B01

© UDE/Bettina Engel-Albustin

Project Area B - Chemical Biology

Prof. Dr. Markus Kaiser

Chemical Biology

University of Duisburg-Essen

Phone: +49 201 183 4980
Email

Developing chemical tools for investigating cell state transitions

This project deals with the development of chemical tools for deciphering molecular mechanisms of cell state transitions. In subproject 1, we will investigate chemical strategies to achieve targeted protein degradation, e.g. by the design and synthesis of chemically novel PROTACs. These studies will include the development of new E3 ubiquitin ligase recruiting units. In subproject 2, we will generate small molecule tools for acute perturbation of the metastatic switch. To this end, we will explore structure-activity relationships as well as the biological scope and selectivity of established inhibitors of metastasis. In the long term, these studies should result in the development of novel anticancer agents with complementary bioactivities to current chemotherapeutics.

Project Members

Niko Molke

niko.molke@.uni-due.de

Lukas Schrapp

lukas.schrapp@.uni-due.de

Publications

    Journal articles

  • Reinders, Maike; Kravic, Bojana; Gahlot, Pinki; Koska, Sandra; van den Boom, Johannes; Schulze, Nina; Levantovsky, Sophie; Kleine, Stefan; Kaiser, Markus; Kulathu, Yogesh; Behrends, Christian; Meyer, Hemmo
    ATXN3 regulates lysosome regeneration after damage by targeting K48-K63-branched ubiquitin chains
    In: The EMBO Journal, Vol. 44, 2025, Nr. 18, pp. 5086 – 5111
    DOI (Open Access)
  • Brenner, Joel Cyrille; Zirden, Linda; Almeida-Hernandez, Yasser; Kaschani, Farnusch; Kaiser, Markus; Sanchez-Garcia, Elsa; Poepsel, Simon; Hellerschmied-Jelinek, Doris
    Conformational plasticity of a BiP-GRP94 chaperone complex
    In: Nature Structural & Molecular Biology, Vol. 32, 2025, Nr. 10, pp. 1947 – 1958
    DOI (Open Access)
  • Führer, Siska; Gallant, Kai; Kaschani, Farnusch; Kaiser, Markus; Janning, Petra; Waldmann, Herbert; Gersch, Malte
    Small Molecule-Induced Alterations of Protein Polyubiquitination Revealed by Mass-Spectrometric Ubiquitome Analysis
    In: Angewandte Chemie International Edition, Vol. 64, 2025, Nr. 32, e202508916
    DOI (Open Access)
  • Sewald, Leonard; Tabak, Werner W. A.; Fehr, Lorenz; Zolg, Samuel; Najdzion, Maja; Verhoef, Carlo J. A.; Podlesainski, David; Geiss-Friedlander, Ruth; Lammens, Alfred; Kaschani, Farnusch; Hellerschmied, Doris; Huber, Robert; Kaiser, Markus
    Sulphostin-inspired N-phosphonopiperidones as selective covalent DPP8 and DPP9 inhibitors
    In: Nature Communications, Vol. 16, 2025, Nr. 1, 3208
    DOI (Open Access)
  • Huang, Jing; Jaekel, Andreas; van den Boom, Johannes; Podlesainski, David; Elnaggar, M.; Heuer-Jungemann, A.; Kaiser, Markus; Meyer, Hemmo; Saccà, Barbara
    A modular DNA origami nanocompartment for engineering a cell-free, protein unfolding and degradation pathway
    In: Nature Nanotechnology, Vol. 19, 2024, Nr. 10, pp. 1521 – 1531
    DOI (Open Access)
  • Schillinger, Jasmin; Koci, Michelle; Bravo-Rodriguez, Kenny; Heilmann, Geronimo; Kaschani, Farnusch; Kaiser, Markus; Beuck, Christine; Luecke, Hartmut; Huber, Robert; Hellerschmied-Jelinek, Doris; Burston, Steven G.; Ehrmann, Michael
    High resolution analysis of proteolytic substrate processing
    In: The Journal of Biological Chemistry (JBC), Vol. 300, 2024, Nr. 11, 107812
    DOI, Online Full Text (Open Access)
  • Pol, Savina Abraham; Liljenberg, Sara; Barr, Jack; Simon, Gina; Wong-Dilworth, Luis; Paterson, Danielle L.; Berishvili, Vladimir P.; Bottanelli, Francesca; Kaschani, Farnusch; Kaiser, Markus; Pettersson, Mariell; Hellerschmied, Doris
    Induced degradation of SNAP-fusion proteins
    In: RSC Chemical Biology, Vol. 5, 2024, Nr. 12, pp. 1232 – 1247
    DOI (Open Access)
  • Pleuger, Richard; Cozma, Christian; Hohoff, Simone; Denkhaus, Christian; Dudziak, Alexander; Kaschani, Farnusch; Kaiser, Markus; Musacchio, Andrea; Vetter, Ingrid R.; Westermann, Stefan
    Microtubule end-on attachment maturation regulates Mps1 association with its kinetochore receptor
    In: Current Biology, Vol. 34, 2024, Nr. 11, pp. 2279 – 2293.e6
    DOI (Open Access)
