstein, J., Adeniyi, E.T., Kalscheuer, R., Poschmann, G., Stühler, K., Smits, S.H., Schmitt, L. (2020) Insights in the antimicrobial potential of the natural nisin variant nisin H. Front Microbiol 11:573614 doi: 10.3389/fmicb.2020.573614

  • 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
  • Lazewska, D., Olejarz-Maceij, A., Reiner, D., Kaleta, M., Latacz, G., Zygmunt, M., Doroz-Plonka, A., Karcz, T., Frank, A., Stark, H., Kiec-Kononowicz, K. (2020) Dual Target Ligands with 4-tert-Butylphenoxy Scaffold as Histamine H3 Receptor Antagonists and Monoamine Oxidase B Inhibitors. Int. J. Mol. Sci. 21(10), 3411
  • Alachkar, A., Ojha, S.K., Sadeq, A., Adem, A., Frank, A., Stark, H., Sadek, B. (2020) Experimental models for discovery of novel anticonvulsant drugs: Focus on Pentylenetetrazole-induced seizures and associated memory deficits. Curr Pharm Des. 26(15): 1693-1711

  • 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

  • Drießen, D., Biesen, L., Müller, T.J.J. (2020) Sequentially Catalyzed Three-Component Masuda–Suzuki–Sonogashira Synthesis of Fluorescent 2-Alkynyl-4-(7-azaindol-3-yl)pyrimidines: Three Palladium-Catalyzed Processes in a One-Pot Fashion. Synlett 31, DOI: 10.1055/s-0040-1707818.
  • Wu, W., Wang, X., Berleth, N., Deitersen, J., Wallot-Hieke, N., Böhler, P., Schlütermann, D., Stuhldreier, F., Cox, J., Schmitz, K., Seggewiß, S., Peter, C., Kasof, G., Stefanski, A., Stühler, K., Tschapek, A., Gödecke, A., Stork, B. (2020) The Autophagy-Initiating Kinase ULK1 Controls RIPK1-Mediated Cell Death. Cell Reports 31:107547
  • Ceccacci, S., Deitersen, J., Mozzicafreddo, M., Moretta, E., Proksch, P., Wesselborg, S., Stork, B., Monti, M.C. (2020) Carbamoyl-Phosphate Synthase 1 as a Novel Target of Phomoxanthone A, a Bioactive Fungal Metabolite.  Biomolecules 10(6), 846; doi.org/10.3390/biom10060846  
  • van Stuijvenberg, J., Proksch, P., Fritz, G. (2020) Targeting the DNA damage response (DDR) by natural compounds. Bioorg Med Chem. 28(4):115279. doi: 10.1016/j.bmc.2019.115279 (special issue, see below)
  • 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
  • Asfaha, Y., Schrenk, C., Avelar, L.A.A., Lange, F., Wang, C., Bandolik, J.J., Hamacher, A., Kassack, M.U., Kurz, T. (2020) Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresitant cancer cells. Bioorg Med Chem 28(1):115108 (special issue, see below)
  • 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, doi: 10.1007/s00253-020-10654-4
  • Xie, B.,  Hänsel, J.,  Mundorf, V.,  Betz, J.,  Reimche, I.,  Erkan, M.,  Büdeyri, I.,  Gesell, A.,  Kerr, R. G.,  Ariantari, N. P.,  Yu, H.,  Proksch, P.,  Teusch, N., Mrsny, R. J. (2020) Pseudopterosin and O-Methyltylophorinidine Suppress Cell Growth in a 3D Spheroid Co-Culture Model of Pancreatic Ductal Adenocarcinoma. Bioengineering 2020, 7 (2), 57
  • Gao, Y., Stuhldreier, F., Schmitt, L., Wesselborg, S., Wang, L., Müller, W.E.G., Kalscheuer, R., Guo, Z., Zou, K., Liu, Z., Proksch, P. (2020) Sesterterpenes and macrolide derivatives from the endophytic fungus Aplosporella javeedii. Fitoterapia, doi: 10.1016/j.fitote.2020.10465
  • Wang, C., Hamacher, A., Petzsch, P., Köhrer, K., Niegisch, G., Hoffmann, M.J., Schulz, W.A., Kassack, M.U. (2020) Combination of Decitabine and Entinostat Synergistically Inhibits Urothelial Bladder Cancer Cells via Activation of FoxO1. Cancers 12: 337 doi.org/10.3390/cancers12020337
  • Alachkar, A., Ojha, S.K., Sadeq, A., Adem, A., Frank, A., Stark, H., Sadek, B. (2020) Experimental models for discovery of novel anticonvulsant drugs: Focus on Pentylenetetrazole-induced seizures and associated memory deficits. Curr Pharm Des. 26(15):1693-1711
  • Liu, Z., Frank, M., Yu, X., Yu, H., Tran-Cong, N.M., Gao, Y., Proksch, P. (2020) Secondary Metabolites from Marine-Derived Fungi from China. Progress in the Chemistry of Organic Natural Products 111. A. D. Kinghorn, H. Falk, S. Gibbons et al. Cham, Springer International Publishing: 81-153.
