Portrait

Prof. Dr.

Marc Nazaré

Head Nazaré Group

 +49 30 94793 581

+49 30 94063 084

 nazare@fmp-berlin.de

0000-0002-1602-2330

Marc Nazare studied chemistry at the University of Karlsruhe and obtained his PhD in organic chemistry with Herbert Waldmann in the field of natural product total synthesis in 1999. He then joined pharmaceutical industry at Sanofi in Frankfurt as a medicinal chemist. In 2013, Dr. Nazaré started a medicinal chemistry group at the Leibniz Research Institute for Molecular Pharmacology FMP. His current research interests are focused on the design and optimization of chemical probes and imaging tools for chemical biology and translational applications. He is a honorary professor at the University Bielefeld.


Chemical Biology


Nazaré Group


FMP
UB

Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.

  • Aebi J; Atz K; Ametamey SM; Benz J; Blaising J; Butini S; Campiani G; Carreira EM; Collin L; De Lago E; Gazzi T; Gertsch J; Gobbi L; Guba W; Grether U

Chimia 2024

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A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand binding assay

  • Borrega-Roman L; Hoare BL; Kosar M; Sarott RC; Patej KJ; Bouma J; Scott-Dennis M; Koers EJ; Gazzi T; Mach L; Barrondo S; Sallés J; Guba W; Kusznir E; Veprintsev DB
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Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB<sub>1</sub>R).

  • Mach L; Omran A; Bouma J; Radetzki S; Sykes DA; Guba W; Li X; Höffelmeyer C; Hentsch A; Gazzi T; Mostinski Y; Wasinska-Kalwa M; de Molnier F; Nazare M

Journal of medicinal chemistry 2024

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DOTA-Based Plectin-1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue.

  • Gazzi T; Lesina M; Wang Q; Berninger A; Radetzki S; Demir IE; Kohlmann L; Meiser W; Wilke S; von Kries JP; Algül H; Hu HY; Nazare M

Angewandte Chemie (International ed. in English) 2024

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An activatable biphotonic lanthanide probe for detection of nitroreductase in live bacteria and cancer cells

  • Carolina Vinagreiro; Qian Liu; Qinghua Wang; Xiang Wang; Hai-Yu Hu; Marc Nazare
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Patent review of cannabinoid receptor type 2 (CB <sub>2</sub> R) modulators (2016-present)

  • Miroslav Kosar; Leonard Mach; Erick M. Carreira; Marc Nazaré; Pal Pacher; Uwe Grether

Expert Opinion on Therapeutic Patents 2024

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Benzo‐Crown‐Ether functionalized O‐BODIPY Probes for Cations– A Selective Fluorescent Probe for Ba2+

  • Thomas Schwarze; Tobias Sprenger; Marc Nazare; Hans-Jürgen Holdt; Axel Hentsch

Chemistry – A European Journal 2024

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Novel Tryptophan Hydroxylase Inhibitor TPT-001 Reverses PAH, Vascular Remodeling, and Proliferative-Proinflammatory Gene Expression

  • Ekaterina Legchenko; Philippe Chouvarine; Fatimunnisa Qadri; Edgar Specker; Marc Nazaré; Radoslaw Wesolowski; Susann Matthes; Michael Bader; Georg Hansmannn

JACC: Basic to Translational Science 2024

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DOTA‐Based Plectin‐1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue

  • Thais Gazzi; Marina Lesina; Qinghua Wang; Alexandra Berninger; Silke Radetzki; Ihsan Ekin Demir; Larissa Kohlmann; Waldemar Meiser; Sebastian Wilke; Jens Peter von Kries; Hana Algül; Hai-Yu Hu; Marc Nazare

Angewandte Chemie 2024

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Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.

  • Specker E; Wesolowski R; Schütz A; Matthes S; Mallow K; Wasinska-Kalwa M; Winkler L; Oder A; Alenina N; Pleimes D; von Kries JP; Heinemann U; Bader M; Nazaré M

Journal of medicinal chemistry 2023

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Discovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis.

  • Yan S; Schöpe PC; Lewis J; Putzker K; Uhrig U; Specker E; von Kries JP; Lindemann P; Omran A; Sanchez-Ibarra HE; Unger A; Zischinsky ML; Klebl B; Stein U

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2023

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Structural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.

  • Kücükdisli M; Bel-Abed H; Cirillo D; Lo WT; Efrém NL; Horatscheck A; Perepelittchenko L; Prokofeva P; Ehret TAL; Radetzki S; Neuenschwander M; Nazaré M

Journal of medicinal chemistry 2023

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Selective and pH-Independent Detection of Ba<sup>2+</sup> in Water by a Benzo-21-crown-7-Functionalized BODIPY.

  • Sprenger T; Schwarze T; Müller H; Sperlich E; Holdt HJ; Nazaré M; Hentsch A; Eidner S; Kraft R; Kumke MU

Chemistry (Weinheim an der Bergstrasse, Germany) 2023

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CLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors.

  • Mucka P; Lindemann P; Bosco B; Willenbrock M; Radetzki S; Neuenschwander M; Brischetto C; Peter von Kries J; Nazaré M; Scheidereit C

Cell chemical biology 2023

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Aβ Chronic Exposure Promotes an Activation State of Microglia through Endocannabinoid Signalling Imbalance.

  • Scipioni L; Tortolani D; Ciaramellano F; Fanti F; Gazzi T; Sergi M; Nazaré M; Oddi S; Maccarrone M

International journal of molecular sciences 2023

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CB2R agonists in the clinics: A treasure chest for treating inflammatory diseases

  • Uwe Grether; Marc Nazaré

Open Access Government 2023

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CB₂R ligands to treat inflammatory diabetes

  • Uwe Grether; Marc Nazaré

Open Access Government 2023

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First<i> in</i><i> vivo</i> fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod

  • Starke, Ludger; Millward, Jason M.; Prinz, Christian; Sherazi, Fatima; Waiczies, Helmar; Lippert, Christoph; Nazare, Marc; Paul, Friedemann; Niendorf, Thoralf; Waiczies, Sonia

Theranostics 2023

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Novel tetrazolopyridazine based MACC1 transcriptional inhibitors as promising anti-metastatic therapy

  • Schope, Paul Curtis; Yan, Shixian; Kobelt, Dennis; Lewis, Joe; Putzker, Kerstin; Uhrig, Ulrike; Specker, Edgar; von Kries, Jens Peter; Dahlmann, Mathias; Sanchez-Ibarra, Hector E.; Unger, Anke; Zischinsky, Mia-Lisa; Klebl, Bert; Lindemann, Peter; Walther, Wolfgang; Nazare, Marc; Stein, Ulrike

Cancer Research 2023

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Isoform-selective targeting of PI3K: time to consider new opportunities?

  • Cirillo, Davide; Diceglie, Marta; Nazare, Marc

Trends in Pharmacological Sciences 2023

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Small molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation

  • Jordan, Philipp; Costa, Amanda; Specker, Edgar; Popp, Oliver; Volkamer, Andrea; Piske, Regina; Obrusnik, Tessa; Kleissle, Sabrina; Stuke, Kevin; Rex, Andre; Neuenschwander, Martin; von Kries, Jens Peter; Nazare, Marc; Mertins, Phillip; Kettenmann, Helmut; Wolf, Susanne A.

Plos One 2023

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Development of selective inhibitors of phosphatidylinositol 3-kinase C2α

  • Lo, Wen-Ting; Belabed, Hassane; Kuecuekdisli, Murat; Metag, Juliane; Roske, Yvette; Prokofeva, Polina; Ohashi, Yohei; Horatscheck, Andre; Cirillo, Davide; Krauss, Michael; Schmied, Christopher; Neuenschwander, Martin; von Kries, Jens Peter; Medard, Guillaume; Kuster, Bernhard; Perisic, Olga; Williams, Roger L.; Daumke, Oliver; Payrastre, Bernard; Severin, Sonia; Nazare, Marc; Haucke, Volker

Nature Chemical Biology 2023

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An LPAR <sub><b>5</b></sub> -antagonist that reduces nociception and increases pruriception.

  • Langedijk J; Araya EI; Barroso AR; Tolenaars D; Nazaré M; Belabed H; Schoene J; Chichorro JG; Oude Elferink R

Frontiers in pain research (Lausanne, Switzerland) 2022

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Donor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles

  • Liu, Qian; Yang, Miao; Meng, Xiangchuan; Han, Xiaowan; Nazare, Marc; Xu, Youjun; Hu, Hai-Yu; Zhang, Qingyang

Talanta 2022

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Reverse Design toward Optimized Labeled Chemical Probes - Examples from the Endocannabinoid System

  • Guberman, Monica; Kosar, Miroslav; Omran, Anahid; Carreira, Erick M.; Nazare, Marc; Grether, Uwe

Chimia 2022

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Antagonistic control of active surface integrins by myotubularin and phosphatidylinositol 3-kinase C2β in a myotubular myopathy model

  • Samso, Paula; Koch, Philipp A.; Posor, York; Lo, Wen-Ting; Belabed, Hassane; Nazare, Marc; Laporte, Jocelyn; Haucke, Volker

Proceedings of the National Academy of Sciences 2022

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Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors

  • Specker, Edgar; Matthes, Susann; Wesolowski, Radoslaw; Schuetz, Anja; Grohmann, Maik; Alenina, Natalia; Pleimes, Dirk; Mallow, Keven; Neuenschwander, Martin; Gogolin, Angelina; Weise, Marie; Pfeifer, Jochen; Ziebart, Nandor; Heinemann, Udo; von Kries, Jens Peter; Nazare, Marc; Bader, Michael

Journal of Medicinal Chemistry 2022

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Weizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+Probability and CASE-3D

  • Li, Xiao-Lu; Ru, Tong; Navarro-Vazquez, Armando; Lindemann, Peter; Nazare, Marc; Li, Xu-Wen; Guo, Yue-Wei; Sun, Han

Journal of Natural Products 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin

  • Zhang, Hengxi; Modenutti, Carlos; Nekkanti, Yelha Phani Kumar; Denis, Maxime; Bermejo, Iris A. .; Lefebre, Jonathan; Che, Kateryna; Kim, Dongyoon; Kagelmacher, Marten; Kurzbach, Dennis; Nazare, Marc; Rademacher, Christoph

ACS Chemical Biology 2022

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Phosphoinositide Conversion Inactivates R-RAS and Drives Metastases in Breast Cancer

  • Li, Huayi; Prever, Lorenzo; Hsu, Myriam Y.; Lo, Wen-Ting; Margaria, Jean Piero; De Santis, Maria Chiara; Zanini, Cristina; Forni, Marco; Novelli, Francesco; Pece, Salvatore; Di Fiore, Pier Paolo; Porporato, Paolo Ettore; Martini, Miriam; Belabed, Hassane; Nazare, Marc; Haucke, Volker; Gulluni, Federico; Hirsch, Emilio

Advanced Science 2022

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BODIPY-Equipped Benzo-Crown-Ethers as Fluorescent Sensors for pH Independent Detection of Sodium and Potassium Ions

