Veröffentlichungen

 

  • Publikationen 1993 - 2000
  • E/Z-Diastereoselective enzymatic hydrolysis of esters and diesters
    T. Schirmeister, H.-H. Otto, Angew. Chem. Int. Ed. Engl. 32, 572-574 (1993)
  • Enzyme-catalyzed hydrolyses of E/Z-diastereotopic and E/Z-diastereomeric esters - Affect on selectivity by reaction media
    T. Schirmeister, H.-H. Otto, J. Org. Chem. 58, 4819-4822 (1993)
  • Aziridine-2,3-dicarboxylic acid derivatives as inhibitors of papain
    T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 329, 239-244 (1996)
  • Stereoselective Synthesis of aziridine-2,3-dicarboxylic acid containing peptides as inhibitors of cysteine proteases
    T. Schirmeister, Europ. J. Pharm. Sci. 4, Suppl. 1, S106 (1996)
  • Aziridine-2,2-dicarboxylates: synthesis, reactions, photochromism
    T. Schirmeister, Liebigs Ann./Recueil, 1895-1899 (1997)
  • Cysteine proteases and their inhibitors
    H.-H. Otto, T. Schirmeister, Chem. Rev. 97, 133-171 (1997)
  • Synthesis of peptides with aziridine-2,3-dicarboxylic acid as an a-amino acid equivalent building block
    T. Schirmeister, Peptide Science - Present and Future 654-656 (1998)
  • Cystein-Protease-Inhibitoren mit Aziridin-2,3-dicarbonsäurebausteinen
    T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 331, Suppl. 1, 11 (1998)
  • Metall-Ionen als Co-Inhibitoren von Serin-Proteasen: Ein neuer Ansatz bei der Suche nach hochaffinen und spezifischen Liganden
    T. Schirmeister, Angew. Chem. 110, 1930-1932 (1998)
  • New peptidic cysteine protease inhibitors derived from the electrophilic a-amino acid aziridine-2,3-dicarboxylic acid
    T. Schirmeister, J. Med. Chem. 42, 560-572 (1999)
  • Inhibition of cysteine proteases by peptides containing aziridine-2,3-dicarboxylic acid building blocks
    T. Schirmeister, Biopolymers (Peptide Science) 51, 87-97 (1999)
  • Aziridinyl peptides as inhibitors of cysteine proteases: Effect of a free carboxylic acid function on inhibition
    T. Schirmeister, M. Peric, Bioorg. Med. Chem. 8, 1281-1291 (2000)
  • b-Lactam derivatives as enzyme inhibitors: N-Substituted derivatives of (S)-4-oxoazetidine-2-carboxylate as inhibitors of elastase and papain
    K. Achilles, M. Schneider, T. Schirmeister, H.-H. Otto, Pharmazie 55, 798-802 (2000)
  • b-Lactam derivatives as enzyme inhibitors: 1-Peptidyl derivatives of 4-phenylazetidin-2-one as inhibitors of elastase and papain
    K. Achilles, T. Schirmeister, H.-H. Otto, Arch. Pharm. Pharm. Med. Chem. 333, 243-253 (2000)
  • (S)-Thiirancarboxylic acid as a reactive building block for a new class of cysteine protease inhibitors
    T. Schirmeister, Bioorg. Med. Chem. Lett. 10, 2647-2651 (2000)

