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Prof. Dr.
Marc Nazaré studierte Chemie an der Universität Karlsruhe und erhielt 1999 seinen Doktortitel in organischer Chemie in der Gruppe von Herbert Waldmann im Gebiet der Naturstoff-Totalsynthese. Danach arbeitete er in der pharmazeutischen Industrie als Medizinalchemiker bei Sanofi in Frankfurt. 2013 gründete er die Forschungsgruppe medizinische Chemie am Leibniz Forschungsinstitut für molekulare Pharmakologie. Seine gegenwärtigen Forschungsinteressen sind fokussiert auf Design und Optimierung chemischer Sonden und Bildgebungs-Tools für Anwendungen in der Chemischen Biologie und der translatorischen Forschung. Er ist Honorarprofessor an der Universität Bielefeld.
Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
Journal of medicinal chemistry 2023
online lesenDiscovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2023
online lesenStructural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.
Journal of medicinal chemistry 2023
online lesenSelective and pH-Independent Detection of Ba<sup>2+</sup> in Water by a Benzo-21-crown-7-Functionalized BODIPY.
Chemistry (Weinheim an der Bergstrasse, Germany) 2023
online lesenCLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors.
Cell chemical biology 2023
online lesenAβ Chronic Exposure Promotes an Activation State of Microglia through Endocannabinoid Signalling Imbalance.
International journal of molecular sciences 2023
online lesenFirst <i>in vivo</i> fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod.
Theranostics 2023
online lesenSmall molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation.
PloS one 2023
online lesenIsoform-selective targeting of PI3K: time to consider new opportunities?
Trends in Pharmacological Sciences 2023
online lesenCB2R agonists in the clinics: A treasure chest for treating inflammatory diseases
Open Access Government 2023
online lesenCB₂R ligands to treat inflammatory diabetes
Open Access Government 2023
online lesenPhosphoinositide Conversion Inactivates R-RAS and Drives Metastases in Breast Cancer.
Advanced science (Weinheim, Baden-Wurttemberg, Germany) 2022
online lesenProbing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands.
Journal of medicinal chemistry 2022
online lesenIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin.
ACS chemical biology 2022
online lesenDevelopment of selective inhibitors of phosphatidylinositol 3-kinase C2α.
Nature chemical biology 2022
online lesenStructure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors.
Journal of medicinal chemistry 2022
online lesenAn LPAR <sub><b>5</b></sub> -antagonist that reduces nociception and increases pruriception.
Frontiers in pain research (Lausanne, Switzerland) 2022
online lesenDetection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe.
Chemical science 2022
online lesenRational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis
Journal of Medicinal Chemistry 2022
online lesenDonor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles
Talanta 2022
online lesenAntagonistic control of active surface integrins by myotubularin and phosphatidylinositol 3-kinase C2β in a myotubular myopathy model
Proceedings of the National Academy of Sciences 2022
online lesenReverse-Design toward Optimized Labeled Chemical Probes – Examples from the Endocannabinoid System
CHIMIA 2022
online lesenCompound Interaction Screen on a Photoactivatable Cellulose Membrane (CISCM) Identifies Drug Targets
ChemMedChem 2022
online lesenWeizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+ Probability and CASE-3D
Journal of Natural Products 2022
online lesenDevelopment of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II.
Journal of medicinal chemistry 2021
online lesenTopical inflammasome inhibition with disulfiram prevents irritant contact dermatitis.
Clinical and translational allergy 2021
online lesenFunctional Imaging Using Fluorine (<sup>19</sup>F) MR Methods: Basic Concepts.
Methods in molecular biology (Clifton, N.J.) 2021
online lesen<i>In vivo</i> detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy.
Theranostics 2021
online lesenDOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells
Bioconjugate Chemistry 2021
online lesenEnhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer
Journal of Medicinal Chemistry 2021
online lesenPentafluorosulfanyl (SF<sub>5</sub>) as a Superior <sup>19</sup>F Magnetic Resonance Reporter Group: Signal Detection and Biological Activity of Teriflunomide Derivatives.
ACS sensors 2021
online lesenCannabinoid receptor type 2 ligands: an analysis of granted patents since 2010
Pharmaceutical Patent Analyst 2021
online lesenDiverse chemotypes drive biased signaling by cannabinoid receptors
Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells.
