• The Bacterial Product Violacein Exerts an Immunostimulatory Effect Via TLR8
    F. A. Venegas, G. Köllisch, K. Mark, W. E. Diederich, A. Kaufmann, S. Bauer, M. Chavarría, J.J. Araya, A.J. García-Piñeres
    Scientific Reports 2019, 9(1), 13661, doi: 10.1038/s41598-019-50038-x.

  • PPARβ/δ recruits NCOR and regulates transcription reinitiation of ANGPTL4
    N. Legrand, C. L. Bretscher, S. Zielke, B. Wilke, M. Daude, B. Fritz, W. E. Diederich, T. Adhikary
    Nucleic Acids Research 2019 Aug 20, doi: 10.1093/nar/gkz685. [Epub ahead of print]

  • Structural basis for catalysis and substrate specificity of a 3C-like cysteine protease from a mosquito mesonivirus
    M. Kanitz, S. Blanck, A. Heine, A. A. Gulyaeva, A. E. Gorbalenya, J. Ziebuhr, W. E. Diederich
    Virology 2019, (533), 21–33

  • Binding-Site Compatible Fragment Growing Applied to the Design of β2-Adrenergic Receptor Ligands.
    F. Chevillard, H. Rimmer, C. Betti, E. Pardon, S. Ballet, N. van Hilten, J. Steyaert, W. E. Diederich, P. Kolb
    Journal of Medicinal Chemistry 2018, 61, 1118−1129.

  • Mitochondrial rescue prevents glutathione peroxidase-dependent ferroptosis.
    A. Jelinek, L. Heyder, M. Daude, M. Plessner, S. Krippner, R. Grosse, W. E. Diederich, C. Culmsee
    Free Radical Biology and Medicine 2018, 117, 45–57.

  • What Are We Missing? The Detergent Triton X-100 Added to Avoid Compound Aggregation Can Affect Assay Results in an Unpredictable Manner
    F. G. R. Ehlert, K. Linde, W.E. Diederich
    ChemMedChem 2017, 12 (17), 1419 – 1423.

  • A Small-Molecule Inhibitor of Bax and Bak Oligomerization Prevents Genotoxic Cell Death and Promotes Neuroprotection
    X. Niu, H. Brahmbhatt, P. Mergenthaler, Z. Zhang, J. Sang, M. Daude, F. G.R. Ehlert, W.E. Diederich, E. Wong, W. Zhu, J. Pogmore, J. P. Nandy, M. Satyanarayana, R. K. Jimmidi, P. Arya, B. Leber, J. Lin, C. Culmsee, J. Yi, D. W. Andrews
    Cell Chemical Biology 2017, 24 (4), 493-506

  • Price for Opening the Transient Specificity Pocket in Human Aldose Reductase upon Ligand Binding: Structural, Thermodynamic, Kinetic, and Computational Analysis
    C. Rechlin, F. Scheer, F. Terwesten, T. Wulsdorf, E. Pol, V. Fridh, P. Toth, W.E. Diederich, A. Heine, G. Klebe
    Chemical Biology 2017 May 19;12 (5), 1397-1415. doi: 10.1021/acschembio.7b00062

  • Design and Synthesis of Highly Active Peroxisome Proliferator-Activated Receptor (PPAR) β/δ Inverse Agonists with Prolonged Cellular Activity
    P. M. Toth, S. Lieber, F. M. Scheer, T. Schumann, Y. Schober, W. A. Nockher, T. Adhikary, S. Müller-Brüsselbach, R. Müller, W.E. Diederich
    ChemMedChem 2016, 11 (5), 488-496.
    Abstract Cover picture

  • Identification of inhibitors of the transmembrane protease FlaK of Methanococcus maripaludis
    I. Coburger, Y. Schaub, D. Roeser, K. Hardes, P. Maeder, N. Klee, T. Steinmetzer, D. Imhof, W. E. Diederich, M.E. Than
    Microbiology Open 2016 Aug, 5 (4), 637-646.

