Rob Leurs

Publication Activity (10 Years)

Years Active: 2018-2024
Publications (10 Years): 54

Top Topics

Molecular Docking

Structural Basis

Binding Protein

Top Venues

Journal of medicinal chemistry

International journal of molecular sciences

Molecular pharmacology

This page only lists publications with an associated author ORCID identifier.

Publications

Yang Zheng, Magali van den Kerkhof, Mohamed Ibrahim, Iwan J P de Esch, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy. Journal of medicinal chemistry (2024)
Justyna M Adamska, Spyridon Leftheriotis, Reggie Bosma, Henry F Vischer, Rob Leurs
Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET. International journal of molecular sciences 25 (9) (2024)
Yang Zheng, Magali van den Kerkhof, Mohamed Ibrahim, Iwan J P de Esch, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy. Journal of medicinal chemistry 67 (4) (2024)
Yang Zheng, Meichun Gao, Maikel Wijtmans, Henry F Vischer, Rob Leurs
Synthesis and Pharmacological Characterization of New Photocaged Agonists for Histamine H 3 and H 4 Receptors. Pharmaceuticals (Basel, Switzerland) 17 (4) (2024)
Yang Zheng, Meichun Gao, Maikel Wijtmans, Henry F Vischer, Rob Leurs
Synthesis and Pharmacological Characterization of New Photocaged Agonists for Histamine H 3 and H 4 Receptors. Pharmaceuticals (Basel, Switzerland) 17 (4) (2024)
Justyna M Adamska, Spyridon Leftheriotis, Reggie Bosma, Henry F Vischer, Rob Leurs
Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET. International journal of molecular sciences 25 (9) (2024)
Yang Zheng, Magali van den Kerkhof, Mohamed Ibrahim, Iwan J P de Esch, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy. Journal of medicinal chemistry 67 (4) (2024)
Meichun Gao, Jasper F Ooms, Rob Leurs, Henry F Vischer
Histamine H 3 Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity. Biomolecules 14 (7) (2024)
Aurelien M Zarca, Ilze Adlere, Cristina P Viciano, Marta Arimont-Segura, Max Meyrath, Icaro A Simon, Jan Paul Bebelman, Dennis Laan, Hans G J Custers, Elwin Janssen, Kobus L Versteegh, Maurice C M L Buzink, Desislava N Nesheva, Reggie Bosma, Iwan J P de Esch, Henry F Vischer, Maikel Wijtmans, Martyna Szpakowska, Andy Chevigné, Carsten Hoffmann, Chris de Graaf, Barbara A Zarzycka, Albert D Windhorst, Martine J Smit, Rob Leurs
Pharmacological Characterization and Radiolabeling of VUF15485, a High-Affinity Small-Molecule Agonist for the Atypical Chemokine Receptor ACKR3. Molecular pharmacology 105 (4) (2024)
Aurelien M Zarca, Ilze Adlere, Cristina P Viciano, Marta Arimont-Segura, Max Meyrath, Icaro A Simon, Jan Paul Bebelman, Dennis Laan, Hans G J Custers, Elwin Janssen, Kobus L Versteegh, Maurice C M L Buzink, Desislava N Nesheva, Reggie Bosma, Iwan J P de Esch, Henry F Vischer, Maikel Wijtmans, Martyna Szpakowska, Andy Chevigné, Carsten Hoffmann, Chris de Graaf, Barbara A Zarzycka, Albert D Windhorst, Martine J Smit, Rob Leurs
Pharmacological Characterization and Radiolabeling of VUF15485, a High-Affinity Small-Molecule Agonist for the Atypical Chemokine Receptor ACKR3. Molecular pharmacology 105 (4) (2024)
Meichun Gao, Jasper F Ooms, Rob Leurs, Henry F Vischer
Histamine H 3 Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity. Biomolecules 14 (7) (2024)
Yang Zheng, Magali van den Kerkhof, Mohamed Ibrahim, Iwan J P de Esch, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy. Journal of medicinal chemistry 67 (4) (2024)
Yang Zheng, Magali van den Kerkhof, Mohamed Ibrahim, Iwan J P de Esch, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy. Journal of medicinal chemistry 67 (4) (2024)
Ruixue Xia, Shuang Shi, Zhenmei Xu, Henry F Vischer, Albert D Windhorst, Yu Qian, Yaning Duan, Jiale Liang, Kai Chen, Anqi Zhang, Changyou Guo, Rob Leurs, Yuanzheng He
Structural basis of ligand recognition and design of antihistamines targeting histamine H 4 receptor. Nature communications 15 (1) (2024)
