Rob Leurs - Publications

Affiliations: 
Medicinal Chemistry Vrije Universiteit Amsterdam, Amsterdam, Netherlands 
Area:
GPCRs, Histamine receptors, Chemokine receptors
Website:
http://www.chem.vu.nl/en/research/division-of-medicinal-chemistry/index.asp

250 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2020 Munday JC, Kunz S, Kalejaiye TD, Siderius M, Schroeder S, Paape D, Alghamdi AH, Abbasi Z, Huang SX, Donachie AM, William S, Sabra AN, Sterk GJ, Botros SS, Brown DG, ... ... Leurs R, et al. Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages. Plos Neglected Tropical Diseases. 14: e0008447. PMID 32730343 DOI: 10.1371/journal.pntd.0008447  0.6
2020 Schihada H, Ma X, Zabel U, Vischer HF, Schulte G, Leurs R, Pockes S, Lohse MJ. Development of a conformational histamine H receptor biosensor for the synchronous screening of agonists and inverse agonists. Acs Sensors. PMID 32397705 DOI: 10.1021/acssensors.0c00397  0.76
2020 Verweij EWE, Al Araaj B, Prabhata WR, Prihandoko R, Nijmeijer S, Tobin AB, Leurs R, Vischer HF. Differential Role of Serines and Threonines in Intracellular Loop 3 and C-Terminal Tail of the Histamine H Receptor in β-Arrestin and G Protein-Coupled Receptor Kinase Interaction, Internalization, and Signaling. Acs Pharmacology & Translational Science. 3: 321-333. PMID 32296771 DOI: 10.1021/acsptsci.0c00008  0.76
2020 Sijm M, Sterk GJ, Caljon G, Maes L, de Esch IJP, Leurs R. Structure activity relationship of phenylpyrazolones against Trypanosoma cruzi. Chemmedchem. PMID 32249532 DOI: 10.1002/cmdc.202000136  0.6
2020 G Salado I, Singh AK, Moreno-Cinos C, Sakaine G, Siderius M, Van der Veken P, Matheeussen A, Van der Meer T, Sadek P, Gul S, Maes L, Sterk GJ, Leurs R, Brown DG, Augustyns K. Lead optimization of phthalazinone phosphodiesterase inhibitors as novel antitrypanosomal compounds. Journal of Medicinal Chemistry. PMID 32196340 DOI: 10.1021/acs.jmedchem.9b00985  0.6
2019 Wágner G, Mocking TAM, Kooistra AJ, Slynko I, Ábrányi-Balogh P, Keserű GM, Wijtmans M, Vischer HF, de Esch IJP, Leurs R. Covalent Inhibition of the Histamine H Receptor. Molecules (Basel, Switzerland). 24. PMID 31835873 DOI: 10.3390/molecules24244541  0.76
2019 Gómez-Santacana X, de Munnik SM, Mocking TAM, Hauwert NJ, Sun S, Vijayachandran P, de Esch IJP, Vischer HF, Wijtmans M, Leurs R. A toolbox of molecular photoswitches to modulate the CXCR3 chemokine receptor with light. Beilstein Journal of Organic Chemistry. 15: 2509-2523. PMID 31728165 DOI: 10.3762/bjoc.15.244  0.76
2019 Kanev GK, de Graaf C, de Esch IJP, Leurs R, Würdinger T, Westerman BA, Kooistra AJ. The Landscape of Atypical and Eukaryotic Protein Kinases. Trends in Pharmacological Sciences. 40: 818-832. PMID 31677919 DOI: 10.1016/j.tips.2019.09.002  0.6
2019 Wágner G, Mocking T, Arimont M, Provensi G, Rani B, Silva-Marques B, Latacz G, Da Costa Pereira D, Karatzidou C, Vischer HF, Wijtmans M, Kiec-Kononowicz K, De Esch IJP, Leurs R. 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. PMID 31675226 DOI: 10.1021/acs.jmedchem.9b01462  0.76
2019 Adlere I, Caspar B, Arimont M, Dekkers S, Visser K, Stuijt J, de Graaf C, Stocks M, Kellam B, Briddon S, Wijtmans M, de Esch I, Hill S, Leurs R. Modulators of CXCR4 and CXCR7/ACKR3 function. Molecular Pharmacology. PMID 31548340 DOI: 10.1124/mol.119.117663  0.56
2019 van Senten JR, Bebelman MP, Fan TS, Heukers R, Bergkamp ND, van Gasselt P, Langemeijer EV, Slinger E, Lagerweij T, Rahbar A, Stigter-van Walsum M, Maussang D, Leurs R, Musters RJ, van Dongen GAMS, et al. The human cytomegalovirus-encoded G protein-coupled receptor UL33 exhibits oncomodulatory properties. The Journal of Biological Chemistry. PMID 31519750 DOI: 10.1074/jbc.RA119.007796  0.76
2019 de Heuvel E, Singh AK, Boronat P, Kooistra AJ, van der Meer T, Sadek P, Blaazer AR, Shaner NC, Bindels DS, Caljon G, Maes L, Sterk GJ, Siderius M, Oberholzer M, de Esch IJP, ... ... Leurs R, et al. Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2). Bioorganic & Medicinal Chemistry. PMID 31378593 DOI: 10.1016/j.bmc.2019.06.026  0.6
2019 Sebastián-Pérez V, Schroeder S, Munday JC, van der Meer T, Zaldívar-Díez J, Siderius M, de Koning HP, Brown D, Martínez A, Campillo NE, Leurs R, Gil C. Discovery of novel PDE4A inhibitors as potential agents against schistosomiasis. Future Medicinal Chemistry. PMID 31370708 DOI: 10.4155/fmc-2018-0592  0.6
2019 Mocking TAM, Buzink MCML, Leurs R, Vischer HF. Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H Receptor. International Journal of Molecular Sciences. 20. PMID 31366084 DOI: 10.3390/ijms20153724  0.76
2019 de Heuvel E, Singh AK, Edink E, van der Meer T, van der Woude M, Sadek P, Krell-Jørgensen MP, van den Bergh T, Veerman J, Caljon G, Kalejaiye TD, Wijtmans M, Maes L, de Koning HP, Jan Sterk G, ... ... Leurs R, et al. Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors. Bioorganic & Medicinal Chemistry. PMID 31327675 DOI: 10.1016/j.bmc.2019.06.027  0.6
2019 Sijm M, Siciliano de Araújo J, Llorca AR, Orrling K, Stiny L, Matheeussen A, Maes L, de Esch IJP, Soeiro MNC, Sterk GJ, Leurs R. Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents. Chemmedchem. PMID 31319019 DOI: 10.1002/cmdc.201900370  0.6
2019 Bosma R, Wang Z, Kooistra AJ, Bushby N, Kuhne S, van den Bor J, Waring MJ, de Graaf C, de Esch IJ, Vischer HF, Sheppard RJ, Wijtmans M, Leurs R. Route to Prolonged Residence Time at the Histamine H Receptor: Growing from Desloratadine to Rupatadine. Journal of Medicinal Chemistry. PMID 31274307 DOI: 10.1021/acs.jmedchem.9b00447  0.76
2019 Arimont M, Hoffmann C, de Graaf C, Leurs R. Chemokine receptor crystal structures: what can be learnt from them? Molecular Pharmacology. PMID 31266800 DOI: 10.1124/mol.119.117168  0.36
2019 Bosma R, Stoddart LA, Georgi V, Bouzo-Lorenzo M, Bushby N, Inkoom L, Waring MJ, Briddon SJ, Vischer HF, Sheppard RJ, Fernández-Montalván A, Hill SJ, Leurs R. Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor. Scientific Reports. 9: 7906. PMID 31133718 DOI: 10.1038/s41598-019-44025-5  0.76
2019 Hauwert NJ, Mocking TAM, Da Costa Pereira D, Lion K, Huppelschoten Y, Vischer HF, De Esch IJP, Wijtmans M, Leurs R. A Photoswitchable Agonist for the Histamine H3 Receptor, a prototypic family A G protein-coupled receptor. Angewandte Chemie (International Ed. in English). PMID 30735597 DOI: 10.1002/anie.201813110  0.76
2019 Botros SS, William S, Sabra AA, El-Lakkany NM, Seif El-Din SH, García-Rubia A, Sebastián-Pérez V, Blaazer AR, de Heuvel E, Sijm M, Zheng Y, Salado IG, Munday JC, Maes L, de Esch IJP, ... ... Leurs R, et al. Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity. International Journal For Parasitology. Drugs and Drug Resistance. 9: 35-43. PMID 30669086 DOI: 10.1016/j.ijpddr.2019.01.001  0.6
2018 Vass M, Podlewska S, De Esch IJP, Bojarski AJ, Leurs R, Kooistra AJ, de Graaf C. Aminergic GPCR-ligand interactions: A chemical and structural map of receptor mutation data. Journal of Medicinal Chemistry. PMID 30351004 DOI: 10.1021/acs.jmedchem.8b00836  0.6
2018 Mocking TAM, Verweij EWE, Vischer HF, Leurs R. Homogeneous, real-time NanoBRET binding assays for the histamine H and H receptor on living cells. Molecular Pharmacology. PMID 30249614 DOI: 10.1124/mol.118.113373  0.76
2018 Bosma R, van den Bor J, Vischer HF, Labeaga L, Leurs R. The long duration of action of the second generation antihistamine bilastine coincides with its long residence time at the histamine H receptor. European Journal of Pharmacology. 838: 107-111. PMID 30201377 DOI: 10.1016/j.ejphar.2018.09.011  0.76
2018 Leurs R, Gómez-Santacana X, de Munnik SM, Vijayachandran P, Da Costa Pereira D, Bebelman JPM, de Esch IJP, Vischer HF, Wijtmans M. Photoswitching the efficacy of a small-molecule ligand for a peptidergic GPCR: from antagonism to agonism. Angewandte Chemie (International Ed. in English). PMID 29926530 DOI: 10.1002/anie.201804875  0.76
2018 Heukers R, Fan TS, de Wit RH, van Senten JR, De Groof TWM, Bebelman MP, Lagerweij T, Vieira J, de Munnik SM, Smits-de Vries L, van Offenbeek J, Rahbar A, van Hoorick D, Söderberg-Naucler C, Würdinger T, ... Leurs R, et al. The constitutive activity of the virally encoded chemokine receptor US28 accelerates glioblastoma growth. Oncogene. PMID 29706656 DOI: 10.1038/s41388-018-0255-7  0.76
2018 Blaazer AR, Singh AK, de Heuvel E, Edink E, Orrling KM, Veerman JJN, van den Bergh T, Jansen C, Balasubramaniam E, Mooij WJ, Custers H, Sijm M, Tagoe DNA, Kalejaiye TD, Munday JC, ... ... Leurs R, et al. Targeting a subpocket in Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) enables the structure-based discovery of selective inhibitors with trypanocidal activity. Journal of Medicinal Chemistry. PMID 29672041 DOI: 10.1021/acs.jmedchem.7b01670  0.6
