ZMB Member Markus Kaiser, Publications

Prof. Dr. Markus Kaiser

Peer-reviewed papers

Weith M, Seiler J, van den Boom J, Kracht M, Hülsmann J, Primorac I, del Pino Garcia J, Kaschani F, Kaiser M, Musacchio A, Bollen M, Meyer H. Ubiquitin-independent disassembly by a p97 AAA-ATPase complex drives PP1 holoenzyme formation. Mol Cell, 2018, doi: 10.1016/j.molcel.2018.09.020.

Bongard J, Lorenz M, Vetter IR, Stege P, Porfetye AT, Schmitz AL, Kaschani F, Wolf A, Koch U, Nussbaumer P, Klebl B, Kaiser M, Ehrmann M. Identification of Noncatalytic Lysine Residues from Allosteric Circuits via Covalent Probes. ACS Chem Biol. 2018 May 18;13(5):1307-1312.

Dong X, Greening C, Brüls T, Conrad R, Guo K, Blaskowski S, Kaschani F, Kaiser M, Laban NA, Meckenstock RU. 2018. Fermentative Spirochaetes mediate necromass recycling in anoxic hydrocarbon-contaminated habitats. ISME Journal. 12(8):2039-2050.

Grosse-Holz F, Kelly S, Blaskowski S, Kaschani F, Kaiser M, van der Hoorn RAL. 2018. The transcriptome, extracellular proteome and active secretome of agroinfiltrated Nicotiana benthamiana uncover a large, diverse protease repertoire. Plant Biotechnology Journal. 16(5):1068-1084.

Grosse-Holz F, Madeira L, Zahid MA, Songer M, Kourelis J, Fesenko M, Ninck S, Kaschani F, Kaiser M, van der Hoorn RA. 2018. Three unrelated protease inhibitors enhance accumulation of pharmaceutical recombinant proteins in Nicotiana benthamiana. Plant Biotechnology Journal.

Halder V, Oeljeklaus J, Heilmann G, Krahn JH, Liu Y, Xiong Y, Schlicht M, Schillinger J, Kracher B, Ehrmann M, Kombrink E, Kaschani F, Kaiser M. 2018. Identification of the Natural Product RotihibinA as a TOR Kinase Signaling Inhibitor by Unbiased Transcriptional Profiling. Chemistry - A European Journal.

Planas-Marquès M, Bernardo-Faura M, Paulus J, Kaschani F, Kaiser M, Valls M, Van Der Hoorn RAL, Coll NS. 2018. Protease Activities Triggered by Ralstonia solanacearum Infection in Susceptible and Tolerant Tomato Lines. Molecular and Cellular Proteomics. 17(6):1112-1125.

Pöhler R, Krahn JH, van den Boom J, Dobrynin G, Kaschani F, Eggenweiler HM, Zenke FT, Kaiser M, Meyer H. 2018. A Non-Competitive Inhibitor of VCP/p97 and VPS4 Reveals Conserved Allosteric Circuits in Type I and II AAA ATPases. Angewandte Chemie - International Edition. 57(6):1576-1580.

Santos RB, Chandrasekar B, Mandal MK, Kaschani F, Kaiser M, Both L, van der Hoorn RAL, Schiermeyer A, Abranches R. 2018. Low Protease Content in Medicago truncatula Cell Cultures Facilitates Recombinant Protein Production. Biotechnology Journal. 13(7).

Schillinger J, Severin K, Kaschani F, Kaiser M, Ehrmann M. 2018. HTRA1-Dependent Cell Cycle Proteomics. Journal of Proteome Research. 17(8):2679-2694.

Ziemann S, Van Der Linde K, Lahrmann U, Acar B, Kaschani F, Colby T, Kaiser M, Ding Y, Schmelz E, Huffaker A, Holton N, Zipfel C, Doehlemann G. 2018. An apoplastic peptide activates salicylic acid signalling in maize. Nature Plants. 4(3):172-180.

Beisser D, Kaschani F, Graupner N, Grossmann L, Jensen M, Ninck S, Schulz F, Rahmann S, Boenigk J, Kaiser M. 2017. Quantitative proteomics reveals ecophysiological effects of light and silver stress on the mixotrophic protist Poterioochromonas malhamensis. PLoS ONE. 12(1).

Bongard J, Lorenz M, Vetter IR, Stege P, Porfetye AT, Schmitz AL, Kaschani F, Wolf A, Koch U, Nussbaumer P, Klebl B, Kaiser M, Ehrmann M. Identification of Noncatalytic Lysine Residues from Allosteric Circuits via Covalent Probes. ACS Chem Biol. 2018 May 18;13(5):1307-1312.