  • Sprenger, Tobias; Schwarze, Thomas; Mueller, Holger; Sperlich, Eric; Kelling, Alexandra; Holdt, Hans-Juergen; Paul, Jerome; Riano, Vera Martos; Nazare, Marc

ChemPhotoChem 2022

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Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe

  • Gazzi, Thais; Brennecke, Benjamin; Atz, Kenneth; Korn, Claudia; Sykes, David; Forn-Cuni, Gabriel; Pfaff, Patrick; Sarott, Roman C.; Westphal, Matthias, V; Mostinski, Yelena; Mach, Leonard; Wasinska-Kalwa, Malgorzata; Weise, Marie; Hoare, Bradley L.; Miljus, Tamara; Mexi, Maira; Roth, Nicolas; Koers, Eline J.; Guba, Wolfgang; Alker, Andre; Rufer, Arne C.; Kusznir, Eric A.; Huber, Sylwia; Raposo, Catarina; Zirwes, Elisabeth A.; Osterwald, Anja; Pavlovic, Anto; Moes, Svenja; Beck, Jennifer; Nettekoven, Matthias; Benito-Cuesta, Irene; Grande, Teresa; Drawnel, Faye; Widmer, Gabriella; Holzer, Daniela; van der Wel, Tom; Mandhair, Harpreet; Honer, Michael; Fingerle, Jurgen; Scheffel, Joerg; Broichhagen, Johannes; Gawrisch, Klaus; Romero, Julian; Hillard, Cecilia J.; Varga, Zoltan V.; van der Stelt, Mario; Pacher, Pal; Gertsch, Jurg; Ullmer, Christoph; McCormick, Peter J.; Oddi, Sergio; Spaink, Herman P.; Maccarrone, Mauro; Veprintsev, Dmitry B.; Carreira, Erick M.; Grether, Uwe; Nazare, Marc

Chemical Science 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the Lectin Langerin

  • Zhang, Hengxi; Modenutti, Carlos; Nekkanti, Yelha Phani Kumar; Denis, Maxime; Bermejo, Iris A.; Lefebre, Jonathan; Che, Kateryna; Kim, Dongyoon; Kagelmacher, Marten; Kurzbach, Dennis; Nazare, Marc; Rademacher, Christoph

ACS Chemical Biology 2022

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Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands

  • Fernandez-Bachiller, Maria Isabel; Hwang, Songhwan; Schembri, Maria Elena; Lindemann, Peter; Guberman, Monica; Herziger, Svenja; Specker, Edgar; Matter, Hans; Will, David W.; Czech, Jorg; Wagner, Michael; Bauer, Armin; Schreuder, Herman; Ritter, Kurt; Urmann, Matthias; Wehner, Volkmar; Sun, Han; Nazare, Marc

Journal of Medicinal Chemistry 2022

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Compound Interaction Screen on a Photoactivatable Cellulose Membrane (CISCM) Identifies Drug Targets

  • Melder, F. Teresa, I; Lindemann, Peter; Welle, Alexander; Trouillet, Vanessa; Heissler, Stefan; Nazare, Marc; Selbach, Matthias

ChemMedChem 2022

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Rational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis

  • Halland, Nis; Schmidt, Friedemann; Weiss, Tilo; Li, Ziyu; Czech, Jorg; Saas, Joachim; Ding-Pfennigdorff, Danping; Dreyer, Matthias K.; Strubing, Carsten; Nazare, Marc

Journal of Medicinal Chemistry 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin

  • Hengxi Zhang; Carlos Modenutti; N. Y. Phani Kumar; Maxime Denis; Iris Bermejo; Jonathan Lefebre; Kateryna Che; Dongyoon Kim; Marten Kagelmacher; Dennis Kurzbach; Marc Nazare; Christoph Rademacher

OpenAlex 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin

  • Hengxi Zhang; Carlos Modenutti; N. Y. Phani Kumar; Maxime Denis; Iris Bermejo; Jonathan Lefebre; Kateryna Che; Dongyoon Kim; Marten Kagelmacher; Dennis Kurzbach; Marc Nazare; Christoph Rademacher

OpenAlex 2022

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In vivo detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy

  • Prinz, Christian; Starke, Ludger; Millward, Jason M.; Fillmer, Ariane; Delgado, Paula Ramos; Waiczies, Helmar; Pohlmann, Andreas; Rothe, Michael; Nazare, Marc; Paul, Friedemann; Niendorf, Thoralf; Waiczies, Sonia

Theranostics 2021

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Cannabinoid receptor type 2 ligands: an analysis of granted patents since 2010

  • Brennecke, Benjamin; Gazzi, Thais; Atz, Kenneth; Fingerle, Jurgen; Kuner, Pascal; Schindler, Torsten; de Weck, Guy; Nazare, Marc; Grether, Uwe

Pharmaceutical Patent Analyst 2021

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Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer

  • Carter, David M.; Specker, Edgar; Malecki, Piotr H.; Przygodda, Jessica; Dudaniec, Krystyna; Weiss, Manfred S.; Heinemann, Udo; Nazare, Marc; Gohlke, Ulrich

Journal of Medicinal Chemistry 2021

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Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

  • Leenders, Ruben G. G.; Brinch, Shoshy Alam; Sowa, Sven T.; Amundsen-Isaksen, Enya; Galera-Prat, Albert; Murthy, Sudarshan; Aertssen, Sjoerd; Smits, Johannes N.; Nieczypor, Piotr; Damen, Eddy; Wegert, Anita; Nazare, Marc; Lehtio, Lari; Waaler, Jo; Krauss, Stefan

Journal of Medicinal Chemistry 2021

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Topical inflammasome inhibition with disulfiram prevents irritant contact dermatitis

  • Bonnekoh, Hanna; Vera, Carolina; Abad-Perez, Angela; Radetzki, Silke; Neuenschwander, Martin; Specker, Edgar; Mahnke, Niklas Amadeus; Frischbutter, Stefan; Latz, Eicke; Nazare, Marc; Kries, Jens V.; Maurer, Marcus; Scheffel, Joerg; Krause, Karoline

Clinical and Translational Allergy 2021

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Functional Imaging Using Fluorine (F-19) MR Methods: Basic Concepts

  • Waiczies, Sonia; Prinz, Christian; Starke, Ludger; Millward, Jason M.; Delgado, Paula Ramos; Rosenberg, Jens; Nazare, Marc; Waiczies, Helmar; Pohlmann, Andreas; Niendorf, Thoralf

Methods in Molecular Biology 2021

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Structural Basis for Gating of the Two-Pore Domain K+ (K-2P) Channels TASK-1 and TALK-2

  • Schewe, Marcus; Riel, Elena B.; Rinne, Susanne; Kopec, Wojciech; Langer, Jan; Lindemann, Peter; Juers, Bjoern C.; Nazare, Marc; de Groot, Bert L.; Decher, Niels; Baukrowitz, Thomas

Biophysical Journal 2021

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DOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells

  • Brennecke, Benjamin; Wang, Qinghua; Haap, Wolfgang; Grether, Uwe; Hu, Hai-Yu; Nazare, Marc

Bioconjugate Chemistry 2021

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Pentafluorosulfanyl (SF<sub>5</sub>) as a Superior <SUP>19</SUP>F Magnetic Resonance Reporter Group: Signal Detection and Biological Activity of Teriflunomide Derivatives

  • Prinz, Christian; Starke, Ludger; Ramspoth, Tizian-Frank; Kerkering, Janis; Riano, Vera Martos; Paul, Jerome; Neuenschwander, Martin; Oder, Andreas; Radetzki, Silke; Adelhoefer, Siegfried; Delgado, Paula Ramos; Aravina, Mariya; Millward, Jason M.; Fillmer, Ariane; Paul, Friedemann; Siffrin, Volker; Von Kries, Jens-Peter; Niendorf, Thoralf; Nazare, Marc; Waiczies, Sonia

ACS Sensors 2021

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Generation of a TR-FRET-based assay for the determination of cannabinoid CB1 receptor ligand binding kinetics

  • Borrega, Leire; Hoare, Brad; Gazzi, Thais; Nazare, Marc; Grether, Uwe; Sykes, David; Veprintsev, Dmitry

British Journal of Pharmacology 2021

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Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor

  • Waaler, Jo; Leenders, Ruben G. G.; Sowa, Sven T.; Brinch, Shoshy Alam; Lycke, Max; Nieczypor, Piotr; Aertssen, Sjoerd; Murthy, Sudarshan; Galera-Prat, Albert; Damen, Eddy; Wegert, Anita; Nazare, Marc; Lehtio, Lari; Krauss, Stefan

Journal of Medicinal Chemistry 2020

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Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells

  • Barone, Matthias; Mueller, Matthias; Chiha, Slim; Ren, Jiang; Albat, Dominik; Soicke, Arne; Dohmen, Stephan; Klein, Marco; Bruns, Judith; van Dinther, Maarten; Opitz, Robert; Lindemann, Peter; Beerbaum, Monika; Motzny, Kathrin; Roske, Yvette; Schmieder, Peter; Volkmer, Rudolf; Nazare, Marc; Heinemann, Udo; Oschkinat, Hartmut; ten Dijke, Peter; Schmalz, Hans-Guenther; Kuehne, Ronald

Proceedings of the National Academy of Sciences 2020

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Development and application of a kinetic ligand binding assay for the cannabinoid receptor 1 using resonance energy transfer approaches

  • Hoare, Bradley; Sykes, David; Gazzi, Thais; Nazare, Marc; Grether, Uwe; Veprintsev, Dmitry

British Journal of Pharmacology 2020

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From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement

  • Mostinski, Yelena; Heynen, Guus J. J. E.; Lopez-Alberca, Maria Pascual; Paul, Jerome; Miksche, Sandra; Radetzki, Silke; Schaller, David; Shanina, Elena; Seyffarth, Carola; Kolomeets, Yuliya; Ziebart, Nandor; de Schryver, Judith; Oestreich, Sylvia; Neuenschwander, Martin; Roske, Yvette; Heinemann, Udo; Rademacher, Christoph; Volkamer, Andrea; von Kries, Jens Peter; Birchmeier, Walter; Nazare, Marc

Journal of Medicinal Chemistry 2020

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Revealing cytotoxic substructures in molecules using deep learning

  • Webel, Henry E.; Kimber, Talia B.; Radetzki, Silke; Neuenschwander, Martin; Nazare, Marc; Volkamer, Andrea

Journal of Computer-Aided Molecular Design 2020

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NMR quality control of fragment libraries for screening

  • Sreeramulu, Sridhar; Richter, Christian; Kuehn, Till; Azzaoui, Kamal; Blommers, Marcel Jules Jose; Del Conte, Rebecca; Fragai, Marco; Trieloff, Nils; Schmieder, Peter; Nazare, Marc; Specker, Edgar; Ivanov, Vladimir; Oschkinat, Hartmut; Banci, Lucia; Schwalbe, Harald

Journal of Biomolecular NMR 2020

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Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells

  • Sarott, Roman C.; Westphal, Matthias, V; Pfaff, Patrick; Korn, Claudia; Sykes, David A.; Gazzi, Thais; Brennecke, Benjamin; Atz, Kenneth; Weise, Marie; Mostinski, Yelena; Hompluem, Pattarin; Koers, Eline; Miljus, Tamara; Roth, Nicolas J.; Asmelash, Hermon; Vong, Man C.; Piovesan, Jacopo; Guba, Wolfgang; Rufer, Arne C.; Kusznir, Eric A.; Huber, Sylwia; Raposo, Catarina; Zirwes, Elisabeth A.; Osterwald, Anja; Pavlovic, Anto; Moes, Svenja; Beck, Jennifer; Benito-Cuesta, Irene; Grande, Teresa; de Martin Esteban, Samuel Ruiz; Yeliseev, Alexei; Drawnel, Faye; Widmer, Gabriella; Holzer, Daniela; van der Wel, Tom; Mandhair, Harpreet; Yuan, Cheng-Yin; Drobyski, William R.; Saroz, Yurii; Grimsey, Natasha; Honer, Michael; Fingerle, Juergen; Gawrisch, Klaus; Romero, Julian; Hillard, Cecilia J.; Varga, Zoltan V.; van der Stelt, Mario; Pacher, Pal; Gertsch, Juerg; McCormick, Peter J.; Ullmer, Christoph; Oddi, Sergio; Maccarrone, Mauro; Veprintsev, Dmitry B.; Nazare, Marc; Grether, Uwe; Carreira, Erick M.