2018 Hauwert NJ, Mocking TAM, Da Costa Pereira D, Kooistra AJ, Wijnen LM, Vreeker G, Verweij NWE, De Boer BH, Smit MJ, de Graaf C, Vischer HF, De Esch IJP, Wijtmans M, Leurs R. Synthesis and characterization of a bi-directional photoswitchable antagonist toolbox for real-time GPCR photopharmacology. Journal of the American Chemical Society. PMID 29470065 DOI: 10.1021/jacs.7b11422  0.76
2018 Stoddart LA, Vernall AJ, Bouzo-Lorenzo M, Bosma R, Kooistra AJ, de Graaf C, Vischer HF, Leurs R, Briddon SJ, Kellam B, Hill SJ. Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells. Scientific Reports. 8: 1572. PMID 29371669 DOI: 10.1038/s41598-018-19714-2  0.76
2018 Kooistra AJ, Vass M, McGuire R, Leurs R, de Esch IJ, Vriend G, Verhoeven S, de Graaf C. 3D-e-Chem: Structural Cheminformatics Workflows for Computer-Aided Drug Discovery. Chemmedchem. PMID 29337438 DOI: 10.1002/cmdc.201700754  0.4
2017 Bosma R, Witt G, Vaas LAI, Josimovic I, Gribbon P, Vischer HF, Gul S, Leurs R. The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor. Frontiers in Pharmacology. 8: 667. PMID 29033838 DOI: 10.3389/fphar.2017.00667  0.76
2017 Schuetz DA, de Witte WEA, Wong YC, Knasmueller B, Richter L, Kokh DB, Sadiq SK, Bosma R, Nederpelt I, Segala E, Amaral M, Guo D, Andres D, Georgi V, Stoddart LA, ... ... Leurs R, et al. Kinetics for Drug Discovery: an industry-driven effort to target drug residence time. Drug Discovery Today. PMID 28412474 DOI: 10.1016/j.drudis.2017.02.002  0.36
2017 Arimont M, Sun S, Leurs R, Smit M, De Esch IJ, de Graaf C. Structural Analysis of Chemokine Receptor-Ligand Interactions. Journal of Medicinal Chemistry. PMID 28165741 DOI: 10.1021/acs.jmedchem.6b01309  0.4
2017 McGuire R, Verhoeven S, Vass M, Vriend G, De Esch IJ, Lusher SJ, Leurs R, Ridder L, Kooistra AJ, Ritschel T, de Graaf C. 3D-e-Chem-VM: Structural cheminformatics research infrastructure in a freely available Virtual Machine. Journal of Chemical Information and Modeling. PMID 28125221 DOI: 10.1021/acs.jcim.6b00686  0.4
2016 Kuhne S, Kooistra AJ, Bosma R, Bortolato A, Wijtmans M, Vischer HF, Mason JS, de Graaf C, De Esch IJ, Leurs R. Identification of Ligand Binding Hot Spots of the Histamine H1 Receptor Following Structure-Based Fragment Optimization. Journal of Medicinal Chemistry. PMID 27643714 DOI: 10.1021/acs.jmedchem.6b00981  0.76
2016 Vass M, Kooistra AJ, Ritschel T, Leurs R, de Esch IJ, de Graaf C. Molecular interaction fingerprint approaches for GPCR drug discovery. Current Opinion in Pharmacology. 30: 59-68. PMID 27479316 DOI: 10.1016/j.coph.2016.07.007  0.4
2016 Bosma R, Moritani R, Leurs R, Vischer HF. BRET-based β-arrestin2 recruitment to the histamine H1 receptor for investigating antihistamine binding kinetics. Pharmacological Research. PMID 27468652 DOI: 10.1016/j.phrs.2016.07.034  0.76
2016 Kooistra AJ, Vischer HF, McNaught-Flores D, Leurs R, de Esch IJ, de Graaf C. Function-specific virtual screening for GPCR ligands using a combined scoring method. Scientific Reports. 6: 28288. PMID 27339552 DOI: 10.1038/srep28288  0.76
2016 Nijmeijer S, Vischer H, Leurs R. Adhesion GPCRs in immunology. Biochemical Pharmacology. PMID 27131861 DOI: 10.1016/j.bcp.2016.04.013  0.52
2016 Siderius M, Shanmugham A, England P, van der Meer T, Bebelman JP, Blaazer AR, de Esch IJ, Leurs R. Surface plasmon resonance biosensor assay for the analysis of small-molecule inhibitor binding to human and parasitic phosphodiesterases. Analytical Biochemistry. PMID 27033007 DOI: 10.1016/j.ab.2016.03.013  1
2016 de Munnik SM, van der Lee R, Velders DM, van Offenbeek J, Smits-de Vries L, Leurs R, Smit MJ, Vischer HF. The viral G protein-coupled receptor ORF74 unmasks phospholipase C signaling of the receptor tyrosine kinase IGF-1R. Cellular Signalling. PMID 26931381 DOI: 10.1016/j.cellsig.2016.02.017  0.76
2016 de Wit RH, de Munnik SM, Leurs R, Vischer HF, Smit MJ. Molecular Pharmacology of Chemokine Receptors. Methods in Enzymology. 570: 457-515. PMID 26921959 DOI: 10.1016/bs.mie.2015.12.002  0.76
2016 Jansen C, Kooistra AJ, Kanev GK, Leurs R, De Esch IJ, de Graaf C. PDEStrIAn: A phosphodiesterase structure and ligand interaction annotated database as a tool for structure-based drug design. Journal of Medicinal Chemistry. PMID 26908025 DOI: 10.1021/acs.jmedchem.5b01813  0.4
2016 de Wit RH, de Munnik SM, Leurs R, Vischer HF, Smit MJ. Molecular Pharmacology of Chemokine Receptors Methods in Enzymology. DOI: 10.1016/bs.mie.2015.12.002  1
2015 Ganghammer S, Gutjahr J, Hutterer E, Krenn PW, Pucher S, Zelle-Rieser C, Jöhrer K, Wijtmans M, Leurs R, Smit MJ, Gattei V, Greil R, Hartmann TN. Combined CXCR3/CXCR4 measurements are of high prognostic value in chronic lymphocytic leukemia due to negative cooperativity of the receptors. Haematologica. PMID 26589908 DOI: 10.3324/haematol.2015.133470  0.76
2015 Kooistra AJ, Kanev GK, van Linden OP, Leurs R, de Esch IJ, de Graaf C. KLIFS: a structural kinase-ligand interaction database. Nucleic Acids Research. PMID 26496949 DOI: 10.1093/nar/gkv1082  0.4
2015 Mladic M, Scholten DJ, Wijtmans M, Falck D, Leurs R, Niessen WM, Smit MJ, Kool J. Metabolic profiling of ligands for the chemokine receptor CXCR3 by liquid chromatography-mass spectrometry coupled to bioaffinity assessment. Analytical and Bioanalytical Chemistry. 407: 7067-81. PMID 26164305 DOI: 10.1007/s00216-015-8867-z  1
2015 Hoffmann C, Castro M, Rinken A, Leurs R, Hill SJ, Vischer HF. Ligand Residence Time at G-protein-Coupled Receptors-Why We Should Take Our Time To Study It. Molecular Pharmacology. 88: 552-60. PMID 26152198 DOI: 10.1124/mol.115.099671  1
2015 Panula P, Chazot PL, Cowart M, Gutzmer R, Leurs R, Liu WL, Stark H, Thurmond RL, Haas HL. International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. Pharmacological Reviews. 67: 601-55. PMID 26084539 DOI: 10.1124/pr.114.010249  1
2015 de Munnik SM, Kooistra AJ, van Offenbeek J, Nijmeijer S, de Graaf C, Smit MJ, Leurs R, Vischer HF. The Viral G Protein-Coupled Receptor ORF74 Hijacks β-Arrestins for Endocytic Trafficking in Response to Human Chemokines. Plos One. 10: e0124486. PMID 25894435 DOI: 10.1371/journal.pone.0124486  1
2015 Kooistra AJ, Leurs R, de Esch IJ, de Graaf C. Structure-Based Prediction of G-Protein-Coupled Receptor Ligand Function: A β-Adrenoceptor Case Study. Journal of Chemical Information and Modeling. 55: 1045-61. PMID 25848966 DOI: 10.1021/acs.jcim.5b00066  1
2015 Schultes S, Kooistra AJ, Vischer HF, Nijmeijer S, Haaksma EE, Leurs R, de Esch IJ, de Graaf C. Combinatorial Consensus Scoring for Ligand-Based Virtual Fragment Screening: A Comparative Case Study for Serotonin 5-HT3A, Histamine H1, and Histamine H4 Receptors. Journal of Chemical Information and Modeling. 55: 1030-44. PMID 25815783 DOI: 10.1021/ci500694c  1
2015 de Munnik SM, Smit MJ, Leurs R, Vischer HF. Modulation of cellular signaling by herpesvirus-encoded G protein-coupled receptors. Frontiers in Pharmacology. 6: 40. PMID 25805993 DOI: 10.3389/fphar.2015.00040  1
2015 Scholten DJ, Wijtmans M, van Senten JR, Custers H, Stunnenberg A, de Esch IJ, Smit MJ, Leurs R. Pharmacological characterization of [3H]VUF11211, a novel radiolabeled small-molecule inverse agonist for the chemokine receptor CXCR3. Molecular Pharmacology. 87: 639-48. PMID 25576486 DOI: 10.1124/mol.114.095265  1
2015 Blaazer AR, Orrling KM, Shanmugham A, Jansen C, Maes L, Edink E, Sterk GJ, Siderius M, England P, Bailey D, de Esch IJ, Leurs R. Fragment-based screening in tandem with phenotypic screening provides novel antiparasitic hits. Journal of Biomolecular Screening. 20: 131-40. PMID 25231971 DOI: 10.1177/1087057114549735  1
2015 Istyastono EP, Kooistra AJ, Vischer HF, Kuijer M, Roumen L, Nijmeijer S, Smits RA, De Esch IJP, Leurs R, De Graaf C. Structure-based virtual screening for fragment-like ligands of the G protein-coupled histamine H4 receptor Medchemcomm. 6: 1003-1017. DOI: 10.1039/c5md00022j  1
2015 Wijtmans M, Scholten D, Mooij W, Smit MJ, De Esch IJP, De Graaf C, Leurs R. Exploring the cxcr3 chemokine receptor with small-molecule antagonists and agonists Topics in Medicinal Chemistry. 14: 119-186. DOI: 10.1007/7355_2014_75  1
2014 Vischer HF, Siderius M, Leurs R, Smit MJ. Herpesvirus-encoded GPCRs: neglected players in inflammatory and proliferative diseases? Nature Reviews. Drug Discovery. 13: 123-39. PMID 24445563 DOI: 10.1038/nrd4189  1
2014 Scholten DJ, Roumen L, Wijtmans M, Verkade-Vreeker MC, Custers H, Lai M, de Hooge D, Canals M, de Esch IJ, Smit MJ, de Graaf C, Leurs R. Identification of overlapping but differential binding sites for the high-affinity CXCR3 antagonists NBI-74330 and VUF11211. Molecular Pharmacology. 85: 116-26. PMID 24174496 DOI: 10.1124/mol.113.088633  1
2014 Kooistra AJ, Leurs R, de Esch IJ, de Graaf C. From three-dimensional GPCR structure to rational ligand discovery. Advances in Experimental Medicine and Biology. 796: 129-57. PMID 24158804 DOI: 10.1007/978-94-007-7423-0_7  1