De Montaigu A, Oeljeklaus J, Krahn JH, Suliman MNS, Halder V, De Ansorena E, Nickel S, Schlicht M, Plíhal O, Kubiasová K, Radová L, Kracher B, Tóth R, Kaschani F, Coupland G, Kombrink E, Kaiser M. 2017. The Root Growth-Regulating Brevicompanine Natural Products Modulate the Plant Circadian Clock. ACS Chemical Biology. 12(6):1466-1471.

Ehrmann M, Kaiser M. 2017. Small Molecules from Deep within the Gut. ChemBioChem. 18(11):967-968.

Klein D, Steens J, Wiesemann A, Schulz F, Kaschani F, Röck K, Yamaguchi M, Wirsdörfer F, Kaiser M, Fischer JW, Stuschke M, Jendrossek V. 2017. Mesenchymal Stem Cell Therapy Protects Lungs from Radiation-Induced Endothelial Cell Loss by Restoring Superoxide Dismutase 1 Expression. Antioxidants and Redox Signaling. 26(11):563-582.

Köcher S, Rey J, Bongard J, Tiaden AN, Meltzer M, Richards PJ, Ehrmann M, Kaiser M. 2017. Tailored Ahp-cyclodepsipeptides as Potent Non-covalent Serine Protease Inhibitors. Angewandte Chemie - International Edition. 56(29):8555-8558.

Kovács J, Poór P, Kaschani F, Chandrasekar B, Hong TN, Misas-Villamil JC, Xin BT, Kaiser M, Overkleeft HS, Tari I, van der Hoorn RAL. Proteasome activity profiling uncovers alteration of catalytic β2 and β5 subunits of the stress-induced proteasome during salinity stress in tomato roots. Front Plant Sci. 2017 Feb 3;8:107.

Krahn JH, Kaschani F, Kaiser M. 2017. Turning-ON Proteasomes. Cell Chemical Biology. 24(6):653-655.

Lu H, Chandrasekar B, Oeljeklaus J, Misas-Villamil JC, Wang Z, Shindo T, Bogyo M, Kaiser M, van der Misas-Villamil JC, van der Burgh AM, Grosse-Holz F, Bach-Pages M, Kovács J, Kaschani F, Schilasky S, Emon AEK, Ruben M, Kaiser M, Overkleeft HS, van der Hoorn RAL. 2017. Subunit-selective proteasome activity profiling uncovers uncoupled proteasome subunit activities during bacterial infections. Plant Journal. 90(2):418-430.

Zweerink S, Kallnik V, Ninck S, Nickel S, Verheyen J, Blum M, Wagner A, Feldmann I, Sickmann A, Albers SV, Bräsen C, Kaschani F, Siebers B, Kaiser M. 2017. Activity-based protein profiling as a robust method for enzyme identification and screening in extremophilic Archaea. Nature Communications. 8.

Zweerink S, Pollmann T, Ninck S, Kaschani F, Kaiser M. Activity-based protein profiling with natural product-derived chemical probes in human cell lysates. Methods in Molecular Biology. 2017. p. 23-46.

van den Boom J, Wolf M, Weimann L, Schulze N, Li F, Kaschani F, Riemer A, Zierhut C, Kaiser M, Iliakis G, Funabiki H, Meyer H. 2016. VCP/p97 Extracts Sterically Trapped Ku70/80 Rings from DNA in Double-Strand Break Repair. Molecular Cell. 64(1):189-198.

Shaulov-Rotem Y, Merquiol E, Weiss-Sadan T, Moshel O, Salpeter S, Shabat D, Kaschani F, Kaiser M, Blum G. 2016. A novel quenched fluorescent activity-based probe reveals caspase-3 activity in the endoplasmic reticulum during apoptosis. Chemical Science. 7(2):1322-1337.

Kaschani F, Wei Q, Dingemans J, van der Hoorn RAL, Cornelis P, Kaiser M. 2016. Capture of endogenously biotinylated proteins from Pseudomonas aeruginosa displays unexpected downregulation of LiuD upon iron nutrition. Bioorganic and Medicinal Chemistry. 24(15):3330-3335.

Kombrink E, Kaiser M. 2016. Editorial: When chemistry meets biology– Generating innovative concepts, methods and tools for scientific discovery in the plant sciences. Frontiers in Plant Science. 7(FEB2016).