  • Beaufort, Nathalie; Ingendahl, Linda; Merdanovic, Melisa; Schmidt, Andree; Podlesainski, David; Richter, Tim; Neumann, Thorben; Kuszner, Michael; Vetter, Ingrid R.; Stege, Patricia; Burston, Steven G.; Filipovic, Anto; Ruiz-Blanco, Yasser B.; Bravo Rodriguez, Kenny; Mieres-Perez, Joel; Beuck, Christine; Uebel, Stephan; Zobawa, Monika; Schillinger, Jasmin; Malik, Rainer; Todorov-Völgyi, Katalin; Rey, Juliana; Roberti, Annabell; Hagemeier, Birte; Wefers, Benedikt; Müller, Stephan A.; Wurst, Wolfgang; Sanchez-Garcia, Elsa; Zimmermann, Alexander; Hu, Xiao-Yu; Clausen, Tim; Huber, Robert; Lichtenthaler, Stefan F.; Schmuck, Carsten; Giese, Michael; Kaiser, Markus; Ehrmann, Michael; Dichgans, Martin
    Rational correction of pathogenic conformational defects in HTRA1
    In: Nature Communications, Vol. 15, 2024, Nr. 1, 5944
    DOI (Open Access)
  • Day, Matthew; Tetik, Bilal; Parlak, Milena; Almeida-Hernández, Yasser; Räschle, Markus; Kaschani, Farnusch; Siegert, Heike; Marko, Anika; Sanchez-Garcia, Elsa; Kaiser, Markus; Barker, Isabel A.; Pearl, Laurence H.; Oliver, Antony W.; Boos, Dominik
    TopBP1 utilises a bipartite GINS binding mode to support genome replication
    In: Nature Communications, Vol. 15, 2024, Nr. 1, 1797
    DOI, Online Full Text (Open Access)
  • Hoi, David M.; Junker, Sabryna; Junk, Lukas; Schwechel, Kristin; Fischel, Katharina; Podlesainski, David; Hawkins, Paige M.E.; van Geelen, Lasse; Kaschani, Farnusch; Leodolter, Julia; Morreale, Francesca Ester; Kleine, Stefan; Guha, Somraj; Rumpel, Klaus; Schmiedel, Volker M.; Weinstabl, Harald; Meinhart, Anton; Payne, Richard J.; Kaiser, Markus; Hartl, Markus; Boehmelt, Guido; Kazmaier, Uli; Kalscheuer, Rainer; Clausen, Tim
    Clp-targeting BacPROTACs impair mycobacterial proteostasis and survival
    In: Cell, Vol. 186, 2023, Nr. 10, pp. 2176 – 2192.e22
    DOI (Open Access)
  • Fehr, Lorenz; Sewald, Leonard; Huber, Robert; Kaiser, Markus
    Facile Multicomponent Synthesis of Oxazolidinones from Primary Amines and Cesium (Hydrogen)Carbonate
    In: European Journal of Organic Chemistry, Vol. 26, 2023, Nr. 27, e202300135
    DOI (Open Access)
  • Blüggel, Mike; Kröning, Alexander; Kracht, Matthias; van den Boom, Johannes; Dabisch, Matthias; Göhring, Anna; Kaschani, Farnusch; Kaiser, Markus; Bayer, Peter; Meyer, Hemmo; Beuck, Christine
    The UBX domain in UBXD1 organizes ubiquitin binding at the C-terminus of the VCP/p97 AAA-ATPase
    In: Nature Communications, Vol. 14, 2023, Nr. 1, 3258
    DOI, Online Full Text (Open Access)
  • Carvalho, Luís A. R.; Ross, Breyan; Fehr, Lorenz; Bolgi, Oguz; Wöhrle, Svenja; Lum, Kenneth M.; Podlesainski, David; Vieira, Andreia C.; Kiefersauer, Reiner; Félix, Rita; Rodrigues, Tiago; Lucas, Susana D.; Groß, Olaf; Geiss‐Friedlander, Ruth; Cravatt, Benjamin F.; Huber, Robert; Kaiser, Markus; Moreira, Rui
    Chemoproteomics‐Enabled Identification of 4‐Oxo‐β‐Lactams as Inhibitors of Dipeptidyl Peptidases 8 and 9
    In: Angewandte Chemie International Edition, Vol. 61, 2022, Nr. 47, e202210498
    DOI (Open Access)
  • Chauvistré, Heike; Shannan, Batool; Daignault-Mill, Sheena M.; Ju, Robert J.; Picard, Daniel; Egetemaier, Stefanie; Váraljai, Renáta; Gibhardt, Christine S.; Sechi, Antonio; Kaschani, Farnusch; Keminer, Oliver; Stehbens, Samantha J.; Liu, Qin; Yin, Xiangfan; Jeyakumar, Kirujan; Vogel, Felix C. E.; Krepler, Clemens; Rebecca, Vito W.; Kubat, Linda; Lueong, Smiths S.; Forster, Jan; Horn, Susanne; Remke, Marc; Ehrmann, Michael; Paschen, Annette; Becker, Jürgen; Helfrich, Iris; Rauh, Daniel; Kaiser, Markus; Gul, Sheraz; Herlyn, Meenhard; Bogeski, Ivan; Rodríguez-López, José Neptuno; Haass, Nikolas K.; Schadendorf, Dirk; Rösch, Alexander
    Persister state-directed transitioning and vulnerability in melanoma
    32. Deutscher Hautkrebskongress (ADO-Jahrestagung), 14.–17. September 2022, Hannover, Germany,
    In: Nature Communications, Vol. 13, 2022, Nr. 1, pp. 35 – 36
    DOI, Online Full Text (Open Access)
  • Dorsch, Madeleine; Kowalczyk, Manuela; Planque, Mélanie; Heilmann, Geronimo; Urban, Sebastian; Dujardin, Philip; Forster, Jan; Ueffing, Kristina; Nothdurft, Silke; Oeck, Sebastian; Paul, Annika; Liffers, Sven T.; Kaschani, Farnusch; Kaiser, Markus; Schramm, Alexander; Siveke, Jens T.; Winslow, Monte M.; Fendt, Sarah-Maria; Nalbant, Perihan; Grüner, Barbara M.
    Statins affect cancer cell plasticity with distinct consequences for tumor progression and metastasis
    In: Cell Reports, Vol. 37, 2021, Nr. 8, 110056
    DOI, Online Full Text (Open Access)

