„”
Prof. Dr.
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.
Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.
Chimia 2024
read onlineA universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand binding assay
Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB<sub>1</sub>R).
Journal of medicinal chemistry 2024
read onlineDOTA-Based Plectin-1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue.
Angewandte Chemie (International ed. in English) 2024
read onlineAn activatable biphotonic lanthanide probe for detection of nitroreductase in live bacteria and cancer cells
Patent review of cannabinoid receptor type 2 (CB <sub>2</sub> R) modulators (2016-present)
Expert Opinion on Therapeutic Patents 2024
read onlineBenzo‐Crown‐Ether functionalized O‐BODIPY Probes for Cations– A Selective Fluorescent Probe for Ba2+
Chemistry – A European Journal 2024
read onlineNovel Tryptophan Hydroxylase Inhibitor TPT-001 Reverses PAH, Vascular Remodeling, and Proliferative-Proinflammatory Gene Expression
JACC: Basic to Translational Science 2024
read onlineDOTA‐Based Plectin‐1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue
Angewandte Chemie 2024
read onlineStructure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
Journal of medicinal chemistry 2023
read onlineDiscovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2023
read onlineStructural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.
Journal of medicinal chemistry 2023
read onlineSelective 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
read onlineCLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors.
Cell chemical biology 2023
read onlineAβ Chronic Exposure Promotes an Activation State of Microglia through Endocannabinoid Signalling Imbalance.
International journal of molecular sciences 2023
read onlineCB2R agonists in the clinics: A treasure chest for treating inflammatory diseases
Open Access Government 2023
read onlineCB₂R ligands to treat inflammatory diabetes
Open Access Government 2023
read onlineFirst<i> in</i><i> vivo</i> fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod
Theranostics 2023
read onlineNovel tetrazolopyridazine based MACC1 transcriptional inhibitors as promising anti-metastatic therapy
Cancer Research 2023
read onlineIsoform-selective targeting of PI3K: time to consider new opportunities?
Trends in Pharmacological Sciences 2023
read onlineSmall molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation
Plos One 2023
read onlineDevelopment of selective inhibitors of phosphatidylinositol 3-kinase C2α
Nature Chemical Biology 2023
read onlineAn LPAR <sub><b>5</b></sub> -antagonist that reduces nociception and increases pruriception.
Frontiers in pain research (Lausanne, Switzerland) 2022
read onlineDonor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles
Talanta 2022
read onlineReverse Design toward Optimized Labeled Chemical Probes - Examples from the Endocannabinoid System
Chimia 2022
read onlineAntagonistic 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
read onlineStructure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors
Journal of Medicinal Chemistry 2022
read onlineWeizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+Probability and CASE-3D
Journal of Natural Products 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin
ACS Chemical Biology 2022
read onlinePhosphoinositide Conversion Inactivates R-RAS and Drives Metastases in Breast Cancer
Advanced Science 2022
read onlineBODIPY-Equipped Benzo-Crown-Ethers as Fluorescent Sensors for pH Independent Detection of Sodium and Potassium Ions
ChemPhotoChem 2022
read onlineDetection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe
Chemical Science 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the Lectin Langerin
ACS Chemical Biology 2022
read onlineProbing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands
Journal of Medicinal Chemistry 2022
read onlineCompound Interaction Screen on a Photoactivatable Cellulose Membrane (CISCM) Identifies Drug Targets
ChemMedChem 2022
read onlineRational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis
Journal of Medicinal Chemistry 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin
OpenAlex 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin
OpenAlex 2022
read onlineIn vivo detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy
Theranostics 2021
read onlineCannabinoid receptor type 2 ligands: an analysis of granted patents since 2010
Pharmaceutical Patent Analyst 2021
read onlineEnhanced 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
read onlineDevelopment of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II
Journal of Medicinal Chemistry 2021
read onlineTopical inflammasome inhibition with disulfiram prevents irritant contact dermatitis
Clinical and Translational Allergy 2021
read onlineFunctional Imaging Using Fluorine (F-19) MR Methods: Basic Concepts
Methods in Molecular Biology 2021
read onlineStructural Basis for Gating of the Two-Pore Domain K<SUP>+</SUP> (K<sub>2P</sub>) Channels TASK-1 and TALK-2
Biophysical Journal 2021
read onlineDOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells
Bioconjugate Chemistry 2021