Ilyas M, Hörger AC, Bozkurt TO, Van Den Burg HA, Kaschani F, Kaiser M, Belhaj K, Smoker M, Joosten MHAJ, Kamoun S, Van Der Hoorn RAL. 2015. Functional Divergence of Two Secreted Immune Proteases of Tomato. Current Biology. 25(17):2300-2306.

Nickel S, Serwa RA, Kaschani F, Ninck S, Zweerink S, Tate EW, Kaiser M. 2015. Chemoproteomic Evaluation of the Polyacetylene Callyspongynic Acid. Chemistry - A European Journal. 21(30):10721-10728.

Hoorn RAL. 2015. Subfamily-specific fluorescent probes for cysteine proteases display dynamic protease activities during seed germination. Plant Physiology. 168(4):1462-1475.

Kellermann G, Kaiser M, Dingli F, Lahuna O, Naud-Martin D, Mahuteau-Betzer F, Loew D, Ségal-Bendirdjian E, Teulade-Fichou MP, Bombard S. 2015. Identification of human telomerase assembly inhibitors enabled by a novel method to produce hTERT. Nucleic Acids Research. 43(15).

Poepsel S, Sprengel A, Sacca B, Kaschani F, Kaiser M, Gatsogiannis C, Raunser S, Clausen T, Ehrmann M. Determinants of amyloid fibril degradation by the PDZ protease HTRA1. Nat Chem Biol.  2015 Nov;11(11):862-9.

Nickel S, Nickel P, Hellmert M, Ernst S, Jewell R, Pearce CA, Jones G, Hamza D, Kaiser M. Synthesis of a hexahydropyrrolo indole (HPI) compound library. Bioorg Med Chem. 2015 Jun 1;23(11):2636-45.

Ehrmann M, Kaschani F, Kaiser M. Chemical proteomics versus leishmaniasis. Chem Biol. 2015 Mar 19;22(3):309-10.

van den Boom J, Mamić M, Baccelliere D, Zweerink S, Kaschani F, Knauer S, Bayer P, Kaiser M. Peptidyl Succinimidyl Peptides as Taspase 1 Inhibitors. Chembiochem. 2014 Aug 21.

Meesters C, Mönig T, Oeljeklaus J, Krahn D, Westfall CS, Hause B, Jez JM, Kaiser M, Kombrink E. A chemical inhibitor of jasmonate signaling targets JAR1 in Arabidopsis thaliana. Nat Chem Biol. 2014 Aug 17.

Köhn M, Meijler MM, Kaiser M. Building up a chemical proteomics network in europe and beyond. ACS Chem Biol. 2014 Aug 15;9(8):1647-8.

Bruss H, Schuster H, Martinez R, Kaiser M, Antonchick AP, Waldmann H. Synthesis of the B-seco limonoid core scaffold. Beilstein J Org Chem. 2014 Jan 16;10:194-208.

Villamor JG, Kaschani F, Colby T, Oeljeklaus J, Zhao D, Kaiser M, Patricelli MP, van der Hoorn RA. Profiling protein kinases and other ATP binding proteins in Arabidopsis using acyl-ATP probes. Mol Cell Proteomics. 2013 Sep;12(9):2481-96.

Kaiser M, John M, Borsdorf A, Nöttling A, Neumuth T. A Hybird Optimization Approach for 2D-3D Registrationbased Fusion of Ultrasound and X-Ray. Biomed Tech (Berl). 2013 Sep 7.

Stolze SC, Meltzer M, Ehrmann M, Kaiser M. Ahp cyclodepsipeptides: the impact of the ahp residue on the "canonical inhibition" of s1 serine proteases. Chembiochem.. 2013 Jul 22;14(11):1301-8.

van der Hoorn RA, Kaiser M. Probes for activity-based profiling of plant proteases.Physiol Plant. 2012 May;145(1):18-27.

Gu C, Shannon DA, Colby T, Wang Z, Shabab M, Kumari S, Villamor JG, McLaughlin CJ, Weerapana E, Kaiser M, Cravatt BF, van der Hoorn RA.Chemical proteomics with sulfonyl fluoride probes reveals selective labeling of functional tyrosines in glutathione transferases. Chem Biol. 2013 Apr 18;20(4):541-8.

Lu H, Wang Z, Shabab M, Oeljeklaus J, Verhelst SH, Kaschani F, Kaiser M, Bogyo M, van der Hoorn RA. A substrate-inspired probe monitors translocation, activation, and subcellular targeting of bacterial type III effector protease AvrPphB. Chem Biol. 2013 Feb 21;20(2):168-76.

