Marc Nazaré

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

• Li H; Prever L; Hsu MY; Lo WT; Margaria JP; De Santis MC; Zanini C; Forni M; Novelli F; Pece S; Di Fiore PP; Porporato PE; Martini M; Belabed H; Hirsch E

Advanced science (Weinheim, Baden-Wurttemberg, Germany) 2022

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

• Fernández-Bachiller MI; Hwang S; Schembri ME; Lindemann P; Guberman M; Herziger S; Specker E; Matter H; Will DW; Czech J; Wagner M; Bauer A; Nazaré M

Journal of medicinal chemistry 2022

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

• Zhang H; Modenutti C; Nekkanti YPK; Denis M; Bermejo IA; Lefèbre J; Che K; Kim D; Kagelmacher M; Kurzbach D; Nazaré M; Rademacher C

ACS chemical biology 2022

Development of selective inhibitors of phosphatidylinositol 3-kinase C2α.

• Lo WT; Belabed H; Kücükdisli M; Metag J; Roske Y; Prokofeva P; Ohashi Y; Horatscheck A; Cirillo D; Krauss M; Schmied C; Neuenschwander M; Haucke V

Nature chemical biology 2022

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

• Specker E; Matthes S; Wesolowski R; Schütz A; Grohmann M; Alenina N; Pleimes D; Mallow K; Neuenschwander M; Gogolin A; Weise M; Pfeifer J; Ziebart N; Bader M

Journal of medicinal chemistry 2022

An LPAR _<b>5</b> -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

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

• Gazzi T; Brennecke B; Atz K; Korn C; Sykes D; Forn-Cuni G; Pfaff P; Sarott RC; Westphal MV; Mostinski Y; Mach L; Wasinska-Kalwa M; Weise M; Hoare BL; Nazaré M

Chemical science 2022

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

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

Journal of Medicinal Chemistry 2022

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

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

Talanta 2022

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

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

Proceedings of the National Academy of Sciences 2022

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

• Mónica Guberman; Miroslav Kosar; Anahid Omran; Erick M. Carreira; Marc Nazaré; Uwe Grether

CHIMIA 2022

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

• F. Teresa I. Melder; Peter Lindemann; Alexander Welle; Vanessa Trouillet; Stefan Heißler; Marc Nazaré; Matthias Selbach

ChemMedChem 2022

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

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

Journal of Natural Products 2022

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

• Leenders RGG; Brinch SA; Sowa ST; Amundsen-Isaksen E; Galera-Prat A; Murthy S; Aertssen S; Smits JN; Nieczypor P; Damen E; Wegert A; Nazaré M; Krauss S

Journal of medicinal chemistry 2021

Topical inflammasome inhibition with disulfiram prevents irritant contact dermatitis.

• Bonnekoh H; Vera C; Abad-Perez A; Radetzki S; Neuenschwander M; Specker E; Mahnke NA; Frischbutter S; Latz E; Nazaré M; Kries JV; Maurer M; Scheffel J; Krause K

Clinical and translational allergy 2021

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

• Waiczies S; Prinz C; Starke L; Millward JM; Delgado PR; Rosenberg J; Nazaré M; Waiczies H; Pohlmann A; Niendorf T

Methods in molecular biology (Clifton, N.J.) 2021

<i>In vivo</i> detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy.

• Prinz C; Starke L; Millward JM; Fillmer A; Delgado PR; Waiczies H; Pohlmann A; Rothe M; Nazaré M; Paul F; Niendorf T; Waiczies S

Theranostics 2021

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

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

Bioconjugate Chemistry 2021

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

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

Journal of Medicinal Chemistry 2021

Pentafluorosulfanyl (SF₅) as a Superior ¹⁹F Magnetic Resonance Reporter Group: Signal Detection and Biological Activity of Teriflunomide Derivatives.

• Prinz C; Starke L; Ramspoth TF; Kerkering J; Martos Riaño V; Paul J; Neuenschwander M; Oder A; Radetzki S; Adelhoefer S; Ramos Delgado P; Aravina M; Waiczies S

ACS sensors 2021

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

• Benjamin Brennecke; Thais Gazzi; Kenneth Atz; Jürgen Fingerle; Pascal Kuner; Torsten Schindler; Guy de Weck; Marc Nazaré; Uwe Grether

Pharmaceutical Patent Analyst 2021

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

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

• Sarott RC; Westphal MV; Pfaff P; Korn C; Sykes DA; Gazzi T; Brennecke B; Atz K; Weise M; Mostinski Y; Hompluem P; Koers E; Miljuš T; Roth NJ; Carreira EM

Journal of the American Chemical Society 2020

Revealing cytotoxic substructures in molecules using deep learning

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

Journal of Computer-Aided Molecular Design 2020

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

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

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

Angewandte Chemie International Edition 2020

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

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

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

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

• Rana Alsalim; Peter Lindemann; María Pascual López-Alberca; Sandra Miksche; Werngard Czechtizky; Nis Halland; Marc Nazaré

Organic Letters 2020

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

• Waaler J; Leenders RGG; Sowa ST; Alam Brinch S; Lycke M; Nieczypor P; Aertssen S; Murthy S; Galera-Prat A; Damen E; Wegert A; Nazaré M; Lehtiö L; Krauss S

Journal of medicinal chemistry 2020

NMR quality control of fragment libraries for screening.