2014 van Linden OP, Kooistra AJ, Leurs R, de Esch IJ, de Graaf C. KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space. Journal of Medicinal Chemistry. 57: 249-77. PMID 23941661 DOI: 10.1021/jm400378w  1
2013 Blanchetot C, Verzijl D, Mujić-Delić A, Bosch L, Rem L, Leurs R, Verrips CT, Saunders M, de Haard H, Smit MJ. Neutralizing nanobodies targeting diverse chemokines effectively inhibit chemokine function. The Journal of Biological Chemistry. 288: 25173-82. PMID 23836909 DOI: 10.1074/jbc.M113.467969  1
2013 Kooistra AJ, Kuhne S, de Esch IJ, Leurs R, de Graaf C. A structural chemogenomics analysis of aminergic GPCRs: lessons for histamine receptor ligand design. British Journal of Pharmacology. 170: 101-26. PMID 23713847 DOI: 10.1111/bph.12248  1
2013 Flores-Clemente C, Osorio-Espinoza A, Escamilla-Sánchez J, Leurs R, Arias JM, Arias-Montaño JA. A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H₃ receptor stably expressed in CHO-K1 cells. British Journal of Pharmacology. 170: 127-35. PMID 23713487 DOI: 10.1111/bph.12257  1
2013 Engelhardt H, Schultes S, de Graaf C, Nijmeijer S, Vischer HF, Zuiderveld OP, Dobler J, Stachurski K, Mayer M, Arnhof H, Scharn D, Haaksma EE, de Esch IJ, Leurs R. Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode. Journal of Medicinal Chemistry. 56: 4264-76. PMID 23668417 DOI: 10.1021/jm301886t  1
2013 Thompson AJ, Verheij MH, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ. Structure-activity relationships of quinoxaline-based 5-HT3A and 5-HT3AB receptor-selective ligands. Chemmedchem. 8: 946-55. PMID 23640722 DOI: 10.1002/cmdc.201300032  1
2013 Andaloussi M, Lim HD, van der Meer T, Sijm M, Poulie CB, de Esch IJ, Leurs R, Smits RA. A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787. Bioorganic & Medicinal Chemistry Letters. 23: 2663-70. PMID 23558237 DOI: 10.1016/j.bmcl.2013.02.091  1
2013 Jansen C, Wang H, Kooistra AJ, de Graaf C, Orrling KM, Tenor H, Seebeck T, Bailey D, de Esch IJ, Ke H, Leurs R. Discovery of novel Trypanosoma brucei phosphodiesterase B1 inhibitors by virtual screening against the unliganded TbrPDEB1 crystal structure. Journal of Medicinal Chemistry. 56: 2087-96. PMID 23409953 DOI: 10.1021/jm3017877  1
2013 Kooistra AJ, Roumen L, Leurs R, de Esch IJ, de Graaf C. From heptahelical bundle to hits from the Haystack: structure-based virtual screening for GPCR ligands. Methods in Enzymology. 522: 279-336. PMID 23374191 DOI: 10.1016/B978-0-12-407865-9.00015-7  1
2013 Nijmeijer S, Vischer HF, Sirci F, Schultes S, Engelhardt H, de Graaf C, Rosethorne EM, Charlton SJ, Leurs R. Detailed analysis of biased histamine H₄ receptor signalling by JNJ 7777120 analogues. British Journal of Pharmacology. 170: 78-88. PMID 23351115 DOI: 10.1111/bph.12117  1
2013 Nijmeijer S, Engelhardt H, Schultes S, van de Stolpe AC, Lusink V, de Graaf C, Wijtmans M, Haaksma EE, de Esch IJ, Stachurski K, Vischer HF, Leurs R. Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor. British Journal of Pharmacology. 170: 89-100. PMID 23347159 DOI: 10.1111/bph.12113  1
2013 Watts AO, Verkaar F, van der Lee MM, Timmerman CA, Kuijer M, van Offenbeek J, van Lith LH, Smit MJ, Leurs R, Zaman GJ, Vischer HF. β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR. The Journal of Biological Chemistry. 288: 7169-81. PMID 23341447 DOI: 10.1074/jbc.M112.406108  1
2013 de Graaf C, Vischer HF, de Kloe GE, Kooistra AJ, Nijmeijer S, Kuijer M, Verheij MH, England PJ, van Muijlwijk-Koezen JE, Leurs R, de Esch IJ. Small and colorful stones make beautiful mosaics: fragment-based chemogenomics. Drug Discovery Today. 18: 323-30. PMID 23266367 DOI: 10.1016/j.drudis.2012.12.003  1
2013 Watts AO, van Lipzig MM, Jaeger WC, Seeber RM, van Zwam M, Vinet J, van der Lee MM, Siderius M, Zaman GJ, Boddeke HW, Smit MJ, Pfleger KD, Leurs R, Vischer HF. Identification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes. British Journal of Pharmacology. 168: 1662-74. PMID 23170857 DOI: 10.1111/bph.12064  1
2013 Schultes S, Engelhardt H, Roumen L, Zuiderveld OP, Haaksma EE, de Esch IJ, Leurs R, de Graaf C. Combining quantum mechanical ligand conformation analysis and protein modeling to elucidate GPCR-ligand binding modes. Chemmedchem. 8: 49-53. PMID 23161844 DOI: 10.1002/cmdc.201200412  1
2013 Vinet J, van Zwam M, Dijkstra IM, Brouwer N, van Weering HR, Watts A, Meijer M, Fokkens MR, Kannan V, Verzijl D, Vischer HF, Smit MJ, Leurs R, Biber K, Boddeke HW. Inhibition of CXCR3-mediated chemotaxis by the human chemokine receptor-like protein CCX-CKR. British Journal of Pharmacology. 168: 1375-87. PMID 23121557 DOI: 10.1111/bph.12042  1
2013 Schultes S, Nijmeijer S, Engelhardt H, Kooistra AJ, Vischer HF, De Esch IJP, Haaksma EEJ, Leurs R, De Graaf C. Mapping histamine H4 receptor-ligand binding modes Medchemcomm. 4: 193-204. DOI: 10.1039/c2md20212c  1
2012 Cordova-Sintjago TC, Fang L, Bruysters M, Leurs R, Booth RG. Molecular determinants of ligand binding at the human histamine H1 receptor: Site-directed mutagenesis results analyzed with ligand docking and molecular dynamics studies at H1 homology and crystal structure models. Journal of Chemical and Pharmaceutical Research. 4: 2937-2951. PMID 25013351  0.36
2012 Roumen L, Scholten DJ, de Kruijf P, de Esch IJ, Leurs R, de Graaf C. C(X)CR in silico: Computer-aided prediction of chemokine receptor-ligand interactions. Drug Discovery Today. Technologies. 9: e281-91. PMID 24990665 DOI: 10.1016/j.ddtec.2012.05.002  1
2012 Wijtmans M, Scholten DJ, Roumen L, Canals M, Custers H, Glas M, Vreeker MC, de Kanter FJ, de Graaf C, Smit MJ, de Esch IJ, Leurs R. Chemical subtleties in small-molecule modulation of peptide receptor function: the case of CXCR3 biaryl-type ligands. Journal of Medicinal Chemistry. 55: 10572-83. PMID 23150943 DOI: 10.1021/jm301240t  1
2012 Langemeijer EV, Slinger E, de Munnik S, Schreiber A, Maussang D, Vischer H, Verkaar F, Leurs R, Siderius M, Smit MJ. Constitutive β-catenin signaling by the viral chemokine receptor US28. Plos One. 7: e48935. PMID 23145028 DOI: 10.1371/journal.pone.0048935  1
2012 Sirci F, Istyastono EP, Vischer HF, Kooistra AJ, Nijmeijer S, Kuijer M, Wijtmans M, Mannhold R, Leurs R, de Esch IJ, de Graaf C. Virtual fragment screening: discovery of histamine H3 receptor ligands using ligand-based and protein-based molecular fingerprints. Journal of Chemical Information and Modeling. 52: 3308-24. PMID 23140085 DOI: 10.1021/ci3004094  1
2012 Verheij MH, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ. Design, synthesis, and structure-activity relationships of highly potent 5-HT₃ receptor ligands. Journal of Medicinal Chemistry. 55: 8603-14. PMID 23006041 DOI: 10.1021/jm300801u  1
2012 Nijmeijer S, Vischer HF, Rosethorne EM, Charlton SJ, Leurs R. Analysis of multiple histamine H₄ receptor compound classes uncovers Gαi protein- and β-arrestin2-biased ligands. Molecular Pharmacology. 82: 1174-82. PMID 22973061 DOI: 10.1124/mol.112.080911  1
2012 Orrling KM, Jansen C, Vu XL, Balmer V, Bregy P, Shanmugham A, England P, Bailey D, Cos P, Maes L, Adams E, van den Bogaart E, Chatelain E, Ioset JR, van de Stolpe A, ... ... Leurs R, et al. Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1. Journal of Medicinal Chemistry. 55: 8745-56. PMID 22963052 DOI: 10.1021/jm301059b  1
2012 van Linden OP, Wijtmans M, Roumen L, Rotteveel L, Leurs R, de Esch IJ. Regiochemistry of the condensation of 2-aroyl-cyclohexanones and 2-cyanoacetamide: 13C-labeling studies and semiempirical MO calculations. The Journal of Organic Chemistry. 77: 7355-63. PMID 22897640 DOI: 10.1021/jo301138w  1
2012 Engelhardt H, de Esch IJ, Kuhn D, Smits RA, Zuiderveld OP, Dobler J, Mayer M, Lips S, Arnhof H, Scharn D, Haaksma EE, Leurs R. Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands. European Journal of Medicinal Chemistry. 54: 660-8. PMID 22749391 DOI: 10.1016/j.ejmech.2012.06.016  1
2012 Nijmeijer S, Vischer HF, Rudebeck AF, Fleurbaaij F, Falck D, Leurs R, Niessen WM, Kool J. Development of a profiling strategy for metabolic mixtures by combining chromatography and mass spectrometry with cell-based GPCR signaling. Journal of Biomolecular Screening. 17: 1329-38. PMID 22740245 DOI: 10.1177/1087057112451922  1
2012 Nijmeijer S, de Graaf C, Leurs R, Vischer HF. Molecular pharmacology of histamine H4 receptors. Frontiers in Bioscience (Landmark Edition). 17: 2089-106. PMID 22652766 DOI: 10.2741/4039  1
2012 Sanders MP, Roumen L, van der Horst E, Lane JR, Vischer HF, van Offenbeek J, de Vries H, Verhoeven S, Chow KY, Verkaar F, Beukers MW, McGuire R, Leurs R, Ijzerman AP, de Vlieg J, et al. A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design. Journal of Medicinal Chemistry. 55: 5311-25. PMID 22563707 DOI: 10.1021/jm300280e  1
2012 Adami M, Pozzoli C, Menozzi A, Bertini S, Passeri B, Cantoni AM, Smits R, de Esch I, Leurs R, Coruzzi G. Effects of histamine H4 receptor ligands in a mouse model of gastric ulceration. Pharmacology. 89: 287-94. PMID 22538763 DOI: 10.1159/000337736  1