  • One Question, Multiple Answers: Biochemical and Biophysical Screening Methods Retrieve Deviating Fragment Hit Lists
    J. Schiebel, N. Radeva, H. Köster, A. Metz, T. Krotzky, M. Kuhnert, W.E. Diederich, A. Heine, L. Neumann, C. Atmanene, D. Roecklin, V. Vivat-Hannah, J.-P. Renaud, R. Meinecke, N. Schlinck, A. Sitte, F. Popp, M. Zeeb and G. Klebe
    ChemMedChem 2015, 10 (9), 1511-1521.

  • Privileged Structures Meet Human T-Cell Leukemia Virus-1 (HTLV-1): C2-Symmetric 3,4-Disubstituted Pyrrolidines as Nonpeptidic HTLV-1 Protease Inhibitors.
    M. Kuhnert, A. Blum, H. Steuber, W.E. Diederich
    Journal of Medicinal Chemistry 2015, 58 (11), 4845-4850.

  • Deregulation of PPARβ/δ target genes in tumor-associated macrophages by fatty acid ligands in the ovarian cancer microenvironment.
    T. Schumann, T. Adhikary, A. Wortmann, F. Finkernagel, S. Lieber, E. Schnitzer, N. Legrand, Y. Schober, W.A. Nockher, P.M. Toth, W.E. Diederich, A. Nist, T. Stiewe, U. Wagner, S. Reinartz, S. Müller-Brüsselbach, R. Müller
    Oncotarget 2015, 6 (15), 13416-13433.

  • The transcriptional PPARβ/δ network in human macrophages defines a unique agonist-induced activation state.
    T. Adhikary, A. Wortmann, T. Schumann, F. Finkernagel, S. Lieber, K. Roth, P.M. Toth, W.E. Diederich, A. Nist, T. Stiewe, L. Kleinesudeik, S. Reinartz, S. Müller-Brüsselbach, R. Müller.
    Nucleic Acids Research, 2015, 43 (10):5033-5051.

  • Tracing Binding Modes in Hit-to-Lead Optimization: Chameleon-Like Poses of Aspartic Protease Inhibitors.
    M. Kuhnert, H. Köster, R. Bartholomäus, AY. Park, A. Shahim, A. Heine, H. Steuber, G. Klebe, W.E. Diederich
    Angewandte Chemie International Edition, 2015, 54 (9), 2849-2853.

  • Flavonoids as noncompetitive inhibitors of Dengue virus NS2B-NS3 protease: Inhibition kinetics and docking studies.
    L.R. de Sousa, H. Wu, L. Nebo, J.B. Fernandes, M.F. da Silva, W. Kiefer, M. Kanitz, J. Bodem, W.E. Diederich, T. Schirmeister, P.C. Vieira
    Bioorganic & Medicinal Chemistry 2015, 23 (3), 466-470.

  • 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.G. Acosta, R. Bartenschlager, B. Engels, T. Schirmeister, J. Bodem
    Antimicrobial Agents and Chemotherapy 2015, 59 (2), 1100-1109.

  • The Inverse Agonist DG172 Triggers a PPARβ/δ-Independent Myeloid Lineage Shift and Promotes GM-CSF/IL-4-Induced Dendritic Cell Differentiation
    S. Lieber, F. Scheer, F. Finkernagel, W. Meissner, G. Giehl, C. Brendel, W.E. Diederich, S. Müller-Brüsselbach, R. Müller
    Journal of Molecular Pharmacology 2015, 87 (2), 162-173.

  • Structural Basis for HTLV‑1 Protease Inhibition by the HIV‑1 Protease Inhibitor Indinavir
    M. Kuhnert, H. Steuber, and W. E. Diederich
    Journal of Medicinal Chemistry 2014, 57, 6266-6272.