Journal of the American Chemical Society 2020

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Diverse chemotypes drive biased signaling by cannabinoid receptors

  • Miljuš T; Heydenreich FM; Gazzi T; Kimbara A; Rogers-Evans M; Nettekoven M; Zirwes E; Osterwald A; Rufer AC; Ullmer C; Guba W; Le Gouill C; Veprintsev DB
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Dual-Mode Detection of Bacterial 16S Ribosomal RNA in Tissues

  • Shengnan Xu; Qingyang Zhang; Xiaowan Han; Yali Wang; Xiang Wang; Marc Nazare; Jian-Dong Jiang; Hai-Yu Hu

ACS Sensors 2020

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Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie 2020

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Back Cover: An Activatable Lanthanide Luminescent Probe for Time‐Gated Detection of Nitroreductase in Live Bacteria (Angew. Chem. Int. Ed. 22/2020)

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie International Edition 2020

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Rücktitelbild: Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien (Angew. Chem. 22/2020)

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie 2020

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A Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles

  • Alsalim, Rana; Lindemann, Peter; Lopez-Alberca, Maria Pascual; Miksche, Sandra; Czechtizky, Werngard; Halland, Nis; Nazare, Marc

Organic Letters 2020

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An Activatable Lanthanide Luminescent Probe for Time-Gated Detection of Nitroreductase in Live Bacteria

  • Brennecke, Benjamin; Wang, Qinghua; Zhang, Qingyang; Hu, Hai-Yu; Nazare, Marc

Angewandte Chemie International Edition 2020

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Preclinical efficacy of NLRP3 small molecule inflammasome inhibitors: Implications for future treatment of autoinflammatory syndromes

  • Abad-Perez, A.; Frischbutter, S.; Mahnke, N. A.; Kries, J. V.; Nazare, M.; Maurer, M.; Scheffel, J.; Krause, K.

Experimental Dermatology 2019

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Topical inflammasome inhibition-a novel treatment strategy for contact dermatitis

  • Bonnekoh, H.; Vera, C.; Abad-Perez, A.; van Kries, J.; Nazare, M.; Mahnke, N. A.; Maurer, M.; Scheffel, J.; Krause, K.

Experimental Dermatology 2019

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Probing 2<i>H</i>-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors

  • Schoene, Jens; Gazzi, Thais; Lindemann, Peter; Christmann, Mathias; Volkamer, Andrea; Nazare, Marc

ChemMedChem 2019

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Small-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells

  • Marc Nazaré

Frontiers in Cellular Neuroscience 2019

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A New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves' Orbitopathy

  • Marcinkowski, Patrick; Hoyer, Inna; Specker, Edgar; Furkert, Jens; Rutz, Claudia; Neuenschwander, Martin; Sobottka, Sebastian; Sun, Han; Nazare, Marc; Berchner-Pfannschmidt, Utta; Von kries, Jens Peter; Eckstein, Anja; Schuelein, Ralf; Krause, Gerd

Thyroid 2019

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EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

  • Brennecke, Philip; Rasina, Dace; Aubi, Oscar; Herzog, Katja; Landskron, Johannes; Cautain, Bastien; Vicente, Francisca; Quintana, Jordi; Mestres, Jordi; Stechmann, Bahne; Ellinger, Bernhard; Brea, Jose; Kolanowski, Jacek L.; Pilarski, Radoslaw; Orzaez, Mar; Pineda-Lucena, Antonio; Laraia, Luca; Nami, Faranak; Zielenkiewicz, Piotr; Paruch, Kamil; Hansen, En; von Kries, Jens P.; Neuenschwander, Martin; Specker, Edgar; Bartunek, Petr; Simova, Sarka; Lesnikowski, Zbigniew; Krauss, Stefan; Lehtio, Lari; Bilitewski, Ursula; Broenstrup, Mark; Tasken, Kjetil; Jirgensons, Aiprs; Lickert, Heiko; Clausen, Mads H.; Andersen, Jeanette H.; Vicent, Maria J.; Genilloud, Olga; Martinez, Aurora; Nazare, Marc; Fecke, Wolfgang; Gribbon, Philip

SLAS Discovery: Advancing Life Sciences R & D 2019

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A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels

  • Schewe, Marcus; Sun, Han; Mert, Umit; Mackenzie, Alexandra; Pike, Ashley C. W.; Schulz, Friederike; Constantin, Cristina; Vowinkel, Kirsty S.; Conrad, Linus J.; Kiper, Aytug K.; Gonzalez, Wendy; Musinszki, Marianne; Tegtmeier, Marie; Pryde, David C.; Belabed, Hassane; Nazare, Marc; de Groot, Bert L.; Decher, Niels; Fakler, Bernd; Carpenter, Elisabeth P.; Tucker, Stephen J.; Baukrowitz, Thomas

Science 2019

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Rapid Synthesis of gamma-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen

  • Zhang, Qingyang; Xu, Shengnan; Lai, Fangfang; Wang, Yali; Zhang, Na; Nazare, Marc; Hu, Hai-Yu

Organic Letters 2019

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Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin

  • Wenskowsky, Lea; Schreuder, Herman; Derdau, Volker; Matter, Hans; Volkmar, Julia; Nazare, Marc; Opatz, Till; Petry, Stefan

Angewandte Chemie International Edition 2018

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A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging

  • Liu, Yun; Zhang, Leilei; Nazare, Marc; Yao, Qingqiang; Hu, Hai-Yu

Acta Pharmaceutica Sinica B 2018

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Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase

  • Ruess, Dietrich A.; Heynen, Guus J.; Ciecielski, Katrin J.; Ai, Jiaoyu; Berninger, Alexandra; Kabacaoglu, Derya; Goerguelue, Kivanc; Dantes, Zahra; Woermann, Sonja M.; Diakopoulos, Kalliope N.; Karpathaki, Angeliki F.; Kowalska, Marlena; Kaya-Aksoy, Ezgi; Song, Liang; van der Laan, Eveline A. Zeeuw; Lopez-Alberca, Maria P.; Nazare, Marc; Reichert, Maximilian; Saur, Dieter; Erkan, Mert M.; Hopt, Ulrich T.; Sainz, Bruno, Jr.; Birchmeier, Walter; Schmid, Roland M.; Lesina, Marina; Alguel, Hana

Nature Medicine 2018

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Allosteric Inhibition of a Mammalian Lectin

  • Aretz, Jonas; Anumala, Upendra R.; Fuchsberger, Felix F.; Molavi, Narges; Ziebart, Nandor; Zhang, Hengxi; Nazare, Marc; Rademacher, Christoph

Journal of the American Chemical Society 2018

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In Vivo Imaging of MMP-13 Activity Using a Specific Polymer-FRET Peptide Conjugate Detects Early Osteoarthritis and Inhibitor Efficacy

  • Duro-Castano, Aroa; Lim, Ngee Han; Tranchant, Isabelle; Amoura, Mehdi; Beau, Fabrice; Wieland, Heike; Kingler, Otmar; Herrmann, Matthias; Nazare, Marc; Plettenburg, Oliver; Dive, Vincent; Vicent, Maria J.; Nagase, Hideaki

Advanced Functional Materials 2018

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A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System

  • Schoene, Jens; Bel Abed, Hassen; Schmieder, Peter; Christmann, Mathias; Nazare, Marc

Chemistry - A European Journal 2018

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CellFy: A Cell-Based Fragment Screen against C-Type Lectins

  • Schulze, Jessica; Baukmann, Hannes; Wawrzinek, Robert; Fuchsberger, Felix F.; Specker, Edgar; Aretz, Jonas; Nazare, Marc; Rademacher, Christoph

ACS Chemical Biology 2018

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Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway

  • Klein, Wolfgang; Rutz, Claudia; Eckhard, Jamina; Provinciael, Becky; Specker, Edgar; Neuenschwander, Martin; Kleinau, Gunnar; Scheerer, Patrick; von Kries, Jens-Peter; Nazare, Marc; Vermeire, Kurt; Schuelein, Ralf

Plos One 2018

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Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives

  • Abed, Hassen Bel; Weissing, Nils; Schoene, Jens; Paulus, Jannik; Sewald, Norbert; Nazare, Marc

Tetrahedron Letters 2018

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Regulation of Two-pore Domain K plus Channels by Natural Effectors and Pharmacological Agents

  • Schewe, M.; Schulz, F.; Mert, U.; Sun, H.; Belabed, H.; Musinszki, M.; Koehler, T.; Tegtmeier, M.; Nazare, M.; Carpenter, E. P.; Tucker, S. J.; Baukrowitz, T.

Acta Physiologica 2017

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A straightforward approach to N-substituted-2H-indazol-2-amines through reductive cyclization

  • Schoene, Jens; Abed, Hassen Bel; Christmann, Mathias; Nazare, Marc

Tetrahedron Letters 2017

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Novel compounds targeting microglial nitric oxide release

  • Jordan, P.; Wolf, S. A.; Specker, E.; Nazare, M.; Kettenmann, H.