2012 Kool J, Rudebeck AF, Fleurbaaij F, Nijmeijer S, Falck D, Smits RA, Vischer HF, Leurs R, Niessen WM. High-resolution metabolic profiling towards G protein-coupled receptors: rapid and comprehensive screening of histamine H₄ receptor ligands. Journal of Chromatography. A. 1259: 213-20. PMID 22520160 DOI: 10.1016/j.chroma.2012.03.052  1
2012 Canals M, Scholten DJ, de Munnik S, Han MK, Smit MJ, Leurs R. Ubiquitination of CXCR7 controls receptor trafficking. Plos One. 7: e34192. PMID 22457824 DOI: 10.1371/journal.pone.0034192  1
2012 Wijtmans M, Maussang D, Sirci F, Scholten DJ, Canals M, Mujić-Delić A, Chong M, Chatalic KL, Custers H, Janssen E, de Graaf C, Smit MJ, de Esch IJ, Leurs R. Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists. European Journal of Medicinal Chemistry. 51: 184-92. PMID 22424612 DOI: 10.1016/j.ejmech.2012.02.041  1
2012 Gutzmer R, Werfel T, Bäumer W, Kietzmann M, Chazot PL, Leurs R. Well characterized antihistamine 4 receptor antibodies contribute to current knowledge of the expression and biology of the human and murine histamine 4 receptor. Naunyn-Schmiedeberg's Archives of Pharmacology. 385: 853-4; author reply . PMID 22411357 DOI: 10.1007/s00210-012-0744-0  1
2012 Watts AO, Scholten DJ, Heitman LH, Vischer HF, Leurs R. Label-free impedance responses of endogenous and synthetic chemokine receptor CXCR3 agonists correlate with Gi-protein pathway activation. Biochemical and Biophysical Research Communications. 419: 412-8. PMID 22349504 DOI: 10.1016/j.bbrc.2012.02.036  1
2012 Edink E, Akdemir A, Jansen C, van Elk R, Zuiderveld O, de Kanter FJ, van Muijlwijk-Koezen JE, Smit AB, Leurs R, de Esch IJ. Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein. Bioorganic & Medicinal Chemistry Letters. 22: 1448-54. PMID 22243960 DOI: 10.1016/j.bmcl.2011.12.008  1
2012 Pardo LA, Gómez-Varela D, Major F, Sansuk K, Leurs R, Downie BR, Tietze LF, Stühmer W. Approaches targeting K(V)10.1 open a novel window for cancer diagnosis and therapy. Current Medicinal Chemistry. 19: 675-82. PMID 22204340 DOI: 10.2174/092986712798992011  1
2012 Smits RA, Lim HD, van der Meer T, Kuhne S, Bessembinder K, Zuiderveld OP, Wijtmans M, de Esch IJ, Leurs R. Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics. Bioorganic & Medicinal Chemistry Letters. 22: 461-7. PMID 22153663 DOI: 10.1016/j.bmcl.2011.10.104  1
2012 Coruzzi G, Pozzoli C, Adami M, Grandi D, Guido N, Smits R, de Esch I, Leurs R. Strain-dependent effects of the histamine H₄ receptor antagonist JNJ7777120 in a murine model of acute skin inflammation. Experimental Dermatology. 21: 32-7. PMID 22151388 DOI: 10.1111/j.1600-0625.2011.01396.x  1
2012 van Linden OP, Farenc C, Zoutman WH, Hameetman L, Wijtmans M, Leurs R, Tensen CP, Siegal G, de Esch IJ. Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase. European Journal of Medicinal Chemistry. 47: 493-500. PMID 22137457 DOI: 10.1016/j.ejmech.2011.11.020  1
2012 Scholten DJ, Canals M, Wijtmans M, de Munnik S, Nguyen P, Verzijl D, de Esch IJ, Vischer HF, Smit MJ, Leurs R. Pharmacological characterization of a small-molecule agonist for the chemokine receptor CXCR3. British Journal of Pharmacology. 166: 898-911. PMID 21883151 DOI: 10.1111/j.1476-5381.2011.01648.x  1
2012 Scholten DJ, Canals M, Maussang D, Roumen L, Smit MJ, Wijtmans M, de Graaf C, Vischer HF, Leurs R. Pharmacological modulation of chemokine receptor function. British Journal of Pharmacology. 165: 1617-43. PMID 21699506 DOI: 10.1111/j.1476-5381.2011.01551.x  1
2012 Schultes S, De Graaf C, Berger H, Mayer M, Steffen A, Haaksma EEJ, De Esch IJP, Leurs R, Krämer O. A medicinal chemistry perspective on melting point: Matched molecular pair analysis of the effects of simple descriptors on the melting point of drug-like compounds Medchemcomm. 3: 584-591. DOI: 10.1039/c2md00313a  1
2012 Siderius M, Wal M, Scholten DJ, Smit MJ, Sakmar TP, Leurs R, De Graaf C. Unnatural amino acids for the study of chemokine receptor structure and dynamics Drug Discovery Today: Technologies. 9: e301-e313. DOI: 10.1016/j.ddtec.2012.07.008  1
2012 Wijtmans M, Scholten DJ, De Esch IJP, Smit MJ, Leurs R. Therapeutic targeting of chemokine receptors by small molecules Drug Discovery Today: Technologies. 9: e229-e236. DOI: 10.1016/j.ddtec.2012.03.004  1
2012 Cordova-Sintjago TC, Fang L, Bruysters M, Leurs R, Booth RG. Molecular determinants of ligand binding at the human histamine H 1 receptor: Site-directed mutagenesis results analyzed with ligand docking and molecular dynamics studies at H 1 homology and crystal structure models Journal of Chemical and Pharmaceutical Research. 4: 2937-2951.  1
2011 de Graaf C, Kooistra AJ, Vischer HF, Katritch V, Kuijer M, Shiroishi M, Iwata S, Shimamura T, Stevens RC, de Esch IJ, Leurs R. Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor. Journal of Medicinal Chemistry. 54: 8195-206. PMID 22007643 DOI: 10.1021/jm2011589  1
2011 Istyastono EP, Nijmeijer S, Lim HD, van de Stolpe A, Roumen L, Kooistra AJ, Vischer HF, de Esch IJ, Leurs R, de Graaf C. Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies. Journal of Medicinal Chemistry. 54: 8136-47. PMID 22003888 DOI: 10.1021/jm201042n  1
2011 Kuhne S, Wijtmans M, Lim HD, Leurs R, de Esch IJ. Several down, a few to go: histamine H3 receptor ligands making the final push towards the market? Expert Opinion On Investigational Drugs. 20: 1629-48. PMID 21992603 DOI: 10.1517/13543784.2011.625010  1
2011 de Kruijf P, Lim HD, Roumen L, Renjaän VA, Zhao J, Webb ML, Auld DS, Wijkmans JC, Zaman GJ, Smit MJ, de Graaf C, Leurs R. Identification of a novel allosteric binding site in the CXCR2 chemokine receptor. Molecular Pharmacology. 80: 1108-18. PMID 21948388 DOI: 10.1124/mol.111.073825  1
2011 Akdemir A, Rucktooa P, Jongejan A, Elk Rv, Bertrand S, Sixma TK, Bertrand D, Smit AB, Leurs R, de Graaf C, de Esch IJ. Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors. Bioorganic & Medicinal Chemistry. 19: 6107-19. PMID 21920761 DOI: 10.1016/j.bmc.2011.08.028  1
2011 Coruzzi G, Adami M, Pozzoli C, de Esch IJ, Smits R, Leurs R. Selective histamine H₃ and H₄ receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. European Journal of Pharmacology. 669: 121-7. PMID 21839070 DOI: 10.1016/j.ejphar.2011.07.038  1
2011 Kufareva I, Rueda M, Katritch V, Stevens RC, Abagyan R. Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment. Structure (London, England : 1993). 19: 1108-26. PMID 21827947 DOI: 10.1016/j.str.2011.05.012  1
2011 Kool J, Heus F, de Kloe G, Lingeman H, Smit AB, Leurs R, Edink E, De Esch IJ, Irth H, Niessen WM. High-resolution bioactivity profiling of mixtures toward the acetylcholine binding protein using a nanofractionation spotter technology. Journal of Biomolecular Screening. 16: 917-24. PMID 21799121 DOI: 10.1177/1087057111413921  1
2011 Verheij MH, de Graaf C, de Kloe GE, Nijmeijer S, Vischer HF, Smits RA, Zuiderveld OP, Hulscher S, Silvestri L, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ. Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine Hâ‚„ and the ion channel serotonin 5-HT₃A. Bioorganic & Medicinal Chemistry Letters. 21: 5460-4. PMID 21782429 DOI: 10.1016/j.bmcl.2011.06.123  1
2011 van Loenen PB, de Graaf C, Verzijl D, Leurs R, Rognan D, Peters SL, Alewijnse AE. Agonist-dependent effects of mutations in the sphingosine-1-phosphate type 1 receptor. European Journal of Pharmacology. 667: 105-12. PMID 21663738 DOI: 10.1016/j.ejphar.2011.05.071  1
2011 Wijtmans M, Verzijl D, Bergmans S, Lai M, Bosch L, Smit MJ, de Esch IJ, Leurs R. CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors. Bioorganic & Medicinal Chemistry. 19: 3384-93. PMID 21570852 DOI: 10.1016/j.bmc.2011.04.035  1
2011 Leurs R, Vischer HF, Wijtmans M, de Esch IJ. En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family. Trends in Pharmacological Sciences. 32: 250-7. PMID 21414671 DOI: 10.1016/j.tips.2011.02.004  1
2011 Wijtmans M, de Graaf C, de Kloe G, Istyastono EP, Smit J, Lim H, Boonnak R, Nijmeijer S, Smits RA, Jongejan A, Zuiderveld O, de Esch IJ, Leurs R. Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity. Journal of Medicinal Chemistry. 54: 1693-703. PMID 21348462 DOI: 10.1021/jm1013488  1
2011 Edink E, Rucktooa P, Retra K, Akdemir A, Nahar T, Zuiderveld O, van Elk R, Janssen E, van Nierop P, van Muijlwijk-Koezen J, Smit AB, Sixma TK, Leurs R, de Esch IJ. Fragment growing induces conformational changes in acetylcholine-binding protein: a structural and thermodynamic analysis. Journal of the American Chemical Society. 133: 5363-71. PMID 21322593 DOI: 10.1021/ja110571r  1
2011 Hough LB, Nalwalk JW, Yang J, Conroy JL, VanAlstine MA, Yang W, Gargano J, Shan Z, Zhang SZ, Wentland MP, Phillips JG, Knapp BI, Bidlack JM, Zuiderveld OP, Leurs R, et al. Brain P450 epoxygenase activity is required for the antinociceptive effects of improgan, a nonopioid analgesic. Pain. 152: 878-87. PMID 21316152 DOI: 10.1016/j.pain.2011.01.001  1
