54. Davies, L. J., Shuttleworth, L. M., Zhang, X., Peng, S., Nitsche, C., Bioorthogonal Peptide Macrocyclization using Oxime Ligation, Org. Lett. 2023, 25 (16), 2806–2809.
53. Nitsche, C., Targeting the Proteases of Arboviruses with Cyclic and Bicyclic Peptides, Proc. Roy. Soc. Victoria 2023, in press.
52. Ekanayake, K. B., Mahawaththa, M. C., Qianzhu, H., Abdelkader, E. H., George, J., Ullrich, S., Murphy, R. B., Fry, S. E., Johansen-Leete, J., Payne, R. J., Nitsche, C., Huber, T., Otting, G., Probing Ligand Binding Sites on Large Proteins by NMR Spectroscopy of Genetically Encoded Non-Canonical Amino Acids, J. Med. Chem. 2023, 66 (7), 5289–5304.
51. Sasi, V. M., Ullrich, S., Ton, J., Fry, S. E., Johansen-Leete, J., Payne, R., Nitsche, C., Jackson, C. J., Predicting Antiviral Resistance Mutations in SARS-CoV-2 Main Protease with Computational and Experimental Screening, Biochemistry 2022, 61 (22), 2495–2505.
50. Morewood, R., Nitsche, C., Bioinspired Peptide Stapling Generates Stable Enzyme Inhibitors, Chem. Commun. 2022, 58, 10817–10820.
49. Ullrich, S., Nitsche, C., Structure, Function and Inhibition of the SARS-CoV-2 Papain-Like Protease, ChemBioChem 2022, 23 (19), e202200327.
48. Tharayil, S. M., Mahawaththa, M. C., Feintuch, A., Maleckis, A., Ullrich, S., Morewood, R., Huber, T., Nitsche, C., Goldfarb, D., Otting, G., Site-selective Generation of Lanthanoid Binding Sites on Proteins using 4-Fluoro-2,6-dicyanopyridine, Magn. Reson. 2022, 3, 169–182.
47. Ullrich, S., George, J., Coram, A. E., Morewood, R., Nitsche, C., Biocompatible and Selective Generation of Bicyclic Peptides, Angew. Chem. Int. Ed. 2022, 61(43), e202208400.
46. Johansen-Leete, J., Ullrich, S., Fry, S. E., Frkic, R., Bedding, M. J., Aggarwal, A., Ashhurst, A. S., Ekanayake, K. B., Mahawaththa, M. C., Sasi, V. M., Passioura, T., Larance, M., Otting, G., Turville, S., Jackson, C. J., Nitsche, C., Payne, R. J., Antiviral Cyclic Peptides Targeting the Main Protease of SARS-CoV-2, Chem. Sci. 2022, 13, 3826–3836.
45. Abdelkader, E., Qianzhu, H., George, J., Frkic, R., Jackson, C., Nitsche, C., Otting, G., Huber, T., Genetic Encoding of Cyanopyridylalanine for In-Cell Protein Macrocyclization by the Nitrile-Aminothiol Click Reaction, Angew. Chem. Int. Ed. 2022, 61 (13), e202114154.
44. Ullrich, S., Ekanayake, K. B., Otting, G., Nitsche, C., Main Protease Mutants of SARS-CoV-2 Variants Remain Susceptible to Nirmatrelvir, Bioorg. Med. Chem. Lett. 2022, 62, 128629.
43. Qing, M., Nitsche, C., Orton, H. W., Overhand, M., Otting, G., Ubbink, M., Paramagnetic Chemical Probes for Studying Biological Macromolecules, Chem. Rev. 2022, 122 (10), 9571–9642.
42. Mahawatha, M. C., Orton, H. W., Adekoya, I., Huber, T., Otting, G., Nitsche, C., Organoarsenic Probes to Study Proteins by NMR Spectroscopy, Chem. Commun. 2022, 58, 701–704.