Publikationen 2001 - 2009
  • Thiirancarboxylic acid as electrophilic building block for new cysteine protease inhibitors
    G. Bruno, T. Schirmeister, Drugs Fut. 27, Suppl. A, 443 (2002)
  • Inhibitors of cysteine proteases containing an aziridine unit
    A. Breuning, R. Vicik, T. Schirmeister, Drugs Fut. 27, Suppl. A, 444 (2002)
  • Thiirancarboxamides as a new class oc cysteine protease inhibitors
    G. Bruno, T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 335, Suppl. 1, 76 (2002)
  • Ex-chiral-pool synthesis of aziridine-2,3-dicarboxylates
    A. Breuning, T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 335, Suppl. 1, 76 (2002)
  • Non-peptidic inhibitors of cysteine proteases
    U. Käppler, T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 335, Suppl. 1, 86 (2002)
  • Peptidomimetic inhibitors of cysteine proteases
    R. Vicik, T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 335, Suppl. 1, 102 (2002)
  • Non-peptidic inhibitors of cysteine proteases
    T. Schirmeister, U. Käppler, Mini Rev. Med. Chem. 3, 361-373 (2003)
  • Cysteine protease inhibitors containing small rings
    T. Schirmeister, A. Klockow, Mini Rev. Med. Chem. 3, 585-596 (2003)
  • Improved synthesis of aziridine-2,3-dicarboxylates via azidoalcohols - studies on epimerization
    A. Breuning, R. Vicik, T. Schirmeister, Tetrahedron Asymmetry, 3301-3312 (2003)
  • Thiirancarboxamides as inhibitors of papain
    G. Bruno, T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 335, 90-95 (2004)
  • Synthesis and antiplasmodial activity of a cysteine-protease inhibiting biotinylated aziridine-2,3-dicarboxylate
    C. Gelhaus, R. Vicik, R. Hilgenfeld, C. L. Schmidt, M. Leippe, T. Schirmeister, Biol. Chem. 435-438 (2004)
  • Identification of cysteine proteases of intraerythrocytic life stages of Plasmodium falciparum by a biotinylated small-molecule probe
    T. Schirmeister, C. Gelhaus, R. Vicik, M. Leippe, Int. J. Med. Microbiol. 293, Suppl. 38, 89 (2004)
  • Model calculations about the influence of protic environments on the alkylation step of the epoxides, aziridine and thiirane based cysteine protease inhibitors
    H. Helten, T. Schirmeister, B. Engels, J. Phys. Chem. A 108, 7691-7701 (2004)
  • Conformation and hydrogen bonding properties of an aziridinyl peptide: X-ray structure analysis, Raman spectroscopy and theoretical investigations
    T. Schirmeister, A. Breuning, A. Murso, D. Stalke, M. Mladenovic, B. Engels, A. Szeghalmi, M. Schmitt, W. Kiefer, J. Popp, J. Phys. Chem. A 108, 11398-11408 (2004)
  • Using cysteine protease inhibitors to target proteins involved in survival and egression of intraerythrocytic stages of Plasmodium falciparum
    C. Gelhaus, R. Vicik, T. Schirmeister, M. Leippe, Int. J. Med. Microbiol. 293, Suppl. 38, 93 (2004)
  • Theoretical studies about the influence of different ring substituents on the nucleophilic ring opening of three-membered heterocycles and possible implications for the mechanisms of cysteine protease inhibitors
    H. Helten, T. Schirmeister, B. Engels, J. Org. Chem. 70, 233-237 (2005)
  • Development and validation of a separation method for the diastereomers and enantiomers of aziridine-type protease inhibitors
    Y. Bitar, B. Degel, T. Schirmeister, U. Holzgrabe, Electrophoresis 26, 2313-2319 (2005)
  • New non-peptidic inhibitors of papain derived from etacrynic acid
    U. Käppler, T. Schirmeister, Med. Chem. 1, 361-370 (2005)
  • Blocking effect of a biotinylated aziridine-2,3-dicarboxylate on the egress from infected red blood cells of Plasmodium falciparum merozoites
    C. Gelhaus, R. Vicik, T. Schirmeister, M. Leippe, Biol. Chem. 386, 499-502 (2005)
  • Comparison of the separation of aziridine isomers applying HDMS and HDAS in aqueous and non-aqueous systems
    Y. Bitar, B. Degel, T. Schirmeister, U. Holzgrabe, Electrophoresis 26, 3897-3903 (2005)
  • A new lead for non-peptidic active-site-directed inhibitors of the SARS coronavirus main protease discovered by a combination of screening and docking methods
    U. Käppler, N. Stiefl, M. Schiller, R. Vicik, A. Breuning, W. Schmitz, D. Rupprecht, C. Schmuck, K. Baumann, J. Ziebuhr, T. Schirmeister, J. Med. Chem. 48, 6832-6842 (2005)
  • Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitors
    E. Martina, N. Stiefl, B. Degel, F. Schulz, A. Breuning, M. Schiller, R. Vicik, K. Baumann, J. Ziebuhr, T. Schirmeister, Bioorg. Med. Chem. Lett. 15, 5365-5369 (2005)
  • Inhibitors of cysteine proteases
    R. Vicik, M. Busemann, K. Baumann, T. Schirmeister, Curr. Top. Med. Chem. 6, 331-353 (2006)
  • Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease ofTrypanosoma brucei as lead trypanocidal agents
    R. Vicik, V. Hoerr, M. Glaser, M. Schultheis, E. Hansell, J. H. McKerrow, U. Holzgrabe, C. R. Caffrey, A. Ponte-Sucre, H. Moll, A. Stich, T. Schirmeister, Bioorg. Med. Chem. Lett. 16, 2753-2757 (2006)
  • Aziridide based inhibitors of cathepsin L - Synthesis, inhibition activitiy, and docking studies
    R. Vicik, M. Busemann, C. Gelhaus, N. Stiefl, J. Scheiber, W. Schmitz, F. Schulz, M. Mladenovic, B. Engels, M. Leippe, K. Baumann, T. Schirmeister, ChemMedChem 1, 1126-1141 (2006)
  • Aziridine-2,3-dicarboxylates: peptidomimetic cysteine protease inhibitors with antileishmanial activity
    A. Ponte-Sucre, R. Vicik, M. Schultheis, T. Schirmeister, H. Moll, Antimicrob. Agents Chemother. 50, 2439-2447 (2006)
  • Rational design of aziridine containing cysteine protease inhibitors with improved potency - Studies on inhibition mechanism
    R. Vicik, H. Helten, T. Schirmeister, B. Engels, ChemMedChem 1, 1021-1028 (2006)
  • About the importance of the active site histidine for the activity of epoxide or aziridine based inhibitors of cysteine proteases
    M. Mladenovic, T. Schirmeister, S. Thiel, W. Thiel, B. Engels, ChemMedChem 2, 120-128 (2007)
  • Electron Density Determination of Electrophilic Building Blocks as Model Compounds for Protease Inhibitors
    S. Grabowsky, T. Pfeuffer, L. Checinska, M. Weber, W. Morgenroth, P. Luger, T. Schirmeister, Eur. J. Org. Chem. 2759-2768 (2007)
  • Bis-acridines as lead anti-parasitic agents: structure activity analysis of a discrete compound library in vitro
    C. R. Caffrey, J. Weismann, R.K. Swinerton, B. Kelly, A. T. Fafarman, M. Rodgers, L. W. Deady, J. A. Zorn, D. Walshe, A. Debnath, K. Land, J. Beauchene, K. Schreiber, F. E. Cohen, J. H. McKerrow, Y.-M. Zhou, P. Doyle, H. Moll, A. Ponte-Sucre, T. Schirmeister, A. Saravanamuthu, A. H. Fairlamb, D. Steverding, B. C. H. May, Antimicrob. Agents Chemother. 51, 2164-2172 (2007)
  • Screening of Protease Inhibitors as Antiplasmodial Agents. Part I: Aziridines and Epoxides
    F. Schulz, C. Gelhaus, B. Degel, R. Vicik, S. Heppner, A. Breuning, M. Leippe, J. Gut, P. J. Rosenthal, T. Schirmeister, ChemMedChem 2, 1214-1224 (2007)
  • Tetracycline-inducible expression of individual Secreted Aspartic Proteases inCandida albicans allows isoenzyme-specific inhibitor screening
    P. Staib, J. Blaß-Warmuth, U. Lermann, B. Degel, R. Würzner, M. Monod, T. Schirmeister, J. Morschhäuser, Antimicrob. Agents Chemother. 52, 146-156 (2008)
  • Cis-configured aziridines are new pseudo-irreversible dual-mode Inhibitors ofCandida albicans Secreted Aspartic Protease 2
    B. Degel, P. Staib, S. Rohrer, J. Scheiber, E. Martina, C. Büchold, K. Baumann, J. Morschhäuser, T. Schirmeister, ChemMedChem 3, 302-315 (2008)
  • Development of peptidomimetids with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors
    R. Ettari, E. Nizi, M. E. Di Francesco, M.-A. Dude, G. Pradel, R. Vicik, T. Schirmeister, N. Micale, S. Grasso, M. Zappala, J. Med. Chem. 51, 988-996 (2008)
  • Atomistic insights into the inhibition of cysteine proteases: First QM/MM calculations clarifying the regiospecificity and the inhibition potency of epoxide- and aziridine-based inhibitors
    M. Mladenovic, K. Junold, R. F. Fink, W. Thiel, T. Schirmeister, B. Engels, J. Phys. Chem. B. 112, 5458-5469 (2008)
  • Development of nonpeptidic vinyl- and allyl phosphonates as falcipain-2 active site-directed Michael acceptors
    R. Ettari, E. Nizi, M. E. Di Francesco, N. Micale, S. Grasso, M. Zappala, R. Vicik, T. Schirmeister, ChemMedChem 3, 1030-1033 (2008)
  • A comparative study on the experimentally derived electron density of three protease inhibitor model compounds
    S. Grabowsky, T. Pfeuffer, W. Morgenroth, C. Paulmann, T. Schirmeister, P. Luger, Org Biomol Chem. 6, 2295-2307 (2008)
    DOI: 10.1039/b802831a
  • On the origin of the stabilization of the zwitterionic resting state of cysteine proteases: A theoretical study
    M. Mladenovic, R. F. Fink, W. Thiel, T. Schirmeister, B. Engels, J. Am. Chem. Soc. 130, 8696-8705 (2008)
  • Atomistic insights into the inhibition of cysteine proteases: First QM/MM calculations clarifying the stereoselectivity of epoxide-based inhibitors
    M. Mladenovic, K. Ansorg, R. F. Fink, W. Thiel, T. Schirmeister, B. Engels, J. Phys. Chem. B. 112, 11798-11808 (2008)
  • Electronic situation in the oxirane ring - charge density and ELF study on several oxirane derivatives
    S. Grabowsky, T. Pfeuffer, M. Weber, S. Mebs, J. Buschmann, C. Paulmann, T. Schirmeister, P. Luger, Acta Cryst. A64, C567 (2008)
  • Effect of protease inhibitors on exflagellation in Plasmodium falciparum
    I. Rupp, R. Bosse, T. Schirmeister, G. Pradel, Mol. Biochem. Parasitol. 158, 208-212 (2008)
  • Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparumderived from etacrynic acid
    M.-A. Dude, U. Kaeppler, M. Herb, M. Schiller, F. Schulz, B. Vedder, S. Heppner, G. Pradel, J. Gut, P. J. Rosenthal, T. Schirmeister, M. Leippe, and C. Gelhaus, Molecules 14, 19-35 (2009)
  • Novel Peptidomimetics containing a Vinyl Ester Moiety as Highly Potent and Selective Falcipain-2 Inhibitors
    R. Ettari, N. Micale, T. Schirmeister, C. Gelhaus, M. Leippe, E. Nizi, M. E. Di Francesco, S. Grasso, M. Zappalà, J. Med. Chem. 52, 2157-2160, (2009)
  • Insight into the reactivity of biologically active molecules from ground-state electron densities
    S. Grabowsky, T. Pfeuffer, W. Morgenroth, C. Paulmann, T. Schirmeister, P. Luger, Research Highlight, Hasylab (2009)
  • Rational design of improved aziridine-based inhibitors of cysteine proteases
    V. Buback, M. Mladenovic, B. Engels, and T. Schirmeister, J. Phys. Chem. B 113, 5282-5289 (2009)
  • Transcriptome and functional analysis of the eukaryotic-type ser/thr kinase PknB in Staphylococcus aureus
    S. Donat, K. Streker, T. Schirmeister, S. Rakette, T. Stehle, M. Liebeke, M. Lalk, K. Ohlsen, J. Bacteriol. 191, 4056-4069 (2009)
  • Origin of the reactivity differences of substituted aziridines: CN vs. CC bond breakages
    Paasche, M. Arnone, R. F. Fink, T. Schirmeister, B. Engels, J. Org. Chem. 74, 5244-5249 (2009)
  • On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences
    U. Machon, C. Büchold, M. Stempka, T. Schirmeister*, C. Gelhaus, M. Leippe, J. Gut, P. J. Rosenthal, C. Kisker, M. Leyh, C. Schmuck*, J. Med. Chem. 52, 5662-5672 (2009)
  • Novel 2H-isoquinoline-3-ones as antiplasmodial falcipain-2 inhibitors
    N. Micale, R. Ettari, T. Schirmeister, A. Evers, C. Gelhaus, M. Leippe, M. Zappala, S. Grasso, Bioorg. Med. Chem. 17, 6505-6511 (2009)
  • Neue Angriffspunkte in der Infektionstherapie: Ein erfolgreiches Konzept auch für andere Infektionskrankheiten: Proteasen als Zielstrukturen für Antiinfektiva
    T. Schirmeister, A. Welker, Pharm. i. u. Z. 38 (6), 564-574 (2009)