Oeljeklaus J, Kaschani F, Kaiser M. Streamlining chemical probe discovery: libraries of "fully functionalized" small molecules for phenotypic screening. Angew Chem Int Ed Engl. 2013 Jan 28;52(5):1368-70.

Stolze SC, Kaiser M. 2013. Case studies of the synthesis of bioactive cyclodepsipeptide natural products. Molecules, 18: 1337-1367.

Merdanovic M, Mönig T, Ehrmann M, Kaiser M. 2013. Diversity of allosteric regulation of proteases. ACS Chem. Biol., 8: 19-26.

Solze SC, Deu E, Kaschani F, Richau KH, Li N, Florea BI, Colby T, van der Hoorn RA, Overkleeft HS, Bogyo M, Kaiser M. 2012. The antimalarial natural product symplostatin 4 is a nanomolar inhibitor of the food vacuole falcipains. Chem. Biol., 19: 1546-1555.

Stein ML, Beck P, Kaiser M, Dudler R, Becker CF, Groll M. One-shot NMR analysis of microbial secretions identifies highly potent proteasome inhibitor. Proc Natl Acad Sci U S A. 2012 Oct 22.

Shannon DA, Gu C, McLaughlin CJ, Kaiser M, van der Hoorn RA, Weerapana E. Sulfonyl fluoride analogues as activity-based probes for serine proteases. Chembiochem. 2012 Nov 5;13(16):2327-30. Epub 2012 Sep 24.

Archer C, Groll M, Stein M, Schellenberg B, Clerc J, Kaiser M, Tondratyuk T, Pezzuto J, Dudler R, Bachmann A. 2012. Activity enhancement of the synthetic syrbactin proteasome inhibitor hybrid and biological evaluation in tumor cells. Biochemistry, 51: 6880-6888.

Tennstaedt A, Pöpsel S, Truebestein L, Hauske P, Brockmann A, Schmidt N, Irle I, Sacca B, Niemeyer CM, Brandt R, Ksiezak-Reding H, Tirniceriu AL, Egensperger R, Baldi A, Dehmelt L, Kaiser M, Huber R, Clausen T, Ehrmann M. Human high temperature requirement serine protease A1 (HTRA1) degrades tau protein aggregates. J Biol Chem. 2012 Jun 15;287(25):20931-41. Epub 2012 Apr 25.

Bier C, Knauer SK, Wünsch D, Kunst L, Scheiding S, Kaiser M, Ottmann C, Krämer OH, Stauber RH. Allosteric inhibition of Taspase1's pathobiological activity by enforced dimerization in vivo. FASEB J. 2012 Aug;26(8):3421-9. Epub 2012 May 23.

Stolze SC, Kaiser M. 2012. Challenges in the Syntheses of Peptidic Natural Products. Synthesis, 44: 1755-1777.

Lütticke C, Hauske P, Lewandrowski U, Sickmann A, Kaiser M, Ehrmann M. 2012. E. coli LoiP (YggG), a metalloprotease hydrolyzing Phe-Phe bonds. Mol. Biosyst.,8: 1775-1782.

Kaschani F, Clerc J, Krahn D, Bier D, Hong TN, Ottmann C, Niessen S, Colby T, van der Hoorn RA, Kaiser M. Identification of a selective, activity-based probe for glyceraldehyde 3-phosphate dehydrogenases. Angew Chem Int Ed Engl. 2012 May 21;51(21):5230-3. Epub 2012 Apr 5. No abstract available

Kaiser M, Ottmann C. In silico identification of an interferon inhibitor. ChemMedChem. 2012 Apr;7(4):555-7. Epub 2012 Jan 20. Review. No abstract available.

Kaiser M, van der Hoorn RA. 2012. Probes for activity-based profiling of plant proteases. Physiol. Plant, 145: 18-27.

Ottmann C, van der Hoorn RA, Kaiser M. The impact of plant-pathogen studies on medicinal drug discovery. Chem Soc Rev. 2012 Apr 21;41(8):3168-78. Epub 2012 Feb 1. Review.

Stolze SC, Meltzer M, Ehrmann M, Kaiser M. 2012. Developmen of a solid-phase approach to the natural poduct class o Ahp containing cyclodepsipeptides. Eur. J. Org. Chem., 1616-1625.

Thiel P, Kaiser M, Ottmann C. Small-molecule stabilization of protein-protein interactions: an underestimated concept in drug discovery? Angew Chem Int Ed Engl. 2012 Feb 27;51(9):2012-8. Epub 2012 Feb 3. Review.