read onlinePentafluorosulfanyl (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
read onlineGeneration of a TR-FRET-based assay for the determination of cannabinoid CB1 receptor ligand binding kinetics
British Journal of Pharmacology 2021
read onlinePreclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor
Journal of Medicinal Chemistry 2020
read onlineDesigned nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells
Proceedings of the National Academy of Sciences 2020
read onlineDevelopment and application of a kinetic ligand binding assay for the cannabinoid receptor 1 using resonance energy transfer approaches
British Journal of Pharmacology 2020
read onlineFrom Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement
Journal of Medicinal Chemistry 2020
read onlineRevealing cytotoxic substructures in molecules using deep learning
Journal of Computer-Aided Molecular Design 2020
read onlineNMR quality control of fragment libraries for screening
Journal of Biomolecular NMR 2020
read onlineDevelopment of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells
Journal of the American Chemical Society 2020
read onlineDiverse chemotypes drive biased signaling by cannabinoid receptors
Dual-Mode Detection of Bacterial 16S Ribosomal RNA in Tissues
ACS Sensors 2020
read onlineEine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien
Angewandte Chemie 2020
read onlineBack 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
read onlineRücktitelbild: Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien (Angew. Chem. 22/2020)
Angewandte Chemie 2020
read onlineA Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles
Organic Letters 2020
read onlineAn Activatable Lanthanide Luminescent Probe for Time-Gated Detection of Nitroreductase in Live Bacteria
Angewandte Chemie International Edition 2020
read onlinePreclinical efficacy of NLRP3 small molecule inflammasome inhibitors: Implications for future treatment of autoinflammatory syndromes
Experimental Dermatology 2019
read onlineTopical inflammasome inhibition-a novel treatment strategy for contact dermatitis
Experimental Dermatology 2019
read onlineProbing 2<i>H</i>-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors
ChemMedChem 2019
read onlineSmall-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells
Frontiers in Cellular Neuroscience 2019
read onlineA New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves' Orbitopathy
Thyroid 2019
read onlineEU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology
SLAS Discovery: Advancing Life Sciences R & D 2019
read onlineA pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels
Science 2019
read onlineRapid Synthesis of gamma-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen
Organic Letters 2019
read onlineIdentification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin
Angewandte Chemie International Edition 2018
read onlineA novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging
Acta Pharmaceutica Sinica B 2018
read onlineMutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase
Nature Medicine 2018
read onlineAllosteric Inhibition of a Mammalian Lectin
Journal of the American Chemical Society 2018
read onlineIn Vivo Imaging of MMP-13 Activity Using a Specific Polymer-FRET Peptide Conjugate Detects Early Osteoarthritis and Inhibitor Efficacy
Advanced Functional Materials 2018
read onlineA General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System
Chemistry - A European Journal 2018
read onlineCellFy: A Cell-Based Fragment Screen against C-Type Lectins
ACS Chemical Biology 2018
read onlineUse of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway
Plos One 2018
read onlineNovel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives
Tetrahedron Letters 2018
read onlineRegulation of Two-pore Domain K plus Channels by Natural Effectors and Pharmacological Agents
Acta Physiologica 2017
read onlineA straightforward approach to N-substituted-2H-indazol-2-amines through reductive cyclization
Tetrahedron Letters 2017
read onlineNovel compounds targeting microglial nitric oxide release
Glia 2017
read onlineN-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals
Official Gazette of the United States Patent and Trademark Office Patents 2017
read onlineIdentification 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
read onlineDirect Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances
Angewandte Chemie 2017
read onlineA conserved drug-binding site controls the selectivity filter gate in K2P K+ channels
Acta Physiologica 2017
read onlineLoss of Ptpn11 (Shp2) drives satellite cells into quiescence
eLife 2017
read onlineDiscovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach
Journal of Medicinal Chemistry 2017
read onlineTemperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures
Physical Chemistry Chemical Physics 2016
read online5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors
Organic & Biomolecular Chemistry 2016
read onlinePyrazole derivatives and their use as LPAR5 antagonists
Official Gazette of the United States Patent and Trademark Office Patents 2016
read onlineChemInform Abstract: Organophosphorus-Mediated N-N Bond Formation: Facile Access to 3-Amino-2H-indazoles