41. Voss, S., Rademann, J., Nitsche, C., Peptide-Bismuth Bicycles: In Situ Access to Stable Constrained Peptides with Superior Bioactivity, Angew. Chem. Int. Ed. 2022, 61 (4), e202113857.
40. Schroeder, B., Demirel, P., Fischer, C., Masri, E., Kallis, S., Redl, L., Rudolf, T., Bergemann, S., Arkona, C., Nitsche, C., Bartenschlager, R., Rademann, J., Nanoparticular Inhibitors of Flavivirus Proteases from Zika, West Nile and Dengue Virus Are Cell-Permeable Antivirals, ACS Med. Chem. Lett. 2021, 12 (12), 1955–1961.
39. Ullrich, S., Sasi, V. M., Mahawaththa, M. C., Ekanayake, K. B., Morewood, R., George, J., Shuttleworth, L., Zhang, X., Whitefield, C., Otting, G., Jackson, C., Nitsche, C., Challenges of short substrate analogues as SARS-CoV-2 main protease inhibitors, Bioorg. Med. Chem. Lett. 2021, 50, 128333.
38. Voss, S., Nitsche, C., Targeting the Protease of West Nile Virus, RSC Med. Chem. 2021, 12, 1262–1272.
37. Patil, N. A., Quek, J.-P., Schroeder, B., Morewood, R., Rademann, J., Luo, D., Nitsche, C., 2-Cyanoisonicotinamide Conjugation: A Facile Approach to Generate Potent Peptide Inhibitors of the Zika Virus Protease, ACS Med. Chem. Lett. 2021, 12 (5), 732–737.
36. Morewood, R., Nitsche, C., A Biocompatible Stapling Reaction forin situ Generation of Constrained Peptides, Chem. Sci. 2021, 12 (2), 669–674.
35. Ullrich, S., Nitsche, C., The SARS-CoV-2 Main Protease as Drug Target, Bioorg. Med. Chem. Lett. 2020, 30 (17), 127377.
34. Pach, S., Sarter, T. M., Yousef, R., Schaller, D., Bergemann, S., Arkona, C., Rademann, J., Nitsche, C., Wolber, G., Catching a Moving Target: Comparative Modeling of Flaviviral NS2B-NS3 Reveals Small Molecule Zika Protease Inhibitors, ACS Med. Chem. Lett. 2020, 11 (4), 514–520.
33. Voss, S., Nitsche, C., Inhibitors of the Zika virus protease NS2B-NS3, Bioorg. Med. Chem. Lett. 2020, 30 (5), 126965.
32. Nitsche, C., Onagi, H., Quek, J.-P., Otting, G., Luo, D., Huber, T., Biocompatible Macrocyclization between Cysteine and 2-Cyanopyridine Generates Stable Peptide Inhibitors, Org. Lett. 2019, 21 (12), 4709–4712.
31. Nitsche, C., Proteases from Dengue, West Nile and Zika Viruses as Drug Targets, Biophys. Rev. 2019, 11 (2), 157–165.
30. Nitsche, C., Passioura, T., Varava, P., Mahawaththa, M. C., Leuthold, M. M., Klein, C. D., Suga, H., Otting, G., De Novo Discovery of Nonstandard Macrocyclic Peptides as Noncompetitive Inhibitors of the Zika Virus NS2B-NS3 Protease, ACS Med. Chem. Lett. 2019, 10 (2), 168–174.
29. Mahawaththa, M. C., Lee, M. D., Giannoulis, A., Adams, L. A., Feintuch, A., Swarbrick, J. D., Graham, B., Nitsche, C., Goldfarb, D., Otting, G., Small Neutral Gd(III) Tags for Distance Measurements in Proteins by Double Electron-Electron Resonance Experiments, Phys. Chem. Chem. Phys. 2018, 20 (36), 23535–23545.
