| Year |
Citation |
Score |
| 2024 |
Xia R, Shi S, Xu Z, Vischer HF, Windhorst AD, Qian Y, Duan Y, Liang J, Chen K, Zhang A, Guo C, Leurs R, He Y. Structural basis of ligand recognition and design of antihistamines targeting histamine H receptor. Nature Communications. 15: 2493. PMID 38509098 DOI: 10.1038/s41467-024-46840-5 |
0.421 |
|
| 2024 |
Gao M, Dekker ME, Leurs R, Vischer HF. Pharmacological characterization of seven human histamine H receptor isoforms. European Journal of Pharmacology. 968: 176450. PMID 38387718 DOI: 10.1016/j.ejphar.2024.176450 |
0.448 |
|
| 2024 |
Zarca A, Adlere I, Viciano CP, Arimont-Segura M, Meyrath M, Simon IA, Bebelman JP, Laan D, Custers HGJ, Janssen E, Versteegh KLK, Buzink M, Nesheva D, Bosma R, de Esch IJP, ... ... Leurs R, et al. Pharmacological characterization and radiolabeling of VUF15485, a high-affinity small-molecule agonist for the atypical chemokine receptor ACKR3. Molecular Pharmacology. PMID 38346795 DOI: 10.1124/molpharm.123.000835 |
0.751 |
|
| 2023 |
Dekkers S, Comez D, Karsai N, Arimont-Segura M, Canals M, Caspar B, de Graaf C, Kilpatrick LE, Leurs R, Kellam B, Hill SJ, Briddon SJ, Stocks MJ. Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3). Acs Medicinal Chemistry Letters. 15: 143-148. PMID 38229752 DOI: 10.1021/acsmedchemlett.3c00469 |
0.355 |
|
| 2023 |
Rahman SN, Imhaouran F, Leurs R, Christopoulos A, Valant C, Langmead CJ. Ligand-directed biased agonism at human histamine H receptor isoforms across Gα- and β-arrestin2-mediated pathways. Biochemical Pharmacology. 115988. PMID 38159685 DOI: 10.1016/j.bcp.2023.115988 |
0.361 |
|
| 2023 |
McNaught-Flores DA, Kooistra AJ, Chen YC, Arias-Montano JA, Panula P, Leurs R. Pharmacological characterization of the zebrafish () histamine H receptor reveals the involvement of the second extracellular loop in the binding of histamine. Molecular Pharmacology. PMID 37977823 DOI: 10.1124/molpharm.123.000741 |
0.45 |
|
| 2023 |
Rahman SN, McNaught-Flores DA, Huppelschoten Y, da Costa Pereira D, Christopoulos A, Leurs R, Langmead CJ. Structural and Molecular Determinants for Isoform Bias at Human Histamine H Receptor Isoforms. Acs Chemical Neuroscience. PMID 36702158 DOI: 10.1021/acschemneuro.2c00425 |
0.363 |
|
| 2022 |
Wágner G, Mocking TAM, Ma X, Slynko I, Da Costa Pereira D, Breeuwer R, Rood NJN, van der Horst C, Vischer HF, de Graaf C, de Esch IJP, Wijtmans M, Leurs R. SAR exploration of the non-imidazole histamine H receptor ligand ZEL-H16 reveals potent inverse agonism. Archiv Der Pharmazie. e2200451. PMID 36310109 DOI: 10.1002/ardp.202200451 |
0.419 |
|
| 2022 |
Ma X, Gao M, Vischer HF, Leurs R. A NanoBRET-Based HR Conformational Biosensor to Study Real-Time H Receptor Pharmacology in Cell Membranes and Living Cells. International Journal of Molecular Sciences. 23. PMID 35897787 DOI: 10.3390/ijms23158211 |
0.385 |
|
| 2022 |
Zheng Y, Wágner G, Hauwert N, Ma X, Vischer HF, Leurs R. New Chemical Biology Tools for the Histamine Receptor Family. Current Topics in Behavioral Neurosciences. PMID 35851442 DOI: 10.1007/7854_2022_360 |
0.404 |
|
| 2022 |
Kok ZY, Stoddart LA, Mistry SJ, Mocking TAM, Vischer HF, Leurs R, Hill SJ, Mistry SN, Kellam B. Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H Receptor. Journal of Medicinal Chemistry. 65: 8258-8288. PMID 35734860 DOI: 10.1021/acs.jmedchem.2c00125 |
0.315 |
|
| 2022 |
Verweij EWE, Bosma R, Gao M, van den Bor J, Al Araaj B, de Munnik SM, Ma X, Leurs R, Vischer HF. BRET-Based Biosensors to Measure Agonist Efficacies in Histamine H Receptor-Mediated G Protein Activation, Signaling and Interactions with GRKs and β-Arrestins. International Journal of Molecular Sciences. 23. PMID 35328605 DOI: 10.3390/ijms23063184 |
0.406 |
|
| 2021 |
Ma X, Verweij EWE, Siderius M, Leurs R, Vischer HF. Identification of TSPAN4 as Novel Histamine H Receptor Interactor. Biomolecules. 11. PMID 34439793 DOI: 10.3390/biom11081127 |
0.416 |
|
| 2021 |
Ma X, Leurs R, Vischer HF. NanoLuc-Based Methods to Measure β-Arrestin2 Recruitment to G Protein-Coupled Receptors. Methods in Molecular Biology (Clifton, N.J.). 2268: 233-248. PMID 34085273 DOI: 10.1007/978-1-0716-1221-7_16 |
0.39 |
|
| 2021 |
Wang Z, Bosma R, Kuhne S, van den Bor J, Garabitian W, Vischer HF, Wijtmans M, Leurs R, de Esch IJP. Exploring the Effect of Cyclization of Histamine H Receptor Antagonists on Ligand Binding Kinetics. Acs Omega. 6: 12755-12768. PMID 34056427 DOI: 10.1021/acsomega.0c06358 |
0.397 |
|
| 2021 |
Ma X, Segura MA, Zarzycka B, Vischer HF, Leurs R. Analysis of Missense Variants in the Human Histamine Receptor Family Reveals Increased Constitutive Activity of E410K Variant in the Histamine H Receptor. International Journal of Molecular Sciences. 22. PMID 33918180 DOI: 10.3390/ijms22073702 |
0.479 |
|
| 2021 |
Egyed A, Kelemen ÁA, Vass M, Visegrády A, Thee SA, Wang Z, de Graaf C, Brea J, Loza MI, Leurs R, Keserű GM. Controlling the selectivity of aminergic GPCR ligands from the extracellular vestibule. Bioorganic Chemistry. 111: 104832. PMID 33826962 DOI: 10.1016/j.bioorg.2021.104832 |
0.38 |
|
| 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 |
0.55 |
|
| 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 |
0.358 |
|
| 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 |
0.452 |
|
| 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 |
0.411 |
|
| 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 |
0.429 |
|
| 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 |
0.718 |
|
| 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 |
0.453 |
|
| 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 |
0.491 |
|
| 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 |
0.345 |
|
| 2019 |
Staszewski M, Stasiak A, Karcz T, McNaught Flores D, Fogel WA, Kieć-Kononowicz K, Leurs R, Walczyński K. Design, synthesis, and and characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H receptor antagonists. Medchemcomm. 10: 234-251. PMID 30881612 DOI: 10.1039/C8Md00527C |
0.501 |
|
| 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 |
0.595 |
|
| 2019 |