Ruixue Xia, Shuang Shi, Zhenmei Xu, Henry F Vischer, Albert D Windhorst, Yu Qian, Yaning Duan, Jiale Liang, Kai Chen, Anqi Zhang, Changyou Guo, Rob Leurs, Yuanzheng He
Structural basis of ligand recognition and design of antihistamines targeting histamine H 4 receptor. Nature communications 15 (1) (2024)
Ruixue Xia, Shuang Shi, Zhenmei Xu, Henry F Vischer, Albert D Windhorst, Yu Qian, Yaning Duan, Jiale Liang, Kai Chen, Anqi Zhang, Changyou Guo, Rob Leurs, Yuanzheng He
Structural basis of ligand recognition and design of antihistamines targeting histamine H 4 receptor. Nature communications 15 (1) (2024)
Meichun Gao, Jasper F Ooms, Rob Leurs, Henry F Vischer
Histamine H 3 Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity. Biomolecules 14 (7) (2024)
Ruixue Xia, Shuang Shi, Zhenmei Xu, Henry F Vischer, Albert D Windhorst, Yu Qian, Yaning Duan, Jiale Liang, Kai Chen, Anqi Zhang, Changyou Guo, Rob Leurs, Yuanzheng He
Structural basis of ligand recognition and design of antihistamines targeting histamine H 4 receptor. Nature communications 15 (1) (2024)
Meichun Gao, Jasper F Ooms, Rob Leurs, Henry F Vischer
Histamine H 3 Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity. Biomolecules 14 (7) (2024)
Aurelien Zarca, Ilze Adlere, Cristina P Viciano, Marta Arimont-Segura, Max Meyrath, Icaro A Simon, Jan Paul Bebelman, Dennis Laan, Hans G J Custers, Elwin Janssen, Kobus L K Versteegh, Maurice Buzink, Desislava Nesheva, Reggie Bosma, Iwan J P de Esch, Henry Vischer, Maikel Wijtmans, Martyna Szpakowska, Andy Chevigné, Carsten Hoffmann, Chris de Graaf, Barbara A Zarzycka, Albert D Windhorst, Martine J Smit, Rob Leurs
Pharmacological characterization and radiolabeling of VUF15485, a high-affinity small-molecule agonist for the atypical chemokine receptor ACKR3. Molecular pharmacology (2024)
Sabrina N Rahman, Daniel A McNaught-Flores, Yara Huppelschoten, Daniel da Costa Pereira, Arthur Christopoulos, Rob Leurs, Christopher J Langmead
Structural and Molecular Determinants for Isoform Bias at Human Histamine H 3 Receptor Isoforms. ACS chemical neuroscience 14 (4) (2023)
Yang Zheng, Magali van den Kerkhof, Tiffany van der Meer, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Iwan J P de Esch, Marco Siderius, An Matheeussen, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy. Journal of medicinal chemistry (2023)
Yang Zheng, Susanne Schroeder, Georgi K Kanev, Sanaa S Botros, Samia William Abdel-Sayed, Abdel-Nasser A Sabra, Louis Maes, Guy Caljon, Carmen Gil, Ana Martinez, Irene G Salado, Koen Augustyns, Ewald Edink, Maarten Sijm, Erik de Heuvel, Iwan J P de Esch, Tiffany van der Meer, Marco Siderius, Geert Jan Sterk, David Brown, Rob Leurs
To Target or Not to Target Schistosoma mansoni Cyclic Nucleotide Phosphodiesterase 4A? International journal of molecular sciences 24 (7) (2023)
Icaro A Simon, Evert J Homan, Maikel Wijtmans, Michael Sundström, Rob Leurs, Iwan J P de Esch, Barbara A Zarzycka
PSW-Designer: An Open-Source Computational Platform for the Design and Virtual Screening of Photopharmacological Ligands. Journal of chemical information and modeling (2023)
Sabrina N Rahman, Daniel A McNaught-Flores, Yara Huppelschoten, Daniel da Costa Pereira, Arthur Christopoulos, Rob Leurs, Christopher J Langmead
Structural and Molecular Determinants for Isoform Bias at Human Histamine H 3 Receptor Isoforms. ACS chemical neuroscience (2023)
Yang Zheng, An Matheeussen, Louis Maes, Guy Caljon, Geert Jan Sterk, Rob Leurs
Structural Optimization of BIPPO Analogs as Potent Antimalarials. Molecules (Basel, Switzerland) 28 (13) (2023)
Sabrina N Rahman, Daniel A McNaught-Flores, Yara Huppelschoten, Daniel da Costa Pereira, Arthur Christopoulos, Rob Leurs, Christopher J Langmead
Structural and Molecular Determinants for Isoform Bias at Human Histamine H 3 Receptor Isoforms. ACS chemical neuroscience 14 (4) (2023)