Publikationen 2010 - 2013
  • Inducible Apobec3G-Vif double stable cell line as a high-throughput screening platform to identify antiviral compounds
    B. Nowotny, T. Schirmeister, T. Schneider, G. Pradel, A. Rethwilm, M. Kirschner, Antimicrob. Agents Chemother. 54, 78-87 (2010)
    doi: 10.1128/AAC.00775-09
  • Enzyme kinetics and hit validation in fluorometric protease assays
    S. Ludewig, M. Kossner, M. Schiller, K. Baumann, T. Schirmeister, Curr. Top. Med. Chem. 10, 368-382 (2010)
    doi: 10.2174/156802610790725498
  • Michael-acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids
    A. Breuning, B. Degel, F. Schulz, C. Büchold, M. Stempka, U. Machon, S. Heppner, C. Gelhaus, M. Leippe, M. Leyh, C. Kisker, J. Rath, A. Stich, J. Gut, P. J. Rosenthal, C. Schmuck, T. Schirmeister, J. Med. Chem. 53, 1951-1963 (2010)
    doi: 10.1021/jm900946n
  • Mechanistic study of the reaction of thiol-containing enzymes with alpha,beta-unsaturated carbonyl substrates by computation and chemoassays
    A. Paasche, M. Schiller, T. Schirmeister, B. Engels, ChemMedChem 5, 869-880 (2010)
    doi: 10.1002/cmdc.201000020
  • Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain
    R. Ettari, M. Zappalà, N. Micale, T. Schirmeister, C. Gelhaus, M. Leippe, A. Evers, S. Grasso, Eur. J. Med. Chem. 45, 3228-3233 (2010)
    doi: 10.1016/j.ejmech.2010.04.003
  • Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors
    F. Bova, R. Ettari, N. Micale, C. Carnovale, T. Schirmeister, C. Gelhaus, M. Leippe, S. Grasso, M. Zappala, Bioorg. Med. Chem. 18, 4928-4938 (2010)
    doi: 10.1016/j.bmc.2010.06.010
  • Allicin and derivates are cysteine protease inhibitors with antiparasitic activity
    T. Waag, C. Gelhaus, J. Rath, A. Stich, M. Leippe, T. Schirmeister, Bioorg. Med. Chem. Lett. 20, 5541-5543 (2010)
    doi: 10.1016/j.bmcl.2010.07.062
  • Aziridine-2,3-Dicarboxylate-Based Cysteine Cathepsin Inhibitors Induce Cell Death in Leishmania major Associated with Accumulation of Debris in Autophagy-Related Lysosome-Like Vacuoles
    U. Schurigt, C. Schad, C. Glowa, U. Baum, K. Thomale, J. K. Schnitzer, M. Schultheis, N. Schaschke, T. Schirmeister, H. Moll, Antimicrob Agents Chemother. 54, 5028-5041 (2010)
    doi: 10.1128/AAC.00327-10
  • Anti-protease and immunomodulatory activities of bacteria associated with Caribbean sponges
    P. Tabares, S. M. Pimentel-Elardo, S. Zea, T. Schirmeister, T. Hünig, U. Hentschel, Marine Biotechnol. 13, 883-892 2011
    doi: 10.1007/s10126-010-9349-0
  • New cis-configured aziridine-2-carboxylates as aspartic acid protease inhibitors
    C. Büchold, Y. Hemberger, C. Heindl, A. Welker, B. Degel, T. Pfeuffer, P. Staib, S. Schneider, P. J. Rosenthal, J. Gut, C. Sotriffer, J. Morschhäuser, G. Bringmann, T. Schirmeister, ChemMedChem 6, 141-152 (2011)
    doi: 10.1002/cmdc.201000370
  • Potent and selective inhibition of cysteine proteases from Plasmodium falciparum and Trypanosoma brucei
    V. Ehmke, C. Heindl, M. Rottman, C. Freymond, W. B. Schweizer, R. Brun, A. Stich, T. Schirmeister, F. Diederich, ChemMedChem 6, 273-278 (2011)
    doi: 10.1002/cmdc.201000449
  • Effect of electron-withdrawing substituents on the epoxide ring: an experimental and theoretical electron density analysis of a series of epoxide derivatives
    S. Grabowsky, T. Schirmeister, C. Paulmann, T. Pfeuffer, and P. Luger, J. Org. Chem. 76, 1305-1318 (2011)
    doi: 10.1021/jo102125n
  • Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitor
    R. Ettari, M. Zappala, N. Micale, S. Giofre, T. Schirmeister, S. Grasso, Eur. J. Med. Chem.46, 2058-2065 (2011)
    doi: 10.1016/j.ejmech.2011.02.058
  • Development of novel peptidometics containing a vinyl sulfone moiety as proteasome inhibitors
    R. Ettari, C. Bonaccorso, N. Micale, C. Heindl, T. Schirmeister, M. L. Calabro, S. Grasso, M. Zappala, ChemMedChem 6, 1228-1237 (2011)
    doi: 10.1002/cmdc.201100093
  • Development of antitrypanosomal and antiplasmodial nonpeptidic cysteine protease inhibitors based on N-protected guanidino-furan and -pyrrole building blocks
    S. Langolf, U. Machon, W. Sicking, T. Schirmeister, C. Büchold, C. Gelhaus, P.J. Rosenthal, C. Schmuck, ChemMedChem 6, 1581-1586 (2011)
    doi: 10.1002/cmdc.201100189
  • Peptidomimetic nitriles as selective inhibitors for the malarial cysteine protease falcipain-2
    V. Ehmke, F. Kilchmann, C. Heindl, J. Huang, K. Cui, T. Schirmeister, F. Diederich, MedChemComm, 800-804 (2011)
    doi: 10.1039/c1md00115a
  • Challenging problems in charge density determination: polar bonds and influence of the environment
    B. Engels, T. C. Schmidt, C. Gatti, T. Schirmeister, R. F. Fink, in Structure and Bonding, Springer-Verlag, Berlin Heidelberg, Ed.: D. Stalke, 1-51 (2011)
    doi: 10.1007/430_2010_36
  • Quantitative detection of C-deuterated drugs by CARS microscopy and Raman microspectroscopy
    G. Bergner, C. R. Albert, M. Schiller, G. Bringmann, T. Schirmeister, B. Dietzek, S. Niebling, S. Schlücker, J. Popp, Analyst 136, 3686-3693 (2011)
    doi: 10.1039/C0AN00956C
  • Reactivity differences between a,ß-unsaturated carbonyls and hydrazones investigated by experimental and theoretical electron density and electron localizability analyses
    S. Grabowsky, M. Weber, D. Jayatilaka, Y-S. Chen, M. Grabowski, R. Brehme, M. Hesse, T. Schirmeister, P. Luger, J. Phys. Chem. A 115, 12715-12732 (2011)
    doi: 10.1021/jp203677c
  • Selected gold compounds cause pronounced inhibition of falcipain 2 and effectively block P. falciparum growth in vitro
    N. Micale, M. A. Cinellu, L. Maiore, A. R. Sannella, C. Severini, T. Schirmeister, C. Gabbiani, L. Messori, J. Inorg. Biochem. 105, 1576-1579 (2011)
  • New Tetromycin derivatives with anti-trypanosomal and protease inhibitory activities
    S. M. Pimentel-Elardo, V. Buback, T. A. Gulder, T. S. Bugni, J. Reppart, G. Bringmann, C. M. Ireland, T. Schirmeister, U. Hentschel, Marine Drugs 9, 1682-1697 (2011)
    doi: 10.3390/md9101682
  • Identification of the protease inhibitor miraziridine A in the Red Sea sponge Theonella swinhoie
    P. Tabares, B. Degel, N. Schaschke, U. Hentschel, T. Schirmeister, Pharmacogn. Res. 4, 63-66 (2012)
  • Tuning and predicting biological affinity: Aryl-nitriles as cysteine protease inhibitors
    V. Ehmke, J. E. Quinsaat, P. Rivera-Fuentes, C. Heindl, T. Schirmeister, F. Diederich, Org. Biomol. Chem. 10, 5764-68 (2012)
  • The Signifcance of Ionic Bonding in Sulfur Dioxide-Bond Orders from X-ray Diffraction Data
    S. Grabowsky, P. Luger, J. Buschmann, R. Steudel, T. Schneider, T. Schirmeister, A. N. Sobolev, D. Jayatilakaa, Angew. Chem. Int. Ed. 51, 6776-6779 (2012)
  • Synthesis and molecular modeling studies of derivatives of a highly potent peptidomimetic vinyl ester as falcipain-2 inhibitors
    R. Ettari, N. Micale, G. Grazioso, F. Bova, T. Schirmeister, S. Grasso, M. Zappalà, ChemMedChem 7, 1594-1600 (2012)
    doi: 10.1002/cmdc.201200274
  • Antioxidant and anti-protease activities of diazepinomicin from sponge-associated Micromonospora strain RV115
    U. R. Abdelmohsen, M. Szensny, E. M. Othman, T. Schirmeister, S. Grond, H. Stopper, U. Hentschel, Marine Drugs 10, 2208-2221 (2012)
  • Microwave hydrogenations: Large-size, high pressure microwave reactor.
    E. Heller, A. Gutmann, G. Hiltensperger, W. Lautenschläger, M. J. Lohse, C. Schad, T. Schirmeister, F. Seufert, D. P. Zlotos, U. Holzgrabe, G.I.T. Laboratory Journal 1-2, 32-33 (2013)
  • Optimization studies of the triazine nitrile lead series as rhodesain inhibitors: structure–activity relationships, bioisosteric imidazopyridine nitriles, and X-ray crystal structure analysis with human cathepsin L.
    V. Ehmke, E. Winkler, D. W. Banner, W. Haap, W. B. Schweizer, M. Rottmann, M. Kaiser, C. Freymond, R. Brun, T. Schirmeister, F. Diederich, ChemMedChem (2013) accepted