Chazot P, Cowart M, Fukui H, Ganellin CR, Gutzmer R, Haas HL, Hill SJ, Hills R, Leurs R, Levi R, Liu S, Panula P, Schunack W, Schwartz J, Seifert R, et al. Histamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database Iuphar/Bps Guide to Pharmacology Cite. 2019. DOI: 10.2218/gtopdb/f33/2019.4 |
0.524 |
|
| 2018 |
Adlere I, Sun S, Zarca A, Roumen L, Gozelle M, Viciano Perpiñá C, Caspar B, Arimont M, Bebelman JP, Briddon SJ, Hoffmann C, Hill SJ, Smit MJ, Vischer HF, Wijtmans M, ... ... Leurs R, et al. Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists. European Journal of Medicinal Chemistry. 162: 631-649. PMID 30476826 DOI: 10.1016/J.Ejmech.2018.10.060 |
0.709 |
|
| 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 |
0.369 |
|
| 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 |
0.431 |
|
| 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 |
0.467 |
|
| 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 |
0.313 |
|
| 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 |
0.675 |
|
| 2018 |
Olszewska B, Stasiak A, McNaught Flores D, Fogel WA, Leurs R, Walczyński K. 4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H₃ Receptor Antagonist: Further Structure⁻Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation. International Journal of Molecular Sciences. 19. PMID 29671795 DOI: 10.3390/Ijms19041243 |
0.514 |
|
| 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 |
0.729 |
|
| 2018 |
Guryn R, Staszewski M, Stasiak A, McNaught Flores D, Fogel WA, Leurs R, Walczyński K. Non-Imidazole Histamine H₃ Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines. Molecules (Basel, Switzerland). 23. PMID 29401659 DOI: 10.3390/Molecules23020326 |
0.401 |
|
| 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 |
0.498 |
|
| 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 |
0.37 |
|
| 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 |
0.405 |
|
| 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 |
0.733 |
|
| 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 |
0.442 |
|
| 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 |
0.375 |
|
| 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 |
0.509 |
|
| 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 |
0.433 |
|
| 2016 |
Nijmeijer S, Vischer H, Leurs R. Adhesion GPCRs in immunology. Biochemical Pharmacology. PMID 27131861 DOI: 10.1016/J.Bcp.2016.04.013 |
0.324 |
|
| 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 |
0.708 |
|
| 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 |
0.755 |
|
| 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 |
0.328 |
|
| 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 |
0.738 |
|
| 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 |
0.642 |
|
| 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 |
0.705 |
|
| 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 |
0.477 |
|
| 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 |
0.689 |
|
| 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 |
0.338 |
|
| 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 |
0.488 |
|
| 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 |
0.7 |
|
| 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 |
0.771 |
|
| 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 |
0.486 |
|
| 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 |
0.733 |
|
| 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 |
0.718 |
|
| 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 |
0.706 |
|
| 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 |
0.72 |
|
| 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 |
0.369 |
|
| 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 |
0.488 |
|
| 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 |
0.422 |
|
| 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 |
0.456 |
|
| 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 |
0.384 |
|
| 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 |
0.388 |
|
| 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 |
0.516 |
|
| 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 |
0.737 |
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| 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 |
0.74 |
|
| 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 |
0.409 |
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| 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 |
0.761 |
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| 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 |
0.385 |
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| 2013 |
Thompson AJ, Verheij MHP, van Muijlwijk-Koezen JE, Lummis SCR, Leurs R, de Esch IJP. Back Cover: Structure-Activity Relationships of Quinoxaline-Based 5-HT3A and 5-HT3AB Receptor-Selective Ligands (ChemMedChem 6/2013) Chemmedchem. 8: 1020-1020. DOI: 10.1002/Cmdc.201390024 |
0.47 |
|
| 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 |
0.388 |
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| 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 |
0.361 |
|
| 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 |
0.746 |
|
| 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 |
0.715 |
|
| 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 |
0.497 |
|
| 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 |
0.44 |
|
| 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 |
0.348 |
|
| 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 |
0.55 |
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| 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 |
0.498 |
|
| 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 |
0.565 |
|
| 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 |
0.309 |
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| 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 |
0.327 |
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| 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 |
0.751 |
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| 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 |
0.725 |
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| 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 |
0.479 |
|
| 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 |
0.447 |
|