Weski J, Meltzer M, Spaan L, Mönig T, Oeljeklaus J, Hauske P, Vouilleme L, Volkmer R, Boisguerin P, Boyd D, Huber R, Kaiser M, Ehrmann M. Chemical biology approaches reveal conserved features of a C-terminal processing PDZ protease. Chembiochem. 2012 Feb 13;13(3):402-8. Epub 2012 Jan 20.

Nickel S, Kaschani F, Colby T, van der Hoorn RA, Kaiser M. A para-nitrophenol phosphonate probe labels distinct serine hydrolases of Arabidopsis. Bioorg Med Chem. 2012 Jan 15;20(2):601-6. Epub 2011 Jul 15.Kaschani F, Nickel S, Pandey B, Cravatt BF, Kaiser M, van der Hoorn RA. Selective inhibition of plant serine hydrolases by agrochemicals revealed by competitive ABPP. Bioorg Med Chem. 2012 Jan 15;20(2):597-600. Epub 2011 Jul 18.

van der Linden WA, Willems LI, Shabaneh TB, Li N, Ruben M, Florea BI, van der Marel GA, Kaiser M, Kisselev AF, Overkleeft HS. Discovery of a potent and highly β1 specific proteasome inhibitor from a focused library of urea-containing peptide vinyl sulfones and peptide epoxyketones. Org Biomol Chem. 2012 Jan 7;10(1):181-94. Epub 2011 Nov 22.

Cottier S, Mönig T, Wang Z, Svoboda J, Boland W, Kaiser M, Kombrink E. 2011. The yeast three-hybrid sysem as an experimental platorm to identify proteins interacting with small signalling molecules in plant cells: Potenial un limitaions. Front Plant Sci., 2:101.

van der Hoon RA,Colby T, Nickel S, Richau K, Schmidt J, Kaiser M. 2011. Mining he active poeosome of Arabidopsis thaliana. Front Plant Sci., 2:89.

Krahn D, Ottmann C, Kaiser M. 2011. Macrocyclic poteasome inhibitors. Curr. Med. Chem., 33:5052-5060.

Krahn D, Ottmann C, Kaiser M. The chemistry and biology of syringolins, glidobactins and cepafungins (syrbactins). Nat Prod Rep. 2011 Oct;28(11):1854-67. Epub 2011 Sep 9. Review.

Merdanovic M, Clausen T, Kaiser M, Huber R, Ehrmann M.2011. Orotein quality control in the bacterial periplasm. Annu. Rav. Micobiol., 65:149-168.

Wuest WM, Krahn D, Kaiser M, Walsh CT. Enzymatic timing and tailoring of macrolactamization in syringolin biosynthesis. Org Lett. 2011 Sep 2;13(17):4518-21. Epub 2011 Aug 3.

Schuster H, Martinez R, Bruss H, Antonchick AP, Kaiser, M, Schürmann M, Waldmann H.2011.Synthesis of the B-seco limonoid scaffold.Chem. Commun.,47:6545-6547.

Clausen, T, Kaiser, M, Huber, R and M. Ehrmann. 2011. HtrA proteases: Regulated proteolysis in protein quality control. Nat. Rev. Mol. Cell Biol., 12:152-62.

Trübestein, L., Tennstaedt, A., Mönig, T., Krojer, T., Canellas, F., Kaiser, M. Clausen, T., and M. Ehrmann. 2011. Substrate induced remodeling of the active site regulates human HtrA1 activity. Nat. Struct. Mol. Biol., 18:386-388.

Kolodziejek I, Misas-Villamil JC, Kaschani F, Clerc J, Gu C, Krahn D, Niessen S, Verdoes M, Willems LI, Overkleeft HS, Kaiser M, van der Hoorn RAL. Proteasome activity imaging and profiling characterizes bacterial effector Syringolin A. Plant Physiol. 2011, 155, 477-489.

Clerc J, Li N, Krahn D, Groll M, Bachmann AS, Florea BI, Overkleeft HS, Kaiser M. The natural product hybrid of Syringolin A and Glidobactin A synergizes proteasome inhibition potency with subsite selectivity. Chem. Commun. 2011, 47, 385-387.
Special article for the 2011 Emerging Investigators Issue.

Kim SS, Grienenberger E, Lallemand B, Colpitts CC, Kim SY, Souza CDA, Geoffroy P, Heintz D, Krahn D, Kaiser M, Kombrink E, Heitz T, Suh DS, Legrand M, Douglas CJ. LAP6/POLYKETIDE SYNTHASE A and LAP5/POLYKETIDE SYNTHASE B encode hydroxyalkyl α-pyrone synthases required for pollen development and sporopollenin biosynthesis in Arabidopsis thaliana. Plant Cell 2010, 22, 4045-4066.