 

  • Benchmark study for the cysteine-histidine proton transfer reaction in a protein environment: Gas phase, COSMO, QM/MM approaches.
  • A. Paasche, T. Schirmeister, B. Engels, J. Chem. Theory Comput., 2013, 9, 1765-1777

 

  • Development of peptidomimetic boronates as proteasome inhibitors. N. Micale, R. Ettari, A. Lavecchia, C. Di Giovanni, K. Scarbaci, V. Troiano, S. Grasso, E. Novellino, T. Schirmeister, M. Zappalà, Eur. J. Med. Chem., 2013, 64, 23-34

 

  • Can experimental electron-density studies be used as a tool to predict biologically relevant properties of low-molecular weight enzyme ligands? S. Grabowsky, D. Jayatilaka, R. Fink, T. Schirmeister, B. Engels, Z. Anorg. Allg. Chem. 2013, 639, 1905-1921

 

  • Development of novel inhibitors of rhodesain with a 3-bromo-isoxazoline warhead. R. Ettari, L. Tamborini, I. C. Angelo, S. Grasso, T. Schirmeister, L. Lo Presti, C. De Micheli, A. Pinto, P. Conti, ChemMedChem, 2013, 8, 2070-2076

 

 

 

Publikationen 2014 - 2015

 

  • Identification of a new series of amides as non-covalent proteasome inhibitors K. Scarbaci, V. Troiano, N. Micale, R. Ettari,* L. Tamborini, C. Di Giovanni, C. Cerchia, S. Grasso, E. Novellino, T. Schirmeister, A. Lavecchia, M. Zappalà, Eur. J. Med. Chem. 2014,76, 1-9.

 

  • Identification of plakortide E from the Caribbean sponge Plakortis halichondroides as trypanocidal protease inhibitor using bioactivity-guided fractionation. S. Oli, U. R. Abdelmohsen, U. Hentschel, T. Schirmeister, Marine Drugs 2014, 12, 2614-2622.

 

  • Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors; V. Troiano, K. Scarbaci, R. Ettari, N. Micale, C. Cerchia, A. Pinto, T. Schirmeister, E. Novellino, S. Grasso, A. Lavecchia, M. Zappala, Eur. J. Med. Chem. 2014, 83, 1-14.
  • Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold, as antiprotozoan agents
    R. Ettari, A. Pinto, L. Tamborini, I. C. l Angelo, S. Grasso, M. Zappalà, N. Capodicasa, L. Yzeiraj, E. Gruber, M. N. Aminake, G. Pradel, T. Schirmeister, P. Conti, C. De Micheli, ChemMedChem 2014, 9, 1817-1825. doi:10.1002/cmdc.201402079
  • Development of novel selective peptidomimetics, containing a boronic acid moiety, targeting the 20S proteasome as anticancer agents K. Scarbaci, V. Troiano, R. Ettari, A. Pinto, N. Micale, C. Di Giovanni, C. Cerchia, E. Novellino, A. Lavecchia, T. Schirmeister, M. Zappalà, S. Grasso, Silvana, ChemMedChem 2014, 9, 1801-1816.

 