  • Ariantari, N.P., Ancheeva, E., Frank, M., Stuhldreier, F., Meier, D., Gröner, Y., Reimche, I. Teusch, N., Wesselborg, S., Müller, W.E.G., Kalscheuer, R., Liu, Z., Proksch, P. (2020) Didymellanosine, a new decahydrofluorene analogue, and ascolactone C from Didymella sp. IEA-3B.1, an endophyte of Terminalia catappa. RSC Adv. 10: 7232-7240
  • Tran‐Cong, N.M., Mándi, A., Király, S.B., Kurtán, T.,Lin, W., Liu Z., Proksch, P. (2020)  Furoic acid derivatives from the endophytic fungus Coniothyrium sp. Chirality 1-6 DOI: 10.1002/chir.23209
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  • Harwoko, H., Daletos, G., Stuhldreier, F., Lee, J., Wesselborg, S., Feldbrügge, M., Müller, W.E.G., Kalscheuer, R., Ancheeva, E., Proksch, P. (2019) Dithiodiketopiperazine derivatives from endophytic fungi Trichoderma harzianum and Epicoccum nigru. Nat. Prod. Res.DOI: 10.1080/14786419.2019.1627348
  • Mayer, S., Prechtl, M., Liebfried, P., Cadeddu, R-P., Stuhldreier, F., Kohl, M., Wenzel, F., Stork, B., Wesselborg, S., Proksch, P., Germing, U., Haas, R., Jäger, P. (2019) First Results from a Screening of 300 Naturally Occurring Compounds: 4,6-dibromo-2-(2′,4′-dibromophenoxy)phenol, 4,5,6-tribromo-2-(2′,4′-dibromophenoxy)phenol, and 5-epi-nakijinone Q as Substances with the Potential for Anticancer Therapy. Mar. Drugs 17(9), 521 https://doi.org/10.3390/md17090521
  • Sachs, J., Kadioglu, O., Weber, A., Mundorf, V., Betz, J., Efferth, T., Pietruszka, J., Teusch, N. (2019) Selective inhibition of P-gp transporter by goniothalamin derivatives sensitizes resistant cancer cells to chemotherapy. J Nat Med 73, 226-235
  • Stank, L., Frank, A., Hagenow, S., Stark, H. (2019) Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands, Med Chem Comm 10: 1926-1929 DOI: 10.1039/C9MD00379G.
  • Frank, A., Meza, F., Salas, C. O., Fierro, A., Espinosa-Bustos, C., and Stark, H. (2019) From Natural Compounds to Small Molecules Targeting the Histamine H3 Receptor. Inflamm Res 58, S42
  • Yu, H., Höfert, S-P., Moussa, M., Janiak, C., Müller, W.E.G., Umeokoli, B.O., Dai, H., Liu, Z., Proksch, P. (2019) Polyketides and nitrogenous metabolites from the endophytic fungus Phomopsis sp. D15a2a. Tetrahydron Lett 60(15). 1513125
  • Carbone, C., Russo, S.L.M.L., Lacivita, E., Frank, A., Alleva, E., Stark, H., Saso, L., Leopoldo, M., Adriani, W. (2019) Prior activation of 5-HT7 receptors modulates the conditioned place preference with methylphenidate. Front Behav Neurosci doi.org/10.3389/fnbeh.2019.00208
  • Ariantari, N.P., Ancheeva, E., Wang, C., Mándi, A., Knedel, T.O, Kurtán, T., Chaidir, C., Müller, W.E.G., Kassack, M.U., Janiak, C., Daletos, G., Proksch, P. (2019) Indole diterpenoids from the fungal endophyte Penicillium sp. J Nat Prod 82(6): 1412-23
  • Schmidt, D., Boehm, M., McClendon, C.L., Torella, R., Gohlke, H. (2019) Cosolvent-enhanced sampling and unbiased identification of cryptic pockets suitable for structure-based drug design. J. Chem. Theory Comput. 15, 3331-3343.