  • Inverse PPARβ/δ agonists suppress oncogenic signaling to the ANGPTL4 gene and inhibit cancer cell invasion
    T. Adhikary, D. T. Brandt, K. Kaddatz, J. Stockert, S. Naruhn, W. Meissner, F. Finkernagel, J. Obert, S. Lieber, M. Scharfe, M. Jarek, P. M. Toth, F. Scheer, W. E. Diederich, S. Reinartz, R. Grosse, S. Müller-Brüsselbach, R. Müller
    Oncogene 2013, 32, 5241–5252.

  • Z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile (DG172): an orally bioavailable PPARβ/δ-selective ligand with inverse agonistic properties
    S. Lieber, F. Scheer, W. Meissner, S. Naruhn, T. Adhikary, S. Müller-Brüsselbach, W. E. Diederich, R. Müller
    Journal of Medicinal Chemistry 2012, 55, 2858-2868.

  • Development of Improved PPARβ/δ Inhibitors
    P. M. Toth, S. Naruhn, V. F. S. Pape, S. M. A. Dörr, G. Klebe, R. Müller, W. E. Diederich
    ChemMedChem 2012, 7, 159-170.

  • High affinity PPARβ/δ-specific ligands with pure antagonistic or inverse agonistic properties
    S. Naruhn, P. M. Toth, T. Adhikary, K. Kaddatz, V. Pape, S. Dörr, G. Klebe, S. Müller-Brüsselbach, W. E. Diederich, R. Müller
    Mol Pharmacol 2011, 80, 828-838

  • Two Solutions for the same Problem: Multiple Binding Modes of Pyrrolidine-based HIV-1 Protease Inhibitors
    A. Blum, J. Böttcher, S. Dörr, A. Heine, G. Klebe, W. E. Diederich
    Journal of Molecular Biology 2011, 410, 745-755.

  • Stability-indicating HPLC assays for the determination of piritramide and droperidol in PCA solution
    S. Selbach, W. E. Diederich, S. Fett, D. Fründ, T. Koch, L. H.J. Eberhart
    Journal of Clinical Pharmacy and Therapeutics 2011, 36(2), 161-165.
  • Fragment-based lead discovery: Screening and Optimising Fragments for Thermolysin Inhibition
    L. Englert, K. Silber, H. Steuber, S. Brass, B. Over, H.-D. Gerber, A. Heine, W. E. Diederich, G. Klebe
    ChemMedChem 2010, 5, 930-940.

  • Pyrrolidine Derivatives as Plasmepsin Inhibitors: Binding Mode Analysis Assisted by Molecular Dynamics Simulations of a Highly Flexible Protein
    T. Luksch, A. Blum, N. Klee, W. E. Diederich, C. A. Sotriffer, G. Klebe
    ChemMedChem 2010, 5, 443-454

  • Achiral Oligoamines as Versatile Tool for the Development of Aspartic Protease Inhibitors
    A. Blum, J. Böttcher, B. Sammet, T. Luksch, A. Heine, G. Klebe, W. E. Diederich
    Bioorganic Medicinal Chemistry 2008, 16, 8574-8586

  • Targeting the Open Flap Conformation of HIV-1 Protease with Pyrrolidine-based Inhibitors
    J. Böttcher, A. Blum, S. Dörr, A. Heine, W. E. Diederich, G. Klebe
    ChemMedChem 2008, 3, 1337-1344

  • Structural and Kinetic Analysis of Pyrrolidine-Based Inhibitors of the Drug-Resistant Ile84Val Mutant of HIV-1 Protease
    J. Böttcher, A. Blum, A. Heine, W. E. Diederich, G. Klebe
    Journal of Molecular Biology 2008, 383 (2), 347-357

  • Computer-aided Design and Synthesis of non-peptidic Plasmepsin II and IV Inhibitors
    T. Luksch, N.-S. Chan, S. Brass, C. A. Sotriffer, G. Klebe, W. E. Diederich
    ChemMedChem 2008, 3, 1323-1336