Journal of the American Chemical Society 2020
online lesenRevealing cytotoxic substructures in molecules using deep learning
Journal of Computer-Aided Molecular Design 2020
online lesenEine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien
Angewandte Chemie 2020
online lesenAn Activatable Lanthanide Luminescent Probe for Time‐Gated Detection of Nitroreductase in Live Bacteria
Angewandte Chemie International Edition 2020
online lesenBack Cover: An Activatable Lanthanide Luminescent Probe for Time‐Gated Detection of Nitroreductase in Live Bacteria (Angew. Chem. Int. Ed. 22/2020)
Angewandte Chemie International Edition 2020
online lesenRücktitelbild: Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien (Angew. Chem. 22/2020)
Angewandte Chemie 2020
online lesenDual-Mode Detection of Bacterial 16S Ribosomal RNA in Tissues
ACS Sensors 2020
online lesenA Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles
Organic Letters 2020
online lesenPreclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.
Journal of medicinal chemistry 2020
online lesenNMR quality control of fragment libraries for screening.
Journal of biomolecular NMR 2020
online lesenDesigned nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells.
Proceedings of the National Academy of Sciences of the United States of America 2020
online lesenFrom Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
Journal of medicinal chemistry 2020
online lesenSmall-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells
Frontiers in Cellular Neuroscience 2019
online lesenEU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology.
SLAS discovery : advancing life sciences R & D 2019
online lesenA pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels.
Science (New York, N.Y.) 2019
online lesenRapid Synthesis of γ-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen
Organic Letters 2019
online lesenProbing 2H‐Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors
ChemMedChem 2019
online lesenA novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging
Acta Pharmaceutica Sinica B 2018
online lesenMutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase.
Nature medicine 2018
online lesenIdentification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin.
Angewandte Chemie (International ed. in English) 2018
online lesenA General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System.
Chemistry (Weinheim an der Bergstrasse, Germany) 2018
online lesenAllosteric Inhibition of a Mammalian Lectin
Journal of the American Chemical Society 2018
online lesenCellFy-A Cell-Based Fragment Screen against C-Type Lectins.
ACS chemical biology 2018
online lesenA new highly thyrotropin receptor-selective small molecule antagonist with potential for the treatment of Graves' orbitopathy.
Thyroid : official journal of the American Thyroid Association 2018
online lesenUse of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway.
PloS one 2018
online lesenNovel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives
Tetrahedron Letters 2018
online lesenDirect Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances
Angewandte Chemie 2017
online lesenA straightforward approach to N -substituted-2 H -indazol-2-amines through reductive cyclization
Tetrahedron Letters 2017
online lesenLoss of Ptpn11 (Shp2) drives satellite cells into quiescence
eLife 2017
online lesenIdentification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells
SLAS DISCOVERY: Advancing Life Sciences R&D 2017
online lesenDiscovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach.
Journal of medicinal chemistry 2017
online lesen5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors.
Organic & biomolecular chemistry 2016
online lesenChemical fragment arrays for rapid druggability assessment.
Chemical communications (Cambridge, England) 2016
online lesenChemInform Abstract: Organophosphorus-Mediated N-N Bond Formation: Facile Access to 3-Amino-2H-indazoles.
ChemInform 2016
online lesenOrganophosphorus-mediated N–N bond formation: facile access to 3-amino-2H-indazoles
Org. Biomol. Chem. 2016
online lesenModulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5
ChemBioChem 2016
online lesenTemperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures.
Physical chemistry chemical physics : PCCP 2016
online lesenDiscovery ofN-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors
ACS Medicinal Chemistry Letters 2015
online lesenDOTAM Derivatives as Active Cartilage-Targeting Drug Carriers for the Treatment of Osteoarthritis
Bioconjugate Chemistry 2015
online lesenIn vivo visualization of osteoarthritic hypertrophic lesions
Chem. Sci. 2015
online lesenN-[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.
