Nazaré, Marc - Leibniz-Forschungsinstitut für Molekulare Pharmakologie -

研究领域

Our group is focused on developing new chemical tools to answer fundamental biological questions. These tools cover a broad range of applications from modulation of protein-ligand and protein-protein interactions, SAR studies, in order to allow for a deeper understanding of signal transduction pathways, molecular recognition phenomena of particular drug targets and other cellular events. Together with our collaboration partners, the medicinal chemistry group optimizes small molecule hits emerging from screening or from rational drug design approaches. SAR studies and the molecular recognition phenomena underlying protein ligand interactions Synthetic methods to access privileged or novel scaffolds useful in drug discovery

近期论文

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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, early access, https://doi.org/10.1002/anie.202002391. 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, https://doi.org/10.1007/s10822-020-00310-4. 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. 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. 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. 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. 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. 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. 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. 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. Aretz, J.; Anumala, U. R.; Fuchsberger, F. F.; Molavi, N.; Ziebart, N.; Zhang, H.; Nazare, M.; Rademacher, C. Allosteric Inhibition of a Mammalian Lectin. J. Am. Chem. Soc. 2018, 140, 14924-14934. Duro-Castano, A.; Lim, N. H.; Tranchant, I.; Amoura, M.; Beau, F.; Wieland, H.; Kingler, O.; Hermann, M.; Nazare, 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. Mater. 2018, 28, 1802738. Ruess, D. A.; Heynen, G. J.; Ciecielski, K. J.; Ai, J.; Berninger, A.; Kabacaoglu, D.; Görgülü, K.; Dantes, Z.; Wörmann, S. M.; Diakopoulus, K. N.; Karpathaki, M. K.; Kowalska, M.; Kaya-Aksoy; E.; Song, L.; Zeeuw van der Laan, E. A.; López-Alberca, M. P.; Nazaré, M.; Reichert, M.; Saur, D.; Erkan, M. M.; Hopt, U. T.; Sainz Jr, 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. Schoene, J.; Bel Abed, H., Schmieder, P.; Christmann, M.; Nazare, M. A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorous-Silane System. Chem. Eur. J. 2018, 24, 9090-9100. Bel Abed, H.; Weißing, N.; Schoene, J.; Paulus, J.; Sewald, N., Nazare, M. Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives. Tetrahedron Lett. 2018, 59, 1813-1815. 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. Int Ed. 2018, 57, 1044-1048. 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. 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. Griger, J.; Schneider, R.; Lahmann, I.; Schowel, V.; Keller, C.; Spuler, S.; Nazaré, M.; Birchmeier, C. Loss of Ptpn11 (Shp2) drives satellite cells into quiescence. eLife2017, 6, e21552. Schoene, J.; Bel Abed, H.; Christmann, M.; Nazaré, M. A straightforward approach to N-substituted-2H-indazol-2-amines through reductive cyclization. Tetrahedron Lett. 2017, 58, 1633-1635.