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Wasinska-Kałwa, M.; Omran, A.; Mach, L.; Scipioni, L.; Bouma, J.; Li, X.; Radetzki, S.; Mostinski, Y.; Schippers, M.; Gazzi, T.; van der Horst, C.; Brennecke, B.; Hanske, A.; Kolomeets, Y.; Guba, W.; Sykes, D.; von Kries, J. P.; Broichhagen, J.; Hua, T.; Veprintsev, D.; Heitman, L. H.; Oddi, S.; Maccarrone, M.; Grether, U.; Nazaré, M., Visualization of Membrane Localization and the Functional State of CB2R Pools Using Matched Agonist and Inverse Agonist Probe Pairs, Chem. Sci., 2024, Advance Article. https://doi.org/10.1039/D4SC00402G
Mach, L.; Omran, A.; Bouma, J.; Radetzki, S.; Sykes, D. A.; Guba, W.; Li, X.; Höffelmeyer, C.; Hentsch, A.; Gazzi, T.; Mostinski, Y.; Wasinska-Kalwa, M.; de Molnier, F.; van der Horst, C.; von Kries, J. P.; Vendrell, M.; Hua, T.; Veprintsev, D. B.; Heitman, L. H.; Grether, U.; Nazare, M., Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB1R), J. Med. Chem. 2024, 67, 11841-11867. https://doi.org/10.1021/acs.jmedchem.4c00465
Legchenko, E.; Chouvarine, P.; Qadri, F.; Specker, E.; Nazaré, M.; Wesolowski, R.; Matthes, S.; Bader, M.; Hansmann, G., Novel Tryptophan Hydroxylase Inhibitor TPT-001 Reverses PAH, Vascular Remodeling, and Proliferative-Proinflammatory Gene Expression, JACC: Basic to Translational Science, 2024, 9, 890-902. https://doi.org/10.1016/j.jacbts.2024.04.006
Schwarze, T.; Sprenger, T.; Nazare, M.; Holdt, H.-J.; Hentsch, A., Benzo-Crown-Ether functionalized O-BODIPY Probes for Cations – A Selective Fluorescent Probe for Ba2+, Chem Eur. J., 2024, 30, e202401928. https://doi.org/10.1002/chem.202401928
Gazzi, A. T., Lesina, M., Wang, Q., Radetzki, S., Demir, I. E., Meiser, W., Wilke, S., Peter, J., Kries, V., Algül, H., Hu, H., & Nazaré, M., DOTA-based plectin-1 targeted contrast agent enables detection of pancreatic cancer in human tissue. Angew. Chem. Int. Ed., 2024, 63, e20231848. doi.org/10.1002/anie.202318485
Yan, S.; Schöpe, P. C.; Lewis, J.; Putzker, K.; Uhrig, U.; Specker, E.; von Kries, J. P.; Lindemann, P.; Omran, A.; Sanchez-Ibarra, H. E.; Unger, A.; Zischinsky, M.-L.; Klebl, B.; Walther, W.; Nazaré, M.; Kobelt, D.; Stein, U., Discovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis. Biomedicine & Pharmacotherapy 2023, 168, 115698. doi.org/10.1016/j.biopha.2023.115698
Specker, E.; Wesolowski, R.; Schütz, A.; Matthes, S.; Mallow, K.; Wasinska-Kalwa, M.; Winkler, L.; Oder, A.; Alenina, N.; Pleimes, D.; von Kries, J. P.; Heinemann, U.; Bader, M.; Nazaré, M., Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors. J. Med. Chem. 2023, 66, 14866-14896. doi.org/10.1021/acs.jmedchem.3c01454
Kücükdisli, M.; Bel-Abed, H.; Cirillo, D.; Lo, W.-T.; Efrém, N.-L.; Horatscheck, A.; Perepelittchenko, L.; Prokofeva, P.; Ehret, T. A. L.; Radetzki, S.; Neuenschwander, M.; Specker, E.; Médard, G.; Müller, S.; Wilhelm, S.; Kuster, B.; von Kries, J. P.; Haucke, V.; Nazaré, M., Structural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition, J Med. Chem. 2023, 66, 14278-14302. doi.org/10.1021/acs.jmedchem.3c01319
Mucka P.; Lindemann P.; Bosco B.; Willenbrock M.; Radetzki S.; Neuenschwander M.; Brischetto C.; von Kries J.P.; Nazaré M.; Scheidereit C., CLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors, Cell Chem. Biol., 2023, 30, 1303-1312. doi.org/10.1016/j.chembiol.2023.06.027