  • Selected Cytotoxic Gold Compounds cause remarkable Inhibition of 20S proteasome catalytic activities N. Micale, T. Schirmeister, R. Ettari, M. A. Cinellu, L. Maiore, M. Serratrice, C. Gabbiani, L. Massai, L. Messori, J. Inorg. Biochem. 2014, 141, 79-82
  • Cathepsin B in antigen-presenting cells control mediators of the TH1 immune response during Leishmania major infection,
    I. J. Gonzalez-Leal, B. Röger, A. Schwarz, T. Schirmeister, T. Reinheckel, M. B. Lutz, H. Moll, PLOS Negl. Trop. Dis. 2014, 8, e3194
  • Evidence for substrate binding-induced zwitterion formation in the catalytic Cys-His dyad of the SARS-CoV main protease,
    A. Paasche, A. Zipper, S. Schäfer, J. Ziebuhr, T. Schirmeister, B. Engels, Biochemistry 2014, 53, 5930-5946
  • Biochemistry and medicinal chemistry of the Dengue virus protease,
    C. Nitsche, S. Holloway, T. Schirmeister, C. D. Klein, Chem. Rev., 2014, 114, 11348–11381
  • Protocol for a rational design of covalently interacting inhibitors
    T. C. Schmidt, A. Welker, M. Rieger, P. K. Sahu, C. Sotriffer, T. Schirmeister, B. Engels, ChemPhysChem 2014,15, 3226-3235.
  • Leishmanicidal compounds as inhibitors of cathepsin L
    L. R. F. de Sousa, L.Nebo, J. B. Fernandes, M. F. das, G. F. da Silva, W. Kiefer, T. Schirmeister, P. C. Vieira, Planta Medica 2014, Vol. 156, 42-48
  • Electrostatic complementarity in pseudoreceptor modeling based on drug molecule crystal structures: the case of loxistatin acid (E64c)
    M. Shi, A. Sobolev, T. Schirmeister, B. Engels, T. Schmidt, P. Luger, S. Mebs, B. Dittrich, Y.-S. Chen, J. Bak, D. Jayatilaka, C. S. Bond, M. J. Turner, S. G. Stewart, M. A. Spackman, S. Grabowsky, New J. Chem., 2015, 39, 1628-1633
  • Anti-trypanosomal activity and structural chemical properties of selected compound classes
    A. Ponte-Sucre, H. Bruhn, T. Schirmeister, A. Cecil, C. R. Albert, C. Buechold, M. Tischer, S. Schlesinger, T. Goebel, A. Fuß, D. Mathein, B. Merget, C. Sotriffer, A. Stich, G. Krohne, M. Engstler, G. Bringmann, U. Holzgrabe, Parasitol Res (2015) 114:501–512
  • Novel Dengue virus NS2B/NS3 protease inhibitors
    H. Wu, S. Bock, M. Snitko, T. Berger, T. Weidner, S. Holloway, M. Kanitz, W. E. Diederich, H. Steuber, C. Walter, D. Hofmann, B. Weißbrich, R. Spannaus, E. Acosta, R. Bartenschlager, B. Engels, T. Schirmeister, J. Bodem, Antimicrob. Agents Chemother. 2015, 59, 1100-1109.
  • Fly versus Man: Evolutionary impairment of nucleolar targeting affects the degradome of Drosophila’s Taspase1
    D. Wünsch, A. Hahlbrock, C. Heiselmayer, S. Bäcker, P. Heun, D. Gößwein, W. Stöcker, T. Schirmeister, G. Schneider, O. H. Krämer, S. K. Knauer, R. H. Stauber, FASEB J. 2015, 29, 1-13
  • .
  • Flavonoids as noncompetitive inhibitors of Dengue virus NS3/NS2B protease: inhibition kinetics and docking studies
    L. R. Freitas de Sousa, H. Wu, L. Nebo, J. B. Fernandes, M. F. das Graças Fernandes da Silva, W. Kiefer, M. Kanitz, J. Bodem, W. E. Diederich, T. Schirmeister, P. C. Vieira, Bioorg. Med. Chem. 2015, 23, 466-470
  • Electrostatic complementarity in pseudoreceptor modeling based on drug molecule crystal structures: the case of loxistatin acid (E64c)
    M. Shi, A. Sobolev, T. Schirmeister, B. Engels, T. Schmidt, P. Luger, S. Mebs, B. Dittrich, Y.-S. Chen, J. Bak, D. Jayatilaka, C. S. Bond, M. J. Turner, S. G. Stewart, M. A. Spackman, S. Grabowsky, New J. Chem. 2015, 39, 1628-1633.
  • Natural products as inhibitors of recombinant cysteine protease L of Leishmania mexicana
    L. R. F. de Sousa, H. Wu, L. Nebo, J. B. Fernandes, M. F. das G. F. da Silva, W. Kiefer, T. Schirmeister, P. C. Vieira, Exp. Parasitol. 2015, 156, 42-48.
  • Vinyl sulfone building blocks in covalently reversible reactions with thiols
    T. H. Schneider, M. Rieger, K. Ansorg, A. N. Sobolev, T. Schirmeister, B. Engels, S. Grabowsky, New J. Chem. 2015, 39, 5841-5853.
  • Synthesis of C3/C1-substituted tetrahydroisoquinolines
    M. Mihoubi, N. Micale, A. Scala, R. M. Jarraya, A. Bouaziz, T. Schirmeister, F. Risitano, A. Piperno, G. Grassi, Molecules 2015, 20, 14902-14914.
  • Dipeptidyl enoates as potent rhodesain inhibitors that display a dual mode of action
    S. Royo, S. Rodriguez, T. Schirmeister, J. Kesselring, M. Kaiser, F. V. Gonzalez, ChemMedChem 2015, 10, 1481-1487.
  • Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation
    R. Ettari, S. Previti, A. Pinto, L. Tamborini, M. Zappala, L. Marinelli, E. Novellino, T. Schirmeister, S. Grasso, C. de Micheli, P. Conti, Bioorg. Med. Chem. 2015, 23, 7053-7060.
  • Hyaluronic acid-pentamidine bioconjugate as macrophage mediated drug targeting delivery system for the treatment of Leishmaniasis
    N. Micale, A. Piperno, N. Mahfoudh, U. Schurigt, M. Schultheis, G. P. Mineo, T. Schirmeister, A. Scala, G. Grassi, RCS Advances 2015, 5, 95545-95550.
  • From basic chemistry to new drugs.
    T. Schirmeister, Pan European Networks: Science & Technology 2015, 14, 144-145.
  • Taspase 1: A ,misunderstood' protease with translational cancer relevance
    D. Wünsch, A. Hahlbrock, S. Jung, T. Schirmeister, J. van den Boom, O. Schilling, S. K. Knauer, R. Stauber, Oncogene 2015, 1-14. doi:10.1038/onc.2015.436
  • Publikationen 2016 bis 2018
  • Development of a new antileishmanial aziridine-2,3-dicarboxylate-based inhibitor with high selectivity for parasite cysteine proteases
    C. Schad, U. Baum, B. Frank, U. Dietzel, C. Gomes, A. Ponte-Sucre, H. Moll, U. Schurigt*, T. Schirmeister,* Antimicrobial. Agents Chemother. 2016, 60, 797-805.
  • Synthesis and biological evaluation of novel peptidomimetics as rhodesain inhibitors
    R. Ettari, S. Previti, S. Cosconati, J. Kesselring, T. Schirmeister, S. Grasso, M. Zappala, J. Enz. Inh. Med. Chem. 2016, 31, 1184-1191, published online Nov 2015; doi:10.3109/14756366.2015.1108972.