2011 Istyastono EP, de Graaf C, de Esch IJ, Leurs R. Molecular determinants of selective agonist and antagonist binding to the histamine H₄ receptor. Current Topics in Medicinal Chemistry. 11: 661-79. PMID 21261593  1
2011 Vischer HF, Watts AO, Nijmeijer S, Leurs R. G protein-coupled receptors: walking hand-in-hand, talking hand-in-hand? British Journal of Pharmacology. 163: 246-60. PMID 21244374 DOI: 10.1111/j.1476-5381.2011.01229.x  1
2011 Kool J, de Kloe G, Denker AD, van Altena K, Smoluch M, van Iperen D, Nahar TT, Limburg RJ, Niessen WM, Lingeman H, Leurs R, de Esch IJ, Smit AB, Irth H. Nanofractionation spotter technology for rapid contactless and high-resolution deposition of LC eluent for further off-line analysis. Analytical Chemistry. 83: 125-32. PMID 21117623 DOI: 10.1021/ac102001g  1
2011 Sansuk K, Deupi X, Torrecillas IR, Jongejan A, Nijmeijer S, Bakker RA, Pardo L, Leurs R. A structural insight into the reorientation of transmembrane domains 3 and 5 during family A G protein-coupled receptor activation. Molecular Pharmacology. 79: 262-9. PMID 21081645 DOI: 10.1124/mol.110.066068  1
2011 Qin Y, Verdegaal EM, Siderius M, Bebelman JP, Smit MJ, Leurs R, Willemze R, Tensen CP, Osanto S. Quantitative expression profiling of G-protein-coupled receptors (GPCRs) in metastatic melanoma: the constitutively active orphan GPCR GPR18 as novel drug target. Pigment Cell & Melanoma Research. 24: 207-18. PMID 20880198 DOI: 10.1111/j.1755-148X.2010.00781.x  1
2011 Roumen L, Sanders MPA, Vroling B, de Esch IJP, de Vlieg J, Leurs R, Klomp JPG, Nabuurs SB, de Graaf C. In Silico Veritas: The pitfalls and challenges of predicting GPCR-ligand interactions Pharmaceuticals. 4: 1196-1215. DOI: 10.3390/ph4091196  1
2010 Bongers G, de Esch I, Leurs R. Molecular pharmacology of the four histamine receptors. Advances in Experimental Medicine and Biology. 709: 11-9. PMID 21618883 DOI: 10.1007/978-1-4419-8056-4-2  1
2010 Thompson AJ, Verheij MH, Leurs R, De Esch IJ, Lummis SC. An efficient and information-rich biochemical method design for fragment library screening on ion channels. Biotechniques. 49: 822-9. PMID 21091447 DOI: 10.2144/000113538  1
2010 Jähnichen S, Blanchetot C, Maussang D, Gonzalez-Pajuelo M, Chow KY, Bosch L, De Vrieze S, Serruys B, Ulrichts H, Vandevelde W, Saunders M, De Haard HJ, Schols D, Leurs R, Vanlandschoot P, et al. CXCR4 nanobodies (VHH-based single variable domains) potently inhibit chemotaxis and HIV-1 replication and mobilize stem cells. Proceedings of the National Academy of Sciences of the United States of America. 107: 20565-70. PMID 21059953 DOI: 10.1073/pnas.1012865107  1
2010 Nijmeijer S, Leurs R, Vischer HF. Constitutive activity of the histamine H(1) receptor. Methods in Enzymology. 484: 127-47. PMID 21036230 DOI: 10.1016/B978-0-12-381298-8.00007-1  1
2010 Bongers G, Maussang D, Muniz LR, Noriega VM, Fraile-Ramos A, Barker N, Marchesi F, Thirunarayanan N, Vischer HF, Qin L, Mayer L, Harpaz N, Leurs R, Furtado GC, Clevers H, et al. The cytomegalovirus-encoded chemokine receptor US28 promotes intestinal neoplasia in transgenic mice. The Journal of Clinical Investigation. 120: 3969-78. PMID 20978345 DOI: 10.1172/JCI42563  1
2010 Adami M, Pozzoli C, Leurs R, Stark H, Coruzzi G. Histamine H(3) receptors are involved in the protective effect of ghrelin against HCl-induced gastric damage in rats. Pharmacology. 86: 259-66. PMID 20975320 DOI: 10.1159/000320110  1
2010 de Kloe GE, Retra K, Geitmann M, Källblad P, Nahar T, van Elk R, Smit AB, van Muijlwijk-Koezen JE, Leurs R, Irth H, Danielson UH, de Esch IJ. Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptor α7 ligands. Journal of Medicinal Chemistry. 53: 7192-201. PMID 20828128 DOI: 10.1021/jm100834y  1
2010 Nijmeijer S, Leurs R, Smit MJ, Vischer HF. The Epstein-Barr virus-encoded G protein-coupled receptor BILF1 hetero-oligomerizes with human CXCR4, scavenges Gαi proteins, and constitutively impairs CXCR4 functioning. The Journal of Biological Chemistry. 285: 29632-41. PMID 20622011 DOI: 10.1074/jbc.M110.115618  1
2010 de Kruijf P, Lim HD, Overbeek SA, Zaman GJ, Kraneveld AD, Folkerts G, Leurs R, Smit MJ. The collagen-breakdown product N-acetyl-Proline-Glycine-Proline (N-alpha-PGP) does not interact directly with human CXCR1 and CXCR2. European Journal of Pharmacology. 643: 29-33. PMID 20599927 DOI: 10.1016/j.ejphar.2010.06.017  1
2010 Kool J, de Kloe GE, Bruyneel B, de Vlieger JS, Retra K, Wijtmans M, van Elk R, Smit AB, Leurs R, Lingeman H, de Esch IJ, Irth H. Online fluorescence enhancement assay for the acetylcholine binding protein with parallel mass spectrometric identification. Journal of Medicinal Chemistry. 53: 4720-30. PMID 20518527 DOI: 10.1021/jm100230k  1
2010 Smits RA, Adami M, Istyastono EP, Zuiderveld OP, van Dam CM, de Kanter FJ, Jongejan A, Coruzzi G, Leurs R, de Esch IJ. Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists. Journal of Medicinal Chemistry. 53: 2390-400. PMID 20192225 DOI: 10.1021/jm901379s  1
2010 Conroy JL, Fang C, Gu J, Zeitlin SO, Yang W, Yang J, VanAlstine MA, Nalwalk JW, Albrecht PJ, Mazurkiewicz JE, Snyder-Keller A, Shan Z, Zhang SZ, Wentland MP, Behr M, ... ... Leurs R, et al. Opioids activate brain analgesic circuits through cytochrome P450/epoxygenase signaling. Nature Neuroscience. 13: 284-6. PMID 20139973 DOI: 10.1038/nn.2497  1
2010 Lim HD, de Graaf C, Jiang W, Sadek P, McGovern PM, Istyastono EP, Bakker RA, de Esch IJ, Thurmond RL, Leurs R. Molecular determinants of ligand binding to H4R species variants. Molecular Pharmacology. 77: 734-43. PMID 20103609 DOI: 10.1124/mol.109.063040  1
2010 Vischer HF, Hulshof JW, Hulscher S, Fratantoni SA, Verheij MH, Victorina J, Smit MJ, de Esch IJ, Leurs R. Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28. Bioorganic & Medicinal Chemistry. 18: 675-88. PMID 20031418 DOI: 10.1016/j.bmc.2009.11.060  1
2010 Wijtmans M, Denonne F, Célanire S, Gillard M, Hulscher S, Delaunoy C, Van Houtvin N, Bakker RA, Defays S, Gérard J, Grooters L, Hubert D, Timmerman H, Leurs R, Talaga P, et al. Histamine H3 receptor ligands with a 3-cyclobutoxy motif: A novel and versatile constraint of the classical 3-propoxy linker Medchemcomm. 1: 39-44. DOI: 10.1039/c0md00056f  1
2010 Edink E, Jansen C, Leurs R, De Esch IJP. The heat is on: Thermodynamic analysis in fragment-based drug discovery Drug Discovery Today: Technologies. 7: e189-e201. DOI: 10.1016/j.ddtec.2010.12.001  1
2010 Schultes S, De Graaf C, Haaksma EEJ, De Esch IJP, Leurs R, Krämer O. Ligand efficiency as a guide in fragment hit selection and optimization Drug Discovery Today: Technologies. 7: e157-e162. DOI: 10.1016/j.ddtec.2010.11.003  1
2009 Rossbach K, Stark H, Sander K, Leurs R, Kietzmann M, Bäumer W. The histamine H receptor as a new target for treatment of canine inflammatory skin diseases. Veterinary Dermatology. 20: 555-61. PMID 20178494 DOI: 10.1111/j.1365-3164.2009.00854.x  1
2009 Engelhardt H, Smits RA, Leurs R, Haaksma E, de Esch IJ. A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic. Current Opinion in Drug Discovery & Development. 12: 628-43. PMID 19736622  1
2009 Maussang D, Vischer HF, Leurs R, Smit MJ. Herpesvirus-encoded G protein-coupled receptors as modulators of cellular function. Molecular Pharmacology. 76: 692-701. PMID 19570946 DOI: 10.1124/mol.109.057091  1
2009 Richter R, Casarosa P, Ständker L, Münch J, Springael JY, Nijmeijer S, Forssmann WG, Vischer HF, Vakili J, Detheux M, Parmentier M, Leurs R, Smit MJ. Significance of N-terminal proteolysis of CCL14a to activity on the chemokine receptors CCR1 and CCR5 and the human cytomegalovirus-encoded chemokine receptor US28. Journal of Immunology (Baltimore, Md. : 1950). 183: 1229-37. PMID 19553544 DOI: 10.4049/jimmunol.0802145  1
2009 Mariottini C, Scartabelli T, Bongers G, Arrigucci S, Nosi D, Leurs R, Chiarugi A, Blandina P, Pellegrini-Giampietro DE, Passani MB. Activation of the histaminergic H3 receptor induces phosphorylation of the Akt/GSK-3 beta pathway in cultured cortical neurons and protects against neurotoxic insults. Journal of Neurochemistry. 110: 1469-78. PMID 19549072 DOI: 10.1111/j.1471-4159.2009.06249.x  1
2009 Smits RA, Leurs R, de Esch IJ. Major advances in the development of histamine H4 receptor ligands. Drug Discovery Today. 14: 745-53. PMID 19477292 DOI: 10.1016/j.drudis.2009.05.007  1
2009 de Kloe GE, Bailey D, Leurs R, de Esch IJ. Transforming fragments into candidates: small becomes big in medicinal chemistry. Drug Discovery Today. 14: 630-46. PMID 19443265 DOI: 10.1016/j.drudis.2009.03.009  1
2009 Lim HD, Istyastono EP, van de Stolpe A, Romeo G, Gobbi S, Schepers M, Lahaye R, Menge WM, Zuiderveld OP, Jongejan A, Smits RA, Bakker RA, Haaksma EE, Leurs R, de Esch IJ. Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies. Bioorganic & Medicinal Chemistry. 17: 3987-94. PMID 19414267 DOI: 10.1016/j.bmc.2009.04.007  1