Sprenger, T.; Schwarze, T.; Müller, H.; Sperlich, E.; Holdt, H.-J.; Nazaré, M.; Hentsch, A.; Eidner, S.; Kraft, R.; Kumke, M. U., Selective and pH-Independent Detection of Ba2+ in Water by a Benzo-21-Crown-7-Functionalized BODIPY, Chem. Eur. J. 2023, 29, e202301622. doi.org/10.1002/chem.202301622
Scipioni, L.; Tortolani, D.; Ciaramellano, F.; Fanti, F.; Gazzi, T.; Sergi, M.; Nazaré, M.; Oddi, S.; Maccarrone, M., Aβ Chronic Exposure Promotes an Activation State of Microglia through Endocannabinoid Signalling Imbalance. Int. J. Mol. Sci. 2023, 24, 6684. doi.org/10.3390/ijms24076684
Jordan, P.; Costa, A.; Specker, E.; Popp, O.; Volkamer, A.; Piske, R.; Obrusnik, T.; Kleissle, S.; Stuke, K.; Rex, A.; Neuenschwander, M.; von Kries, J. P.; Nazare, M.; Mertins, P.; Kettenmann, H.; Wolf, S. A., Small molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation. PLOS ONE 2023, 18, e0278325. doi.org/10.1371/journal.pone.0278325
Starke, L.; Millward, J.M.; Prinz, C.; Sherazi, F.; Waiczies, H.; Lippert, C.; Nazaré, M.; Paul, F.; Niendorf, T.; Waiczies, S. First in vivo fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod. Theranostics 2023, 13, 1217-1234. doi:10.7150/thno.77041
Lo, W. T.; Belabed, H.; Kucukdisli, M.; Metag, J.; Roske, Y.; Prokofeva, P.; Ohashi, Y.; Horatscheck, A.; Cirillo, D.; Krauss, M.; Schmied, C.; Neuenschwander, M.; von Kries, J. P.; Medard, G.; Kuster, B.; Perisic, O.; Williams, R. L.; Daumke, O.; Payrastre, B.; Severin, S.; Nazare, M.; Haucke, V., Development of selective inhibitors of phosphatidylinositol 3-kinase C2alpha. Nat. Chem. Biol. 2023. 19, 18–27. doi.org/10.1038/s41589-022-01118-z
Sprenger, T.; Schwarze, T.; Müller, H.; Sperlich, E.; Kelling, A.; Holdt, H. J.; Paul, J.; Martos Riaño, V.; Nazaré, M., BODIPY‐Equipped Benzo‐Crown‐Ethers as Fluorescent Sensors for pH Independent Detection of Sodium and Potassium Ions. ChemPhotoChem 2022. doi.org/10.1002/cptc.202200270
Fernandez-Bachiller, M. I.; Hwang, S.; Schembri, M. E.; Lindemann, P.; Guberman, M.; Herziger, S.; Specker, E.; Matter, H.; Will, D. W.; Czech, J.; Wagner, M.; Bauer, A.; Schreuder, H.; Ritter, K.; Urmann, M.; Wehner, V.; Sun, H.; Nazare, M., Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands. J. Med. Chem. 2022, 65, 13013–13028. doi.org/10.1021/acs.jmedchem.2c00865
Zhang, H.; Modenutti, C.; Nekkanti, Y. P. K.; Denis, M.; Bermejo, I. A.; Lefebre, J.; Che, K.; Kim, D.; Kagelmacher, M.; Kurzbach, D.; Nazare, M.; Rademacher, C., Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin. ACS Chem. Biol. 2022, 17, 2728–2733. doi.org/10.1021/acschembio.2c00626
Samsó, P.; Koch, P. A.; Posor, Y.; Lo, W.-T.; Belabed, H.; Nazare, M.; Laporte, J.; Haucke, V., Antagonistic control of active surface integrins by myotubularin and phosphatidylinositol 3-kinase C2β; in a myotubular myopathy model. PNAS 2022, 119. doi.org/10.1073/pnas.2202236119
Specker, E.; Matthes, S.; Wesolowski, R.; Schütz, A.; Grohmann, M.; Alenina, N.; Pleimes, D.; Mallow, K.; Neuenschwander, M.; Gogolin, A.; Weise, M.; Pfeifer, J.; Ziebart, N.; Heinemann, U.; von Kries, J. P.; Nazaré, M.; Bader, M., Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors. J. Med. Chem. 2022, 65, 16, 11126–11149. doi.org/10.1021/acs.jmedchem.2c00598