Glia 2017

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N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals

  • Marc Nazaré

Official Gazette of the United States Patent and Trademark Office Patents 2017

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Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells

  • Carter, David M.; Specker, Edgar; Przygodda, Jessica; Neuenschwander, Martin; von Kries, Jens Peter; Heinemann, Udo; Nazare, Marc; Gohlke, Ulrich

SLAS Discovery: Advancing Life Sciences R & D 2017

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Direct Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances

  • Han Sun; André Horatscheck; Vera Martos; Max Bartetzko; Ulrike Uhrig; Dieter Lentz; Peter Schmieder; Marc Nazaré

Angewandte Chemie 2017

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A conserved drug-binding site controls the selectivity filter gate in K2P K+ channels

  • Schewer, M.; Schulz, F.; Mert, Ue.; Sun, H.; Koehler, T.; Tegtmeier, M.; Musinszki, M.; Belabed, H.; Nazare, M.; Tucker, S. J.; Baukrowitz, T.

Acta Physiologica 2017

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Loss of Ptpn11 (Shp2) drives satellite cells into quiescence

  • Griger, Joscha; Schneider, Robin; Lahmann, Ines; Schoewel, Verena; Keller, Charles; Spuler, Simone; Nazare, Marc; Birchmeier, Carmen

eLife 2017

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Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach

  • Anumala, Upendra Rao; Waaler, Jo; Nkizinkiko, Yves; Ignatev, Alexander; Lazarow, Katina; Lindemann, Peter; Olsen, Petter Angell; Murthy, Sudarshan; Obaii, Ezeogo; Majouga, Alexander G.; Leonov, Sergey; von Kries, Jens Peter; Lehtio, Lari; Krauss, Stefan; Nazare, Marc

Journal of Medicinal Chemistry 2017

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Temperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures

  • Geiger, Michel-Andreas; Orwick-Rydmark, Marcella; Marker, Katharina; Franks, W. Trent; Akhmetzyanov, Dmitry; Stoppler, Daniel; Zinke, Maximilian; Specker, Edgar; Nazare, Marc; Diehl, Anne; van Rossum, Barth-Jan; Aussenac, Fabien; Prisner, Thomas; Akbey, Umit; Oschkinat, Hartmut

Physical Chemistry Chemical Physics 2016

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5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors

  • Robertson, Mark J.; Horatscheck, Andre; Sauer, Samantha; von Kleist, Lisa; Baker, Jennifer R.; Stahlschmidt, Wiebke; Nazare, Marc; Whiting, Ainslie; Chau, Ngoc; Robinson, Phillip J.; Haucke, Volker; McCluskey, Adam

Organic & Biomolecular Chemistry 2016

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Pyrazole derivatives and their use as LPAR5 antagonists

  • Marc Nazaré

Official Gazette of the United States Patent and Trademark Office Patents 2016

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ChemInform Abstract: Organophosphorus-Mediated N-N Bond Formation: Facile Access to 3-Amino-2H-indazoles

  • Hassen Bel Abed; Jens Schoene; Mathias Christmann; Marc Nazare

ChemInform 2016

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Pharmacological targeting of human tryptophan hydroxylase - novel inhibitors for the treatment of serotonin-related diseases

  • Matthes, S.; Specker, E.; Schuetz, A.; Grohmann, M.; von Kries, J.; Nazare, M.; Bader, M.

Naunyn-Schmiedeberg's Archives of Pharmacology 2016

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Modulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5

  • Kozian, Detlef H.; von Haeften, Elisabeth; Joho, Sabrina; Czechtizky, Werngard; Anumala, Upendra R.; Roux, Pascale; Dudda, Angela; Evers, Andreas; Nazare, Marc

Chembiochem 2016

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Organophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles

  • Abed, Hassen Bel; Schoene, Jens; Christmann, Mathias; Nazare, Marc

Organic & Biomolecular Chemistry 2016

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Chemical fragment arrays for rapid druggability assessment

  • Aretz, J.; Kondoh, Y.; Honda, K.; Anumala, U. R.; Nazare, M.; Watanabe, N.; Osada, H.; Rademacher, C.

Chemical Communications 2016

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Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes

  • Marc Nazaré; Hans Matter; David W. Will; Michael Wagner; Matthias Urmann; Jörg Czech; Herman Schreuder; Armin Bauer; Kurt Ritter; Volkmar Wehner

Angewandte Chemie 2011

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Innenrücktitelbild: Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes (Angew. Chem. 4/2012)

  • Marc Nazaré; Hans Matter; David W. Will; Michael Wagner; Matthias Urmann; Jörg Czech; Herman Schreuder; Armin Bauer; Kurt Ritter; Volkmar Wehner

Angewandte Chemie 2011

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ChemInform Abstract: A General and Mild Domino Approach to Substituted 1-Aminoindoles

  • Nis Halland; Marc Nazare; Jorge Alonso; Omar R'kyek; Andreas Lindenschmidt

ChemInform 2011

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ChemInform Abstract: A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines

  • Jorge Alonso; Nis Halland; Marc Nazare; Omar R'kyek; Matthias Urmann; Andreas Lindenschmidt

ChemInform 2011

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A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines

  • Alonso, Jorge; Halland, Nis; Nazare, Marc; R'kyek, Omar; Urmann, Matthias; Lindenschmid, Andreas

European Journal of Organic Chemistry 2011

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A general and mild domino approach to substituted 1-aminoindoles

  • Halland, Nis; Nazare, Marc; Alonso, Jorge; R'kyek, Omar; Lindenschmidt, Andreas

Chemical Communications 2011

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Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand

  • Nazare, M; Essrich, M; Will, DW; Matter, H; Ritter, K; Urmann, M; Bauer, A; Schreuder, H; Czech, J; Lorenz, M; Laux, V; Wehner, V

Bioorganic & Medicinal Chemistry Letters 2004

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Novel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Ligand

  • Marc Nazare; et al. et al.

ChemInform 2004

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Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents

  • Marc Nazare; et al. et al.

ChemInform 2004

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Eine flexible, palladiumkatalysierte Indol- und Azaindolsynthese durch direkte Anellierung von Chloranilinen und Chloraminopyridinen mit Ketonen

  • Marc Nazaré; Claudia Schneider; Andreas Lindenschmidt; David William Will

Angewandte Chemie 2004

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A Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones

  • Marc Nazare; Claudia Schneider; Andreas Lindenschmidt; David William Will

ChemInform 2004

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Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand

  • Nazare, M; Matter, H; Klingler, O; Al-Obeidi, F; Schreuder, H; Zoller, G; Czech, J; Lorenz, M; Dudda, A; Peyman, A; Nestler, HP; Urmann, M; Bauer, A; Laux, V; Wehner, V; Will, DW

Bioorganic & Medicinal Chemistry Letters 2004

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Flexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones

  • Nazare, M; Schneider, C; Lindenschmidt, A; Will, DW

Angewandte Chemie International Edition 2004

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Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral PI substituents

  • Nazare, M; Essrich, M; Will, DW; Matter, H; Ritter, K; Urmann, M; Bauer, A; Schreuder, H; Dudda, A; Czech, J; Lorenz, M; Laux, V; Wehner, V

Bioorganic & Medicinal Chemistry Letters 2004

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Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.

  • Aebi J; Atz K; Ametamey SM; Benz J; Blaising J; Butini S; Campiani G; Carreira EM; Collin L; De Lago E; Gazzi T; Gertsch J; Gobbi L; Guba W; Grether U

Chimia 2024

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A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand binding assay

  • Borrega-Roman L; Hoare BL; Kosar M; Sarott RC; Patej KJ; Bouma J; Scott-Dennis M; Koers EJ; Gazzi T; Mach L; Barrondo S; Sallés J; Guba W; Kusznir E; Veprintsev DB
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Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB<sub>1</sub>R).

  • Mach L; Omran A; Bouma J; Radetzki S; Sykes DA; Guba W; Li X; Höffelmeyer C; Hentsch A; Gazzi T; Mostinski Y; Wasinska-Kalwa M; de Molnier F; Nazare M

Journal of medicinal chemistry 2024

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DOTA-Based Plectin-1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue.

  • Gazzi T; Lesina M; Wang Q; Berninger A; Radetzki S; Demir IE; Kohlmann L; Meiser W; Wilke S; von Kries JP; Algül H; Hu HY; Nazare M

Angewandte Chemie (International ed. in English) 2024

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An activatable biphotonic lanthanide probe for detection of nitroreductase in live bacteria and cancer cells

  • Carolina Vinagreiro; Qian Liu; Qinghua Wang; Xiang Wang; Hai-Yu Hu; Marc Nazare
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Patent review of cannabinoid receptor type 2 (CB <sub>2</sub> R) modulators (2016-present)

  • Miroslav Kosar; Leonard Mach; Erick M. Carreira; Marc Nazaré; Pal Pacher; Uwe Grether

Expert Opinion on Therapeutic Patents 2024

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Benzo‐Crown‐Ether functionalized O‐BODIPY Probes for Cations– A Selective Fluorescent Probe for Ba2+

  • Thomas Schwarze; Tobias Sprenger; Marc Nazare; Hans-Jürgen Holdt; Axel Hentsch

Chemistry – A European Journal 2024

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Novel Tryptophan Hydroxylase Inhibitor TPT-001 Reverses PAH, Vascular Remodeling, and Proliferative-Proinflammatory Gene Expression

  • Ekaterina Legchenko; Philippe Chouvarine; Fatimunnisa Qadri; Edgar Specker; Marc Nazaré; Radoslaw Wesolowski; Susann Matthes; Michael Bader; Georg Hansmannn

JACC: Basic to Translational Science 2024

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DOTA‐Based Plectin‐1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue

  • Thais Gazzi; Marina Lesina; Qinghua Wang; Alexandra Berninger; Silke Radetzki; Ihsan Ekin Demir; Larissa Kohlmann; Waldemar Meiser; Sebastian Wilke; Jens Peter von Kries; Hana Algül; Hai-Yu Hu; Marc Nazare

Angewandte Chemie 2024

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Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.

  • Specker E; Wesolowski R; Schütz A; Matthes S; Mallow K; Wasinska-Kalwa M; Winkler L; Oder A; Alenina N; Pleimes D; von Kries JP; Heinemann U; Bader M; Nazaré M

Journal of medicinal chemistry 2023

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Discovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis.

  • Yan S; Schöpe PC; Lewis J; Putzker K; Uhrig U; Specker E; von Kries JP; Lindemann P; Omran A; Sanchez-Ibarra HE; Unger A; Zischinsky ML; Klebl B; Stein U

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2023

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Structural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.

  • Kücükdisli M; Bel-Abed H; Cirillo D; Lo WT; Efrém NL; Horatscheck A; Perepelittchenko L; Prokofeva P; Ehret TAL; Radetzki S; Neuenschwander M; Nazaré M

Journal of medicinal chemistry 2023

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Selective and pH-Independent Detection of Ba<sup>2+</sup> in Water by a Benzo-21-crown-7-Functionalized BODIPY.

  • Sprenger T; Schwarze T; Müller H; Sperlich E; Holdt HJ; Nazaré M; Hentsch A; Eidner S; Kraft R; Kumke MU

Chemistry (Weinheim an der Bergstrasse, Germany) 2023

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CLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors.

  • Mucka P; Lindemann P; Bosco B; Willenbrock M; Radetzki S; Neuenschwander M; Brischetto C; Peter von Kries J; Nazaré M; Scheidereit C

Cell chemical biology 2023

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Aβ Chronic Exposure Promotes an Activation State of Microglia through Endocannabinoid Signalling Imbalance.