Stolze SC, Meltzer M, Ehrmann M, Kaiser M. Solid phase total synthesis of the 3-amino-6-hydroxy-2-piperidone (Ahp) cyclodepsipeptide and protease inhibitor Symplocamide A. Chem. Commun. 2010, 46, 8857-8859.
Highlighted in Synfacts 2011, 2, 233.

Imker HJ, Krahn D, Clerc J, Kaiser M, Walsh CT. N-Acylation during Glidobactin biosynthesis by the tridomain nonribosomal peptide synthetase module GlbF. Chem. Biol. 2010, 17, 1077-1083.

Kaiser M, Ottmann C. The first small molecule inhibitor of 14-3-3s: modulating the master regulator. Chembiochem 2010, 11, 2085-2087.

Molzan M, Schumacher B, Ottmann C, Baljuls A, Polzien L, Weyand M, Thiel P, Rose R, Rose M, Kuhenne P, Kaiser M, Rapp U, Kuhlmann J, Ottmann C. Impaired binding of 14-3-3 to C-RAF in Noonan syndrome suggests new approaches in diseases with increased Ras signaling. Mol. Cell Biol. 2010, 30, 4698-4711.

Clerc J, Schellenberg B, Groll M, Bachmann AS, Huber R, Dudler R, Kaiser M. Convergent synthesis and biological evaluation of Syringolin A and derivatives as eukaryotic 20S proteasome inhibitors. Eur. J. Org. Chem. 2010, 3991-4003. Cover picture.

Merdanovic M, Mamant N, Meltzer M, Poepsel S, Auckenthaler A, Melgaard R, Hauske P, Nagel-Steger L, Clarke AR, Kaiser M, Huber R, Ehrmann M. 2010. Determinants of structural and functional plasticity of a widely conserved protease chaperone complex. Nat Struct Mol Biol 17, 837-843.

Wetzel S, Wilk W, Chamma S, Sperl B, Roth A, Yektaoglu A, Renner S, Berg T, Arenz C, Giannis A, Oprea TI, Rauh D, Kaiser M, Waldmann H. A scaffold tree-merging strategy for prospective bioactivity annotation of γ-pyrones. Angew. Chem. Int. Ed. 2010, 49, 3666-3670.

Wilk W, Zimmermann TJ, Kaiser M, Waldmann H. Principles, implementation, and application of biology-oriented synthesis (BIOS). Biol. Chem. 2010, 391, 491-497.

Archer CR, Koomoa DLT, Mitsunaga EM, Clerc J, Shimizu M, Kaiser M, Schellenberg B, Dudler R, Bachmann AS. Syrbactin class proteasome inhibitor-induced apoptosis and autophagy occurs in association with p53 accumulation and Akt/PKB activation in neuroblastoma. Biochem. Pharmacol. 2010, 80, 170-178.

Hasenbein S, Meltzer M, Hauske P, Kaiser M, Huber R, Clausen T, Ehrmann M. Conversion of a regulatory into a degradative protease. J. Mol. Biol. 2010, 397, 957-966.

Ottmann C, Hauske P, Kaiser M. Activation instead of inhibition: Targeting proenzymes for small molecule intervention. Chembiochem 2010, 11, 637-639.

Meltzer M, Hasenbein S, Mamant N, Merdanovic M, Poepsel S, Hauske P, Kaiser M, Huber R, Krojer T, Clausen T, Ehrmann M. Structure, function and regulation of the conserved serine proteases DegP and DegS. Res. Microbiol. 2009, 160, 660-666.

Wilk W, Nören-Müller A, Kaiser M, Waldmann H. Biology-oriented combined solid- and solution phase synthesis of a macroline-like compound collection. Chem. Eur. J. 2009, 15, 11976-11984.

Clerc J, Florea BI, Kraus M, Groll M, Huber R, Bachmann AS, Dudler R, Driessen C, Overkleeft HS, Kaiser M. Syringolin A selectively labels the 20S proteasome in murine EL4 and wildtype and bortezomib adapted leukemic cell lines. Chembiochem 2009, 10, 2638-2643. Inside cover picture.

Ottmann C, Rose R, Huttenlocher F, Cedzich A, Hauske P, Kaiser M, Huber R, Schaller A. The plant protease SBT3 is Ca2+ independent and activated by PA domain-mediated homo-dimerization. Proc. Natl. Acad. Sci. USA 2009, 106, 17223-17228.