Langedijk, J.; Araya, E. I.; Barroso, A. R.; Tolenaars, D.; Nazare, M.; Belabed, H.; Schoene, J.; Chichorro, J. G.; Oude Elferink, R., An LPAR 5 -antagonist that reduces nociception and increases pruriception. Front. Pain Res. 2022, 3. doi.org/10.3389/fpain.2022.963174
Melder, F. T.; Lindemann, P.; Welle, A.; Trouillet, V.; Heißler, S.; Nazaré, M.; Selbach, M., Compound interaction screen on a photoactivatable cellulose membrane (CISCM) identifies drug targets. ChemMedChem 2022, 17, 1-5. doi.org/10.1002/cmdc.202200346
Liu, Q.; Yang, M.; Meng, X.; Han, X.; Nazare, M.; Xu, Y.; Hu, H.-Y.; Zhang, Q., Donor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles. Talanta 2022, 246, 123493. doi.org/10.1016/j.talanta.2022.123493
Li, X.-L.; Ru, T.; Navarro-Vázquez, A.; Lindemann, P.; Nazaré, M.; Li, X.-W.; Guo, Y.-W.; Sun, H., Weizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+ Probability and CASE-3D. J. Nat. Prod. 2022, 85, 1730-1737. doi.org/10.1021/acs.jnatprod.2c00257
Gazzi, T., Brennecke, B., Atz, K., Korn, C., Sykes, Forn-Cuni, G.; D., Pfaff, P., Sarott, R. C., Westphal, M. V., Mostinski, Y., Mach, L.; Wasinska-Kalwa, M.; Weise, M., Hoare, B. L., Miljuš, T., Mexi, M., Roth, N.; Koers, E. J.; Guba, W., Anker, A., Rufer, A. C., A. Kusznir, E., Huber, S., Raposo, C., Zirwes, E. A., Osterwald, A., Pavlovic, A., Moes, S., Beck, J., Benito-Cuesta, I., Grande, T., Drawnel, F., Widmer, G., Holzer, D., Wel, T. van der, Mandhair, H., Honer, M., Fingerle, J., Scheffel, J.; Broichhagen, J.; Gawrisch, K., Romero, J., Hillard, C. J., McCormick, P. J., Varga, Z. V., Stelt, M. van der, Pacher, P., Gertsch, J., Ullmer, C., Oddi, S., Spaink, H. P.; Maccarrone, M., Veprintsev, D. B., Carreira, E. M., Grether, U., and Nazare, M., Detection of Cannabinoid Receptor Type 2 in Native Cells and Zebrafish with a Highly Potent, Cell-Permeable Fluorescent Probe. Chem. Sci. 2022, 13, 5539-5545. doi.org/10.1039/D1SC06659E
Li, H.; Prever, L.; Hsu, M. Y.; Lo, W. T.; Margaria, J. P.; De Santis, M. C.; Zanini, C.; Forni, M.; Novelli, F.; Pece, S.; Di Fiore, P. P.; Porporato, P. E.; Martini, M.; Belabed, H.; Nazare, M.; Haucke, V.; Gulluni, F.; Hirsch, E., Phosphoinositide Conversion Inactivates R-RAS and Drives Metastases in Breast Cancer. Adv. Sci. 2022, e2103249. doi.org/10.1002/advs.202103249
Halland, N.; Schmidt, F.; Weiss, T.; Li, Z.; Czech, J.; Saas, J.; Ding-Pfennigdorff, D.; Dreyer, M. K.; Strübing, C.; Nazare, M., Rational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis. J. Med. Chem. 2022, 65, 1567-1584. 10.1021/acs.jmedchem.1c01601
Carter, D. M.; Specker, E.; Malecki, P. H.; Przygodda, J.; Dudaniec, K.; Weiss, M. S.; Heinemann, U.; Nazare, M.; Gohlke, U., Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer. J. Med. Chem. 2021, 64, 14266-14282. doi.org/10.1021/acs.jmedchem.1c00693
Leenders, R. G. G.; Brinch, S. A.; Sowa, S. T.; Amundsen-Isaksen, E.; Galera-Prat, A.; Murthy, S.; Aertssen, S.; Smits, J. N.; Nieczypor, P.; Damen, E.; Wegert, A.; Nazare, M.; Lehtio, L.; Waaler, J.; Krauss, S., Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II. J. Med. Chem. 2021, 64, 17936–17949. doi/10.1021/acs.jmedchem.1c01264