  • Scipioni L; Tortolani D; Ciaramellano F; Fanti F; Gazzi T; Sergi M; Nazaré M; Oddi S; Maccarrone M

International journal of molecular sciences 2023

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CB2R agonists in the clinics: A treasure chest for treating inflammatory diseases

  • Uwe Grether; Marc Nazaré

Open Access Government 2023

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CB₂R ligands to treat inflammatory diabetes

  • Uwe Grether; Marc Nazaré

Open Access Government 2023

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First<i> in</i><i> vivo</i> fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod

  • Starke, Ludger; Millward, Jason M.; Prinz, Christian; Sherazi, Fatima; Waiczies, Helmar; Lippert, Christoph; Nazare, Marc; Paul, Friedemann; Niendorf, Thoralf; Waiczies, Sonia

Theranostics 2023

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Novel tetrazolopyridazine based MACC1 transcriptional inhibitors as promising anti-metastatic therapy

  • Schope, Paul Curtis; Yan, Shixian; Kobelt, Dennis; Lewis, Joe; Putzker, Kerstin; Uhrig, Ulrike; Specker, Edgar; von Kries, Jens Peter; Dahlmann, Mathias; Sanchez-Ibarra, Hector E.; Unger, Anke; Zischinsky, Mia-Lisa; Klebl, Bert; Lindemann, Peter; Walther, Wolfgang; Nazare, Marc; Stein, Ulrike

Cancer Research 2023

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Isoform-selective targeting of PI3K: time to consider new opportunities?

  • Cirillo, Davide; Diceglie, Marta; Nazare, Marc

Trends in Pharmacological Sciences 2023

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Small molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation

  • Jordan, Philipp; Costa, Amanda; Specker, Edgar; Popp, Oliver; Volkamer, Andrea; Piske, Regina; Obrusnik, Tessa; Kleissle, Sabrina; Stuke, Kevin; Rex, Andre; Neuenschwander, Martin; von Kries, Jens Peter; Nazare, Marc; Mertins, Phillip; Kettenmann, Helmut; Wolf, Susanne A.

Plos One 2023

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Development of selective inhibitors of phosphatidylinositol 3-kinase C2α

  • Lo, Wen-Ting; Belabed, Hassane; Kuecuekdisli, Murat; Metag, Juliane; Roske, Yvette; Prokofeva, Polina; Ohashi, Yohei; Horatscheck, Andre; Cirillo, Davide; Krauss, Michael; Schmied, Christopher; Neuenschwander, Martin; von Kries, Jens Peter; Medard, Guillaume; Kuster, Bernhard; Perisic, Olga; Williams, Roger L.; Daumke, Oliver; Payrastre, Bernard; Severin, Sonia; Nazare, Marc; Haucke, Volker

Nature Chemical Biology 2023

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An LPAR <sub><b>5</b></sub> -antagonist that reduces nociception and increases pruriception.

  • Langedijk J; Araya EI; Barroso AR; Tolenaars D; Nazaré M; Belabed H; Schoene J; Chichorro JG; Oude Elferink R

Frontiers in pain research (Lausanne, Switzerland) 2022

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Donor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles

  • Liu, Qian; Yang, Miao; Meng, Xiangchuan; Han, Xiaowan; Nazare, Marc; Xu, Youjun; Hu, Hai-Yu; Zhang, Qingyang

Talanta 2022

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Reverse Design toward Optimized Labeled Chemical Probes - Examples from the Endocannabinoid System

  • Guberman, Monica; Kosar, Miroslav; Omran, Anahid; Carreira, Erick M.; Nazare, Marc; Grether, Uwe

Chimia 2022

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Antagonistic control of active surface integrins by myotubularin and phosphatidylinositol 3-kinase C2β in a myotubular myopathy model

  • Samso, Paula; Koch, Philipp A.; Posor, York; Lo, Wen-Ting; Belabed, Hassane; Nazare, Marc; Laporte, Jocelyn; Haucke, Volker

Proceedings of the National Academy of Sciences 2022

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Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors

  • Specker, Edgar; Matthes, Susann; Wesolowski, Radoslaw; Schuetz, Anja; Grohmann, Maik; Alenina, Natalia; Pleimes, Dirk; Mallow, Keven; Neuenschwander, Martin; Gogolin, Angelina; Weise, Marie; Pfeifer, Jochen; Ziebart, Nandor; Heinemann, Udo; von Kries, Jens Peter; Nazare, Marc; Bader, Michael

Journal of Medicinal Chemistry 2022

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Weizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+Probability and CASE-3D

  • Li, Xiao-Lu; Ru, Tong; Navarro-Vazquez, Armando; Lindemann, Peter; Nazare, Marc; Li, Xu-Wen; Guo, Yue-Wei; Sun, Han

Journal of Natural Products 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin

  • Zhang, Hengxi; Modenutti, Carlos; Nekkanti, Yelha Phani Kumar; Denis, Maxime; Bermejo, Iris A. .; Lefebre, Jonathan; Che, Kateryna; Kim, Dongyoon; Kagelmacher, Marten; Kurzbach, Dennis; Nazare, Marc; Rademacher, Christoph

ACS Chemical Biology 2022

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Phosphoinositide Conversion Inactivates R-RAS and Drives Metastases in Breast Cancer

  • Li, Huayi; Prever, Lorenzo; Hsu, Myriam Y.; Lo, Wen-Ting; Margaria, Jean Piero; De Santis, Maria Chiara; Zanini, Cristina; Forni, Marco; Novelli, Francesco; Pece, Salvatore; Di Fiore, Pier Paolo; Porporato, Paolo Ettore; Martini, Miriam; Belabed, Hassane; Nazare, Marc; Haucke, Volker; Gulluni, Federico; Hirsch, Emilio

Advanced Science 2022

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BODIPY-Equipped Benzo-Crown-Ethers as Fluorescent Sensors for pH Independent Detection of Sodium and Potassium Ions

  • Sprenger, Tobias; Schwarze, Thomas; Mueller, Holger; Sperlich, Eric; Kelling, Alexandra; Holdt, Hans-Juergen; Paul, Jerome; Riano, Vera Martos; Nazare, Marc

ChemPhotoChem 2022

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Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe

  • Gazzi, Thais; Brennecke, Benjamin; Atz, Kenneth; Korn, Claudia; Sykes, David; Forn-Cuni, Gabriel; Pfaff, Patrick; Sarott, Roman C.; Westphal, Matthias, V; Mostinski, Yelena; Mach, Leonard; Wasinska-Kalwa, Malgorzata; Weise, Marie; Hoare, Bradley L.; Miljus, Tamara; Mexi, Maira; Roth, Nicolas; Koers, Eline J.; Guba, Wolfgang; Alker, Andre; Rufer, Arne C.; Kusznir, Eric A.; Huber, Sylwia; Raposo, Catarina; Zirwes, Elisabeth A.; Osterwald, Anja; Pavlovic, Anto; Moes, Svenja; Beck, Jennifer; Nettekoven, Matthias; Benito-Cuesta, Irene; Grande, Teresa; Drawnel, Faye; Widmer, Gabriella; Holzer, Daniela; van der Wel, Tom; Mandhair, Harpreet; Honer, Michael; Fingerle, Jurgen; Scheffel, Joerg; Broichhagen, Johannes; Gawrisch, Klaus; Romero, Julian; Hillard, Cecilia J.; Varga, Zoltan V.; van der Stelt, Mario; Pacher, Pal; Gertsch, Jurg; Ullmer, Christoph; McCormick, Peter J.; Oddi, Sergio; Spaink, Herman P.; Maccarrone, Mauro; Veprintsev, Dmitry B.; Carreira, Erick M.; Grether, Uwe; Nazare, Marc

Chemical Science 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the Lectin Langerin

  • Zhang, Hengxi; Modenutti, Carlos; Nekkanti, Yelha Phani Kumar; Denis, Maxime; Bermejo, Iris A.; Lefebre, Jonathan; Che, Kateryna; Kim, Dongyoon; Kagelmacher, Marten; Kurzbach, Dennis; Nazare, Marc; Rademacher, Christoph

ACS Chemical Biology 2022

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Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands

  • Fernandez-Bachiller, Maria Isabel; Hwang, Songhwan; Schembri, Maria Elena; Lindemann, Peter; Guberman, Monica; Herziger, Svenja; Specker, Edgar; Matter, Hans; Will, David W.; Czech, Jorg; Wagner, Michael; Bauer, Armin; Schreuder, Herman; Ritter, Kurt; Urmann, Matthias; Wehner, Volkmar; Sun, Han; Nazare, Marc

Journal of Medicinal Chemistry 2022

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Compound Interaction Screen on a Photoactivatable Cellulose Membrane (CISCM) Identifies Drug Targets

  • Melder, F. Teresa, I; Lindemann, Peter; Welle, Alexander; Trouillet, Vanessa; Heissler, Stefan; Nazare, Marc; Selbach, Matthias

ChemMedChem 2022

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Rational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis

  • Halland, Nis; Schmidt, Friedemann; Weiss, Tilo; Li, Ziyu; Czech, Jorg; Saas, Joachim; Ding-Pfennigdorff, Danping; Dreyer, Matthias K.; Strubing, Carsten; Nazare, Marc

Journal of Medicinal Chemistry 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin

  • Hengxi Zhang; Carlos Modenutti; N. Y. Phani Kumar; Maxime Denis; Iris Bermejo; Jonathan Lefebre; Kateryna Che; Dongyoon Kim; Marten Kagelmacher; Dennis Kurzbach; Marc Nazare; Christoph Rademacher

OpenAlex 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin

  • Hengxi Zhang; Carlos Modenutti; N. Y. Phani Kumar; Maxime Denis; Iris Bermejo; Jonathan Lefebre; Kateryna Che; Dongyoon Kim; Marten Kagelmacher; Dennis Kurzbach; Marc Nazare; Christoph Rademacher

OpenAlex 2022

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In vivo detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy

  • Prinz, Christian; Starke, Ludger; Millward, Jason M.; Fillmer, Ariane; Delgado, Paula Ramos; Waiczies, Helmar; Pohlmann, Andreas; Rothe, Michael; Nazare, Marc; Paul, Friedemann; Niendorf, Thoralf; Waiczies, Sonia

Theranostics 2021

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Cannabinoid receptor type 2 ligands: an analysis of granted patents since 2010

  • Brennecke, Benjamin; Gazzi, Thais; Atz, Kenneth; Fingerle, Jurgen; Kuner, Pascal; Schindler, Torsten; de Weck, Guy; Nazare, Marc; Grether, Uwe

Pharmaceutical Patent Analyst 2021

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Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer

  • Carter, David M.; Specker, Edgar; Malecki, Piotr H.; Przygodda, Jessica; Dudaniec, Krystyna; Weiss, Manfred S.; Heinemann, Udo; Nazare, Marc; Gohlke, Ulrich