| 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 |
0.31 |
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| 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 |
0.75 |
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| 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 |
0.587 |
|
| 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 |
0.336 |
|
| 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 |
0.784 |
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| 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 |
0.739 |
|
| 2012 |
Langemeijer EV, Slinger E, Munnik Sd, Schreiber A, Maussang D, Vischer H, Verkaar F, Leurs R, Siderius M, Smit MJ. Schematic representation of the classic Wnt signaling pathway and model of US28-mediated activation of ß-catenin signaling pathway. Plos One. DOI: 10.1371/Journal.Pone.0048935.G005 |
0.632 |
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| 2012 |
Leurs R, Vischer HF, Wijtmans M, de Esch IJ. Erratum to “En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family” [Trends Pharmacol. Sci. 32 (4) (2011) 250–257] Trends in Pharmacological Sciences. 33: 49. DOI: 10.1016/J.Tips.2011.10.003 |
0.351 |
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| 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 |
0.761 |
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| 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 |
0.718 |
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| 2012 |
Malan SF, van Marle A, Menge WM, Zuliani V, Hoffman M, Timmerman H, Leurs R. Corrigendum to “Fluorescent ligands for the histamine H2 receptor: Synthesis and preliminary characterization” [Bioorg. Med. Chem. 12 (2004) 6495–6503 Bioorganic & Medicinal Chemistry. 20: 6003. DOI: 10.1016/J.Bmc.2012.03.053 |
0.754 |
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| 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. |
0.387 |
|
| 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 |
0.473 |
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| 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 |
0.421 |
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| 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 |
0.378 |
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| 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 |
0.749 |
|
| 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 |
0.525 |
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| 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 |
0.604 |
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| 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 |
0.449 |
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| 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 |
0.719 |
|
| 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 |
0.53 |
|
| 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 |
0.486 |
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| 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 |
0.341 |
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| 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 |
0.524 |
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| 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 |
0.438 |
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| 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 |
0.839 |
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| 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 |
0.729 |
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| 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 |
0.439 |
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| 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 |
0.708 |
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| 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 |
0.456 |
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| 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 |
0.644 |
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| 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 |
0.345 |
|
| 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 |
0.769 |
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| 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 |
0.676 |
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| 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 |
0.427 |
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| 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 |
0.431 |
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| 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 |
0.741 |
|
| 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 |
0.695 |
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| 2010 |
VAN DER GOOT H, ERIKS JC, LEURS R, TIMMERMAN H. ChemInform Abstract: Amselamine, a New Selective Histamine H2-Receptor Agonist. Cheminform. 26: no-no. DOI: 10.1002/CHIN.199509165 |
0.482 |
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| 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 |
0.584 |
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| 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 |
0.394 |
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| 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 |
0.764 |
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| 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 |
0.763 |
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| 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 |
0.334 |
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| 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 |
0.549 |
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| 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 |
0.412 |
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| 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 |
0.581 |
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| 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 |
0.601 |
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| 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 |
0.634 |
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| 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 |