Prinz, C.; Starke, L.; Ramspoth, T. F.; Kerkering, J.; Martos Riano, V.; Paul, J.; Neuenschwander, M.; Oder, A.; Radetzki, S.; Adelhoefer, S.; Ramos Delgado, P.; Aravina, M.; Millward, J. M.; Fillmer, A.; Paul, F.; Siffrin, V.; von Kries, J. P.; Niendorf, T.; Nazare, M.; Waiczies, S., Pentafluorosulfanyl (SF5) as a Superior (19)F Magnetic Resonance Reporter Group: Signal Detection and Biological Activity of Teriflunomide Derivatives. ACS Sens. 2021, 6, 11, 3948–3956. doi.org/10.1021/acssensors.1c01024
Brennecke, Benjamin; Wang, Qinghua; Haap, Wolfgang; Grether, Uwe; Hu, Hai-Yu; Nazare, Marc, DOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells, Bioconjugate Chem. 2021, 32, 702-712. doi.org/10.1021/acs.bioconjchem.0c00699
Prinz C, Starke L, Millward JM, Fillmer A, Delgado PR, Waiczies H, Pohlmann A, Rothe M, Nazaré M, Paul F, Niendorf T, Waiczies S. In vivo detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy. Theranostics 2021, 11, 2490-2504. doi:10.7150/thno.47130
Bonnekoh, H.; Vera, C.; Abad-Perez, A.; Radetzki, S.; Neuenschwander, M.; Specker, E.; Mahnke, N. A.; Frischbutter, S.; Latz, E.; Nazaré, M.; Kries, J. V.; Maurer, M.; Scheffel, J.; Krause, K., Topical inflammasome inhibition with disulfiram prevents irritant contact dermatitis. Clin. Transl. Allergy 2021, 11, e12045. doi.org/10.1002/clt2.12045
Mostinski, Y.; Heynen, G. J. J. E.; López-Alberca, M. P.; Paul, J.; Miksche, S.; Radetzki, S.; Schaller, D.; Shanina, E.; Seyffarth, C.; Kolomeets, Y.; Ziebart, N.; de Schryver, J.; Oestreich, S.; Neuenschwander, M.; Roske, Y.; Heinemann, U.; Rademacher, C.; Volkamer, A.; von Kries, J. P.; Birchmeier, W.; Nazaré, M. From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement. J. Med. Chem. 2020, 63, 14780 - 14804. doi.org/10.1021/acs.jmedchem.0c01265
Barone, M.; Müller, M.; Chiha, S.; Ren, J.; Albat, D.; Soicke, A.; Dohmen, S.; Klein, M.; Bruns, J.; van Dinther, M.; Opitz, R.; Lindemann, P.; Beerbaum, M.; Motzny, K.; Roske, Y.; Schmieder, P.; Volkmer, R.; Nazaré, M.; Heinemann, U.; Oschkinat, H.; en Dijke, P.; Schmalz, H.-G.; Kühne, R., Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells. Proc. Natl. Acad. Sci. U. S. A. 2020, 117, 29684-29690. doi.org/10.1073/pnas.2007213117
Sarott, R. C.; Westphal, M. V.; Pfaff, P.; Korn, C.; Sykes, D. A.; Gazzi, T.; Brennecke, B.; Atz, K.; Weise, M.; Mostinski, Y.; Hompluem, P.; Koers, E.; Miljus, T.; Roth, N. J.; Asmelash, H.; Vong, M. C.; Piovesan, J.; Guba, W.; Rufer, A. C.; Kusznir, E. A.; Huber, S.; Raposo, C.; Zirwes, E. A.; Osterwald, A.; Pavlovic, A.; Moes, S.; Beck, J.; Benito-Cuesta, I.; Grande, T.; Ruiz de Martín Esteban, S.; Yeliseev, A.; Drawnel, F.; Widmer, G.; Holzer, D.; van der Wel, T.; Mandhair, H.; Yuan, C.-Y.; Drobyski, W. R.; Saroz, Y.; Grimsey, N.; Honer, M.; Fingerle, J.; Gawrisch, K.; Romero, J.; Hillard, C. J.; Varga, Z. V.; van der Stelt, M.; Pacher, P.; Gertsch, J.; McCormick, P. J.; Ullmer, C.; Oddi, S.; Maccarrone, M.; Veprintsev, D. B.; Nazare, M.; Grether, U.; Carreira, E. M., Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells. J. Am. Chem. Soc. 2020, 142, 16953-16964. doi.org/10.1021/jacs.0c05587