Journal of Medicinal Chemistry 2021

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Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II

  • Leenders, Ruben G. G.; Brinch, Shoshy Alam; Sowa, Sven T.; Amundsen-Isaksen, Enya; Galera-Prat, Albert; Murthy, Sudarshan; Aertssen, Sjoerd; Smits, Johannes N.; Nieczypor, Piotr; Damen, Eddy; Wegert, Anita; Nazare, Marc; Lehtio, Lari; Waaler, Jo; Krauss, Stefan

Journal of Medicinal Chemistry 2021

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Topical inflammasome inhibition with disulfiram prevents irritant contact dermatitis

  • Bonnekoh, Hanna; Vera, Carolina; Abad-Perez, Angela; Radetzki, Silke; Neuenschwander, Martin; Specker, Edgar; Mahnke, Niklas Amadeus; Frischbutter, Stefan; Latz, Eicke; Nazare, Marc; Kries, Jens V.; Maurer, Marcus; Scheffel, Joerg; Krause, Karoline

Clinical and Translational Allergy 2021

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Functional Imaging Using Fluorine (F-19) MR Methods: Basic Concepts

  • Waiczies, Sonia; Prinz, Christian; Starke, Ludger; Millward, Jason M.; Delgado, Paula Ramos; Rosenberg, Jens; Nazare, Marc; Waiczies, Helmar; Pohlmann, Andreas; Niendorf, Thoralf

Methods in Molecular Biology 2021

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Structural Basis for Gating of the Two-Pore Domain K+ (K-2P) Channels TASK-1 and TALK-2

  • Schewe, Marcus; Riel, Elena B.; Rinne, Susanne; Kopec, Wojciech; Langer, Jan; Lindemann, Peter; Juers, Bjoern C.; Nazare, Marc; de Groot, Bert L.; Decher, Niels; Baukrowitz, Thomas

Biophysical Journal 2021

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DOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells

  • Brennecke, Benjamin; Wang, Qinghua; Haap, Wolfgang; Grether, Uwe; Hu, Hai-Yu; Nazare, Marc

Bioconjugate Chemistry 2021

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Pentafluorosulfanyl (SF<sub>5</sub>) as a Superior <SUP>19</SUP>F Magnetic Resonance Reporter Group: Signal Detection and Biological Activity of Teriflunomide Derivatives

  • Prinz, Christian; Starke, Ludger; Ramspoth, Tizian-Frank; Kerkering, Janis; Riano, Vera Martos; Paul, Jerome; Neuenschwander, Martin; Oder, Andreas; Radetzki, Silke; Adelhoefer, Siegfried; Delgado, Paula Ramos; Aravina, Mariya; Millward, Jason M.; Fillmer, Ariane; Paul, Friedemann; Siffrin, Volker; Von Kries, Jens-Peter; Niendorf, Thoralf; Nazare, Marc; Waiczies, Sonia

ACS Sensors 2021

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Generation of a TR-FRET-based assay for the determination of cannabinoid CB1 receptor ligand binding kinetics

  • Borrega, Leire; Hoare, Brad; Gazzi, Thais; Nazare, Marc; Grether, Uwe; Sykes, David; Veprintsev, Dmitry

British Journal of Pharmacology 2021

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Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor

  • Waaler, Jo; Leenders, Ruben G. G.; Sowa, Sven T.; Brinch, Shoshy Alam; Lycke, Max; Nieczypor, Piotr; Aertssen, Sjoerd; Murthy, Sudarshan; Galera-Prat, Albert; Damen, Eddy; Wegert, Anita; Nazare, Marc; Lehtio, Lari; Krauss, Stefan

Journal of Medicinal Chemistry 2020

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Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells

  • Barone, Matthias; Mueller, Matthias; Chiha, Slim; Ren, Jiang; Albat, Dominik; Soicke, Arne; Dohmen, Stephan; Klein, Marco; Bruns, Judith; van Dinther, Maarten; Opitz, Robert; Lindemann, Peter; Beerbaum, Monika; Motzny, Kathrin; Roske, Yvette; Schmieder, Peter; Volkmer, Rudolf; Nazare, Marc; Heinemann, Udo; Oschkinat, Hartmut; ten Dijke, Peter; Schmalz, Hans-Guenther; Kuehne, Ronald

Proceedings of the National Academy of Sciences 2020

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Development and application of a kinetic ligand binding assay for the cannabinoid receptor 1 using resonance energy transfer approaches

  • Hoare, Bradley; Sykes, David; Gazzi, Thais; Nazare, Marc; Grether, Uwe; Veprintsev, Dmitry

British Journal of Pharmacology 2020

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From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement

  • Mostinski, Yelena; Heynen, Guus J. J. E.; Lopez-Alberca, Maria Pascual; Paul, Jerome; Miksche, Sandra; Radetzki, Silke; Schaller, David; Shanina, Elena; Seyffarth, Carola; Kolomeets, Yuliya; Ziebart, Nandor; de Schryver, Judith; Oestreich, Sylvia; Neuenschwander, Martin; Roske, Yvette; Heinemann, Udo; Rademacher, Christoph; Volkamer, Andrea; von Kries, Jens Peter; Birchmeier, Walter; Nazare, Marc

Journal of Medicinal Chemistry 2020

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Revealing cytotoxic substructures in molecules using deep learning

  • Webel, Henry E.; Kimber, Talia B.; Radetzki, Silke; Neuenschwander, Martin; Nazare, Marc; Volkamer, Andrea

Journal of Computer-Aided Molecular Design 2020

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NMR quality control of fragment libraries for screening

  • Sreeramulu, Sridhar; Richter, Christian; Kuehn, Till; Azzaoui, Kamal; Blommers, Marcel Jules Jose; Del Conte, Rebecca; Fragai, Marco; Trieloff, Nils; Schmieder, Peter; Nazare, Marc; Specker, Edgar; Ivanov, Vladimir; Oschkinat, Hartmut; Banci, Lucia; Schwalbe, Harald

Journal of Biomolecular NMR 2020

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Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells

  • Sarott, Roman C.; Westphal, Matthias, V; Pfaff, Patrick; Korn, Claudia; Sykes, David A.; Gazzi, Thais; Brennecke, Benjamin; Atz, Kenneth; Weise, Marie; Mostinski, Yelena; Hompluem, Pattarin; Koers, Eline; Miljus, Tamara; Roth, Nicolas J.; Asmelash, Hermon; Vong, Man C.; Piovesan, Jacopo; Guba, Wolfgang; Rufer, Arne C.; Kusznir, Eric A.; Huber, Sylwia; Raposo, Catarina; Zirwes, Elisabeth A.; Osterwald, Anja; Pavlovic, Anto; Moes, Svenja; Beck, Jennifer; Benito-Cuesta, Irene; Grande, Teresa; de Martin Esteban, Samuel Ruiz; Yeliseev, Alexei; Drawnel, Faye; Widmer, Gabriella; Holzer, Daniela; van der Wel, Tom; Mandhair, Harpreet; Yuan, Cheng-Yin; Drobyski, William R.; Saroz, Yurii; Grimsey, Natasha; Honer, Michael; Fingerle, Juergen; Gawrisch, Klaus; Romero, Julian; Hillard, Cecilia J.; Varga, Zoltan V.; van der Stelt, Mario; Pacher, Pal; Gertsch, Juerg; McCormick, Peter J.; Ullmer, Christoph; Oddi, Sergio; Maccarrone, Mauro; Veprintsev, Dmitry B.; Nazare, Marc; Grether, Uwe; Carreira, Erick M.

Journal of the American Chemical Society 2020

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Diverse chemotypes drive biased signaling by cannabinoid receptors

  • Miljuš T; Heydenreich FM; Gazzi T; Kimbara A; Rogers-Evans M; Nettekoven M; Zirwes E; Osterwald A; Rufer AC; Ullmer C; Guba W; Le Gouill C; Veprintsev DB
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Dual-Mode Detection of Bacterial 16S Ribosomal RNA in Tissues

  • Shengnan Xu; Qingyang Zhang; Xiaowan Han; Yali Wang; Xiang Wang; Marc Nazare; Jian-Dong Jiang; Hai-Yu Hu

ACS Sensors 2020

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Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie 2020

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Back Cover: An Activatable Lanthanide Luminescent Probe for Time‐Gated Detection of Nitroreductase in Live Bacteria (Angew. Chem. Int. Ed. 22/2020)

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie International Edition 2020

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Rücktitelbild: Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien (Angew. Chem. 22/2020)

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie 2020

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A Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles

  • Alsalim, Rana; Lindemann, Peter; Lopez-Alberca, Maria Pascual; Miksche, Sandra; Czechtizky, Werngard; Halland, Nis; Nazare, Marc

Organic Letters 2020

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An Activatable Lanthanide Luminescent Probe for Time-Gated Detection of Nitroreductase in Live Bacteria

  • Brennecke, Benjamin; Wang, Qinghua; Zhang, Qingyang; Hu, Hai-Yu; Nazare, Marc

Angewandte Chemie International Edition 2020

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Preclinical efficacy of NLRP3 small molecule inflammasome inhibitors: Implications for future treatment of autoinflammatory syndromes

  • Abad-Perez, A.; Frischbutter, S.; Mahnke, N. A.; Kries, J. V.; Nazare, M.; Maurer, M.; Scheffel, J.; Krause, K.

Experimental Dermatology 2019

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Topical inflammasome inhibition-a novel treatment strategy for contact dermatitis

  • Bonnekoh, H.; Vera, C.; Abad-Perez, A.; van Kries, J.; Nazare, M.; Mahnke, N. A.; Maurer, M.; Scheffel, J.; Krause, K.