28. Nitsche, C., Otting, G., Intrinsic and Extrinsic Paramagnetic Probes, in Paramagnetism in Experimental Biomolecular NMR, Luchinat, C., Parigi, G., Ravera, E. (Eds.), New Developments in NMR, ISBN 978-1-78801-086-3, Royal Society of Chemistry, 2018, 42–84.
27. Nitsche, C., Strategies Towards Protease Inhibitors for Emerging Flaviviruses, in Dengue and Zika: Control and Antiviral Treatment Strategies, Hilgenfeld, R., Vasudevan, S. G. (Eds.), Advances in Experimental Medicine and Biology 1062, ISBN 978-981-10-8727-1, Springer, 2018, 175–186.
26. Becker, W., Adams, L. A., Graham, B., Wagner, G. E., Zangger, K., Otting, G., Nitsche, C., Trimethylsilyl Tag for Probing Protein-Ligand Interactions by NMR, J. Biomol. NMR 2018, 70 (4), 211–218.
25. Nitsche, C., Otting, G., NMR Studies of Ligand Binding, Curr. Opin. Struct. Biol. 2018, 48, 16–22.
24. Nitsche, C., Mahawaththa, M. C., Becker, W., Huber, T., Otting, G., Site-Selective Tagging of Proteins by Pnictogen-Mediated Self-Assembly, Chem. Commun. 2017, 53 (79), 10894–10897.
23. Mahawaththa, M. C., Pearce, B. J. G., Graham, B., Klein, C. D., Nitsche, C., Otting, G., Solution Conformations of a Linked Construct of the Zika Virus NS2B-NS3 Protease, Antiviral Res. 2017, 142, 141–147.
22. Nitsche, C., Zhang, L., Weigel, L., Schilz, J., Graf, D., Bartenschlager, R., Hilgenfeld, R., Klein, C. D., Peptide-Boronic Acid Inhibitors of Flaviviral Proteases: Medicinal Chemistry and Structural Biology, J. Med. Chem. 2017, 60(1), 511–516.
21. Nitsche, C., Otting, G., Pseudocontact Shifts in Biomolecular NMR Using Paramagnetic Metal Tags, Prog. NMR Spectrosc. 2017, 98–99, 20–49.
20. Lei, J., Hansen, G., Nitsche, C., Klein, C. D., Zhang, L., Hilgenfeld, R., Crystal Structure of Zika Virus NS2B-NS3 Protease in Complex with a Boronate Inhibitor, Science 2016, 353(6298), 503–505.
19. Chen, W.-N., Nitsche, C., Pilla, K. B., Graham, B., Huber, T., Klein, C. D., Otting, G., Sensitive NMR Approach for Determining the Binding Mode of Tightly Binding Ligand Molecules to Protein Targets, J. Am. Chem. Soc. 2016, 138 (13), 4539–4546.
18. Behnam, M. A. M., Nitsche, C., Boldescu, V., Klein, C. D., The Medicinal Chemistry of Dengue Virus, J. Med. Chem. 2016, 59 (12), 5622–5649.
17. Nitsche, C., Green Chemistry Strategies for Drug Discovery. Edited by Emily A. Peterson and Julie B. Manley, ChemMedChem 2015, 10 (11), 1932–1933.
16. Weigel, L. F., Nitsche, C., Graf, D., Bartenschlager, R., Klein, C. D., Phenylalanine and Phenylglycine Analogs as Arginine Mimetics in Dengue Protease Inhibitors, J. Med. Chem. 2015, 58 (19), 7719–7733.
15. Bastos Lima, A., Behnam, M. A. M., El Sherif, Y., Nitsche, C., Vechi, S. M., Klein, C. D., Dual Inhibitors of the Dengue and West Nile Virus NS2B-NS3 Proteases: Synthesis, Biological Evaluation and Docking Studies of Novel Peptide-Hybrids, Bioorg. Med. Chem. 2015, 23 (17), 5748–5755.