Sreeramulu, S.; Richter, C.; Kuehn, T.; Azzaoui, K.; Blommers, M. J. J.; Del Conte, R.; Fragai, M.; Trieloff, N.; Schmieder, P.; Nazare, M.; Specker, E.; Ivanov, V.; Oschkinat, H.; Banci, L.; Schwalbe, H., NMR quality control of fragment libraries for screening, J Biomol NMR, 2020, 74, 555–563. doi.org/10.1007/s10858-020-00327-9
Waaler, J.; Leenders, R. G. G.; Sowa, S. T.; Alam Brinch, S.; Lycke, M.; Nieczypor, P.; Aertssen, S.; Murthy, S.; Galera-Prat, A.; Damen, E.; Wegert, A.; Nazare, M.; Lehtio, L.; Krauss, S., Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor. J. Med. Chem. 2020, 63, 6834-6846. doi.org/10.1021/acs.jmedchem.0c00208
Alsalim, R.; Lindemann, P.; Lopez-Alberca, M. P.; Miksche, S.; Czechtizky, W.; Halland, N.; Nazare, M., A Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles. Org. Lett. 2020, 22, 7393-7396. doi.org/10.1021/acs.orglett.0c02766
Xu, S.; Zhang, Q.; Han, X.; Wang, Y.; Wang, X.; Nazare, M.; Jiang, J.-D.; Hu, H.-Y., Dual-Mode Detection of Bacterial 16S Ribosomal RNA in Tissues. ACS Sens. 2020, 5, 1650-1656. doi.org/10.1021/acssensors.0c00252
Webel, H. E.; Kimber, T. B.; Radetzki, S.; Neuenschwander, M.; Nazare, M.; Volkamer, A. Revealing cytotoxic substructures in molecules using deep learning. J. Comput. Aided Mol. Des. 2020, 34, 731–746. doi.org/10.1007/s10822-020-00310-4.
Brennecke, B.; Wang, Q.; Zhang, Q.; Hu, H.-Y.; Nazare, M. An Activatable Lanthanide Luminescent Probe for Time-Gated Detection of Nitroreductase in Live Bacteria. Angew. Chem. Int. Ed. 2020, 59, 8512-8516. doi.org/10.1002/anie.202002391
Plastira, I.; Joshi, L.; Bernhart, E.; Schoene, J.; Specker, E.; Nazare, M., Sattler, W. Small-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells. Front. Cell. Neurosci. 2019, 13, 531. doi.org/10.3389/fncel.2019.00531
Schoene, J.; Gazzi, T.; Lindemann, P.; Christmann, M.; Volkamer, A.; Nazare, M. Probing 2H-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors. ChemMedChem 2019, 14, 1514-1527. doi.org/10.1002/cmdc.201900328
Zhang, Q.; Xu, S.; Lai, F.; Wang, Y.; Zhang, N.; Nazare, M.; Hu, H.-Y. Rapid Synthesis of γ-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen. Org. Lett. 2019, 21, 2121-2125. doi.org/10.1021/acs.orglett.9b00404
Schewe, M.; Sun, H.; Mert, Ü.; Mackenzie, A.; Pike, A. C. W.; Schulz, F.; Constantin, C.; Vowinkel, K. S.; Conrad, L. J.; Kiper, A. K.; Gonzalez, W.; Musinszki, M.; Tegtmeier, M.; Pryde, D. C.; Belabed, H.; Nazare, M.; de Groot, B. L.; Decher, N.; Fakler, B.; Carpenter, E. P.; Tucker, S. J.; Baukrowitz, T. A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels. Science 2019, 363, 875-880. doi.org/10.1126/science.aav0569
Brennecke, P.; Rasina, D.; Aubi, O.; Herzog, K.; Landskron, J.; Cautain, B.; Vicente, F.; Quintana, J.; Mestres, J.; Stechmann, B.; Ellinger, B.; Brea, J.; Kolanowski, J. L.; Pilarski, R.; Orzaez, M.; Pineda-Lucena, A.; Laraia, L.; Nami, F.; Zielenkiewicz, P.; Paruch, K.; Hansen, E.; von Kries, J. P.; Neuenschwander, M.; Specker, E.; Bartunek, P.; Simova, S.; Lesnikowski, Z.; Krauss, S.; Lehtiö, L.; Bilitewski, U.; Brönstrup, M.; Taskén, K.; Jirgensons, K.; Lickert, H.; Clausen, M. H.; Andersen, J. H.; Vicent, M. J.; Genilloud, O.; Martinez, A.; Nazare, M.; Fecke, W.; Gribbon P. EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology. SLAS Discov. 2019, 24, 398-413. doi.org/10.1177/2472555218816276.