Experimental Dermatology 2019

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Probing 2<i>H</i>-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors

  • Schoene, Jens; Gazzi, Thais; Lindemann, Peter; Christmann, Mathias; Volkamer, Andrea; Nazare, Marc

ChemMedChem 2019

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Small-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells

  • Marc Nazaré

Frontiers in Cellular Neuroscience 2019

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A New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves' Orbitopathy

  • Marcinkowski, Patrick; Hoyer, Inna; Specker, Edgar; Furkert, Jens; Rutz, Claudia; Neuenschwander, Martin; Sobottka, Sebastian; Sun, Han; Nazare, Marc; Berchner-Pfannschmidt, Utta; Von kries, Jens Peter; Eckstein, Anja; Schuelein, Ralf; Krause, Gerd

Thyroid 2019

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EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

  • Brennecke, Philip; Rasina, Dace; Aubi, Oscar; Herzog, Katja; Landskron, Johannes; Cautain, Bastien; Vicente, Francisca; Quintana, Jordi; Mestres, Jordi; Stechmann, Bahne; Ellinger, Bernhard; Brea, Jose; Kolanowski, Jacek L.; Pilarski, Radoslaw; Orzaez, Mar; Pineda-Lucena, Antonio; Laraia, Luca; Nami, Faranak; Zielenkiewicz, Piotr; Paruch, Kamil; Hansen, En; von Kries, Jens P.; Neuenschwander, Martin; Specker, Edgar; Bartunek, Petr; Simova, Sarka; Lesnikowski, Zbigniew; Krauss, Stefan; Lehtio, Lari; Bilitewski, Ursula; Broenstrup, Mark; Tasken, Kjetil; Jirgensons, Aiprs; Lickert, Heiko; Clausen, Mads H.; Andersen, Jeanette H.; Vicent, Maria J.; Genilloud, Olga; Martinez, Aurora; Nazare, Marc; Fecke, Wolfgang; Gribbon, Philip

SLAS Discovery: Advancing Life Sciences R & D 2019

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A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels

  • Schewe, Marcus; Sun, Han; Mert, Umit; Mackenzie, Alexandra; Pike, Ashley C. W.; Schulz, Friederike; Constantin, Cristina; Vowinkel, Kirsty S.; Conrad, Linus J.; Kiper, Aytug K.; Gonzalez, Wendy; Musinszki, Marianne; Tegtmeier, Marie; Pryde, David C.; Belabed, Hassane; Nazare, Marc; de Groot, Bert L.; Decher, Niels; Fakler, Bernd; Carpenter, Elisabeth P.; Tucker, Stephen J.; Baukrowitz, Thomas

Science 2019

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Rapid Synthesis of gamma-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen

  • Zhang, Qingyang; Xu, Shengnan; Lai, Fangfang; Wang, Yali; Zhang, Na; Nazare, Marc; Hu, Hai-Yu

Organic Letters 2019

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Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin

  • Wenskowsky, Lea; Schreuder, Herman; Derdau, Volker; Matter, Hans; Volkmar, Julia; Nazare, Marc; Opatz, Till; Petry, Stefan

Angewandte Chemie International Edition 2018

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A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging

  • Liu, Yun; Zhang, Leilei; Nazare, Marc; Yao, Qingqiang; Hu, Hai-Yu

Acta Pharmaceutica Sinica B 2018

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Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase

  • Ruess, Dietrich A.; Heynen, Guus J.; Ciecielski, Katrin J.; Ai, Jiaoyu; Berninger, Alexandra; Kabacaoglu, Derya; Goerguelue, Kivanc; Dantes, Zahra; Woermann, Sonja M.; Diakopoulos, Kalliope N.; Karpathaki, Angeliki F.; Kowalska, Marlena; Kaya-Aksoy, Ezgi; Song, Liang; van der Laan, Eveline A. Zeeuw; Lopez-Alberca, Maria P.; Nazare, Marc; Reichert, Maximilian; Saur, Dieter; Erkan, Mert M.; Hopt, Ulrich T.; Sainz, Bruno, Jr.; Birchmeier, Walter; Schmid, Roland M.; Lesina, Marina; Alguel, Hana

Nature Medicine 2018

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Allosteric Inhibition of a Mammalian Lectin

  • Aretz, Jonas; Anumala, Upendra R.; Fuchsberger, Felix F.; Molavi, Narges; Ziebart, Nandor; Zhang, Hengxi; Nazare, Marc; Rademacher, Christoph

Journal of the American Chemical Society 2018

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In Vivo Imaging of MMP-13 Activity Using a Specific Polymer-FRET Peptide Conjugate Detects Early Osteoarthritis and Inhibitor Efficacy

  • Duro-Castano, Aroa; Lim, Ngee Han; Tranchant, Isabelle; Amoura, Mehdi; Beau, Fabrice; Wieland, Heike; Kingler, Otmar; Herrmann, Matthias; Nazare, Marc; Plettenburg, Oliver; Dive, Vincent; Vicent, Maria J.; Nagase, Hideaki

Advanced Functional Materials 2018

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A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System

  • Schoene, Jens; Bel Abed, Hassen; Schmieder, Peter; Christmann, Mathias; Nazare, Marc

Chemistry - A European Journal 2018

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CellFy: A Cell-Based Fragment Screen against C-Type Lectins

  • Schulze, Jessica; Baukmann, Hannes; Wawrzinek, Robert; Fuchsberger, Felix F.; Specker, Edgar; Aretz, Jonas; Nazare, Marc; Rademacher, Christoph

ACS Chemical Biology 2018

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Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway

  • Klein, Wolfgang; Rutz, Claudia; Eckhard, Jamina; Provinciael, Becky; Specker, Edgar; Neuenschwander, Martin; Kleinau, Gunnar; Scheerer, Patrick; von Kries, Jens-Peter; Nazare, Marc; Vermeire, Kurt; Schuelein, Ralf

Plos One 2018

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Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives

  • Abed, Hassen Bel; Weissing, Nils; Schoene, Jens; Paulus, Jannik; Sewald, Norbert; Nazare, Marc

Tetrahedron Letters 2018

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Regulation of Two-pore Domain K plus Channels by Natural Effectors and Pharmacological Agents

  • Schewe, M.; Schulz, F.; Mert, U.; Sun, H.; Belabed, H.; Musinszki, M.; Koehler, T.; Tegtmeier, M.; Nazare, M.; Carpenter, E. P.; Tucker, S. J.; Baukrowitz, T.

Acta Physiologica 2017

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A straightforward approach to N-substituted-2H-indazol-2-amines through reductive cyclization

  • Schoene, Jens; Abed, Hassen Bel; Christmann, Mathias; Nazare, Marc

Tetrahedron Letters 2017

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Novel compounds targeting microglial nitric oxide release

  • Jordan, P.; Wolf, S. A.; Specker, E.; Nazare, M.; Kettenmann, H.

Glia 2017

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N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals

  • Marc Nazaré

Official Gazette of the United States Patent and Trademark Office Patents 2017

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Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells

  • Carter, David M.; Specker, Edgar; Przygodda, Jessica; Neuenschwander, Martin; von Kries, Jens Peter; Heinemann, Udo; Nazare, Marc; Gohlke, Ulrich

SLAS Discovery: Advancing Life Sciences R & D 2017

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Direct Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances

  • Han Sun; André Horatscheck; Vera Martos; Max Bartetzko; Ulrike Uhrig; Dieter Lentz; Peter Schmieder; Marc Nazaré

Angewandte Chemie 2017

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A conserved drug-binding site controls the selectivity filter gate in K2P K+ channels

  • Schewer, M.; Schulz, F.; Mert, Ue.; Sun, H.; Koehler, T.; Tegtmeier, M.; Musinszki, M.; Belabed, H.; Nazare, M.; Tucker, S. J.; Baukrowitz, T.

Acta Physiologica 2017

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Loss of Ptpn11 (Shp2) drives satellite cells into quiescence

  • Griger, Joscha; Schneider, Robin; Lahmann, Ines; Schoewel, Verena; Keller, Charles; Spuler, Simone; Nazare, Marc; Birchmeier, Carmen

eLife 2017

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Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach

  • Anumala, Upendra Rao; Waaler, Jo; Nkizinkiko, Yves; Ignatev, Alexander; Lazarow, Katina; Lindemann, Peter; Olsen, Petter Angell; Murthy, Sudarshan; Obaii, Ezeogo; Majouga, Alexander G.; Leonov, Sergey; von Kries, Jens Peter; Lehtio, Lari; Krauss, Stefan; Nazare, Marc

Journal of Medicinal Chemistry 2017

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Temperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures

  • Geiger, Michel-Andreas; Orwick-Rydmark, Marcella; Marker, Katharina; Franks, W. Trent; Akhmetzyanov, Dmitry; Stoppler, Daniel; Zinke, Maximilian; Specker, Edgar; Nazare, Marc; Diehl, Anne; van Rossum, Barth-Jan; Aussenac, Fabien; Prisner, Thomas; Akbey, Umit; Oschkinat, Hartmut

Physical Chemistry Chemical Physics 2016

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5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors

  • Robertson, Mark J.; Horatscheck, Andre; Sauer, Samantha; von Kleist, Lisa; Baker, Jennifer R.; Stahlschmidt, Wiebke; Nazare, Marc; Whiting, Ainslie; Chau, Ngoc; Robinson, Phillip J.; Haucke, Volker; McCluskey, Adam

Organic & Biomolecular Chemistry 2016

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Pyrazole derivatives and their use as LPAR5 antagonists

  • Marc Nazaré

Official Gazette of the United States Patent and Trademark Office Patents 2016

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ChemInform Abstract: Organophosphorus-Mediated N-N Bond Formation: Facile Access to 3-Amino-2H-indazoles

  • Hassen Bel Abed; Jens Schoene; Mathias Christmann; Marc Nazare

ChemInform 2016

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Pharmacological targeting of human tryptophan hydroxylase - novel inhibitors for the treatment of serotonin-related diseases

  • Matthes, S.; Specker, E.; Schuetz, A.; Grohmann, M.; von Kries, J.; Nazare, M.; Bader, M.

Naunyn-Schmiedeberg's Archives of Pharmacology 2016

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Modulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5

  • Kozian, Detlef H.; von Haeften, Elisabeth; Joho, Sabrina; Czechtizky, Werngard; Anumala, Upendra R.; Roux, Pascale; Dudda, Angela; Evers, Andreas; Nazare, Marc

Chembiochem 2016

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Organophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles

  • Abed, Hassen Bel; Schoene, Jens; Christmann, Mathias; Nazare, Marc

Organic & Biomolecular Chemistry 2016

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Chemical fragment arrays for rapid druggability assessment

  • Aretz, J.; Kondoh, Y.; Honda, K.; Anumala, U. R.; Nazare, M.; Watanabe, N.; Osada, H.; Rademacher, C.

Chemical Communications 2016

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DEVELOPMENT OF IMAGING AGENTS FOR THE VISUALISATION OF CARTILAGE IN VIVO

  • Lim, N. H.; Hu, H.; Nazare, M.; Plettenburg, O.; Nagase, H.; Schultz, C.