ChemInform 2016
read onlinePharmacological targeting of human tryptophan hydroxylase - novel inhibitors for the treatment of serotonin-related diseases
Naunyn-Schmiedeberg's Archives of Pharmacology 2016
read onlineModulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5
Chembiochem 2016
read onlineOrganophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles
Organic & Biomolecular Chemistry 2016
read onlineChemical fragment arrays for rapid druggability assessment
Chemical Communications 2016
read onlineDEVELOPMENT OF IMAGING AGENTS FOR THE VISUALISATION OF CARTILAGE IN VIVO
Osteoarthritis and Cartilage 2015
read onlineDiscovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]sulfonamides as Highly Active and Selective SGK1 Inhibitors
ACS Medicinal Chemistry Letters 2015
read onlineDOTAM Derivatives as Active Cartilage-Targeting Drug Carriers for the Treatment of Osteoarthritis
Bioconjugate Chemistry 2015
read onlineIn vivo visualization of osteoarthritic hypertrophic lesions
Chemical Science 2015
read onlineTractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform
Molecular Diversity 2014
read onlineQuinoline-carboxamide derivatives as P2Y12 antagonists
Official Gazette of the United States Patent and Trademark Office Patents 2014
read onlineN-[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
read onlineIdentification of High-Affinity P2Y(12) Antagonists Based on a Phenylpyrazole Glutamic Acid Piperazine Backbone
Journal of Medicinal Chemistry 2012
read onlineSelective non-lipid modulator of LPA5 activity in human platelets
Bioorganic & Medicinal Chemistry Letters 2012
read onlineFragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes
Angewandte Chemie 2011
read onlineInnenrücktitelbild: 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
read onlineChemInform Abstract: A General and Mild Domino Approach to Substituted 1-Aminoindoles
ChemInform 2011
read onlineChemInform Abstract: A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines
ChemInform 2011
read onlineA Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines
European Journal of Organic Chemistry 2011
read onlineA general and mild domino approach to substituted 1-aminoindoles
Chemical Communications 2011
read onlineChemInform Abstract: Enantiospecific Synthesis of the (9S,18R)-Diastereomer of the Leukocyte Adhesion Inhibitor Cyclamenol A
ChemInform 2010
read onlineChemInform Abstract: Synthesis of the (9S,18R) Diastereomer of Cyclamenol A
ChemInform 2010
read onlineA General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates
Chemistry - A European Journal 2010
read onlineChemInform Abstract: Synthesis of the (9S,18R)-seco Acid of the Leukocyte Adhesion Inhibitor Cyclamenol A
ChemInform 2010
read onlineChemInform Abstract: A General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates
ChemInform 2010
read onlineChemInform Abstract: A General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles
ChemInform 2010
read onlineA General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles
Angewandte Chemie 2009
read onlineEvidence for CCl/CBr⋅⋅⋅π Interactions as an Important Contribution to Protein-Ligand Binding Affinity
Angewandte Chemie 2009
read onlineStructural 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
read onlineProbing 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
read onlineNovel 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
read onlineNovel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Ligand
ChemInform 2004
read onlineFactor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents
ChemInform 2004
read onlineEine flexible, palladiumkatalysierte Indol- und Azaindolsynthese durch direkte Anellierung von Chloranilinen und Chloraminopyridinen mit Ketonen
Angewandte Chemie 2004
read onlineA Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones
ChemInform 2004
read onlineNovel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand
Bioorganic & Medicinal Chemistry Letters 2004
read onlineFlexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones
Angewandte Chemie International Edition 2004
read onlineFactor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral PI substituents
Bioorganic & Medicinal Chemistry Letters 2004
read onlineEnantiospecific synthesis of the (9S,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol A
Chemistry - A European Journal 2001
read onlineEnantiospecific synthesis of the (95,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol a
Chemistry - A European Journal 2001
read onlineSynthese des (9S,18R)-Diastereomers von Cyclamenol A
Angewandte Chemie 2000
read onlineSynthesis of the (9S,18R) diastereomer of cyclamenol A
Angewandte Chemie International Edition 2000
read onlineSynthesis of the (9S, 18R)-seco acid of the leukocyte adhesion inhibitor cyclamenol A
Tetrahedron Letters 2000
read onlineEnhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.
Chimia 2024
read onlineA universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand binding assay
Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CB<sub>1</sub>R).
Journal of medicinal chemistry 2024
read onlineDOTA-Based Plectin-1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue.