  • Structure-Guided Design of C2-Symmetric HIV-1 Protease Inhibitors Based on a Pyrrolidine Scaffold
    A. Blum, J. Böttcher, A. Heine, G. Klebe, W. E. Diederich
    Journal of Medicinal Chemistry 2008, 51, 2078-2087

  • KNOBLE: a knowledge-based approach for the design and synthesis of readily accessible small molecule chemical probes to test protein binding
    C. Gerlach, M. Münzel, B. Baum, H.-D. Gerber, T. Craan, W. E. Diederich, Gerhard Klebe
    Angewandte Chemie 2007, 119, 9265-9269
    Angewandte Chemie International Edition 2007, 46, 9105-9109

  • Synthesis of 2,3,4,7-tetrahydro-1H-azepines as privileged ligand scaffolds for the design of aspartic
    protease inhibitors via a ring-closing metathesis approach
    S. Brass, N.-S. Chan, C. Gerlach, T. Luksch, J. Böttcher, and W. E. Diederich
    Journal of Organometallic Chemistry 2006, 691, 5406-5422

  • Facile synthesis of substituted 2,3,4,7-tetrahydro-1H-azepines via ring-closing metathesis
    S. Brass, H.-D. Gerber, S. Dörr, and W. E. Diederich
    Tetrahedron 2006, 62, 1777-1786

  • Formal Total Synthesis of (-)-Salicylihalamides A and B from D-Glucose and L-Rhamnose
    T. Haack, K. Haack, W. E. Diederich, B. Blackman, S. Roy, S. Pusuluri, and G. I. Georg
    Journal of Organic Chemistry 2005, 70, 7592-7604

  • Formal Total Synthesis of (+)-Salicylihalamides A and B: A Combined Chiral Pool and RCM Strategy
    K. Yang, B. Blackman, W. Diederich, P. T. Flaherty, C. J. Mossman, S. Roy, Y. M. Ahn, G. I. Georg
    Journal of Organic Chemistry 2003, 68, 10030-10039

  • Enantiospecific Formal Total Syntheses of (-)-Salicylihalamides A and B from D-Glucose and L-Rhamnose
    K. Yang, T. Haack, B. Blackman, W. E. Diederich, S. Roy, S. Pusuluri, G. I. Georg
    Organic Letters 2003, 5(21), 4007-4009.

  • Synthesis and Structure of Novel 1λ4,2,6-Thiadiazines
    W. E. Diederich und M. Haake
    Journal of Organic Chemistry 2003, 68, 3817-3830.


  • Inhibiting Hedgehog: An Update on Pharmacological Compounds and Targeting Strategies.
    I. Galperin, L Dempwolff, W. E. Diederich, M. Lauth
    J. Med. Chem. 2019, 62 (18), 8392-8411

  • Structure-Based Drug Design in Medicinal Chemistry: The Devil is in the Detail
    M. Kuhnert, Wibke E. Diederich
    Synlett 2016, 27, (5), 641-649.

  • Frontiers in Medicinal Chemistry 2015: Meet the Experts of MedChem near the Cradle of Medicinal and Pharmaceutical Chemistry.
    C. Wegscheid-Gerlach, H.-D- Gerber, W.E. Diederich.
    ChemMedChem 2015, 10, (7), 1267-1271.

  • HIV-Protease-Inhibitoren
    M. Kuhnert, W. E. Diederich
    Pharmakon 2014, 4, 262-269.

  • Recent Advances in Targeting Dengue and West Nile Virus Proteases Using Small Molecule Inhibitors
    H. Steuber, M. Kanitz, F.G.R. Ehlert, W. E. Diederich
    Topics in Medicinal Chemistry 2014, 46, Springer Berlin Heidelberg, in press.

  • Proteases of Plasmodium falciparum as potential drug targets and inhibitors thereof
    C. Wegscheid-Gerlach, H.-D. Gerber, W. E. Diederich
    Current Topics in Medicinal Chemistry 2010, 10, 346-367.