Osteoarthritis and Cartilage 2015

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Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]sulfonamides as Highly Active and Selective SGK1 Inhibitors

  • Halland, Nis; Schmidt, Friedemann; Weiss, Tilo; Saas, Joachim; Li, Ziyu; Czech, Joerg; Dreyer, Matthias; Hofmeister, Armin; Mertsch, Katharina; Dietz, Uwe; Struebing, Carsten; Nazare, Marc

ACS Medicinal Chemistry Letters 2015

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DOTAM Derivatives as Active Cartilage-Targeting Drug Carriers for the Treatment of Osteoarthritis

  • Hu, Hai-Yu; Lim, Ngee-Han; Ding-Pfennigdorff, Danping; Saas, Joachim; Wendt, K. Ulrich; Ritzeler, Olaf; Nagase, Hideaki; Plettenburg, Oliver; Schultz, Carsten; Nazare, Marc

Bioconjugate Chemistry 2015

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In vivo visualization of osteoarthritic hypertrophic lesions

  • Hu, Hai-Yu; Lim, Ngee-Han; Juretschke, Hans-Paul; Ding-Pfennigdorff, Danping; Florian, Peter; Kohlmann, Markus; Kandira, Abdullah; von Kries, Jens Peter; Saas, Joachim; Rudolphi, Karl A.; Wendt, K. Ulrich; Nagase, Hideaki; Plettenburg, Oliver; Nazare, Marc; Schultz, Carsten

Chemical Science 2015

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Tractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform

  • Wilde, Felix; Specker, Edgar; Neuenschwander, Martin; Nazare, Marc; Bodtke, Anja; Link, Andreas

Molecular Diversity 2014

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Quinoline-carboxamide derivatives as P2Y12 antagonists

  • Marc Nazare

Official Gazette of the United States Patent and Trademark Office Patents 2014

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N-[6-(4-Butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible, and Directly Acting P2Y12 Antagonist

  • Boldron, Christophe; Besse, Angelina; Bordes, Marie-Francoise; Tissandie, Stephanie; Yvon, Xavier; Gau, Benjamin; Badorc, Alain; Rousseaux, Tristan; Barre, Guillaume; Meneyrol, Jerome; Zech, Gernot; Nazare, Marc; Fossey, Valerie; Pflieger, Anne-Marie; Bonnet-Lignon, Sandrine; Millet, Laurence; Briot, Christophe; Dol, Frederique; Herault, Jean-Pascal; Savi, Pierre; Lassalle, Gilbert; Delesque, Nathalie; Herbert, Jean-Marc; Bono, Francoise

Journal of Medicinal Chemistry 2014

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Targeting Platelet G Protein-Coupled Receptors for Antithrombotic Therapy

  • Falker, Knut; Nazare, Marc; Wonerow, Peter; Kozian, Detlef H.

Drug Development Research 2013

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Identification of High-Affinity P2Y(12) Antagonists Based on a Phenylpyrazole Glutamic Acid Piperazine Backbone

  • Zech, Gernot; Hessler, Gerhard; Evers, Andreas; Weiss, Tilo; Florian, Peter; Just, Melitta; Czech, Joerg; Czechtizky, Werngard; Goerlitzer, Jochen; Ruf, Sven; Kohlmann, Markus; Nazare, Marc

Journal of Medicinal Chemistry 2012

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Selective non-lipid modulator of LPA5 activity in human platelets

  • Kozian, Detlef H.; Evers, Andreas; Florian, Peter; Wonerow, Peter; Joho, Sabrina; Nazare, Marc

Bioorganic & Medicinal Chemistry Letters 2012

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Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes

  • Marc Nazaré; Hans Matter; David W. Will; Michael Wagner; Matthias Urmann; Jörg Czech; Herman Schreuder; Armin Bauer; Kurt Ritter; Volkmar Wehner

Angewandte Chemie 2011

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Innenrücktitelbild: Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes (Angew. Chem. 4/2012)

  • Marc Nazaré; Hans Matter; David W. Will; Michael Wagner; Matthias Urmann; Jörg Czech; Herman Schreuder; Armin Bauer; Kurt Ritter; Volkmar Wehner

Angewandte Chemie 2011

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ChemInform Abstract: A General and Mild Domino Approach to Substituted 1-Aminoindoles

  • Nis Halland; Marc Nazare; Jorge Alonso; Omar R'kyek; Andreas Lindenschmidt

ChemInform 2011

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ChemInform Abstract: A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines

  • Jorge Alonso; Nis Halland; Marc Nazare; Omar R'kyek; Matthias Urmann; Andreas Lindenschmidt

ChemInform 2011

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A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines

  • Alonso, Jorge; Halland, Nis; Nazare, Marc; R'kyek, Omar; Urmann, Matthias; Lindenschmid, Andreas

European Journal of Organic Chemistry 2011

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A general and mild domino approach to substituted 1-aminoindoles

  • Halland, Nis; Nazare, Marc; Alonso, Jorge; R'kyek, Omar; Lindenschmidt, Andreas

Chemical Communications 2011

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ChemInform Abstract: Enantiospecific Synthesis of the (9S,18R)-Diastereomer of the Leukocyte Adhesion Inhibitor Cyclamenol A

  • Marc Nazare; Herbert Waldmann

ChemInform 2010

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ChemInform Abstract: Synthesis of the (9S,18R) Diastereomer of Cyclamenol A

  • Marc Nazare; Herbert Waldmann

ChemInform 2010

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A General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates

  • R'kyek, Omar; Halland, Nis; Lindenschmidt, Andreas; Alonso, Jorge; Lindemann, Peter; Urmann, Matthias; Nazare, Marc

Chemistry - A European Journal 2010

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ChemInform Abstract: Synthesis of the (9S,18R)-seco Acid of the Leukocyte Adhesion Inhibitor Cyclamenol A

  • Marc Nazare; Herbert Waldmann

ChemInform 2010

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ChemInform Abstract: A General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates

  • Omar R'kyek; Nis Halland; Andreas Lindenschmidt; Jorge Alonso; Peter Lindemann; Matthias Urmann; Marc Nazare

ChemInform 2010

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ChemInform Abstract: A General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles

  • Nis Halland; Marc Nazare; Omar R'kyek; Jorge Alonso; Matthias Urmann; Andreas Lindenschmidt

ChemInform 2010

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A General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles

  • Nis Halland; Marc Nazaré; Omar R'kyek; Jorge Alonso; Matthias Urmann; Andreas Lindenschmidt

Angewandte Chemie 2009

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Evidence for CCl/CBr⋅⋅⋅π Interactions as an Important Contribution to Protein-Ligand Binding Affinity

  • Hans Matter; Marc Nazaré; Stefan Güssregen; David W. Will; Herman Schreuder; Armin Bauer; Matthias Urmann; Kurt Ritter; Michael Wagner; Volkmar Wehner

Angewandte Chemie 2009

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Structural requirements for factor xa inhibition by 3-oxybenzamides with neutral P1 substituents: Combining X-ray crystallography, 3D-QSAR, and tailored scoring functions

  • Matter, H; Will, DW; Nazare, M; Schreuder, H; Laux, V; Wehner, V

Journal of Medicinal Chemistry 2005

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Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: A study combining structure-activity relationship and X-ray crystallography

  • Nazare, M; Will, DW; Matter, H; Schreuder, H; Ritter, K; Urmann, M; Essrich, M; Bauer, A; Wagner, M; Czech, J; Lorenz, M; Laux, V; Wehner, V

Journal of Medicinal Chemistry 2005

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Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand

  • Nazare, M; Essrich, M; Will, DW; Matter, H; Ritter, K; Urmann, M; Bauer, A; Schreuder, H; Czech, J; Lorenz, M; Laux, V; Wehner, V

Bioorganic & Medicinal Chemistry Letters 2004

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Novel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Ligand

  • Marc Nazare; et al. et al.

ChemInform 2004

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Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents

  • Marc Nazare; et al. et al.

ChemInform 2004

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Eine flexible, palladiumkatalysierte Indol- und Azaindolsynthese durch direkte Anellierung von Chloranilinen und Chloraminopyridinen mit Ketonen

  • Marc Nazaré; Claudia Schneider; Andreas Lindenschmidt; David William Will

Angewandte Chemie 2004

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A Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones

  • Marc Nazare; Claudia Schneider; Andreas Lindenschmidt; David William Will

ChemInform 2004

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Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand

  • Nazare, M; Matter, H; Klingler, O; Al-Obeidi, F; Schreuder, H; Zoller, G; Czech, J; Lorenz, M; Dudda, A; Peyman, A; Nestler, HP; Urmann, M; Bauer, A; Laux, V; Wehner, V; Will, DW

Bioorganic & Medicinal Chemistry Letters 2004

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Flexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones

  • Nazare, M; Schneider, C; Lindenschmidt, A; Will, DW

Angewandte Chemie International Edition 2004

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Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral PI substituents

  • Nazare, M; Essrich, M; Will, DW; Matter, H; Ritter, K; Urmann, M; Bauer, A; Schreuder, H; Dudda, A; Czech, J; Lorenz, M; Laux, V; Wehner, V

Bioorganic & Medicinal Chemistry Letters 2004

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Enantiospecific synthesis of the (9S,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol A

  • Nazare, M; Waldmann, H

Chemistry - A European Journal 2001

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Enantiospecific synthesis of the (95,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol a

  • Nazaré, M.; Waldmann, H.

Chemistry - A European Journal 2001

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Synthese des (9S,18R)-Diastereomers von Cyclamenol A

  • Marc Nazaré; Herbert Waldmann

Angewandte Chemie 2000

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Synthesis of the (9S,18R) diastereomer of cyclamenol A

  • Nazare, M; Waldmann, H

Angewandte Chemie International Edition 2000

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Synthesis of the (9S, 18R)-seco acid of the leukocyte adhesion inhibitor cyclamenol A

  • Nazare, M; Waldmann, H

Tetrahedron Letters 2000

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Efficient enantioselective synthesis of a beta-hydroxyepoxide building block for the construction of macrocyclic natural products

  • Schlede, U; Nazare, M; Waldmann, H

Tetrahedron Letters 1998

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Halogen…π Interactions as Important Contributors to Binding Affinity in Medicinal Chemistry

  • Marc Nazaré
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Use of substituted heterocyclic compounds for treating disease associated with genotoxic stress-induced I kappa B kinase/nuclear factor kappa-light-chain-enhancer of activated B cells activation which is cancer

  • Marc Nazaré
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Use of substituted heterocyclic compounds for treating a subject afflicted by hyperthyroidism or thyroid disease including Grave's disease, Grave's ophthalmopathy, Grave's dermopathy or thyroid cancer

  • Marc Nazaré
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CRYSTAL STRUCTURE OF FACTOR XA IN COMPLEX WITH COMPOUND 45

  • Marc Nazaré
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Composition to identify compound of interest comprises fluorescent-labeled fatty acid whose fatty acid part binds to fatty acid binding compound, and fluorescent part and compound interact to elicit Forster resonance energy transfer effects

  • Marc Nazaré
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New xanthine derivatives are tryptophan hydroxylases inhibitors used to treat e.g. bone diseases, systemic sclerosis, gastrointestinal diseases, cancer, vascular diseases, inflammatory, metabolic diseases and psychiatric diseases

  • Marc Nazaré
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New N-(4-(azaindazol-6-yl)-phenyl)-sulfonamide compound used in treating e.g. diabetes, cardiovascular diseases, fibrosis, inflammation, epilepsy, pain, tumors, cerebral infarctions, osteoarthritis, obesity, dyslipidemia, gout and tinnitus

  • Marc Nazaré
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New substituted triazole derivatives are tankyrase-1 inhibitors useful for treating or preventing e.g. non-regenerative wound healing, viral infection, dermal, renal, liver or myocardial fibrosis, or aberrant systemic glucose metabolism

  • Marc Nazaré
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New xanthine derivatives are tryptophan hydroxylase inhibitor, used to treat serotonin-related diseases or disorders e.g. osteoporosis, osteoporosis pseudoglioma syndrome, osteopenia, diarrhea, emesis, and peripheral artery disease

  • Marc Nazaré
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Portraitfoto: © Silke Oßwald