0.579 |
|
| 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 |
0.725 |
|
| 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 |
0.461 |
|
| 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 |
0.686 |
|
| 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 |
0.705 |
|
| 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 |
0.754 |
|
| 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 |
0.838 |
|
| 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 |
0.737 |
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| 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 |
0.626 |
|
| 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 |
0.601 |
|
| 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 |
0.452 |
|
| 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 |
0.579 |
|
| 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 |
0.81 |
|
| 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 |
0.678 |
|
| 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 |
0.754 |
|
| 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 |
0.512 |
|
| 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 |
0.866 |
|
| 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 |
0.717 |
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| 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 |
0.512 |
|
| 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 |
0.845 |
|
| 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 |
0.857 |
|
| 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 |
0.31 |
|
| 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 |
0.475 |
|
| 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 |
0.477 |
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| 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 |
0.485 |
|
| 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 |
0.46 |
|
| 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 |
0.557 |
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| 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 |
0.856 |
|
| 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 |
0.478 |
|
| 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 |
0.635 |
|
| 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 |
0.753 |
|
| 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 |
0.471 |
|
| 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 |
0.725 |
|
| 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 |
0.466 |
|
| 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 |
0.549 |
|
| 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 |
0.817 |
|
| 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 |
0.705 |
|
| 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 |
0.621 |
|
| 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 |
0.826 |
|
| 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 |
0.695 |
|
| 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 |
0.5 |
|
| 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 |
0.496 |
|
| 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 |
0.737 |
|
| 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 |
0.431 |
|
| 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 |
0.83 |
|
| 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 |
0.73 |
|
| 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 |
0.73 |
|
| 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 |
0.8 |
|
| 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 |
0.755 |
|
| 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 |
0.736 |
|
| 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 |
0.373 |
|
| 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 |
0.592 |
|
| 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 |
0.468 |
|
| 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 |
0.754 |
|
| 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 |
0.739 |
|
| 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 |
0.487 |
|
| 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 |
0.689 |
|
| 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 |
0.535 |
|
| 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 |
0.523 |
|
| 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 |
0.55 |
|
| 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 |
0.808 |
|
| 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 |
0.84 |
|
| 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 |
0.749 |
|
| 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 |
0.598 |
|
| 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 |
0.722 |
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| 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 |
0.457 |
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| 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 |
0.672 |
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| 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 |
0.818 |
|
| 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 |
0.72 |
|
| 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 |
0.83 |
|
| 2004 |
Klaasse E, de Ligt RA, Roerink SF, Lorenzen A, Milligan G, Leurs R, IJzerman AP. Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits. European Journal of Pharmacology. 499: 91-8. PMID 15363955 DOI: 10.1016/J.Ejphar.2004.07.108 |
0.52 |
|
| 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 |
0.553 |
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| 2004 |
Ratnala VR, Swarts HG, VanOostrum J, Leurs R, DeGroot HJ, Bakker RA, DeGrip WJ. Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor. European Journal of Biochemistry. 271: 2636-46. PMID 15206929 DOI: 10.1111/J.1432-1033.2004.04192.X |
0.522 |
|
| 2004 |
Bakker RA, Dees G, Carrillo JJ, Booth RG, López-Gimenez JF, Milligan G, Strange PG, Leurs R. Domain swapping in the human histamine H1 receptor. The Journal of Pharmacology and Experimental Therapeutics. 311: 131-8. PMID 15159444 DOI: 10.1124/jpet.104.067041 |
0.539 |
|
| 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 |
0.773 |
|
| 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 |
0.599 |
|
| 2004 |