Journal of medicinal chemistry 2014
online lesenTractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform
Molecular Diversity 2014
online lesenHalogen…π Interactions as Important Contributors to Binding Affinity in Medicinal Chemistry
The Importance of Pi-Interactions in Crystal Engineering 2012
online lesenSelective non-lipid modulator of LPA5 activity in human platelets
Bioorganic & Medicinal Chemistry Letters 2012
online lesenIdentification of High-Affinity P2Y12Antagonists Based on a Phenylpyrazole Glutamic Acid Piperazine Backbone
Journal of Medicinal Chemistry 2012
online lesenChemInform Abstract: A General and Mild Domino Approach to Substituted 1-Aminoindoles.
ChemInform 2011
online lesenChemInform Abstract: A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines.
ChemInform 2011
online lesenA general and mild domino approach to substituted 1-aminoindoles
Chem. Commun. 2011
online lesenFragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes
Angewandte Chemie International Edition 2011
online lesenInnenrücktitelbild: Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes (Angew. Chem. 4/2012)
Angewandte Chemie 2011
online lesenA general palladium-catalyzed sonogashira coupling of aryl and heteroaryl tosylates.
Chemistry (Weinheim an der Bergstrasse, Germany) 2010
online lesenChemInform Abstract: Enantiospecific Synthesis of the (9S,18R)-Diastereomer of the Leukocyte Adhesion Inhibitor Cyclamenol A.
ChemInform 2010
online lesenChemInform Abstract: Synthesis of the (9S,18R) Diastereomer of Cyclamenol A.
ChemInform 2010
online lesenChemInform Abstract: A General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates.
ChemInform 2010
online lesenChemInform Abstract: Synthesis of the (9S,18R)-seco Acid of the Leukocyte Adhesion Inhibitor Cyclamenol A.
ChemInform 2010
online lesenChemInform Abstract: A General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles.
ChemInform 2010
online lesenA Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines
European Journal of Organic Chemistry 2010
online lesenEvidence for CCl/CBr⋅⋅⋅π Interactions as an Important Contribution to Protein-Ligand Binding Affinity
Angewandte Chemie 2009
online lesenA General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles
Angewandte Chemie 2009
online lesenProbing 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.
Journal of medicinal chemistry 2005
online lesenStructural requirements for factor Xa inhibition by 3-oxybenzamides with neutral P1 substituents: combining X-ray crystallography, 3D-QSAR, and tailored scoring functions.
Journal of medicinal chemistry 2005
online lesenNovel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Ligand.
ChemInform 2004
online lesenA Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones
Angewandte Chemie International Edition 2004
online lesenNovel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.
Bioorganic & medicinal chemistry letters 2004
online lesenFactor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents.
ChemInform 2004
online lesenEine flexible, palladiumkatalysierte Indol- und Azaindolsynthese durch direkte Anellierung von Chloranilinen und Chloraminopyridinen mit Ketonen
Angewandte Chemie 2004
online lesenA Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones.
ChemInform 2004
online lesenNovel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand
Bioorganic & Medicinal Chemistry Letters 2004
online lesenFactor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents
Bioorganic & Medicinal Chemistry Letters 2004
online lesenEnantiospecific Synthesis of the (9S,18R)-Diastereomer of the Leukocyte Adhesion Inhibitor Cyclamenol A
Chemistry - A European Journal 2001
online lesenEnantiospecific synthesis of the (95,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol a
Chemistry - A European Journal 2001
online lesenSynthese des (9S,18R)-Diastereomers von Cyclamenol A
Angewandte Chemie 2000
online lesenSynthesis of the (9S,18R) Diastereomer of Cyclamenol A
Angewandte Chemie International Edition 2000
online lesenSynthesis of the (9S,18R)-seco acid of the leukocyte adhesion inhibitor cyclamenol A
Tetrahedron Letters 2000
online lesenDas Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP) gehört zum Forschungsverbund Berlin e.V. (FVB), einem Zusammenschluss von sieben natur-, lebens- und umweltwissenschaftlichen Instituten in Berlin. Die Einrichtungen sind Mitglieder der Leibniz-Gemeinschaft.
Leibniz-Forschungsinstitut für Molekulare Pharmakologie im Forschungsverbund Berlin e.V. (FMP)
Campus Berlin-Buch
Robert-Roessle-Str. 10
13125 Berlin, Deutschland