  • Moussa, M., Ebrahim, W., Bonus, M., Gohlke, H., Mándi, A., Kurtán, T., Hartmann, R., Kalscheuer, R., Lin, W., Liu, Z., Proksch, P. (2019) Co-culture of the fungus Fusarium tricinctum with Streptomyces lividans induces production of cryptic naphtoquinone dimers. RSC Adv. 9, 1491–1500.
  • Tran-Cong, N.M., Mandi, A., Kurtán, T., Müller, W.E.G., Kalscheuer, R., Lin, W., Liu, Z., Proksch, P. (2019) Induction of cryptic metabolites of the endophytic fungus Trichocladium sp. through OSMAC and co-cultivation. RSC Adv. 9: 27279
  • Bandolik, J.J., Hamacher, A., Schrenk, C., Weishaupt, R., Kassack, M.U. (2019) Class I-histone deacetylase (HDAC) inhibition is superior to pan-HDAC inhibition in modulating cisplatin potency in high grade serous ovarian cancer cell lines. Int J Mol Sci DOI: 10.3390/ijms20123052
  • Yu, H., Sperlich, J., Hofert, S.-P., Janiak, C., Teusch, N., Stuhldreier, F., Wesselborg, S., Wang, C., Kassack, M.U., Dai, H., Liu, Z., Proksch, P. (2019). Azaphilone pigments and macrodiolides from the coprophilous fungus Coniella fragariaeFitoterapia 137: 104249.
  • Richter, L., Kropp, S., Proksch, P., Scheu, S. (2019) A mouse model-based screening platform for the identification of immune activating compounds such as natural products for novel cancer immunotherapies. Bioorg Med Chem DOI: 10.1016/j.bmc.2019.115145 (special issue, see below)
  • Scheu, S., Ali, S., Mann-Nüttel, R., Richter, L., Arolt, V., Dannlowski, U., Kuhlmann, T., Klotz, L., Alferink, J., (2019) Interferon β-mediated protective functions of microglia in central nervous system autoimmunity. IJMS 20: 190
  • Ali, S., Mann-Nüttel, R., Schulze, A., Richter, L., Alferink, J., Scheu, S. (2019) Sources of type I interferons in infectious immunity: Plasmacytoid dendritic cells not always in the driver's seat. Front Immunol DOI: 10.3389/fimmu.2019.00778
  • Asfaha, Y., Schrenk, C., Avelar, L.A.A., Hamacher, A., Pflieger, M., Kassack, M.U., Kurz, T. (2019) Recent advances in class IIa histone deacetylases research. Bioorg Med Chem DOI: 10.1016/j.bmc.2019.115087 (special issue, see below)
  • Abdel-Wahab, N.M., Harwoko, H., Müller, W.E.G., Hamacher, A., Kassack, M.U., Fouad, M.A., Kamel, M.S., Lin, W., Ebrahim, W., Liu, Z., Proksch, P. (2019) Cyclic heptapeptides from the soil-derived fungus Clonostachys rosea. Bioorg Med Chem 27: 3954-3959 (special issue, see below)
  • 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
  • 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
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  • Frank, A., Abu-Lafi, S., Adawi, A., Schwed, J.S., Stark, H., Rayan, A. (2017) From medicinal plant extracts to defined chemical compounds targeting the histamine H4 receptor: Curcuma longa in the treatment of inflammation. Inflamm Res. 66(10):923-929 
  • 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
  • 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