Poli E, Menozzi A, Pozzoli C, Coruzzi G, Kitbunnadaj R, Timmerman H, Leurs R. Functional characterisation of the novel histamine H3 receptor agonist, VUF 5810, on the guinea-pig isolated ileum Inflammation Research. 53: S77-S78. PMID 15054628 DOI: 10.1007/S00011-003-0337-Y |
0.755 |
|
| 2004 |
Gruijthuijsen YK, Beuken EV, Smit MJ, Leurs R, Bruggeman CA, Vink C. Mutational analysis of the R33-encoded G protein-coupled receptor of rat cytomegalovirus: identification of amino acid residues critical for cellular localization and ligand-independent signalling. The Journal of General Virology. 85: 897-909. PMID 15039532 DOI: 10.1099/Vir.0.19709-0 |
0.712 |
|
| 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 |
0.758 |
|
| 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 |
0.804 |
|
| 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 |
0.72 |
|
| 2004 |
Hensbergen PJ, Verzijl D, Balog CI, Dijkman R, van der Schors RC, van der Raaij-Helmer EM, van der Plas MJ, Leurs R, Deelder AM, Smit MJ, Tensen CP. Furin is a chemokine-modifying enzyme: in vitro and in vivo processing of CXCL10 generates a C-terminally truncated chemokine retaining full activity. The Journal of Biological Chemistry. 279: 13402-11. PMID 14739277 DOI: 10.1074/Jbc.M312814200 |
0.678 |
|
| 2004 |
Bongers G, Leurs R, Robertson J, Raber J. Role of H3-receptor-mediated signaling in anxiety and cognition in wild-type and Apoe-/- mice. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 29: 441-9. PMID 14628000 DOI: 10.1038/Sj.Npp.1300352 |
0.333 |
|
| 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 |
0.823 |
|
| 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 |
0.697 |
|
| 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 |
0.848 |
|
| 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 |
0.605 |
|
| 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 |
0.779 |
|
| 2003 |
Casarosa P, Gruijthuijsen YK, Michel D, Beisser PS, Holl J, Fitzsimons CP, Verzijl D, Bruggeman CA, Mertens T, Leurs R, Vink C, Smit MJ. Constitutive signaling of the human cytomegalovirus-encoded receptor UL33 differs from that of its rat cytomegalovirus homolog R33 by promiscuous activation of G proteins of the Gq, Gi, and Gs classes. The Journal of Biological Chemistry. 278: 50010-23. PMID 14522997 DOI: 10.1074/jbc.M306530200 |
0.7 |
|
| 2003 |
Sallmen T, Lozada AF, Anichtchik OV, Beckman AL, Leurs R, Panula P. Changes in hippocampal histamine receptors across the hibernation cycle in ground squirrels. Hippocampus. 13: 745-54. PMID 12962318 DOI: 10.1002/hipo.10120 |
0.497 |
|
| 2003 |
Hashimoto T, Harusawa S, Araki L, Zuiderveld OP, Smit MJ, Imazu T, Takashima S, Yamamoto Y, Sakamoto Y, Kurihara T, Leurs R, Bakker RA, Yamatodani A. A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine. Journal of Medicinal Chemistry. 46: 3162-5. PMID 12825954 DOI: 10.1021/Jm0300025 |
0.774 |
|
| 2003 |
Smit MJ, Vink C, Verzijl D, Casarosa P, Bruggeman CA, Leurs R. Virally encoded G protein-coupled receptors: targets for potentially innovative anti-viral drug development. Current Drug Targets. 4: 431-41. PMID 12816350 |
0.72 |
|
| 2003 |
Smit MJ, Verdijk P, van der Raaij-Helmer EM, Navis M, Hensbergen PJ, Leurs R, Tensen CP. CXCR3-mediated chemotaxis of human T cells is regulated by a Gi- and phospholipase C-dependent pathway and not via activation of MEK/p44/p42 MAPK nor Akt/PI-3 kinase. Blood. 102: 1959-65. PMID 12750173 DOI: 10.1182/Blood-2002-12-3945 |
0.662 |
|
| 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 |
0.731 |
|
| 2003 |
Waldhoer M, Casarosa P, Rosenkilde MM, Smit MJ, Leurs R, Whistler JL, Schwartz TW. The carboxyl terminus of human cytomegalovirus-encoded 7 transmembrane receptor US28 camouflages agonism by mediating constitutive endocytosis. The Journal of Biological Chemistry. 278: 19473-82. PMID 12646575 DOI: 10.1074/Jbc.M213179200 |
0.82 |
|
| 2003 |
Blomenröhr M, Bogerd J, Leurs R, Goos H. Differences in structure-function relations between nonmammalian and mammalian GnRH receptors: what we have learnt from the African catfish GnRH receptor. Progress in Brain Research. 141: 87-93. PMID 12508563 DOI: 10.1016/S0079-6123(02)41086-2 |
0.546 |
|
| 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 |
0.828 |
|
| 2003 |
Leurs R, Bakker RA, Casarosa P, Verzijl D, Timmerman H, Smit MJ. Modulation of constitutive GPCR activity: a way of life? International Congress Series. 1249: 131-138. DOI: 10.1016/S0531-5131(03)00608-3 |
0.619 |
|
| 2002 |
Bogerd J, Diepenbroek WB, Hund E, van Oosterhout F, Teves AC, Leurs R, Blomenröhr M. Two gonadotropin-releasing hormone receptors in the African catfish: no differences in ligand selectivity, but differences in tissue distribution. Endocrinology. 143: 4673-82. PMID 12446595 DOI: 10.1210/En.2002-220578 |
0.39 |
|
| 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 |
0.711 |
|
| 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 DOI: 10.3109/9780203910375-7 |
0.784 |
|
| 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 |
0.752 |
|
| 2002 |
Leurs R, Church MK, Taglialatela M. H1-antihistamines: Inverse agonism, anti-inflammatory actions and cardiac effects Clinical and Experimental Allergy. 32: 489-498. PMID 11972592 DOI: 10.1046/j.0954-7894.2002.01314.x |
0.547 |
|
| 2002 |
Blomenröhr M, ter Laak T, Kühne R, Beyermann M, Hund E, Bogerd J, Leurs R. Chimaeric gonadotropin-releasing hormone (GnRH) peptides with improved affinity for the catfish (Clarias gariepinus) GnRH receptor. The Biochemical Journal. 361: 515-23. PMID 11802781 DOI: 10.1042/0264-6021:3610515 |
0.466 |
|
| 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 |
0.779 |
|
| 2002 |
Gruijthuijsen YK, Casarosa P, Kaptein SJ, Broers JL, Leurs R, Bruggeman CA, Smit MJ, Vink C. The rat cytomegalovirus R33-encoded G protein-coupled receptor signals in a constitutive fashion. Journal of Virology. 76: 1328-38. PMID 11773407 DOI: 10.1128/Jvi.76.3.1328-1338.2002 |
0.718 |
|
| 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 |
0.847 |
|
| 2001 |
Svokos K, Nalwalk JW, Leurs R, Menge WM, Timmerman H, Hough LB. A role for spinal, but not supraspinal, alpha(2) adrenergic receptors in the actions of improgan, a powerful, non-opioid analgesic. Brain Research. 923: 12-9. PMID 11743967 DOI: 10.1016/S0006-8993(01)03191-2 |