• Sreeramulu S; Richter C; Kuehn T; Azzaoui K; Blommers MJJ; Del Conte R; Fragai M; Trieloff N; Schmieder P; Nazaré M; Specker E; Ivanov V; Schwalbe H

Journal of biomolecular NMR 2020

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

• Barone M; Müller M; Chiha S; Ren J; Albat D; Soicke A; Dohmen S; Klein M; Bruns J; van Dinther M; Opitz R; Lindemann P; Beerbaum M; Motzny K; Kühne R

Proceedings of the National Academy of Sciences of the United States of America 2020

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

• Mostinski Y; Heynen GJJE; López-Alberca MP; Paul J; Miksche S; Radetzki S; Schaller D; Shanina E; Seyffarth C; Kolomeets Y; Ziebart N; de Schryver J; Nazaré M

Journal of medicinal chemistry 2020

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

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

• Brennecke P; Rasina D; Aubi O; Herzog K; Landskron J; Cautain B; Vicente F; Quintana J; Mestres J; Stechmann B; Ellinger B; Brea J; Kolanowski JL; Gribbon P

SLAS discovery : advancing life sciences R & D 2019

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

• Schewe M; Sun H; Mert Ü; Mackenzie A; Pike ACW; Schulz F; Constantin C; Vowinkel KS; Conrad LJ; Kiper AK; Gonzalez W; Musinszki M; Tegtmeier M; Baukrowitz T

Science (New York, N.Y.) 2019

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

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

Organic Letters 2019

Probing 2H‐Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors

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

ChemMedChem 2019

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

• Liu, Y.; Zhang, L.; Nazare, M.; Yao, Q.; Hu, H.-Y.

Acta Pharmaceutica Sinica B 2018

Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase.

• Ruess DA; Heynen GJ; Ciecielski KJ; Ai J; Berninger A; Kabacaoglu D; Görgülü K; Dantes Z; Wörmann SM; Diakopoulos KN; Karpathaki AF; Kowalska M; Algül H

Nature medicine 2018

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

• Wenskowsky L; Schreuder H; Derdau V; Matter H; Volkmar J; Nazaré M; Opatz T; Petry S

Angewandte Chemie (International ed. in English) 2018

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

• Schoene J; Bel Abed H; Schmieder P; Christmann M; Nazaré M

Chemistry (Weinheim an der Bergstrasse, Germany) 2018

Allosteric Inhibition of a Mammalian Lectin

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

Journal of the American Chemical Society 2018

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

• Schulze J; Baukmann H; Wawrzinek R; Fuchsberger F; Specker E; Aretz J; Nazaré M; Rademacher C

ACS chemical biology 2018

A new highly thyrotropin receptor-selective small molecule antagonist with potential for the treatment of Graves' orbitopathy.

• Marcinkowski P; Hoyer I; Specker E; Furkert J; Rutz C; Neuenschwander M; Sobottka S; Sun H; Nazare M; Berchner-Pfannschmidt U; von Kries JP; Krause G

Thyroid : official journal of the American Thyroid Association 2018

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

• Klein W; Rutz C; Eckhard J; Provinciael B; Specker E; Neuenschwander M; Kleinau G; Scheerer P; von Kries JP; Nazaré M; Vermeire K; Schülein R

PloS one 2018

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

• Bel Abed, H.; Weißing, N.; Schoene, J.; Paulus, J.; Sewald, N.; Nazaré, M.

Tetrahedron Letters 2018

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

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

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

Tetrahedron Letters 2017

Loss of Ptpn11 (Shp2) drives satellite cells into quiescence

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

eLife 2017

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

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

SLAS DISCOVERY: Advancing Life Sciences R&D 2017

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

• Anumala UR; Waaler J; Nkizinkiko Y; Ignatev A; Lazarow K; Lindemann P; Olsen PA; Murthy S; Obaji E; Majouga AG; Leonov S; von Kries JP; Lehtiö L; Nazaré M

Journal of medicinal chemistry 2017

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

• Marc Nazaré

Organic & biomolecular chemistry 2016

Chemical fragment arrays for rapid druggability assessment.

• Marc Nazaré

Chemical communications (Cambridge, England) 2016

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

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

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

Org. Biomol. Chem. 2016

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

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

ChemBioChem 2016

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

• Geiger MA; Orwick-Rydmark M; Märker K; Franks WT; Akhmetzyanov D; Stöppler D; Zinke M; Specker E; Nazaré M; Diehl A; van Rossum BJ; Aussenac F; Oschkinat H

Physical chemistry chemical physics : PCCP 2016

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

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

A general and mild domino approach to substituted 1-aminoindoles

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

Chem. Commun. 2011

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 International Edition 2011

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

A general palladium-catalyzed sonogashira coupling of aryl and heteroaryl tosylates.

• Marc Nazaré

Chemistry (Weinheim an der Bergstrasse, Germany) 2010

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

• Marc Nazare; Herbert Waldmann

ChemInform 2010

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

• Marc Nazare; Herbert Waldmann

ChemInform 2010

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

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

• Marc Nazare; Herbert Waldmann

ChemInform 2010

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

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

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

European Journal of Organic Chemistry 2010

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

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

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

Angewandte Chemie International Edition 2004

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

• Marc Nazaré

Bioorganic & medicinal chemistry letters 2004

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

• Marc Nazare; et al. et al.

ChemInform 2004

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

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

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

• Marc Nazaré; Melanie Essrich; David W Will; Hans Matter; Kurt Ritter; Matthias Urmann; Armin Bauer; Herman Schreuder; Jörg Czech; Martin Lorenz; Volker Laux; Volkmar Wehner

Bioorganic & Medicinal Chemistry Letters 2004

Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents

• Marc Nazaré; Melanie Essrich; David W Will; Hans Matter; Kurt Ritter; Matthias Urmann; Armin Bauer; Herman Schreuder; Angela Dudda; Jörg Czech; Martin Lorenz; Volker Laux; Volkmar Wehner

Bioorganic & Medicinal Chemistry Letters 2004