2009 Ferrada C, Moreno E, Casadó V, Bongers G, Cortés A, Mallol J, Canela EI, Leurs R, Ferré S, Lluís C, Franco R. Marked changes in signal transduction upon heteromerization of dopamine D1 and histamine H3 receptors. British Journal of Pharmacology. 157: 64-75. PMID 19413572 DOI: 10.1111/j.1476-5381.2009.00152.x  1
2009 Connelly WM, Shenton FC, Lethbridge N, Leurs R, Waldvogel HJ, Faull RL, Lees G, Chazot PL. The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. British Journal of Pharmacology. 157: 55-63. PMID 19413571 DOI: 10.1111/j.1476-5381.2009.00227.x  1
2009 Lim HD, Adami M, Guaita E, Werfel T, Smits RA, de Esch IJ, Bakker RA, Gutzmer R, Coruzzi G, Leurs R. Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430. British Journal of Pharmacology. 157: 34-43. PMID 19413569 DOI: 10.1111/j.1476-5381.2009.00200.x  1
2009 Leurs R, Chazot PL, Shenton FC, Lim HD, de Esch IJ. Molecular and biochemical pharmacology of the histamine H4 receptor. British Journal of Pharmacology. 157: 14-23. PMID 19413568 DOI: 10.1111/j.1476-5381.2009.00250.x  1
2009 Célanire S, Wijtmans M, Christophe B, Collart P, de Esch I, Dassesse D, Delaunoy C, Denonne F, Durieu V, Gelens E, Gillard M, Lallemand B, Lamberty Y, Lebon F, Nicolas JM, ... ... Leurs R, et al. Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists. Chemmedchem. 4: 1063-8. PMID 19405064 DOI: 10.1002/cmdc.200900055  1
2009 Ulens C, Akdemir A, Jongejan A, van Elk R, Bertrand S, Perrakis A, Leurs R, Smit AB, Sixma TK, Bertrand D, de Esch IJ. Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis. Journal of Medicinal Chemistry. 52: 2372-83. PMID 19331415 DOI: 10.1021/jm801400g  1
2009 Maussang D, Langemeijer E, Fitzsimons CP, Stigter-van Walsum M, Dijkman R, Borg MK, Slinger E, Schreiber A, Michel D, Tensen CP, van Dongen GA, Leurs R, Smit MJ. The human cytomegalovirus-encoded chemokine receptor US28 promotes angiogenesis and tumor formation via cyclooxygenase-2. Cancer Research. 69: 2861-9. PMID 19318580 DOI: 10.1158/0008-5472.CAN-08-2487  1
2009 Wijtmans M, Verzijl D, van Dam CM, Bosch L, Smit MJ, Leurs R, de Esch IJ. Exploring a pocket for polycycloaliphatic groups in the CXCR3 receptor with the aid of a modular synthetic strategy. Bioorganic & Medicinal Chemistry Letters. 19: 2252-7. PMID 19299127 DOI: 10.1016/j.bmcl.2009.02.093  1
2009 de Kruijf P, van Heteren J, Lim HD, Conti PG, van der Lee MM, Bosch L, Ho KK, Auld D, Ohlmeyer M, Smit MJ, Wijkmans JC, Zaman GJ, Smit MJ, Leurs R. Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor. The Journal of Pharmacology and Experimental Therapeutics. 329: 783-90. PMID 19190236 DOI: 10.1124/jpet.108.148387  1
2008 de Esch IJ, Leurs R. [From gene to drug: recent developments in medicinal chemistry]. Nederlands Tijdschrift Voor Geneeskunde. 152: 2795-800. PMID 19177921  1
2008 Smits RA, de Esch IJ, Zuiderveld OP, Broeker J, Sansuk K, Guaita E, Coruzzi G, Adami M, Haaksma E, Leurs R. Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. Journal of Medicinal Chemistry. 51: 7855-65. PMID 19053770 DOI: 10.1021/jm800876b  1
2008 Vischer HF, Nijmeijer S, Smit MJ, Leurs R. Viral hijacking of human receptors through heterodimerization. Biochemical and Biophysical Research Communications. 377: 93-7. PMID 18823943 DOI: 10.1016/j.bbrc.2008.09.082  1
2008 Jiang W, Lim HD, Zhang M, Desai P, Dai H, Colling PM, Leurs R, Thurmond RL. Cloning and pharmacological characterization of the dog histamine H4 receptor. European Journal of Pharmacology. 592: 26-32. PMID 18639542 DOI: 10.1016/j.ejphar.2008.06.095  1
2008 Lim HD, Jongejan A, Bakker RA, Haaksma E, de Esch IJ, Leurs R. Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors. The Journal of Pharmacology and Experimental Therapeutics. 327: 88-96. PMID 18635748 DOI: 10.1124/jpet.108.140343  1
2008 Jongejan A, Lim HD, Smits RA, de Esch IJ, Haaksma E, Leurs R. Delineation of agonist binding to the human histamine H4 receptor using mutational analysis, homology modeling, and ab initio calculations. Journal of Chemical Information and Modeling. 48: 1455-63. PMID 18553960 DOI: 10.1021/ci700474a  1
2008 Ferrada C, Ferré S, Casadó V, Cortés A, Justinova Z, Barnes C, Canela EI, Goldberg SR, Leurs R, Lluis C, Franco R. Interactions between histamine H3 and dopamine D2 receptors and the implications for striatal function. Neuropharmacology. 55: 190-7. PMID 18547596 DOI: 10.1016/j.neuropharm.2008.05.008  1
2008 van Rijn RM, van Marle A, Chazot PL, Langemeijer E, Qin Y, Shenton FC, Lim HD, Zuiderveld OP, Sansuk K, Dy M, Smit MJ, Tensen CP, Bakker RA, Leurs R. Cloning and characterization of dominant negative splice variants of the human histamine H4 receptor. The Biochemical Journal. 414: 121-31. PMID 18452403 DOI: 10.1042/BJ20071583  1
2008 Wijtmans M, Verzijl D, Leurs R, de Esch IJ, Smit MJ. Towards small-molecule CXCR3 ligands with clinical potential. Chemmedchem. 3: 861-72. PMID 18442035 DOI: 10.1002/cmdc.200700365  1
2008 Wijtmans M, Celanire S, Snip E, Gillard MR, Gelens E, Collart PP, Venhuis BJ, Christophe B, Hulscher S, van der Goot H, Lebon F, Timmerman H, Bakker RA, Lallemand BI, Leurs R, et al. 4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists. Journal of Medicinal Chemistry. 51: 2944-53. PMID 18433114 DOI: 10.1021/jm7014149  1
2008 Smits RA, Lim HD, Hanzer A, Zuiderveld OP, Guaita E, Adami M, Coruzzi G, Leurs R, de Esch IJ. Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. Journal of Medicinal Chemistry. 51: 2457-67. PMID 18357976 DOI: 10.1021/jm7014217  1
2008 Booth RG, Fang L, Wilczynski A, Sivendren S, Sun Z, Travers S, Bruysters M, Sansuk K, Leurs R. Molecular determinants of ligand-directed signaling for the histamine H1 receptor. Inflammation Research : Official Journal of the European Histamine Research Society ... [Et Al.]. 57: S43-4. PMID 18345497 DOI: 10.1007/s00011-007-0621-3  1
2008 Verzijl D, Storelli S, Scholten DJ, Bosch L, Reinhart TA, Streblow DN, Tensen CP, Fitzsimons CP, Zaman GJ, Pease JE, de Esch IJ, Smit MJ, Leurs R. Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors. The Journal of Pharmacology and Experimental Therapeutics. 325: 544-55. PMID 18270317 DOI: 10.1124/jpet.107.134783  1
2008 Dijkstra D, Stark H, Chazot PL, Shenton FC, Leurs R, Werfel T, Gutzmer R. Human inflammatory dendritic epidermal cells express a functional histamine H4 receptor. The Journal of Investigative Dermatology. 128: 1696-703. PMID 18239617 DOI: 10.1038/sj.jid.5701250  1
2008 Sansuk K, Balog CI, van der Does AM, Booth R, de Grip WJ, Deelder AM, Bakker RA, Leurs R, Hensbergen PJ. GPCR proteomics: mass spectrometric and functional analysis of histamine H1 receptor after baculovirus-driven and in vitro cell free expression. Journal of Proteome Research. 7: 621-9. PMID 18177001 DOI: 10.1021/pr7005654  1
2008 Bakker RA, Jongejan A, Sansuk K, Hacksell U, Timmerman H, Brann MR, Weiner DM, Pardo L, Leurs R. Constitutively active mutants of the histamine H1 receptor suggest a conserved hydrophobic asparagine-cage that constrains the activation of class A G protein-coupled receptors. Molecular Pharmacology. 73: 94-103. PMID 17959710 DOI: 10.1124/mol.107.038547  1
2007 Kool J, van Marle A, Hulscher S, Selman M, van Iperen DJ, van Altena K, Gillard M, Bakker RA, Irth H, Leurs R, Vermeulen NP. A flow-through fluorescence polarization detection system for measuring GPCR-mediated modulation of cAMP production. Journal of Biomolecular Screening. 12: 1074-83. PMID 18087072 DOI: 10.1177/1087057107308881  1
2007 Bongers G, Krueger KM, Miller TR, Baranowski JL, Estvander BR, Witte DG, Strakhova MI, van Meer P, Bakker RA, Cowart MD, Hancock AA, Esbenshade TA, Leurs R. An 80-amino acid deletion in the third intracellular loop of a naturally occurring human histamine H3 isoform confers pharmacological differences and constitutive activity. The Journal of Pharmacology and Experimental Therapeutics. 323: 888-98. PMID 17855474 DOI: 10.1124/jpet.107.127639  1
2007 Hough LB, Menge WM, van de Stolpe AC, Nalwalk JW, Leurs R, de Esch IJ. Antinociceptive activity of furan-containing congeners of improgan and ranitidine. Bioorganic & Medicinal Chemistry Letters. 17: 5715-9. PMID 17766108 DOI: 10.1016/j.bmcl.2007.07.060  1
2007 Cannon KE, Leurs R, Hough LB. Activation of peripheral and spinal histamine H3 receptors inhibits formalin-induced inflammation and nociception, respectively. Pharmacology, Biochemistry, and Behavior. 88: 122-9. PMID 17719621 DOI: 10.1016/j.pbb.2007.07.014  1
2007 Bongers G, Sallmen T, Passani MB, Mariottini C, Wendelin D, Lozada A, Marle Av, Navis M, Blandina P, Bakker RA, Panula P, Leurs R. The Akt/GSK-3beta axis as a new signaling pathway of the histamine H(3) receptor. Journal of Neurochemistry. 103: 248-58. PMID 17623045 DOI: 10.1111/j.1471-4159.2007.04752.x  1