  • Targeting the Leishmania mexicana cysteine protease CPB2.8ΔCTE by decorated fused benzo[b]thiophene scaffold A. Scala, N. Micale, A. Piperno, A. Rescifina, J. Kesselring, T. Schirmeister, G. Grassi, RCS Advances 2016, 6, 30628-30635
  • Fluorine Scan of Inhibitors of the Cysteine Protease Human Cathepsin L: Dipolar and Quadrupolar Effects in the π-Stacking of Fluorinated Phenyl Rings on Peptide Amide Bonds
    M. Giroud, M. Harder, B. Kuhn, W. Haap, N. Trapp, W. B. Schweizer, T. Schirmeister, F. Diederich, ChemMedChem 2016, 11, 1042-1047
  • Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual screening
    C. Di Giovanni, R. Ettari, S. Sarno, R. Rotondo, A. Bitto, F. Squadrito, D. Altavilla, T. Schirmeister, E. Novellino, S. Grasso, M. Zappalà, A. Lavecchia, Eur. J. Med. Chem. 2016, 121, 578-591.
  • Bistacrine derivatives as new potent antimalarials
    I. Schmidt, G. Pradel, L. Sologub, T. Schirmeister, A. Kucharsky, U. Holzgrabe, Bioorg. Med. Chem. 2016, 24, 3636-3642.
  • Development of novel 1,4-benzodiazepine-based Michael acceptors as antitrypanosomal agents
    R. Ettari, S. Previti, S. Cosconati, S. Maiorana, T. Schirmeister, S. Grasso, M. Zappala, Bioorg. Med. Chem. Lett. 2016, 26, 3453-3456.
  • Quantum chemical-based protocol for the rational design of covalent inhibitors
    T. Schirmeister*, J. Kesselring, S. Jung, T. Schneider, A. Weickert, J. Becker, W. Lee, D. Bamberger, P. Wich, U. Distler, S. Tenzer, P. Johé, U. A. Hellmich, B. Engels*, J. Am. Chem. Soc. 2016, 138, 8332-8335.
  • Dipeptidyl nitroalkenes as potent reversible inhibitors of cysteine proteases rhodesain and cruzain
    A. Latorre, T. Schirmeister, J. Kesselring, S. Jung, P. Johé, U. A. Hellmich, A. Heilos, B. Engels, R. L. Krauth-Siegel, N. Dirdjaja, L. Bou-Iserte, S. Rodriguez, F. V. Gonzalez, ACS Med. Chem. Lett. ACS Med. Chem. Lett. 2016, 7, 1073-1076; DOI: 10.1021/acsmedchemlett.6b00276,
  • Evaluation of dipeptide nitriles as inhibitors of rhodesain, a major cysteine protease of Trypanosoma bruceiT. Schirmeister*, J. Schmitz, S. Jung, T. Schmenger, R. L. Krauth-Siegel, M. Gütschow, Bioorg. Med. Chem. Lett. 2016,27, 45-50.
  • Approaching an experimental electron-density model of the biologically active trans-epoxysuccinyl amide group – substituent effects vs. crystal packing
    M. W. Shi, S. G. Stewart, A. N. Sobolev, B. Dittrich, T. Schirmeister, P. Luger, M. Hesse, Y.-S. Chen, P. R. Spackman, M. A. Spackman, S. Grabowsky, J. Phys. Org. Chem. 2017, e3683. DOI: 10.1002/poc.3683
  • Inhibition of the cysteine protease human cathepsin L by triazine nitriles: Amide-heteroarene p-stacking interactions and chalcogen bonding in the S3 pocket
    M. Giroud, J. Ivkovic, M. Martignoni, M. Fleuti, N. Trapp, W. Haap, A. Kuglstatter, J. Benz, B. Kuhn*, T. Schirmeister*, F. Diederich*, ChemMedChem 2017, 12, 257-270
  • Prospective evaluation of free energy calculations for the prioritization of cathepsin L inhibitors
    B. Kuhn, M. Tichý, L. Wang, S. Robinson, R. Martin, A. Kuglstatter, J. Benz, M. Giroud, T. Schirmeister, R. Abel, F. Diederich, J. Hert, J. Med. Chem. 2017, 60, 2485-2497.
  • Cytotoxicity of endoperoxides from the Caribbean sponge Plakortis halichondrioides towards sensitive and multidrug-resistant leukemia cells: acids vs. esters activity evaluation
    T. Schirmeister*, S. Oli, H. Wu, G. Della Sala, V. Costantino, E.-J. Seo, T. Efferth, Marine Drugs 2017, 15, 63; doi:10.3390/md15030063.
  • Gold compounds as cysteine protease inhibitors: Perspectives for pharmaceutical application as antiparasitic agents. L. Massai, N. Micale, T. Schirmeister, L. Maes, D. Fregona, M. A. Cinellu, L. Messori, C. Gabbiani, Biometals 2017, 30, 313-320
  • Bistacrines as potential antitrypanosomal agents I. Schmidt, S. Göllner, A. Fuß, A. Stich, A. Kucharsky, T. Schirmeister, E. Katzowitsch, H. Bruhn, A. Miliu, R. L. Krauth-Siegel, U. Holzgrabe, Bioorg. Med. Chem. 2017, 25, 4526-4531.
  • Development of novel peptide-based Michael acceptors targeting rhodesain and falcipain-2 for the treatment of neglected tropical diseases (NTDs), S. Previti, R. Ettari, S. Cosconati, G. Amendola, K. Chouchene, A. Wagner, U. A. Hellmich, K. Ulrich, R. L. Krauth-Siegel, P. R. Wich, I. Schmid, T. Schirmeister, J. Gut, P. J. Rosenthal, S. Grasso, M. Zappala, J. Med. Chem. 2017, 60, 6911-6923.
  • Ensemble-based ADME-tox profiling and virtual screening for the discovery of new inhibitors of the Leishmania mexicana cysteine protease CPB2.8ΔCTE. A. Scala, A. Rescifina, N. Micale, A. Piperno, T. Schirmeister, L. Maes, G. Grassi, Chem. Biol. Drug Des. 2018, 91, 597-604.
  • Structure-function evaluation of imidazopyridine derivatives specific for δ-subunit containing γ-aminobutyric acid type A (GABAA) receptorsK. Yakoub, S. Jung, C. Sattler, H. Damerow, J. Weber, A. Kretzschmann, A. S. Cankaya, M. Piel, F. Rösch, A. S. Haugaard, B. Frølund, T. Schirmeister,* H. Lüddens,* J. Med. Chem. 2018, 61, 1951-1968.
  • 2H-1,2,3-Triazole-based dipeptidyl nitriles: potent, selective and trypanocidal rhodesain inhibitors by structure-based design, M. Giroud, B. Kuhn, S. Saint-Auret, C. Kuratli, R. E. Martin, F. Schuler, F. Diederich, M. Kaiser, R. Brun, T. Schirmeister,* W. Haap*, J. Med. Chem. 2018, DOI: 10.1021/acs.jmedchem.7b01870
  • Repurposing a human cathepsin L inhibitors library: Identification of macrocyclic lactams as potent rhodesain and Trypanosoma brucei inhibitors, M. Giroud, U. Dietzel, L. Anselm, D. Banner, J.-B. Blanc, D. Gaufreteau, H. Liu, A. Stich, B. Kuhn, F. Schuler, M. Kaiser, R. Brun, T. Schirmeister, C. Kisker, F. Diederich, W. Haap, J. Med. Chem. 2018, DOI: 10.1021/acs.jmedchem.7b01869
  • Discovery of benzimidazole-based L. mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis. L. de Luca, S. Ferro, M. R. Buemi, A. M. Monforte, R. Gitto, T. Schirmeister, L. Maes, A. Rescifina, N. Micale, Chem. Biol. Drug Des. 2018 accepted