0.676 |
|
| 2001 |
Bakker RA, Schoonus SB, Smit MJ, Timmerman H, Leurs R. Histamine H(1)-receptor activation of nuclear factor-kappa B: roles for G beta gamma- and G alpha(q/11)-subunits in constitutive and agonist-mediated signaling. Molecular Pharmacology. 60: 1133-42. PMID 11641442 DOI: 10.1124/Mol.60.5.1133 |
0.809 |
|
| 2001 |
Alves-Rodrigues A, Lemstra S, Vollinga RC, Menge WM, Timmerman H, Leurs R. Pharmacological analysis of immepip and imetit homologues. Further evidence for histamine H(3) receptor heterogeneity? Behavioural Brain Research. 124: 121-7. PMID 11640964 DOI: 10.1016/S0166-4328(01)00224-8 |
0.743 |
|
| 2001 |
Vink C, Smit MJ, Leurs R, Bruggeman CA. The role of cytomegalovirus-encoded homologs of G protein-coupled receptors and chemokines in manipulation of and evasion from the immune system. Journal of Clinical Virology : the Official Publication of the Pan American Society For Clinical Virology. 23: 43-55. PMID 11595583 DOI: 10.1016/S1386-6532(01)00184-6 |
0.692 |
|
| 2001 |
Hoffmann M, Verzijl D, Lundstrom K, Simmen U, Alewijnse AE, Timmerman H, Leurs R. Recombinant Semliki Forest virus for over-expression and pharmacological characterisation of the histamine H(2) receptor in mammalian cells. European Journal of Pharmacology. 427: 105-14. PMID 11557261 DOI: 10.1016/S0014-2999(01)01264-X |
0.732 |
|
| 2001 |
Blomenröhr M, Kühne R, Hund E, Leurs R, Bogerd J, ter Laak T. Proper receptor signalling in a mutant catfish gonadotropin-releasing hormone receptor lacking the highly conserved Asp(90) residue. Febs Letters. 501: 131-4. PMID 11470271 DOI: 10.1016/S0014-5793(01)02647-3 |
0.52 |
|
| 2001 |
Hough LB, Nalwalk JW, Leurs R, Menge WM, Timmerman H. Significance of GABAergic systems in the action of improgan, a non-opioid analgesic. Life Sciences. 68: 2751-7. PMID 11400917 DOI: 10.1016/S0024-3205(01)01080-3 |
0.632 |
|
| 2001 |
De Esch IJ, Mills JE, Perkins TD, Romeo G, Hoffmann M, Wieland K, Leurs R, Menge WM, Nederkoorn PH, Dean PM, Timmerman H. Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE. Journal of Medicinal Chemistry. 44: 1666-74. PMID 11356102 DOI: 10.1021/Jm001109K |
0.693 |
|
| 2001 |
Lintunen M, Hyytiä P, Sallmen T, Karlstedt K, Tuomisto L, Leurs R, Kiianmaa K, Korpi ER, Panula P. Increased brain histamine in an alcohol-preferring rat line and modulation of ethanol consumption by H(3) receptor mechanisms. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 15: 1074-6. PMID 11292672 DOI: 10.1096/Fj.00-0545Fje |
0.343 |
|
| 2001 |
Drutel G, Peitsaro N, Karlstedt K, Wieland K, Smit MJ, Timmerman H, Panula P, Leurs R. Identification of rat H3 receptor isoforms with different brain expression and signaling properties. Molecular Pharmacology. 59: 1-8. PMID 11125017 DOI: 10.1124/Mol.59.1.1 |
0.86 |
|
| 2001 |
Casarosa P, Bakker RA, Verzijl D, Navis M, Timmerman H, Leurs R, Smit MJ. Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28. The Journal of Biological Chemistry. 276: 1133-7. PMID 11050102 DOI: 10.1074/Jbc.M008965200 |
0.82 |
|
| 2001 |
Leurs R, Watanabe T, Timmerman H. Histamine receptors are finally 'coming out' Trends in Pharmacological Sciences. 22: 337-339. DOI: 10.1016/S0165-6147(00)01691-6 |
0.683 |
|
| 2000 |
Rodriguez-Pena MS, Timmerman H, Leurs R. Modulation of histamine H(2) receptor signalling by G-protein-coupled receptor kinase 2 and 3. British Journal of Pharmacology. 131: 1707-15. PMID 11139450 DOI: 10.1038/Sj.Bjp.0703676 |
0.778 |
|
| 2000 |
Hough LB, Nalwalk JW, Chen Y, Schuller A, Zhu Y, Zhang J, Menge WM, Leurs R, Timmerman H, Pintar JE. Improgan, a cimetidine analog, induces morphine-like antinociception in opioid receptor-knockout mice. Brain Research. 880: 102-8. PMID 11032994 DOI: 10.1016/S0006-8993(00)02776-1 |
0.664 |
|
| 2000 |
Jansen FP, Mochizuki T, Maeyama K, Leurs R, Timmerman H. Characterization of histamine H3 receptors in mouse brain using the H3 antagonist [125I]iodophenpropit. Naunyn-Schmiedeberg's Archives of Pharmacology. 362: 60-7. PMID 10935534 DOI: 10.1007/S002100000227 |
0.728 |
|
| 2000 |
Hough LB, Nalwalk JW, Barnes WG, Leurs R, Menge WM, Timmerman H, Wentland M. A third life for burimamide. Discovery and characterization of a novel class of non-opioid analgesics derived from histamine antagonists. Annals of the New York Academy of Sciences. 909: 25-40. PMID 10911922 DOI: 10.1111/J.1749-6632.2000.Tb06674.X |
0.688 |
|
| 2000 |
Leurs R, Rodriguez Pena MS, Bakker RA, Alewijnse AE, Timmerman H. Constitutive activity of G protein coupled receptors and drug action. Pharmaceutica Acta Helvetiae. 74: 327-31. PMID 10812977 DOI: 10.1016/S0031-6865(99)00042-4 |
0.769 |
|
| 2000 |
Smit MJ, Timmerman H, Verzijl D, Leurs R. Viral-encoded G-protein coupled receptors: new targets for drug research? Pharmaceutica Acta Helvetiae. 74: 299-304. PMID 10812973 DOI: 10.1016/S0031-6865(99)00039-4 |
0.791 |
|
| 2000 |
Windhorst AD, Timmerman H, Worthington EA, Bijloo GJ, Nederkoorn PH, Menge WM, Leurs R, Herscheid JD. Characterization of the binding site of the histamine H(3) receptor. 2. Synthesis, in vitro pharmacology, and QSAR of a series of monosubstituted benzyl analogues of thioperamide. Journal of Medicinal Chemistry. 43: 1754-61. PMID 10794692 DOI: 10.1021/Jm981106W |
0.702 |
|
| 2000 |
Hough LB, Nalwalk JW, Leurs R, Menge WM, Timmerman H. Antinociceptive activity of derivatives of improgran and burimamide. Pharmacology, Biochemistry, and Behavior. 65: 61-6. PMID 10638637 DOI: 10.1016/S0091-3057(99)00187-2 |
0.647 |
|
| 2000 |
Leurs R, Hoffmann M, Wieland K, Timmerman H. H3 receptor gene is cloned at last. Trends in Pharmacological Sciences. 21: 11-2. PMID 10637648 DOI: 10.1016/S0165-6147(99)01411-X |
0.739 |
|
| 2000 |
Bakker RA, Wieland K, Timmerman H, Leurs R. Constitutive activity of the histamine H(1) receptor reveals inverse agonism of histamine H(1) receptor antagonists. European Journal of Pharmacology. 387: R5-7. PMID 10633171 DOI: 10.1016/S0014-2999(99)00803-1 |
0.788 |
|
| 1999 |