Angewandte Chemie (International ed. in English) 2024
read onlineAn activatable biphotonic lanthanide probe for detection of nitroreductase in live bacteria and cancer cells
Patent review of cannabinoid receptor type 2 (CB <sub>2</sub> R) modulators (2016-present)
Expert Opinion on Therapeutic Patents 2024
read onlineBenzo‐Crown‐Ether functionalized O‐BODIPY Probes for Cations– A Selective Fluorescent Probe for Ba2+
Chemistry – A European Journal 2024
read onlineNovel Tryptophan Hydroxylase Inhibitor TPT-001 Reverses PAH, Vascular Remodeling, and Proliferative-Proinflammatory Gene Expression
JACC: Basic to Translational Science 2024
read onlineDOTA‐Based Plectin‐1 Targeted Contrast Agent Enables Detection of Pancreatic Cancer in Human Tissue
Angewandte Chemie 2024
read onlineStructure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
Journal of medicinal chemistry 2023
read onlineDiscovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2023
read onlineStructural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.
Journal of medicinal chemistry 2023
read onlineSelective 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
read onlineCLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors.
Cell chemical biology 2023
read onlineAβ Chronic Exposure Promotes an Activation State of Microglia through Endocannabinoid Signalling Imbalance.
International journal of molecular sciences 2023
read onlineCB2R agonists in the clinics: A treasure chest for treating inflammatory diseases
Open Access Government 2023
read onlineCB₂R ligands to treat inflammatory diabetes
Open Access Government 2023
read onlineFirst<i> in</i><i> vivo</i> fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod
Theranostics 2023
read onlineNovel tetrazolopyridazine based MACC1 transcriptional inhibitors as promising anti-metastatic therapy
Cancer Research 2023
read onlineIsoform-selective targeting of PI3K: time to consider new opportunities?
Trends in Pharmacological Sciences 2023
read onlineSmall molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation
Plos One 2023
read onlineDevelopment of selective inhibitors of phosphatidylinositol 3-kinase C2α
Nature Chemical Biology 2023
read onlineAn LPAR <sub><b>5</b></sub> -antagonist that reduces nociception and increases pruriception.
Frontiers in pain research (Lausanne, Switzerland) 2022
read onlineDonor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles
Talanta 2022
read onlineReverse Design toward Optimized Labeled Chemical Probes - Examples from the Endocannabinoid System
Chimia 2022
read onlineAntagonistic 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
read onlineStructure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors
Journal of Medicinal Chemistry 2022
read onlineWeizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+Probability and CASE-3D
Journal of Natural Products 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin
ACS Chemical Biology 2022
read onlinePhosphoinositide Conversion Inactivates R-RAS and Drives Metastases in Breast Cancer
Advanced Science 2022
read onlineBODIPY-Equipped Benzo-Crown-Ethers as Fluorescent Sensors for pH Independent Detection of Sodium and Potassium Ions
ChemPhotoChem 2022
read onlineDetection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe
Chemical Science 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the Lectin Langerin
ACS Chemical Biology 2022
read onlineProbing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands
Journal of Medicinal Chemistry 2022
read onlineCompound Interaction Screen on a Photoactivatable Cellulose Membrane (CISCM) Identifies Drug Targets
ChemMedChem 2022
read onlineRational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis
Journal of Medicinal Chemistry 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin
OpenAlex 2022
read onlineIdentification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin
OpenAlex 2022
read onlineIn vivo detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy
Theranostics 2021
read onlineCannabinoid receptor type 2 ligands: an analysis of granted patents since 2010
Pharmaceutical Patent Analyst 2021
read onlineEnhanced 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
read onlineDevelopment of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II
Journal of Medicinal Chemistry 2021
read onlineTopical inflammasome inhibition with disulfiram prevents irritant contact dermatitis
Clinical and Translational Allergy 2021
read onlineFunctional Imaging Using Fluorine (F-19) MR Methods: Basic Concepts
Methods in Molecular Biology 2021
read onlineStructural Basis for Gating of the Two-Pore Domain K<SUP>+</SUP> (K<sub>2P</sub>) Channels TASK-1 and TALK-2
Biophysical Journal 2021
read onlineDOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells
Bioconjugate Chemistry 2021
read onlinePentafluorosulfanyl (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
read onlineGeneration of a TR-FRET-based assay for the determination of cannabinoid CB1 receptor ligand binding kinetics
British Journal of Pharmacology 2021
read onlinePreclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor
Journal of Medicinal Chemistry 2020
read onlineDesigned nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells
Proceedings of the National Academy of Sciences 2020