    • Preprints

  • Zaffar, Eman; Vieyto-Nuñez, Julio; Pravi, Katerina; Aslam, Mohammed Faidh; Almeida-Hernández, Yasser; Mieres-Pérez, Joel; Kaschani, Farnusch; Kaiser, Markus; Kroesen, Anika; Boos, Dominik; Sánchez-García, Elsa
    MTBP allosterically activates Cdk8-CycC kinase activity
    2025
    DOI (Open Access)
  • Klink, Nikolas; Urban, Sebastian; Seier, Johanna A.; Adhikari, Bikash; Schwalm, Martin P.; Müller, Juliane; Dorsch, Madeleine; Kaschani, Farnusch; Koch, Johannes; Führer, Siska; Kaiser, Markus; Schulze, Nina; Knapp, Stefan; Wolf, Elmar; Paschen, Annette; Grüner, Barbara M.; Gersch, Malte
    Targeted degradation of USP7 in solid cancer cells reveals disparate effects of deubiquitinase inhibition vs. acute protein depletion
    2025
    DOI, Online Full Text (Open Access)
  • Blümke, Anika; Hagemeier, Birte; Ripkens, Kamilla; Schulze, Nina; Strzala, Michal; Koci, Michelle; Kaschani, Farnusch; Kaiser, Markus; Erkelenz, Michael; Schlücker, Sebastian; Merdanovic, Melisa; Poepsel, Simon; Hellerschmied-Jelinek, Doris; Burston, Steve; Ehrmann, Michael
    A non-autonomous protein quality control mechanism targeting tau aggregate propagation
    2024
    DOI (Open Access)

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