Windhorst AD, Timmerman H, Klok RP, Custers FG, Menge WM, Leurs R, Stark H, Schunack W, Gielen EG, van Kroonenburgh MJ, Herscheid JD. Radiosynthesis and biodistribution of 123I-labeled antagonists of the histamine H3 receptor as potential SPECT ligands. Nuclear Medicine and Biology. 26: 651-9. PMID 10587103 DOI: 10.1016/S0969-8051(99)00014-1 |
0.747 |
|
| 1999 |
Blomenröhr M, Heding A, Sellar R, Leurs R, Bogerd J, Eidne KA, Willars GB. Pivotal role for the cytoplasmic carboxyl-terminal tail of a nonmammalian gonadotropin-releasing hormone receptor in cell surface expression, ligand binding, and receptor phosphorylation and internalization. Molecular Pharmacology. 56: 1229-37. PMID 10570050 DOI: 10.1124/MOL.56.6.1229 |
0.454 |
|
| 1999 |
Windhorst AD, Timmerman H, Klok RP, Menge WM, Leurs R, Herscheid JD. Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor. Bioorganic & Medicinal Chemistry. 7: 1761-7. PMID 10530922 DOI: 10.1016/S0968-0896(99)00108-X |
0.637 |
|
| 1999 |
Wieland K, Laak AM, Smit MJ, Kühne R, Timmerman H, Leurs R. Mutational analysis of the antagonist-binding site of the histamine H(1) receptor. The Journal of Biological Chemistry. 274: 29994-30000. PMID 10514483 DOI: 10.1074/Jbc.274.42.29994 |
0.839 |
|
| 1999 |
Smit MJ, Hoffmann M, Timmerman H, Leurs R. Molecular properties and signalling pathways of the histamine H1 receptor. Clinical and Experimental Allergy : Journal of the British Society For Allergy and Clinical Immunology. 29: 19-28. PMID 10444208 |
0.85 |
|
| 1999 |
Tensen CP, Flier J, Van Der Raaij-Helmer EM, Sampat-Sardjoepersad S, Van Der Schors RC, Leurs R, Scheper RJ, Boorsma DM, Willemze R. Human IP-9: A keratinocyte-derived high affinity CXC-chemokine ligand for the IP-10/Mig receptor (CXCR3). The Journal of Investigative Dermatology. 112: 716-22. PMID 10233762 DOI: 10.1046/J.1523-1747.1999.00581.X |
0.452 |
|
| 1999 |
De Esch IJ, Vollinga RC, Goubitz K, Schenk H, Appelberg U, Hacksell U, Lemstra S, Zuiderveld OP, Hoffmann M, Leurs R, Menge WM, Timmerman H. Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine. Journal of Medicinal Chemistry. 42: 1115-22. PMID 10197956 DOI: 10.1021/Jm9810912 |
0.714 |
|
| 1999 |
Hough LB, Nalwalk JW, Leurs R, Menge WM, Timmerman H. Antinociceptive activity of impentamine, a histamine congener, after CNS administration. Life Sciences. 64: PL79-86. PMID 10072195 DOI: 10.1016/S0024-3205(98)00571-2 |
0.736 |
|
| 1999 |
Leurs R, Blandina P, Tedford C, Timmerman H. Therapeutic potential of histamine H3 receptor agonists and antagonists. Trends in Pharmacological Sciences. 19: 177-83. PMID 9652190 DOI: 10.1016/S0165-6147(98)01201-2 |
0.78 |
|
| 1999 |
Smit MJ, Hoffmann M, Timmerman H, Leurs R. Molecular properties and signalling pathways of the histamine H1
receptor Clinical & Experimental Allergy. 29: 19-28. DOI: 10.1046/J.1365-2222.1999.00007.X-I1 |
0.858 |
|
| 1999 |
Windhorst AD, Timmerman H, Menge WMPB, Leurs R, Herscheid JDM. Synthesis,in vitro pharmacology and radiosynthesis ofN-(cis-4-fluoromethylcycloyhexyl)-4-(1(H)-imidazol-4-yl)piperidine-11-thiocarbonamide (VUF 5000), a potential PET ligand for the histamine H3 receptor Journal of Labelled Compounds and Radiopharmaceuticals. 42: 293-307. DOI: 10.1002/(Sici)1099-1344(199903)42:3<293::Aid-Jlcr191>3.0.Co;2-B |
0.682 |
|
| 1998 |
Leurs R, Smit MJ, Alewijnse AE, Timmerman H. Agonist-independent regulation of constitutively active G-protein-coupled receptors. Trends in Biochemical Sciences. 23: 418-22. PMID 9852759 DOI: 10.1016/S0968-0004(98)01287-0 |
0.818 |
|
| 1998 |
Bannoura MD, Nalwalk JW, Tang Y, Carlile M, Leurs R, Menge WM, Timmerman H, Hough LB. Absence of antinociceptive tolerance to improgan, a cimetidine analog, in rats. Brain Research. 814: 218-21. PMID 9838126 DOI: 10.1016/S0006-8993(98)01024-5 |
0.628 |
|
| 1998 |
Tensen CP, Cox KJ, Burke JF, Leurs R, van der Schors RC, Geraerts WP, Vreugdenhil E, Heerikhuizen H. Molecular cloning and characterization of an invertebrate homologue of a neuropeptide Y receptor. The European Journal of Neuroscience. 10: 3409-16. PMID 9824454 DOI: 10.1046/J.1460-9568.1998.00350.X |
0.44 |
|
| 1998 |
Alewijnse AE, Smit MJ, Hoffmann M, Verzijl D, Timmerman H, Leurs R. Constitutive activity and structural instability of the wild-type human H2 receptor. Journal of Neurochemistry. 71: 799-807. PMID 9681472 DOI: 10.1046/J.1471-4159.1998.71020799.X |
0.864 |
|
| 1998 |
Smit MJ, Timmerman H, Alewijnse AE, Leurs R. From histamine H2 receptor regulation to reclassification of H2 antagonists; inverse agonism as the basis for H2 receptor upregulation. Receptors & Channels. 5: 99-102. PMID 9606714 |
0.844 |
|
| 1998 |
Alves-Rodrigues A, Timmerman H, Willems E, Lemstra S, Zuiderveld OP, Leurs R. Pharmacological characterisation of the histamine H3 receptor in the rat hippocampus Brain Research. 788: 179-186. PMID 9555002 DOI: 10.1016/S0006-8993(97)01537-0 |
0.756 |
|
| 1998 |
Windhorst AD, Leurs R, Menge WMPB, Timmerman H, Herscheid JDM. Synthesis of radioligands for the histamine H3 receptor Pharmacochemistry Library. 30: 159-174. DOI: 10.1016/S0165-7208(98)80029-9 |
0.763 |
|
| 1998 |
Jansen FP, Leurs R, Timmerman H. Radioligands for the histamine H3 receptor and their use in pharmacology Pharmacochemistry Library. 30: 127-144. DOI: 10.1016/S0165-7208(98)80027-5 |
0.791 |
|
| 1998 |
Hoffmann M, Timmermann H, Leurs R. Biochemical properties of the histamine H3 receptor Pharmacochemistry Library. 30: 113-126. DOI: 10.1016/S0165-7208(98)80026-3 |
0.613 |
|
| 1997 |
Alewijnse AE, Smit MJ, Rodriguez Pena MS, Verzijl D, Timmerman H, Leurs R. Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active G(S)-coupled receptors. Febs Letters. 419: 171-4. PMID 9428628 DOI: 10.1016/S0014-5793(97)01440-3 |
0.85 |
|
| 1997 |
Beukers MW, Klaassen CH, De Grip WJ, Verzijl D, Timmerman H, Leurs R. Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells. British Journal of Pharmacology. 122: 867-74. PMID 9384502 DOI: 10.1038/Sj.Bjp.0701466 |
0.755 |
|
| 1997 |
Blomenröhr M, Bogerd J, Leurs R, Schulz RW, Tensen CP, Zandbergen MA, Goos HJ. Differences in structure-function relations between nonmammalian and mammalian gonadotropin-releasing hormone receptors. Biochemical and Biophysical Research Communications. 238: 517-22. PMID 9299543 DOI: 10.1006/BBRC.1997.7331 |