read onlineDevelopment and application of a kinetic ligand binding assay for the cannabinoid receptor 1 using resonance energy transfer approaches
British Journal of Pharmacology 2020
read onlineFrom Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement
Journal of Medicinal Chemistry 2020
read onlineRevealing cytotoxic substructures in molecules using deep learning
Journal of Computer-Aided Molecular Design 2020
read onlineNMR quality control of fragment libraries for screening
Journal of Biomolecular NMR 2020
read onlineDevelopment of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells
Journal of the American Chemical Society 2020
read onlineDiverse chemotypes drive biased signaling by cannabinoid receptors
Dual-Mode Detection of Bacterial 16S Ribosomal RNA in Tissues
ACS Sensors 2020
read onlineEine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien
Angewandte Chemie 2020
read onlineBack 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
read onlineRücktitelbild: Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien (Angew. Chem. 22/2020)
Angewandte Chemie 2020
read onlineA Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles
Organic Letters 2020
read onlineAn Activatable Lanthanide Luminescent Probe for Time-Gated Detection of Nitroreductase in Live Bacteria
Angewandte Chemie International Edition 2020
read onlinePreclinical efficacy of NLRP3 small molecule inflammasome inhibitors: Implications for future treatment of autoinflammatory syndromes
Experimental Dermatology 2019
read onlineTopical inflammasome inhibition-a novel treatment strategy for contact dermatitis
Experimental Dermatology 2019
read onlineProbing 2<i>H</i>-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors
ChemMedChem 2019
read onlineSmall-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells
Frontiers in Cellular Neuroscience 2019
read onlineA New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves' Orbitopathy
Thyroid 2019
read onlineEU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology
SLAS Discovery: Advancing Life Sciences R & D 2019
read onlineA pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels
Science 2019
read onlineRapid Synthesis of gamma-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen
Organic Letters 2019
read onlineIdentification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin
Angewandte Chemie International Edition 2018
read onlineA novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging
Acta Pharmaceutica Sinica B 2018
read onlineMutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase
Nature Medicine 2018
read onlineAllosteric Inhibition of a Mammalian Lectin
Journal of the American Chemical Society 2018
read onlineIn Vivo Imaging of MMP-13 Activity Using a Specific Polymer-FRET Peptide Conjugate Detects Early Osteoarthritis and Inhibitor Efficacy
Advanced Functional Materials 2018
read onlineA General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System
Chemistry - A European Journal 2018
read onlineCellFy: A Cell-Based Fragment Screen against C-Type Lectins
ACS Chemical Biology 2018
read onlineUse of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway
Plos One 2018
read onlineNovel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives
Tetrahedron Letters 2018
read onlineRegulation of Two-pore Domain K plus Channels by Natural Effectors and Pharmacological Agents
Acta Physiologica 2017
read onlineA straightforward approach to N-substituted-2H-indazol-2-amines through reductive cyclization
Tetrahedron Letters 2017
read onlineNovel compounds targeting microglial nitric oxide release
Glia 2017
read onlineN-(4-(azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals
Official Gazette of the United States Patent and Trademark Office Patents 2017
read onlineIdentification 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
read onlineDirect Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances
Angewandte Chemie 2017
read onlineA conserved drug-binding site controls the selectivity filter gate in K2P K+ channels
Acta Physiologica 2017
read onlineLoss of Ptpn11 (Shp2) drives satellite cells into quiescence
eLife 2017
read onlineDiscovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach
Journal of Medicinal Chemistry 2017
read onlineTemperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures
Physical Chemistry Chemical Physics 2016
read online5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors
Organic & Biomolecular Chemistry 2016
read onlinePyrazole derivatives and their use as LPAR5 antagonists
Official Gazette of the United States Patent and Trademark Office Patents 2016
read onlineChemInform Abstract: Organophosphorus-Mediated N-N Bond Formation: Facile Access to 3-Amino-2H-indazoles
ChemInform 2016
read onlinePharmacological targeting of human tryptophan hydroxylase - novel inhibitors for the treatment of serotonin-related diseases
Naunyn-Schmiedeberg's Archives of Pharmacology 2016
read onlineModulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5
Chembiochem 2016
read onlineOrganophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles
Organic & Biomolecular Chemistry 2016
read onlineChemical fragment arrays for rapid druggability assessment
Chemical Communications 2016
read onlineDEVELOPMENT OF IMAGING AGENTS FOR THE VISUALISATION OF CARTILAGE IN VIVO
Osteoarthritis and Cartilage 2015
read onlineDiscovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]sulfonamides as Highly Active and Selective SGK1 Inhibitors
ACS Medicinal Chemistry Letters 2015
read onlineDOTAM Derivatives as Active Cartilage-Targeting Drug Carriers for the Treatment of Osteoarthritis
Bioconjugate Chemistry 2015
read onlineIn vivo visualization of osteoarthritic hypertrophic lesions
Chemical Science 2015
read onlineTractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform
Molecular Diversity 2014
read onlineQuinoline-carboxamide derivatives as P2Y12 antagonists
Official Gazette of the United States Patent and Trademark Office Patents 2014
read onlineN-[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
read onlineTargeting Platelet G Protein-Coupled Receptors for Antithrombotic Therapy
Drug Development Research 2013
read onlineIdentification of High-Affinity P2Y(12) Antagonists Based on a Phenylpyrazole Glutamic Acid Piperazine Backbone
Journal of Medicinal Chemistry 2012
read onlineSelective non-lipid modulator of LPA5 activity in human platelets
Bioorganic & Medicinal Chemistry Letters 2012
read onlineFragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes
Angewandte Chemie 2011
read onlineInnenrücktitelbild: 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
read onlineChemInform Abstract: A General and Mild Domino Approach to Substituted 1-Aminoindoles
ChemInform 2011
read onlineChemInform Abstract: A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines
ChemInform 2011
read onlineA Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines
European Journal of Organic Chemistry 2011
read onlineA general and mild domino approach to substituted 1-aminoindoles
Chemical Communications 2011
read onlineChemInform Abstract: Enantiospecific Synthesis of the (9S,18R)-Diastereomer of the Leukocyte Adhesion Inhibitor Cyclamenol A
ChemInform 2010
read onlineChemInform Abstract: Synthesis of the (9S,18R) Diastereomer of Cyclamenol A
ChemInform 2010
read onlineA General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates
Chemistry - A European Journal 2010
read onlineChemInform Abstract: Synthesis of the (9S,18R)-seco Acid of the Leukocyte Adhesion Inhibitor Cyclamenol A
ChemInform 2010
read onlineChemInform Abstract: A General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates
ChemInform 2010
read onlineChemInform Abstract: A General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles
ChemInform 2010
read onlineA General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles
Angewandte Chemie 2009
read onlineEvidence for CCl/CBr⋅⋅⋅π Interactions as an Important Contribution to Protein-Ligand Binding Affinity
Angewandte Chemie 2009
read onlineStructural 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
read onlineProbing 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
read onlineNovel 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
read onlineNovel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Ligand
ChemInform 2004
read onlineFactor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents
ChemInform 2004
read onlineEine flexible, palladiumkatalysierte Indol- und Azaindolsynthese durch direkte Anellierung von Chloranilinen und Chloraminopyridinen mit Ketonen
Angewandte Chemie 2004
read onlineA Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones
ChemInform 2004
read onlineNovel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand
Bioorganic & Medicinal Chemistry Letters 2004
read onlineFlexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones
Angewandte Chemie International Edition 2004
read onlineFactor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral PI substituents
Bioorganic & Medicinal Chemistry Letters 2004
read onlineEnantiospecific synthesis of the (9S,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol A
Chemistry - A European Journal 2001
read onlineEnantiospecific synthesis of the (95,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol a
Chemistry - A European Journal 2001
read onlineSynthese des (9S,18R)-Diastereomers von Cyclamenol A
Angewandte Chemie 2000
read onlineSynthesis of the (9S,18R) diastereomer of cyclamenol A
Angewandte Chemie International Edition 2000
read onlineSynthesis of the (9S, 18R)-seco acid of the leukocyte adhesion inhibitor cyclamenol A
Tetrahedron Letters 2000
read onlineEfficient enantioselective synthesis of a beta-hydroxyepoxide building block for the construction of macrocyclic natural products
Tetrahedron Letters 1998
read onlineHalogen…π Interactions as Important Contributors to Binding Affinity in Medicinal Chemistry
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
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
CRYSTAL STRUCTURE OF FACTOR XA IN COMPLEX WITH COMPOUND 45
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
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
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
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
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
The Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP) is part of the Forschungsverbund Berlin e.V. (FVB), which legally represents seven non-university research institutes - members of the Leibniz Association - in Berlin.
Leibniz-Forschungsinstitut für Molekulare Pharmakologie im Forschungsverbund Berlin e.V. (FMP)
Campus Berlin-Buch
Robert-Roessle-Str. 10,
13125 Berlin, Germany