CRC 1093 - Principal Investigator Markus Kaiser
Prof. Dr. Markus Kaiser
Phone: +49 201 183 4980
Email
Centre for Medical Biotechnology (ZMB)
Faculty of Biology
University of Duisburg-Essen
Area A: Chemical Ligands and Methods A2: Natural products as starting structures for the development of supramolecular ligands
A2 starts from naturally occuring cyclodepsipeptides and turns them into highly specific inhibitors of S1-serine proteases. Suitable derivatizations are obtained from biochemical digestion experiments or via virtual docking to the specificity pockets known from crystal structures, and are subsequently realized by total synthesis. In order to produce powerful ditopic receptor molecules for neighbouring protein domains, dynamic combinatorial chemistry will merge two series of specific binders and select those building blocks with a perfect match on both binding epitopes.
Read moreCurriculum Vitae
Professional career
2010-today | Professor (C3) of Chemical Biology, University of Duisburg-Essen |
2005-2010 | Independent Juniour Group Leader at the Chemical Genomics Centre of the Max-Planck Society, Dortmund, Mentor: Prof. Dr. H. Waldmann |
2003-2005 | Postdoctoral Research Assistant with Dr. M.-P. Teulade-Fichou and Prof. Dr. J.-M. Lehn, Laboratoire de Chimie des Interactions Moléculaires, Collège de France, Paris |
2003 | Postdoctoral Research Assistant with Prof. Dr. L. Moroder, Department of Bioorganic Chemistry, MPI of Biochemistry, Martinsried |
Scientific education and degrees
2000-2003 | Ph.D. at the MPI of Biochemistry, Martinsried, and the TU Munich with Prof. Dr. L. Moroder |
1994-1999 | Study of Chemistry (Dipl.) at the University of Frankfurt and Tübingen, Diploma thesis with Prof. Dr. G. Jung, Tübingen |
Selected Publications
S. Köcher, J. Rey, J. Bongard, A. N. Tiaden, M. Meltzer, P. Richards, M. Ehrmann, M. Kaiser: Tailored Ahp-cyclodepsipeptides as potent non-covalent serine protease inhibitors. Angew. Chem. Int. Ed. 2017, DOI: 10.1002/anie.201701771R1.
S. Zweerink, V. Kallnik, S. Ninck, S. Nickel, J. Verheyen, M. Blum, A. Wagner, I. Feldmann, A. Sickmann, S.-V. Albers, C. Bräsen, F. Kaschani, B. Siebers, M. Kaiser: Activity-based protein profiling as a robust method for enzyme identification and screening in extremophilic Archaea. Nat. Commun. 2017, DOI 10.1038/NCOMMS15352.
J. van den Boom, M. Wolf, L. Weimann, N. Schulze, F. Li, F. Kaschani, A. Riemer, C. Zierhuts, M. Kaiser, G. Iliakis, H. Funabiki, H. Meyer: VCP/p97 extracts sterically trapped Ku70/80 rings from DNA in double strand break repair. Mol. Cell 2016, 64, 189-198.
S. Poepsel, A. Sprengel, B. Sacca, F. Kaschani, M. Kaiser, C. Gatsogiannis, S. Raunser, T. Clausen, M. Ehrmann: Determinants of amyloid fibril degradation by the PDZ protease HTRA1. Nat. Chem. Biol. 2015, 11, 862-869.
C. Meesters, T. Mönig, J. Oeljeklaus, D. Krahn, C.S. Westfall, B. Hause, J.M. Jez, M. Kaiser*, E. Kombrink*: A chemical inhibitor of jasmonate signaling targets JAR1 in Arabidopsis thaliana. Nat. Chem. Biol. 2014, 10, 830-836. *corresponding authors
F. Kaschani, J. Clerc, D. Krahn, D. Bier, T. N. Hong, C. Ottmann, S. Niessen, T. Colby, R. A. L. van der Hoorn, M. Kaiser: Identification of a selective, activity-based probe for GAPDHs. Angew. Chem. Int. Ed. 2012, 51, 5230-5233.
L. Trübestein, A. Tennstaedt, T. Mönig, T. Krojer, F. Canellas, M. Kaiser, T. Clausen, M. Ehrmann: Substrate induced remodeling of the active site regulates HtrA1 activity. Nat. Struct. Mol. Biol. 2011, 18, 386-388.
M. Merdanovic, N. Mamant, M. Meltzer, S. Poepsel, A. Auckenthaler, R. Melgaard, P. Hauske, L. Nagel-Steger, A. R. Clarke, M. Kaiser, R. Huber, M. Ehrmann: Determinants of structural and functional plasticity of the widely conserved protease chaperone machine DegP. Nat. Struct. Mol. Biol. 2010, 17, 837-843.
Z. Wang, C. Gu, T. Colby, T. Shindo, R. Balamurugan, H. Waldmann, M. Kaiser, R. A. L. van der Hoorn: b-Lactone probes identify a papain-like peptide ligase in Arabidopsis thaliana. Nat. Chem. Biol. 2008, 4, 557-563.
M. Groll, B. Schellenberg, A. S. Bachmann*, C. R. Archer, R. Huber, T. K. Powell, S. Lindow, M. Kaiser*, R. Dudler*: A plant pathogen virulence factor inhibits the eukaryotic proteasome by a novel mechanism. Nature. 2008, 452, 755-758. *corresponding authors