 


Fach- und Lehrbücher
  • Chemie für Mediziner
    Koautoren: Prof. Dr. C. Schmuck, Prof. Dr. B. Engels, PD Dr. R. Fink
    Pearson-Verlag (2008)
  • Arzneibuch-Kommentar, Wissenschaftliche Erläuterungen zum Arzneibuch, ab 2013 (45. Aktualisierung), Herausgeber (F. Bracher, P. Heisig, P. Langguth, E. Mutschler, G. Rücker, T. Schirmeister, G. Scriba, E. Stahl-Biskup, R. Troschütz) und Autor, WVG Stuttgart
  • Zum WS 2014/2015 erscheint neu:
    Lehrbuch der Organischen Chemie, Beyer/Walter
    ; C. Schmuck, T. Schirmeister, P. Wich, S. Hirzel Verlag, Stuttgart
  • Arzneibuch-Kommentar
    Wissenschaftliche Erläuterungen zum Arzneibuch, Fortsetzungswerk
    Im Herausgeber-Team, Autor
    WVG Stuttgart

Patente
  • N-geschützte Guanidin-substituierte Furane, Thiophene und Pyrrole als Cystein-Protease-Inhibitoren
    C. Schmuck, K. Baumann, S. Rohrer, S. Langolf, U. Machon, T. Schirmeister
    Julius-Maximilians Universität Würzburg, 10 2008 049 767.3 (2008) angemeldet

 

 