Knoth T, Warburg K, Katzka C, Rai A, Wolf A, Brockmeyer A, Janning P, Reubold T, Eschenburg S, Manstein D, Hübel K, Kaiser M, Waldmann H. The Ras pathway modulator Melophlin A targets dynamins. Angew. Chem. Int. Ed. 2009, 48, 7240-7245.

Hauske P, Mamant N, Hasenbein S, Nickel S, Ottmann C, Clausen T, Ehrmann M, Kaiser M. Peptidic small molecule activators of the stress sensor DegS. Mol. Biosystems 2009, 5, 980-985.
Special article for the 2009 Emerging Investigators Issue.

Yoshida M, Hedberg C, Kaiser M, Waldmann H. Traceless solid phase synthesis of natural product inspired cis-1,2-dehydrodecalins. Chem. Commun. 2009, 2926-2928.

Rose R, Huttenlocher F, Cedzich A, Kaiser M, Schaller A, Ottmann C. Purification, crystallization and preliminary X-ray diffraction analysis of a plant subtilase. Acta Cryst. 2009, F65, 522-525.

Clerc J, Groll M, Nukic D, Bachmann AS, Huber R, Schellenberg B, Dudler R, Kaiser M. Synthetic and structural studies on Syringolin A and B reveal critical determinants for selectivity and potency of proteasome inhibition. Proc. Natl. Acad. Sci. USA 2009, 106, 6507-6512.

Hauske P, Meltzer M, Ottmann C, Krojer T, Clausen T, Ehrmann M, Kaiser M. Selectivity profiling of DegP substrates and inhibitors. Bioorg. Med. Chem. 2009, 17, 2920-2924. Cover picture.

Wilk W, Waldmann H, Kaiser M. γ-Pyrone natural products – a privileged compound class provided by nature. Bioorg. Med. Chem. 2009, 17, 2304-2309.

Kaschani F, Verhelst SHL, van Swieten PF, Verdoes M, Wong CS, Wang Z, Kaiser M, Overkleeft HS, Bogyo M, van der Hoorn RAL. Minitags for small molecules: detecting targets of reactive small molecules in living plant tissues using ‘click chemistry’. Plant J. 2009, 57, 373-385.

Hauske P, Ottmann C, Meltzer M, Ehrmann M, Kaiser M. Allosteric regulation of proteases. Chembiochem 2008, 9, 2920-2928.

Wang Z, Gu C, Colby T, Shindo T, Balamurugan R, Waldmann H, Kaiser M, van der Hoorn RAL. β-lactone probes identify a papain-like peptide ligase in Arabidopsis thaliana. Nature Chem. Biol. 2008, 4, 557-563.
Highlighted in Nature Chem. Biol. 2008, 4, 525-526.

Nören-Müller A, Wilk W, Saxena K, Schwalbe H, Kaiser M*, Waldmann H*. Discovery of a new class of inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase B by biology-oriented synthesis (BIOS). Angew. Chem. Int. Ed. 2008, 47, 5973-5977.
* cor-responding authors. Flagged as an Hot article.

Amrane S, De Cian A, Rosu F, Kaiser M, De Pauw E, Teulade-Fichou MP, Mergny JL. Identification of CNG trinucleotide repeat ligands with a FRET melting assay. Chembiochem 2008, 9, 1229-1234.

Kaiser M, Wetzel S, Kumar K, Waldmann H. Biology-inspired synthesis of compound libraries. Cell. Mol. Life Sci. 2008, 65, 1186-1201.

Groll M, Schellenberg B, Bachmann AS*, Archer CR, Huber R, Powell TK, Lindow S, Kaiser M*, Dudler R*. A plant pathogen virulence factor inhibits the eukaryotic proteasome by a novel mechanism. Nature 2008, 452, 755-758.
* corresponding authors.
Highlighted in Chem. Eng. News 2008, 86, 39; Chem. Biol. 2008, 15, 419-421.

Meltzer M, Hasenbein S, Hauske P, Kucz N, Merdanovic M, Grau S, Beil A, Jones D, Krojer T, Clausen T, Ehrmann M, Kaiser M. Allosteric activation of HtrA protease DegP by stress signals during bacterial protein quality control. Angew. Chem. Int. Ed. 2008, 47, 1332-1334.

Corrêa Jr IR, Nören-Müller A, Ambrosi HD, Jakupovic S, Saxena K, Schwalbe H, Kaiser M, Waldmann H. Identification of inhibitors for mycobacterial protein tyrosine phosphatase B (MptpB) by biology-oriented synthesis (BIOS). Chem. Asian J. 2007, 2, 1109-1126.