Sebastian Dekkers, Dehan Comez, Noemi Karsai, Marta Arimont-Segura, Meritxell Canals, Birgit Caspar, Chris de Graaf, Laura E Kilpatrick, Rob Leurs, Barrie Kellam, Stephen J Hill, Stephen J Briddon, Michael J Stocks
Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3). ACS medicinal chemistry letters 15 (1) (2023)
Sebastian Dekkers, Dehan Comez, Noemi Karsai, Marta Arimont-Segura, Meritxell Canals, Birgit Caspar, Chris de Graaf, Laura E Kilpatrick, Rob Leurs, Barrie Kellam, Stephen J Hill, Stephen J Briddon, Michael J Stocks
Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3). ACS medicinal chemistry letters 15 (1) (2023)
Sabrina N Rahman, Daniel A McNaught-Flores, Yara Huppelschoten, Daniel da Costa Pereira, Arthur Christopoulos, Rob Leurs, Christopher J Langmead
Structural and Molecular Determinants for Isoform Bias at Human Histamine H 3 Receptor Isoforms. ACS chemical neuroscience 14 (4) (2023)
Daniel A McNaught-Flores, Albert Jelke Kooistra, Yu-Chia Chen, José-Antonio Arias-Montaño, Pertti Panula, Rob Leurs
Pharmacological characterization of the zebrafish ( Danio rerio ) histamine H 1 receptor reveals the involvement of the second extracellular loop in the binding of histamine. Molecular pharmacology (2023)
Eléonore W E Verweij, Reggie Bosma, Meichun Gao, Jelle van den Bor, Betty Al Araaj, Sabrina M de Munnik, Xiaoyuan Ma, Rob Leurs, Henry F Vischer
BRET-Based Biosensors to Measure Agonist Efficacies in Histamine H 1 Receptor-Mediated G Protein Activation, Signaling and Interactions with GRKs and β-Arrestins. International journal of molecular sciences 23 (6) (2022)
Xiaoyuan Ma, Meichun Gao, Henry F Vischer, Rob Leurs
A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology in Cell Membranes and Living Cells. International journal of molecular sciences 23 (15) (2022)
Zhi Yuan Kok, Leigh A Stoddart, Sarah J Mistry, Tamara A M Mocking, Henry F Vischer, Rob Leurs, Stephen J Hill, Shailesh N Mistry, Barrie Kellam
Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H 1 Receptor. Journal of medicinal chemistry 65 (12) (2022)
Xiaoyuan Ma, Marta Arimont Segura, Barbara Zarzycka, Henry F Vischer, Rob Leurs
Analysis of Missense Variants in the Human Histamine Receptor Family Reveals Increased Constitutive Activity of E4106.30×30K Variant in the Histamine H1 Receptor. International journal of molecular sciences 22 (7) (2021)
Zhiyong Wang, Reggie Bosma, Sebastiaan Kuhne, Jelle van den Bor, Wrej Garabitian, Henry F Vischer, Maikel Wijtmans, Rob Leurs, Iwan J P de Esch
Exploring the Effect of Cyclization of Histamine H1 Receptor Antagonists on Ligand Binding Kinetics. ACS omega 6 (19) (2021)
Barbara Rani, Bruna Silva-Marques, Rob Leurs, Maria Beatrice Passani, Patrizio Blandina, Gustavo Provensi
Short- and Long-Term Social Recognition Memory Are Differentially Modulated by Neuronal Histamine. Biomolecules 11 (4) (2021)
Xiaoyuan Ma, Eléonore W E Verweij, Marco Siderius, Rob Leurs, Henry F Vischer
Identification of TSPAN4 as Novel Histamine H4 Receptor Interactor. Biomolecules 11 (8) (2021)
Irene G Salado, Abhimanyu K Singh, Carlos Moreno-Cinos, Guna Sakaine, Marco Siderius, Pieter Van Der Veken, An Matheeussen, Tiffany van der Meer, Payman Sadek, Sheraz Gul, Louis Maes, Geert-Jan Sterk, Rob Leurs, David Brown, Koen Augustyns
Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds. Journal of medicinal chemistry 63 (7) (2020)
Hannes Schihada, Xiaoyuan Ma, Ulrike Zabel, Henry F Vischer, Gunnar Schulte, Rob Leurs, Steffen Pockes, Martin J Lohse
Development of a Conformational Histamine H3 Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists. ACS sensors 5 (6) (2020)
Maarten Sijm, Geert Jan Sterk, Guy Caljon, Louis Maes, Iwan J P de Esch, Rob Leurs
Structure-Activity Relationship of Phenylpyrazolones against Trypanosoma cruzi. ChemMedChem 15 (14) (2020)