Marcinkowski, P.; Hoyer, I.; Specker, E.; Furkert, J.; Rutz, C.; Neuenschwander, M.; Sobottka, S.; Sun, H.; Nazare, M.; Berchner-Pfannschmidt, U.; von Kries, J.-P.; Eckstein, A.; Schülein, R.; Krause, G. A new highly thyrotropin receptor-selective small molecule antagonist wih potential for the treatment of Graves' orbitopathy. Thyroid 2019, 29, 111-123. doi.org/10.1089/thy.2018.0349
Klein, W.; Rutz, C.; Eckhard, J.; Provinciael, B.; Specker, E.; Neuenschwander, M.; Kleinau, G.; Scheerer, P.; von Kries, J.-P.; Nazare, M.; Vermeire, K.; Schülein, R. Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway. PLoS ONE 2018, 13, e0208641. doi.org/10.1371/journal.pone.0208641.
Schulze, J.; Baukmann, H.; Wawrzinek, R.; Fuchsberger, F. F.; Specker, E.; Aretz, J.; Nazare, M.; Rademacher, C. CellFy: A Cell-Based Fragment Screen against C-Type Lectins. ACS Chem. Biol. 2018, 13, 3229-3235. doi.org/10.1021/acschembio.8b00875.
Aretz, J., Anumala, U. R., Fuchsberger, F. F., Molavi, N., Ziebart, N., Zhang, H., Nazaré, M., & Rademacher, C., Allosteric Inhibition of a Mammalian Lectin. JACS 2018, 44, 14915–14925. doi.org/10.1021/jacs.8b08644.
Duro-Castano, A., Lim, N. H., Tranchant, I., Amoura, M., Beau, F., Wieland, H., Kingler, O., Herrmann, M., Nazaré, M., Plettenburg, O., Dive, V., Vicent, M. J., & Nagase, H., In Vivo Imaging of MMP-13 Activity Using a Specific Polymer-FRET Peptide Conjugate Detects Early Osteoarthritis and Inhibitor Efficacy. Adv. Funct. Mat. 2018, 28, 1802738. doi.org/10.1002/adfm.201802738.
Ruess, D. A., Heynen, G. J., Ciecielski, K. J., Ai, J., Berninger, A., Kabacaoglu, D., Görgülü, K., Dantes, Z., Wörmann, S. M., Diakopoulos, K. N., Karpathaki, A. F., Kowalska, M., Kaya-Aksoy, E., Song, L., Van Der Laan, E. A. Z., López-Alberca, M. P., Nazaré, M., Reichert, M., Saur, D.,Erkan M.,Hopt U.T., Sainz B.,Birchmeier W.,Schmid R.M., Lesina M., Algül, H., Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase. Nat. Med. 2018, 24, 954–960. doi.org/10.1038/s41591-018-0024-8.
Schoene, J., Bel Abed, H., Schmieder, P., Christmann, M., & Nazaré, M., A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus–Silane System. Eur. J. Chem. 2018, 24, 9090–9100. doi.org/10.1002/chem.201800763.
Bel Abed, H., Weißing, N., Schoene, J., Paulus, J., Sewald, N., & Nazaré, M., Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives. Tetrahedron Let. 2018, 59, 1813–1815. doi.org/10.1016/j.tetlet.2018.03.051.
Wenskowsky, L., Schreuder, H., Derdau, V., Matter, H., Volkmar, J., Nazaré, M., Opatz, T., & Petry, S., Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin. Angew. Chem. 2017, 130, 1056–1060. doi.org/10.1002/anie.201710437.