2007 Wijtmans M, Leurs R, de Esch I. Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas. Expert Opinion On Investigational Drugs. 16: 967-85. PMID 17594183 DOI: 10.1517/13543784.16.7.967  1
2007 Storelli S, Verzijl D, Al-Badie J, Elders N, Bosch L, Timmerman H, Smit MJ, De Esch IJ, Leurs R. Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists. Archiv Der Pharmazie. 340: 281-91. PMID 17562560 DOI: 10.1002/ardp.200700037  1
2007 Dijkstra D, Leurs R, Chazot P, Shenton FC, Stark H, Werfel T, Gutzmer R. Histamine downregulates monocyte CCL2 production through the histamine H4 receptor. The Journal of Allergy and Clinical Immunology. 120: 300-7. PMID 17507084 DOI: 10.1016/j.jaci.2007.03.024  1
2007 Hulsman N, Medema JP, Bos C, Jongejan A, Leurs R, Smit MJ, de Esch IJ, Richel D, Wijtmans M. Chemical insights in the concept of hybrid drugs: the antitumor effect of nitric oxide-donating aspirin involves a quinone methide but not nitric oxide nor aspirin. Journal of Medicinal Chemistry. 50: 2424-31. PMID 17441704 DOI: 10.1021/jm061371e  1
2007 Bakker RA, Nicholas MW, Smith TT, Burstein ES, Hacksell U, Timmerman H, Leurs R, Brann MR, Weiner DM. In vitro pharmacology of clinically used central nervous system-active drugs as inverse H(1) receptor agonists. The Journal of Pharmacology and Experimental Therapeutics. 322: 172-9. PMID 17403993 DOI: 10.1124/jpet.106.118869  1
2007 Coruzzi G, Adami M, Guaita E, de Esch IJ, Leurs R. Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation. European Journal of Pharmacology. 563: 240-4. PMID 17382315 DOI: 10.1016/j.ejphar.2007.02.026  1
2007 Dai H, Fu Q, Shen Y, Hu W, Zhang Z, Timmerman H, Leurs R, Chen Z. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. European Journal of Pharmacology. 563: 117-23. PMID 17350613 DOI: 10.1016/j.ejphar.2007.01.069  1
2007 Bongers G, Bakker RA, Leurs R. Molecular aspects of the histamine H3 receptor. Biochemical Pharmacology. 73: 1195-204. PMID 17276412 DOI: 10.1016/j.bcp.2007.01.008  1
2007 Ratnala VR, Kiihne SR, Buda F, Leurs R, de Groot HJ, DeGrip WJ. Solid-state NMR evidence for a protonation switch in the binding pocket of the H1 receptor upon binding of the agonist histamine. Journal of the American Chemical Society. 129: 867-72. PMID 17243823 DOI: 10.1021/ja0652262  1
2007 Smit MJ, Vischer HF, Bakker RA, Jongejan A, Timmerman H, Pardo L, Leurs R. Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity. Annual Review of Pharmacology and Toxicology. 47: 53-87. PMID 17029567 DOI: 10.1146/annurev.pharmtox.47.120505.105126  1
2006 Vischer HF, Hulshof JW, de Esch IJ, Smit MJ, Leurs R. Virus-encoded G-protein-coupled receptors: constitutively active (dys)regulators of cell function and their potential as drug target. Ernst Schering Foundation Symposium Proceedings. 187-209. PMID 17703583  1
2006 Lim HD, Smits RA, Bakker RA, van Dam CM, de Esch IJ, Leurs R. Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. Journal of Medicinal Chemistry. 49: 6650-1. PMID 17154494 DOI: 10.1021/jm060880d  1
2006 Verzijl D, Pardo L, van Dijk M, Gruijthuijsen YK, Jongejan A, Timmerman H, Nicholas J, Schwarz M, Murphy PM, Leurs R, Smit MJ. Helix 8 of the viral chemokine receptor ORF74 directs chemokine binding. The Journal of Biological Chemistry. 281: 35327-35. PMID 16997914 DOI: 10.1074/jbc.M606877200  1
2006 Maussang D, Verzijl D, van Walsum M, Leurs R, Holl J, Pleskoff O, Michel D, van Dongen GA, Smit MJ. Human cytomegalovirus-encoded chemokine receptor US28 promotes tumorigenesis. Proceedings of the National Academy of Sciences of the United States of America. 103: 13068-73. PMID 16924106 DOI: 10.1073/pnas.0604433103  1
2006 Lim HD, Smits RA, Leurs R, De Esch IJ. The emerging role of the histamine H4 receptor in anti-inflammatory therapy. Current Topics in Medicinal Chemistry. 6: 1365-73. PMID 16918455  1
2006 Smits RA, Lim HD, Stegink B, Bakker RA, de Esch IJ, Leurs R. Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. Journal of Medicinal Chemistry. 49: 4512-6. PMID 16854056 DOI: 10.1021/jm051008s  1
2006 Hulshof JW, Vischer HF, Verheij MH, Fratantoni SA, Smit MJ, de Esch IJ, Leurs R. Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28. Bioorganic & Medicinal Chemistry. 14: 7213-30. PMID 16843661 DOI: 10.1016/j.bmc.2006.06.054  1
2006 Hough LB, de Esch IJ, Janssen E, Phillips J, Svokos K, Kern B, Trachler J, Abood ME, Leurs R, Nalwalk JW. Antinociceptive activity of chemical congeners of improgan: optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic. Neuropharmacology. 51: 447-56. PMID 16806300 DOI: 10.1016/j.neuropharm.2006.04.003  1
2006 van Rijn RM, Chazot PL, Shenton FC, Sansuk K, Bakker RA, Leurs R. Oligomerization of recombinant and endogenously expressed human histamine H(4) receptors. Molecular Pharmacology. 70: 604-15. PMID 16645125 DOI: 10.1124/mol.105.020818  1
2006 Govoni M, Lim HD, El-Atmioui D, Menge WM, Timmerman H, Bakker RA, Leurs R, De Esch IJ. A chemical switch for the modulation of the functional activity of higher homologues of histamine on the human histamine H3 receptor: effect of various substitutions at the primary amino function. Journal of Medicinal Chemistry. 49: 2549-57. PMID 16610798 DOI: 10.1021/jm0504353  1
2006 Dai H, Zhang Z, Zhu Y, Shen Y, Hu W, Huang Y, Luo J, Timmerman H, Leurs R, Chen Z. Histamine protects against NMDA-induced necrosis in cultured cortical neurons through H receptor/cyclic AMP/protein kinase A and H receptor/GABA release pathways. Journal of Neurochemistry. 96: 1390-400. PMID 16478529 DOI: 10.1111/j.1471-4159.2005.03633.x  1
2006 Bakker RA, Lozada AF, van Marle A, Shenton FC, Drutel G, Karlstedt K, Hoffmann M, Lintunen M, Yamamoto Y, van Rijn RM, Chazot PL, Panula P, Leurs R. Discovery of naturally occurring splice variants of the rat histamine H3 receptor that act as dominant-negative isoforms. Molecular Pharmacology. 69: 1194-206. PMID 16415177 DOI: 10.1124/mol.105.019299  1
2006 Gelens E, De Kanter FJ, Schmitz RF, Sliedregt LA, Van Steen BJ, Kruse CG, Leurs R, Groen MB, Orru RV. Efficient library synthesis of imidazoles using a multicomponent reaction and microwave irradiation. Molecular Diversity. 10: 17-22. PMID 16404525 DOI: 10.1007/s11030-006-8695-3  1
2006 Vischer HF, Leurs R, Smit MJ. HCMV-encoded G-protein-coupled receptors as constitutively active modulators of cellular signaling networks. Trends in Pharmacological Sciences. 27: 56-63. PMID 16352349 DOI: 10.1016/j.tips.2005.11.006  1
2006 Fitzsimons CP, Gompels UA, Verzijl D, Vischer HF, Mattick C, Leurs R, Smit MJ. Chemokine-directed trafficking of receptor stimulus to different g proteins: selective inducible and constitutive signaling by human herpesvirus 6-encoded chemokine receptor U51. Molecular Pharmacology. 69: 888-98. PMID 16332987 DOI: 10.1124/mol.105.015222  1
2006 Derks RJE, Letzel T, De Jong CF, Van Marle A, Lingeman H, Leurs R, Irth H. SEC-MS as an approach to isolate and directly identifying small molecular GPCR-ligands from complex mixtures without labeling Chromatographia. 64: 379-385. DOI: 10.1365/s10337-006-0058-9  1
2005 Jongejan A, Bruysters M, Ballesteros JA, Haaksma E, Bakker RA, Pardo L, Leurs R. Linking agonist binding to histamine H1 receptor activation. Nature Chemical Biology. 1: 98-103. PMID 16408006 DOI: 10.1038/nchembio714  1
2005 Celanire S, Wijtmans M, Talaga P, Leurs R, de Esch IJ. Keynote review: histamine H3 receptor antagonists reach out for the clinic. Drug Discovery Today. 10: 1613-27. PMID 16376822 DOI: 10.1016/S1359-6446(05)03625-1  1
2005 Jongejan A, de Graaf C, Vermeulen NP, Leurs R, de Esch IJ. The role and application of in silico docking in chemical genomics research. Methods in Molecular Biology (Clifton, N.J.). 310: 63-91. PMID 16350947  1
2005 Kitbunnadaj R, Hoffmann M, Fratantoni SA, Bongers G, Bakker RA, Wieland K, el Jilali A, De Esch IJ, Menge WM, Timmerman H, Leurs R. New high affinity H3 receptor agonists without a basic side chain. Bioorganic & Medicinal Chemistry. 13: 6309-23. PMID 16213736 DOI: 10.1016/j.bmc.2005.09.002  1
2005 Hulshof JW, Casarosa P, Menge WM, Kuusisto LM, van der Goot H, Smit MJ, de Esch IJ, Leurs R. Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28. Journal of Medicinal Chemistry. 48: 6461-71. PMID 16190772 DOI: 10.1021/jm050418d  1
2005 Lozada A, Munyao N, Sallmen T, Lintunen M, Leurs R, Lindsberg PJ, Panula P. Postischemic regulation of central histamine receptors Neuroscience. 136: 371-379. PMID 16181737 DOI: 10.1016/j.neuroscience.2005.06.079  1
2005 Pleskoff O, Casarosa P, Verneuil L, Ainoun F, Beisser P, Smit M, Leurs R, Schneider P, Michelson S, Ameisen JC. The human cytomegalovirus-encoded chemokine receptor US28 induces caspase-dependent apoptosis. The Febs Journal. 272: 4163-77. PMID 16098198 DOI: 10.1111/j.1742-4658.2005.04829.x  1
2005 de Esch IJ, Thurmond RL, Jongejan A, Leurs R. The histamine H4 receptor as a new therapeutic target for inflammation. Trends in Pharmacological Sciences. 26: 462-9. PMID 16054239 DOI: 10.1016/j.tips.2005.07.002  1