14. Sczepek, R., Nitsche, C., Heller, L., Siewert, B., Schäfer, R., Flemming, F., Otgonbayar, C., Csuk, R., Synthesis and Cytotoxic Properties of Alkynic Triterpenoid Mannich Compounds, Mediterr. J. Chem. 2015, 4 (3), 126–137.
13. Nitsche, C., Holloway, S., Schirmeister, T., Klein, C. D., Biochemistry and Medicinal Chemistry of the Dengue Virus Protease, Chem. Rev. 2014, 114 (22), 11348–11381.
12. Jöst, C., Nitsche, C., Scholz, T., Roux, L., Klein, C. D., Promiscuity and Selectivity in Covalent Enzyme Inhibition: A Systematic Study of Electrophilic Fragments, J. Med. Chem. 2014, 57 (18), 7590–7599.
11. Behnam, M. A. M., Nitsche, C., Vechi, S. M., Klein, C. D., C-Terminal Residue Optimization and Fragment Merging: Discovery of a Potent Peptide-Hybrid Inhibitor of Dengue Protease, ACS Med. Chem. Lett. 2014, 5 (9), 1037–1042.
10. Chen, W.-N., Loscha, K. V., Nitsche, C., Graham, B., Otting, G., The Dengue Virus NS2B-NS3 Protease Retains the Closed Conformation in the Complex with BPTI, FEBS Lett. 2014, 588 (14), 2206–2211.
9. Nitsche, C., Schreier, V. N., Behnam, M. A. M., Kumar, A., Bartenschlager, R., Klein, C. D., Thiazolidinone-Peptide Hybrids as Dengue Virus Protease Inhibitors with Antiviral Activity in Cell Culture, J. Med. Chem. 2013, 56 (21), 8389–8403.
8. Nitsche, C., Klein, C. D., Fluorimetric and HPLC-Based Dengue Virus Protease Assays Using a FRET Substrate, Antiviral Methods and Protocols (2nd edition), Gong, E. Y. (Ed.), Methods in Molecular Biology 1030, ISBN 978-1-62703-483-8, Humana Press, 2013, 221–236.
7. Csuk, R., Nitsche, C., Sczepek, R., Schwarz, S., Siewert, B., Synthesis of Antitumor-Active Betulinic Acid-Derived Hydroxypropargylamines by Copper-Catalyzed Mannich Reactions, Arch. Pharm. Chem. Life Sci. 2013, 346 (3), 232–246.
6. Csuk, R., Sczepek, R., Siewert, B., Nitsche, C., Cytotoxic Betulin-Derived Hydroxypropargylamines Trigger Apoptosis, Bioorg. Med. Chem. 2013, 21(2), 425–435.
5. Nitsche, C., Klein, C. D., Aqueous Microwave-Assisted One-Pot Synthesis of N-Substituted Rhodanines, Tetrahedron Lett. 2012, 53 (39), 5197–5201.
4. Csuk, R., Stark, S., Nitsche, C., Barthel, A., Siewert, B., Alkylidene Branched Lupane Derivatives: Synthesis and Antitumor Activity, Eur. J. Med. Chem. 2012, 53, 337–345.
3. Nitsche, C., Behnam, M. A. M., Steuer, C., Klein, C. D., Retro Peptide-Hybrids as Selective Inhibitors of the Dengue Virus NS2B-NS3 Protease, Antiviral Res. 2012, 94 (1), 72–79.
2. Nitsche, C., Steuer, C., Klein, C. D., Arylcyanoacrylamides as Inhibitors of the Dengue and West Nile Virus Proteases, Bioorg. Med. Chem. 2011, 19 (24), 7318–7337.
1. Henze, M., Kreye, O., Brauch, S., Nitsche, C., Naumann, K., Wessjohann, L. A., Westermann, B., Photoaffinity-Labeled Peptoids and Depsipeptides by Multicomponent Reactions, Synthesis 2010, 17, 2997–3003.
NITSCHE LAB 