Vorträge

  • Prodrugs: Bewährtes und neue Konzepte
    T. Schirmeister, Habilitationsvortrag, Fakultät für Chemie und Pharmazie, Albert-Ludwigs-Universität, Freiburg (1999)
  • Neue peptidische Cystein-Protease-Inhibitoren: Die Bedeutung von Aziridindicarbonsäure-Bausteinen
    T. Schirmeister, Pharmazeutisches Institut der Rheinischen Friedrichs-Wilhelm-Universität, Bonn (1999)
  • Neue peptidische Cystein-Protease-Inhibitoren: Die Bedeutung von Aziridindicarbonsäure-Bausteinen
    T. Schirmeister, Institut für Pharmazie und Lebensmittelchemie der Bayerischen Julius-Maximilians-Universität, Würzburg (1999)
  • Peptidische Cystein-Protease-Inhibitoren: Kleine Ringe als elektrophile Fallen
    T. Schirmeister, Organisches Kolloquium, Institut für Organische Chemie, Eberhard Karls Universität, Tübingen (2000)
  • Alzheimer: Puzzle aus 1000 Teilen
    T. Schirmeister, DPhG Landesgruppe Bayern, Würzburg (2000)
  • Entwicklung von Cystein-Protease-Inhibitoren - Kleine Ringe als elektrophile Fallen
    T. Schirmeister, Institut für Pharmazie und LM-Chemie, Friedrich-Alexander-Universität, Erlangen-Nürnberg (2001)
  • Cystein-Proteasen als neue Targets für Arzneistoffe - Dreiring-Heterocyclen als Bausteine für Inhibitoren
    T. Schirmeister, Institut für Pharmazie und LM-Chemie, Westfälische Wilhelms-Universität, Münster (2003)
  • Identification of cysteine proteases of intraerythrocytic life stages of Plasmodium falciparum by a biotinylated small-molecule probe
    T. Schirmeister, C. Gelhaus, R. Vicik, M. Leippe, 3rd General Meeting of the IPS (International Proteolysis Society) associated with the ICPI (International Conference on Protease Inhibitors), Nagoya, Japan. (short oral presentation) (2003)
  • Alzheimer - Was gibt es Neues?
    T. Schirmeister, DPhG-Jahrestagung, Würzburg (2003)
  • Proteasen aus Mikroorganismen - Neue Targets für Antiinfektiva
    T. Schirmeister, Pharmazeutisches Institut, Rheinische Friedrichs-Wilhelm-Universität, Bonn (2004)
  • Faszination kleine Ringe: Synthese und Eigenschaften von ß-Lactamen und ß-Sultamen
    T. Schirmeister, Vortrag anlässlich der Verabschiedung von Prof. Dr. H.-H. Otto, Greifswald (2004)
  • Inhibitoren mikrobieller Cystein-Proteasen - Neue Antiinfektiva?
    T. Schirmeister, Institut für Pharmazie, Philipps-Universität, Marburg (2005)
  • Proteases of microorganisms and viruses as new targets for antiifectives
    T. Schirmeister, Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco (2005)
  • Proteases of microorganisms and viruses as new targets for antiifectives
    T. Schirmeister, San Francisco General Hospital, Department of Medicine, Division of Infectious Diseases, University of California, San Francisco (2005)
  • Proteasen aus Mikroorganismen - Neue Targets für Antiinfektiva
    T. Schirmeister, Institut für Zoophysiologie, Christian-Albrechts-Universität, Kiel (2005)
  • Inhibitors of SARS coronavirus main protease
    T. Schirmeister, Summer School "Medicinal Chemistry", Universität Regensburg (2006)
  • Synthesis, crystallization and electron density determination of electrophilic building blocks as model compounds for protease inhibitors
    T. Pfeuffer, L. Checinska, M. Weber, S. Grabowsky, P. Luger, T. Schirmeister, First Report Colloquium DFG Priority Program SPP 1178, Hamburg (2006)
  • Correlation of electron density derived molecular properties with biological activity: a new tool in rational ligand design
    T. Schirmeister, 2. Proposal Colloquium of the SPP 1178, Kloster Banz (2007)
  • From aspartic acid protease inhibitors to new cysteine protease inhibitors
    T. Schirmeister, Dipartimento Farmaco-Chimico, Universität Messina, Italien (2007)
  • Von Inhibitoren der SAPs aus Candida albicans zu neuen Falcipain-Inhibitoren
    T. Schirmeister, Institut für Pharmazeutische Wissenschaften, Universität Freiburg (2008)
  • Electron Density determination and quantum chemical computations of protease inhibitor model compounds: prediction of reactivity
    R. Fink, T. Schirmeister, S. Grabowsky, M. Anone, T. Pfeuffer, W. Morgenroth, C. Paulmann, P. Luger, B. Engels, 5th European Charge Density Meeting and DFG 1178 Annual Meeting, Como (2008)
  • Correlation of electron density derived molecular properties with biological activity: a new tool in rational ligand design
    T. Schirmeister, 3. Proposal Colloquium of the SPP 1178, Kloster Banz (2009)
  • From inhibitors of the secreted aspartic acid proteases of C. albicans to new falcipain inhibitors
    T. Schirmeister, Annual Meeting of SBBq (Sociedade Brasileira de Bioquimica et Biologia Molecular), Aguas de Lindoia, Brasilien (Mai 2009)
  • How can computational chemistry support development of cysteine protease inhibitors?
    T. Schirmeister, Chemistry Institute of the University of Sao Paulo, Brasilien (Mai 2009)
  • From inhibitors of the secreted aspartic acid proteases of C. albicans to new falcipain inhibitors
    T. Schirmeister, Dept. Quimica Inorganica i Organica Universitat Jaume I Avda. Sos Baynat, Spanien (Mai 2009)
  • Von Inhibitoren der SAPs aus Candida albicans zu neuen Falcipain-Inhibitoren
    T. Schirmeister, Institut für Pharmazie, Universität Mainz (Juli 2009)
  • Leishmania-Cathepsine als neue Targets für antiparasitäre Wirkstoffe
    T. Schirmeister, DPhG Jahrestagung Jena (Oktober 2009)

Vorträge und Veranstaltungen im Rahmen der Öffentlichkeitsarbeit
  • Protease-Hemmstoffe: Entwicklung und Anwendung
    Marathon-Vorlesung, Würzburg (2003)
  • Apotheker: Pillendreher, Kräuterhexe, Giftmischer? (zusammen mit Prof. U. Holzgrabe)
    Kinder-Universität, Würzburg (2007)
  • Was ist drin und was darf rein? - Ein neuer Blick auf Aspirin und Wein (zusammen mit Prof. C. Sotriffer)
    Tag der Offenen Tür, Fakultät für Chemie und Pharmazie, Würzburg (2009)

Buchbeiträge und Monographien

 

Buchbeiträge

  • Synthesis of peptides with aziridine-2,3-dicarboxylic acid as an amino acid equivalent building block
    T. Schirmeister, Peptide Science - Present and Future 1998, 654-656
  • Challenging problems in charge density determination: polar bonds and influence of the environment
    B. Engels, T. C. Schmidt, C. Gatti, T. Schirmeister, R. F. Fink, 2012, in Structure and Bonding, Springer-Verlag, Berlin Heidelberg, Ed.: D. Stalke, 147, 47-98.
  • HIV-Therapeutika – Grundlagen und Arzneistoffe, Pharmakon 4/2014,
    Gastherausgeberschaft zusammen mit U. Holzgrabe und U. Dietrich
  • HIV-Therapeutika – Klinische Anwendung, Pharmakon 5/2014,
    Gastherausgeberschaft zusammen mit U. Holzgrabe und U. Dietrich

 

  • Kommentare zum Europäischen Arzneibuch
    1. Tramazolin
    2. Trimetazidin
    3. Josamycin
    4. Josamycinpropionat
    5. Azithromycin
    6. Clarithromycin
    7. Rifabutin
    8. Progesteron
    9. Estradiolbenzoat
    10. Hydrocortisonacetat
    11. Sulbactam Natrium
    12. Lymecyclin
    13. Deferoxaminmesilat
    14. Glipizid
    15. 2,4-Dichlorbenzylalkohol
    16. Somatostatin

     

  • Monographien HagerROM
    1. Desloratadin
    2. Levetiracetam
    3. Tadalafil
    4. Vardenafil
    5. Zoledronsäure