Carter, D. M., Specker, E., Przygodda, J., Neuenschwander, M., von Kries, J. P., Heinemann, U., Nazaré, M., & Gohlke, U., Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells. SLAS Discov. 2017, 22, 801–812. doi.org/10.1177/2472555217699157.
Anumala, U. R., Waaler, J., Nkizinkiko, Y., Ignatev, A., Lazarow, K., Lindemann, P., Olsen, P. A., Murthy, S., Obaji, E., Majouga, A. G., Leonov, S., Von Kries, J. P., Lehtiö, L., Krauss, S., & Nazaré, M., Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach. J. Med. Chem. 2017, 60, 10013–10025. doi.org/10.1021/acs.jmedchem.7b00883.
Liu, Y., Zhang, L., Nazare, M., Yao, Q., & Hu, H. Y., A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging. Acta Pharm. Sin. B. 2018, 8, 401–408. doi.org/10.1016/j.apsb.2017.11.001.
Sun, H., Horatscheck, A., Martos, V., Bartetzko, M., Uhrig, U., Lentz, D., Schmieder, P., & Nazaré, M., Direct Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances. Angew. Chem. 2017, 129, 6554–6558. doi.org/10.1002/ange.201700520.
J. Aretz, J.; Kondoh, Y.; Honda, K.; Anumala, U. R.; Nazaré, M.; Watanabe, N.; Osada, H.; Rademacher, C., Chemical fragment arrays for rapid druggability assessment. Chem. Commun. 2016, 52, 9067-9070. doi.org/10.1039/c5cc10457b.
Kozian, D. H.; von Haeften, E.; Joho, S.; Czechtizky, W.; Anumala, U.R.; Roux, P.; Dudda, A.; Evers, A.; Nazaré, M. Modulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5., ChemBioChem 2016, 17, 861-865. doi.org/10.1002/cbic.201500559.
Bel Abed, H.; Schoene, J.; Christmann, M.; Nazaré, M. Organophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles., Org. Biomol. Chem., 2016, 14, 8520-8528. doi.org/10.1039/c6ob01544.
Geiger, M.-A.; Orwick-Rydmark, M.; Märker, K.; Franks, W. T.; Akhmetzyanov, D.; Stöppler, D.; Zinke, M.; Specker, E.; Nazaré, M.; Diehl, A.; van Rossum, B.-J.; Aussenac, F.; Prisner, T.; Akbey, Ü.; Oschkinat, H. Temperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures. Phys. Chem. Chem. Phys. 2016, 18, 30696-30704. doi.org/10.1039/C6CP06154K.
Robertson, M. J.; Horatscheck, A.; Sauer, S.; von Kleist, L.; Baker, J. R.; Stahlschmidt, W.; Nazaré, M.; Whiting, A.; Chau, N.; Robinson, P. J.; Haucke, V.; McCluskey, A.; 5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors. Org. Biomol. Chem. 2016, 14, 11266-11278. doi.org/10.1039/c6ob02308h.
Halland, N.; Schmidt, F.; Weiss, T.; Saas, J.; Li, Z.; Czech, J.; Dreyer, M.; Hofmeister, A.; Mertsch, K.; Dietz, U.; Strübing, C.; Nazaré, M. Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors. ACS Med. Chem. Lett. 2015, 6, 73-78. doi.org/10.1021/ml5003376.
Hu, H.-Y.; Lim, N.-H.; Ding-Pfennigdorff, D.; Saas, J.; Wendt, U.; Ritzeler, O.; Nagase, H.; Plettenburg, O.; Schultz, C.; Nazaré, M., DOTAM Derivatives as Active Cartilage-targeting Drug Carriers for the Treatment of Osteoarthritis. Bioconj. Chem., 2015, 26, 383-388. https://doi.org/10.1021/bc500557s.
Hu, H.-Y.; Lim, N.-G.; Juretschke, H.-P.; Ding-Pfennigdorff, D.; Florian, P.; Kohlmann, M.; Kandira, A.; Peter von Kries, J.; Saas, J.; Rudolphi, K.-A., Wendt, K. U.; Nagase, H.; Plettenburg, O.; Nazaré, M.; Schultz, C., In vivo visualization of osteoarthritic hypertrophic lesions. Chem. Sci., 2015, 6, 6256-6261. doi.org/10.1039/c5sc01301a.