De Cian A, Guittat L, Kaiser M, Saccà B, Amrane S, Bourdoncle A, Alberti P, Teulade-Fichou MP, Lacroix L, Mergny JL. Fluorescence-based melting assays for studying quadruplex ligands. Methods 2007, 42, 183-195.

Groll M, Götz M, Kaiser M, Weyher E, Moroder L. TMC-95-based inhibitor design provides evidence for the catalytic versatility of the proteasome. Chem. Biol. 2006, 13, 607-614.

Kaiser M, De Cian A, Sainlos M, Renner C, Mergny JL, Teulade-Fichou MP. Neomycin-capped aromatic platforms: quadruplex DNA recognition and telomerase inhibition. Org. Biomol. Chem. 2006, 4, 1049-1057.
Flagged as an Hot Article. Highlighted in Chemical Biology 2006, 1, B10.

Kaiser M, Sainlos M, Lehn JM, Bombard S, Teulade-Fichou MP. Aminoglycoside-quinacridine conjugates: Towards recognition of the P6.1 element of Telomerase RNA. Chembiochem 2006, 7, 321-329.

Musiol HJ, Dong S, Kaiser M, Bausinger R, Zumbusch A, Bertsch U, Moroder L. Toward semisynthetic lipoproteins by convergent strategies based on click and ligation chemistry. Chembiochem 2005, 6, 625-628.

Kaiser M, Groll M, Siciliano C, Assfalg-Machleidt I, Weyher E, Kohno J, Milbradt AG, Renner C, Huber R, Moroder L. Binding mode of TMC-95A analogues to eukaryotic 20S proteasome. Chembiochem 2004, 5, 1256-1266.

Kaiser M, Milbradt AG, Siciliano C, Assfalg-Machleidt I, Machleidt W, Groll M, Renner C, Moroder L. TMC-95A analogues with endocyclic biphenyl ether group as proteasome inhibitors. Chem. Biodivers. 2004, 1, 161-173.

Kaiser M, Milbradt AG, Renner C, Assfalg-Machleidt I, Groll M, Huber R, Moroder L. Cyclic biphenyl ether tripeptides as proteasome inhibitors. Book chapter in: Peptide Revolution: Genomics, Proteomics & Therapeutics (M. Chorev, T. K. Sawyer, eds.), American Peptide Society, 2003, pp 348-349.

Kaiser M, Siciliano C, Assfalg-Machleidt I, Groll M, Milbradt AG, Moroder L. Synthesis of a TMC-95A ketomethylene analogue by cyclization via intramolecular Suzuki coupling. Org. Lett. 2003, 5, 3435-3437.

Kim JS, Groll M, Musiol HJ, Behrendt R, Kaiser M, Moroder L, Huber R, Brandstetter H. Navigation inside a protease: Substrate selection and product exit in the tricorn protease from Thermoplasma acidophilum. J. Mol. Biol. 2002, 324, 1041-1050.

Kaiser M, Milbradt AG, Moroder L. Synthesis of TMC-95A analogues. Structure-based prediction of cyclization propensities of linear precursors. Lett. Pept. Sci. 2002, 9, 65-70.
Paper on the occasion of the receipt of the Dr. Bert L. Schram Award, see Editorial Lett. Pept. Sci. 2002, 9, 61-63.

Ashcroft AE, Brinker A, Coyle JE, Weber F, Kaiser M, Moroder L, Parsons MR, Jager J, Hartl UF, Hayer-Hartl M, Radford SE. Structural plasticity and non-covalent substrate binding in the GroEL apical domain: A study using electrospray ionisation mass spectrometry and fluorescence binding studies. J. Biol. Chem. 2002, 277, 33115-33126.

Kaiser M, Groll M, Renner C, Huber R, Moroder L. The core structure of TMC-95A is a promising lead for reversible proteasome inhibition. Angew. Chem. Int. Ed. 2002, 41, 780-783.
Highlighted in Chem. Eng. News 2002, 80, 14.


Groll M, Kaiser M, Huber R, Moroder L, Renner C, Kohno J. Crystals of a Proteasome-Inhibitor Complex. Patent WO02081501 (2002).

Kaiser M, Clerc J. Development of a synthesis of Syringolin A and B and derivatives thereof. Patent US 61/129,865 (2008).

Kaiser M, Clerc J. Derivatives of syringolin A. Patent EP09075018.3-2117 (2009).


Chemische Biologie

ZMB/Faculty of Biology
University of Duisburg-Essen
45117 Essen

Room S03 S02 A55