Teemu Suutari, Sabrina N Rahman, Henry F Vischer, Dick van Iperen, Arto Merivaara, Marjo Yliperttula, Rob Leurs, Jeroen Kool, Tapani Viitala
Label-Free Analysis with Multiple Parameters Separates G Protein-Coupled Receptor Signaling Pathways. Analytical chemistry 92 (21) (2020)
Tamara A M Mocking, Maurice C M L Buzink, Rob Leurs, Henry F Vischer
Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H3 Receptor. International journal of molecular sciences 20 (15) (2019)
Xavier Gómez-Santacana, Sabrina M de Munnik, Tamara A M Mocking, Niels J Hauwert, Shanliang Sun, Prashanna Vijayachandran, Iwan J P de Esch, Henry F Vischer, Maikel Wijtmans, Rob Leurs
A toolbox of molecular photoswitches to modulate the CXCR3 chemokine receptor with light. Beilstein journal of organic chemistry 15 (2019)
Marta Arimont, Carsten Hoffmann, Chris de Graaf, Rob Leurs
Chemokine Receptor Crystal Structures: What Can Be Learned from Them? Molecular pharmacology 96 (6) (2019)
Niels J Hauwert, Tamara A M Mocking, Daniel P DA Costa, Ken Lion, Yara Huppelschoten, Henry F Vischer, Iwan J P De Esch, Maikel Wijtmans, Rob Leurs
A Photoswitchable Agonist for the Histamine H3 Receptor, a Prototypic Family A G-Protein-Coupled Receptor. Angewandte Chemie (International ed. in English) 58 (14) (2019)
Reggie Bosma, Zhiyong Wang, Albert Jelke Kooistra, Nick Bushby, Sebastiaan Kuhne, Jelle van den Bor, Michael J Waring, Chris de Graaf, Iwan J de Esch, Henry F Vischer, Robert J Sheppard, Maikel Wijtmans, Rob Leurs
Route to Prolonged Residence Time at the Histamine H1 Receptor: Growing from Desloratadine to Rupatadine. Journal of medicinal chemistry 62 (14) (2019)
Maarten Sijm, Erik de Heuvel, An Matheeussen, Guy Caljon, Louis Maes, Geert-Jan Sterk, Iwan J P de Esch, Rob Leurs
Identification of Phenylphthalazinones as a New Class of Leishmania infantum Inhibitors. ChemMedChem 15 (2) (2019)
Gábor Wágner, Tamara A M Mocking, Marta Arimont, Gustavo Provensi, Barbara Rani, Bruna Silva-Marques, Gniewomir Latacz, Daniel Da Costa Pereira, Christina Karatzidou, Henry F Vischer, Maikel Wijtmans, Katarzyna Kieć-Kononowicz, Iwan J P de Esch, Rob Leurs
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity. Journal of medicinal chemistry 62 (23) (2019)
Antoni R Blaazer, Abhimanyu K Singh, Erik de Heuvel, Ewald Edink, Kristina M Orrling, Johan J N Veerman, Toine van den Bergh, Chimed Jansen, Erin Balasubramaniam, Wouter J Mooij, Hans Custers, Maarten Sijm, Daniel N A Tagoe, Titilola D Kalejaiye, Jane C Munday, Hermann Tenor, An Matheeussen, Maikel Wijtmans, Marco Siderius, Chris de Graaf, Louis Maes, Harry P de Koning, David S Bailey, Geert Jan Sterk, Iwan J P de Esch, David G Brown, Rob Leurs
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity. Journal of medicinal chemistry 61 (9) (2018)
Xavier Gómez-Santacana, Sabrina M de Munnik, Prashanna Vijayachandran, Daniel Da Costa Pereira, Jan Paul M Bebelman, Iwan J P de Esch, Henry F Vischer, Maikel Wijtmans, Rob Leurs
Photoswitching the Efficacy of a Small-Molecule Ligand for a Peptidergic GPCR: from Antagonism to Agonism. Angewandte Chemie (International ed. in English) 57 (36) (2018)
Márton Vass, Sabina Podlewska, Iwan J P de Esch, Andrzej J Bojarski, Rob Leurs, Albert Jelke Kooistra, Chris de Graaf
Aminergic GPCR-Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data. Journal of medicinal chemistry 62 (8) (2018)
Niels J Hauwert, Tamara A M Mocking, Daniel Da Costa Pereira, Albert J Kooistra, Lisa M Wijnen, Gerda C M Vreeker, Eléonore W E Verweij, Albertus H De Boer, Martine J Smit, Chris de Graaf, Henry F Vischer, Iwan J P de Esch, Maikel Wijtmans, Rob Leurs
Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology. Journal of the American Chemical Society 140 (12) (2018)
Tamara A M Mocking, Eléonore W E Verweij, Henry F Vischer, Rob Leurs
Homogeneous, Real-Time NanoBRET Binding Assays for the Histamine H3 and H4 Receptors on Living Cells. Molecular pharmacology 94 (6) (2018)