CRC 1093 - Principal Investigator Markus Kaiser

Prof. Dr. Markus Kaiser

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Phone: +49 201 183 4980
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Chemical Biology

Centre for Medical Biotechnology (ZMB)
Faculty of Biology
University of Duisburg-Essen

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.

more aboutA2: Natural products as starting...

Curriculum Vitae

Professional career

Scientific education and degrees

 

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