  • C2-symmetric pyrrolidines derived from tartaric acids: versatile chiral building blocks for total synthesis, catalyst design, supramolecular and medicinal chemistry
    A. Blum and W. E. Diederich
    Current Organic Synthesis 2009, 6 (1), 38-53.

  • Neue Konzepte zur Arzneistoffsuche und Synthese
    W. Diederich, P. Haebel, A. Heine, K. Reuter, C. Sotriffer, G. Klebe
    LaborPraxis 2004, 11, 24-26.



  • Strukturbasiertes Design Amin-basierter HIV-1 und HTLV-1-Protease-Inhibitoren
    Institutskolloquium, Institut für Pharmazie und Biochemie, Johannes Gutenberg-Universität Mainz, 05.07.2013

  • Auf der Suche nach neuen antiviralen Wirkstoffen: Von HIV-1 zu HTLV-1-Protease-Inhibitoren
    Deutsche Pharmazeutische Gesellschaft, Landesgruppe Hamburg, Hamburg, 09.04.2013

  • Auf der Suche nach neuen Wirkstoffen gegen AIDS
    Ein integrierter Ansatz aus Design, Synthese und Kristallographie
    Deutsche Pharmazeutische Gesellschaft, Landesgruppe Baden-Württemberg, Freiburg, 15.12.2010

  • Auf der Suche nach neuen Wirkstoffen gegen AIDS und Malaria
    Kolloquium im Rahmen des SFB 630 und der GDCh
    Institut für Organische Chemie der Julius-Maximilians-Universität Würzburg, Würzburg, 02.07.2009

  • Protein-Ligand-Interaktionen - Ist die perfekte Passform wirklich alles?
    Bayer-Schering Pharma AG, Berlin, 20.01.2009

  • Rational Design of C2 -Symmetric Pyrrolidines as HIV-1 Protease Inhibitors
    W.E. Diederich,
    A. Blum, J. Böttcher, G. Klebe
    International Conference on Drug Design and Discovery for Developing Countries, Triest, Italien, 3.-5. Juli 2008

  • Design and Synthesis of C2-symmetric Pyrrolidines as HIV Protease Inhibitors
    W.E. Diederich, A. Blum, J. Böttcher, G. Klebe
    New Frontiers in the Search of Bioactive Molecules: from Peptides to Drugs, 11th Naples Workshop on Bioactive Peptides, Neapel, Italien, 24.-27. Mai 2008

  • Azazyklen als bevorzugte Ligandgerüste von Aspartyl-Protease-Inhibitoren – Design, Synthese und Strukturbestimmung
    W.E. Diederich
    Vortragsreihe Organische Chemie, Merck KGaA, Darmstadt, 25.01.2007

  • Design and Synthesis of tailor-made compound libraries via a knowledge-based approach - A case study
    W.E. Diederich, C. Gerlach, A. Blum, J. Böttcher, S. Brass, T. Luksch, G. Klebe
    Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, USA, September 2006

Sonstige Vorträge

  • Functionalized Pyrrolidines – A New Class of HIV-1 Protease Inhibitors
    W.E. Diederich, A. Blum, J. Böttcher, G. Klebe
    Frontiers in Medicinal Chemistry, Joint German-Swiss meeting on Medicinal Chemistry, Berlin, März 2007

  • Identification of azacycles as privileged ligand scaffolds for the design and synthesis of aspartic protease inhibitors
    A. Blum, S. Brass, N.-S. Chan, W.E. Diederich
    Abstracts of Papers, 232nd ACS National Meeting, San Francisco, CA, USA, September 2006

  • Total Synthesis of the Salicylihalamides: Members of a new class of naturally occurring macrolides with promising cytotoxic activity
    Deutsche Pharmazeutische Gesellschaft, Landesgruppe Hessen, Marburg, Februar 2003

  • Synthesis and structure of novel 1λ4,2,6-thiadiazines
    19th International Symposium on the Organic Chemistry of Sulfur (ISOCS-XIX), Sheffield, UK, Juni 2000