2005 Bruysters M, Jongejan A, Akdemir A, Bakker RA, Leurs R. A G(q/11)-coupled mutant histamine H(1) receptor F435A activated solely by synthetic ligands (RASSL). The Journal of Biological Chemistry. 280: 34741-6. PMID 16027157 DOI: 10.1074/jbc.M504165200  1
2005 Jongejan A, Leurs R. Delineation of receptor-ligand interactions at the human histamine H1 receptor by a combined approach of site-directed mutagenesis and computational techniques - or - how to bind the H1 receptor. Archiv Der Pharmazie. 338: 248-59. PMID 15952243 DOI: 10.1002/ardp.200400998  1
2005 Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R. Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. The Journal of Pharmacology and Experimental Therapeutics. 314: 1310-21. PMID 15947036 DOI: 10.1124/jpet.105.087965  1
2005 Storelli S, Verdijk P, Verzijl D, Timmerman H, van de Stolpe AC, Tensen CP, Smit MJ, De Esch IJ, Leurs R. Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 15: 2910-3. PMID 15911279 DOI: 10.1016/j.bmcl.2005.03.070  1
2005 Kitbunnadaj R, Hashimoto T, Poli E, Zuiderveld OP, Menozzi A, Hidaka R, de Esch IJ, Bakker RA, Menge WM, Yamatodani A, Coruzzi G, Timmerman H, Leurs R. N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist. Journal of Medicinal Chemistry. 48: 2100-7. PMID 15771452 DOI: 10.1021/jm049475h  1
2005 Nalwalk JW, Svokos K, Leurs R, Hough LB. Absence of 5-HT3 and cholinergic mechanisms in improgan antinociception. Pharmacology, Biochemistry, and Behavior. 80: 505-10. PMID 15740793 DOI: 10.1016/j.pbb.2005.01.006  1
2005 de Ligt RA, Rivkees SA, Lorenzen A, Leurs R, IJzerman AP. A "locked-on," constitutively active mutant of the adenosine A1 receptor. European Journal of Pharmacology. 510: 1-8. PMID 15740718 DOI: 10.1016/j.ejphar.2005.01.007  1
2005 Leurs R, Bakker RA, Timmerman H, de Esch IJ. The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nature Reviews. Drug Discovery. 4: 107-20. PMID 15665857 DOI: 10.1038/nrd1631  1
2005 Bruysters M, Jongejan A, Gillard M, Van De Manakker F, Bakker RA, Chatelain P, Leurs R. Pharmacological differences between human and guinea pig histamine H 1 receptors: Asn84 (2.61) as key residue within an additional binding pocket in the H1 receptor Molecular Pharmacology. 67: 1046-1052. PMID 15626750 DOI: 10.1124/mol.104.008847  1
2005 Beisser PS, Verzijl D, Gruijthuijsen YK, Beuken E, Smit MJ, Leurs R, Bruggeman CA, Vink C. The Epstein-Barr virus BILF1 gene encodes a G protein-coupled receptor that inhibits phosphorylation of RNA-dependent protein kinase. Journal of Virology. 79: 441-9. PMID 15596837 DOI: 10.1128/JVI.79.1.441-449.2005  1
2005 Casarosa P, Waldhoer M, LiWang PJ, Vischer HF, Kledal T, Timmerman H, Schwartz TW, Smit MJ, Leurs R. CC and CX3C chemokines differentially interact with the N terminus of the human cytomegalovirus-encoded US28 receptor. The Journal of Biological Chemistry. 280: 3275-85. PMID 15546882 DOI: 10.1074/jbc.M407536200  1
2005 Gelens E, Smeets L, Sliedregt LAJM, Van Steen BJ, Kruse CG, Leurs R, Orru RVA. An atom efficient and solvent-free synthesis of structurally diverse amides using microwaves Tetrahedron Letters. 46: 3751-3754. DOI: 10.1002/chin.200537054  1
2004 Malan SF, van Marle A, Menge WM, Zuliani V, Zuliana V, Hoffman M, Timmerman H, Leurs R. Fluorescent ligands for the histamine H2 receptor: synthesis and preliminary characterization. Bioorganic & Medicinal Chemistry. 12: 6495-503. PMID 15556766 DOI: 10.1016/j.bmc.2004.09.018  1
2004 Terzioglu N, van Rijn RM, Bakker RA, De Esch IJ, Leurs R. Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 14: 5251-6. PMID 15454206 DOI: 10.1016/j.bmcl.2004.08.035  1
2004 Nalwalk JW, Svokos K, Taraschenko O, Leurs R, Timmerman H, Hough LB. Activation of brain stem nuclei by improgan, a non-opioid analgesic. Brain Research. 1021: 248-55. PMID 15342273 DOI: 10.1016/j.brainres.2004.06.066  1
2004 Kitbunnadaj R, Zuiderveld OP, Christophe B, Hulscher S, Menge WM, Gelens E, Snip E, Bakker RA, Celanire S, Gillard M, Talaga P, Timmerman H, Leurs R. Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist. Journal of Medicinal Chemistry. 47: 2414-7. PMID 15115383 DOI: 10.1021/jm049932u  1
2004 Huang YW, Hu WW, Chen Z, Zhang LS, Shen HQ, Timmerman H, Leurs R, Yanai K. Effect of the histamine H3-antagonist clobenpropit on spatial memory deficits induced by MK-801 as evaluated by radial maze in Sprague-Dawley rats. Behavioural Brain Research. 151: 287-93. PMID 15084444 DOI: 10.1016/j.bbr.2003.09.002  1
2004 Bruysters M, Pertz HH, Teunissen A, Bakker RA, Gillard M, Chatelain P, Schunack W, Timmerman H, Leurs R. Mutational analysis of the histamine H1-receptor binding pocket of histaprodifens. European Journal of Pharmacology. 487: 55-63. PMID 15033376 DOI: 10.1016/j.ejphar.2004.01.028  1
2004 Verzijl D, Fitzsimons CP, Van Dijk M, Stewart JP, Timmerman H, Smit MJ, Leurs R. Differential activation of murine herpesvirus 68- and Kaposi's sarcoma-associated herpesvirus-encoded ORF74 G protein-coupled receptors by human and murine chemokines. Journal of Virology. 78: 3343-51. PMID 15016856 DOI: 10.1128/JVI.78.7.3343-3351.2004  1
2004 Bakker RA, Weiner DM, ter Laak T, Beuming T, Zuiderveld OP, Edelbroek M, Hacksell U, Timmerman H, Brann MR, Leurs R. 8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist. Molecular Pharmacology. 65: 538-49. PMID 14978232 DOI: 10.1124/mol.65.3.538  1
2004 Bakker RA, Casarosa P, Timmerman H, Smit MJ, Leurs R. Constitutively active Gq/11-coupled receptors enable signaling by co-expressed G(i/o)-coupled receptors. The Journal of Biological Chemistry. 279: 5152-61. PMID 14610092 DOI: 10.1074/jbc.M309200200  1
2004 Hough LB, Nalwalk JW, Menge W, Leurs R, Timmerman H. Improgan-like analgesics: A family of compounds derived from histamine antagonists Medicinal Chemistry Research. 13: 78-87. DOI: 10.1007/s00044-004-0012-z  1
2003 Govoni M, Bakker RA, van de Wetering I, Smit MJ, Menge WM, Timmerman H, Elz S, Schunack W, Leurs R. Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists. Journal of Medicinal Chemistry. 46: 5812-24. PMID 14667234 DOI: 10.1021/jm030936t  1
2003 Zhang L, Chen Z, Ren K, Leurs R, Chen J, Zhang W, Ye B, Wei E, Timmerman H. Effects of clobenpropit on pentylenetetrazole-kindled seizures in rats. European Journal of Pharmacology. 482: 169-75. PMID 14660019 DOI: 10.1016/j.ejphar.2003.09.066  1
2003 Kitbunnadaj R, Zuiderveld OP, De Esch IJ, Vollinga RC, Bakker R, Lutz M, Spek AL, Cavoy E, Deltent MF, Menge WM, Timmerman H, Leurs R. Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists. Journal of Medicinal Chemistry. 46: 5445-57. PMID 14640553 DOI: 10.1021/jm030905y  1
2003 Izadi Mobarakeh J, Nalwalk JW, Watanabe T, Sakurada S, Hoffman M, Leurs R, Timmerman H, Silos-Santiago I, Yanai K, Hough LB. Improgan antinociception does not require neuronal histamine or histamine receptors. Brain Research. 974: 146-52. PMID 12742632 DOI: 10.1016/S0006-8993(03)02572-1  1
2003 Casarosa P, Menge WM, Minisini R, Otto C, van Heteren J, Jongejan A, Timmerman H, Moepps B, Kirchhoff F, Mertens T, Smit MJ, Leurs R. Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G protein-coupled receptor. The Journal of Biological Chemistry. 278: 5172-8. PMID 12456673 DOI: 10.1074/jbc.M210033200  1
2002 Hough LB, Nalwalk JW, Stadel R, Timmerman H, Leurs R, Paria BC, Wang X, Dey SK. Inhibition of improgan antinociception by the cannabinoid (CB)(1) antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A): lack of obligatory role for endocannabinoids acting at CB(1) receptors. The Journal of Pharmacology and Experimental Therapeutics. 303: 314-22. PMID 12235266 DOI: 10.1124/jpet.102.036251  1
2002 Bakker RA, Timmerman H, Leurs R. Histamine receptors: specific ligands, receptor biochemistry, and signal transduction. Clinical Allergy and Immunology. 17: 27-64. PMID 12113220  1
2002 Booth RG, Moniri NH, Bakker RA, Choksi NY, Nix WB, Timmerman H, Leurs R. A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors. The Journal of Pharmacology and Experimental Therapeutics. 302: 328-36. PMID 12065734 DOI: 10.1124/jpet.302.1.328  1
2002 Smit MJ, Verzijl D, Casarosa P, Navis M, Timmerman H, Leurs R. Kaposi's sarcoma-associated herpesvirus-encoded G protein-coupled receptor ORF74 constitutively activates p44/p42 MAPK and Akt via G(i) and phospholipase C-dependent signaling pathways. Journal of Virology. 76: 1744-52. PMID 11799169 DOI: 10.1128/JVI.76.4.1744-1752.2002  1
2002 Leurs R, Hoffmann M, Alewijnse AE, Smit MJ, Timmerman H. Methods to determine the constitutive activity of histamine H2 receptors. Methods in Enzymology. 343: 405-16. PMID 11665581 DOI: 10.1016/S0076-6879(02)43148-5  1
2000 Timmerman H. Preface. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation For Pharmaceutical Sciences. 12: 83-84. PMID 11102734 DOI: 10.1002/9783527614141  1
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