0.31 |
|
| 1997 |
Kuipers W, Link R, Standaar PJ, Stoit AR, Van Wijngaarden I, Leurs R, Ijzerman AP. Study of the interaction between aryloxypropanolamines and Asn386 in helix VII of the human 5-hydroxytryptamine1A receptor. Molecular Pharmacology. 51: 889-96. PMID 9145928 DOI: 10.1124/mol.51.5.889 |
0.575 |
|
| 1997 |
Tensen C, Okuzawa K, Blomenröhr M, Rebers F, Leurs R, Bogerd J, Schulz R, Goos H. Distinct efficacies for two endogenous ligands on a single cognate gonadoliberin receptor. European Journal of Biochemistry. 243: 134-40. PMID 9030732 DOI: 10.1111/J.1432-1033.1997.0134A.X |
0.364 |
|
| 1997 |
Mochizuki T, Jansen FP, Leurs R, Windhorst AD, Yamatodani A, Maeyama K, Timmerman H. Brain penetration of the histamine H3 receptor antagonists thioperamide and clobenpropit in rat and mouse, determined with ex vivo [125I]iodophenpropit binding. Brain Research. 743: 178-83. PMID 9017245 DOI: 10.1016/S0006-8993(96)01040-2 |
0.459 |
|
| 1997 |
Alves-Rodrigues A, Leurs R, Wu TS, Prell GD, Foged C, Timmerman H. [3H]-thioperamide as a radioligand for the histamine H3 receptor in rat cerebral cortex. British Journal of Pharmacology. 118: 2045-52. PMID 8864541 DOI: 10.1111/J.1476-5381.1996.Tb15642.X |
0.725 |
|
| 1996 |
Blandina P, Giorgetti M, Bartolini L, Cecchi M, Timmerman H, Leurs R, Pepeu G, Giovannini MG. Inhibition of cortical acetylcholine release and cognitive performance by histamine H3 receptor activation in rats. British Journal of Pharmacology. 119: 1656-64. PMID 8982515 DOI: 10.1111/J.1476-5381.1996.Tb16086.X |
0.705 |
|
| 1996 |
Alves-Rodrigues A, Leurs R, Willems E, Timmerman H. Binding of clozapine metabolites and analogues to the histamine H3 receptor in rat brain cortex. Archiv Der Pharmazie. 329: 413-6. PMID 8915103 DOI: 10.1002/Ardp.19963290808 |
0.752 |
|
| 1996 |
Smit MJ, Timmerman H, Hijzelendoorn JC, Fukui H, Leurs R. Regulation of the human histamine H1 receptor stably expressed in Chinese hamster ovary cells. British Journal of Pharmacology. 117: 1071-80. PMID 8882599 DOI: 10.1111/J.1476-5381.1996.Tb16699.X |
0.813 |
|
| 1996 |
Smit MJ, Timmerman H, Blauw J, Beukers MW, Roovers E, Jacobs EH, Hoffmann M, Leurs R. The C terminal tail of the histamine H2 receptor contains positive and negative signals important for signal transduction and receptor down-regulation. Journal of Neurochemistry. 67: 1791-800. PMID 8863482 DOI: 10.1046/J.1471-4159.1996.67051791.X |
0.84 |
|
| 1996 |
Blandina P, Giorgetti M, Cecchi M, Leurs R, Timmerman H, Giovannini MG. Histamine H3 receptor inhibition of K(+)-evoked release of acetylcholine from rat cortex in vivo. Inflammation Research : Official Journal of the European Histamine Research Society ... [Et Al.]. S54-5. PMID 8696930 DOI: 10.1007/Bf03354086 |
0.685 |
|
| 1996 |
Smit MJ, Leurs R, Alewijnse AE, Blauw J, Van Nieuw Amerongen GP, Van De Vrede Y, Roovers E, Timmerman H. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proceedings of the National Academy of Sciences of the United States of America. 93: 6802-7. PMID 8692899 DOI: 10.1073/Pnas.93.13.6802 |
0.857 |
|
| 1996 |
Smit MJ, Roovers E, Timmerman H, van de Vrede Y, Alewijnse AE, Leurs R. Two distinct pathways for histamine H2 receptor down-regulation. H2 Leu124 --> Ala receptor mutant provides evidence for a cAMP-independent action of H2 agonists. The Journal of Biological Chemistry. 271: 7574-82. PMID 8631790 DOI: 10.1074/Jbc.271.13.7574 |
0.859 |
|
| 1996 |
Leurs R, Tulp MT, Menge WM, Adolfs MJ, Zuiderveld OP, Timmerman H. Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed. British Journal of Pharmacology. 116: 2315-21. PMID 8564266 DOI: 10.1111/J.1476-5381.1995.Tb15071.X |
0.749 |
|
| 1996 |
Leurs R, Vollinga RC, Timmerman H. The medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor. Progress in Drug Research. Fortschritte Der Arzneimittelforschung. Progres Des Recherches Pharmaceutiques. 45: 107-65. PMID 8545536 DOI: 10.1007/978-3-0348-7164-8_4 |
0.642 |
|
| 1996 |
Leurs R, Timmerman H. New histamine H3 receptor ligands as pharmacological tools Pharmacochemistry Library. 24: 193-204. DOI: 10.1016/S0165-7208(96)80016-X |
0.771 |
|
| 1996 |
Windhorst A, Bechger L, Visser G, Menge W, Leurs R, Timmerman H, Herscheid J. Approaches towards the synthesis of fluoro(cyclo)alkylamines Journal of Fluorine Chemistry. 80: 35-40. DOI: 10.1016/S0022-1139(96)03457-4 |
0.503 |
|
| 1995 |
ter Laak AM, Timmerman H, Leurs R, Nederkoorn PH, Smit MJ, Donné-Op den Kelder GM. Modelling and mutation studies on the histamine H1-receptor agonist binding site reveal different binding modes for H1-agonists: Asp116 (TM3) has a constitutive role in receptor stimulation. Journal of Computer-Aided Molecular Design. 9: 319-30. PMID 8523041 DOI: 10.1007/Bf00125173 |
0.848 |
|
| 1995 |
Vollinga RC, Menge WM, Leurs R, Timmerman H. Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole. Journal of Medicinal Chemistry. 38: 266-71. PMID 7830269 DOI: 10.1021/Jm00002A008 |
0.757 |
|
| 1995 |
Vollinga RC, Menge WM, Leurs R, Timmerman H. New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent. Journal of Medicinal Chemistry. 38: 2244-50. PMID 7783156 DOI: 10.1021/Jm00012A025 |
0.708 |
|
| 1995 |
Leurs R, Smit MJ, Meeder R, Ter Laak AM, Timmerman H. Lysine200 located in the fifth transmembrane domain of the histamine H1 receptor interacts with histamine but not with all H1 agonists. Biochemical and Biophysical Research Communications. 214: 110-7. PMID 7669031 DOI: 10.1006/Bbrc.1995.2263 |
0.856 |
|
| 1995 |
Smit MJ, Timmerman H, Alewijnse AE, Punin M, van den Nieuwenhof I, Blauw J, van Minnen J, Leurs R. Visualization of agonist-induced internalization of histamine H2 receptors. Biochemical and Biophysical Research Communications. 214: 1138-45. PMID 7575521 DOI: 10.1006/Bbrc.1995.2404 |
0.853 |
|
| 1995 |
Rodrigues AA, Jansen FP, Leurs R, Timmerman H, Prell GD. Interaction of clozapine with the histamine H3 receptor in rat brain. British Journal of Pharmacology. 114: 1523-4. PMID 7541279 DOI: 10.1111/J.1476-5381.1995.Tb14934.X |
0.741 |
|
| 1995 |
Leurs R, Smit MJ, Timmerman H. Molecular pharmacological aspects of histamine receptors. Pharmacology & Therapeutics. 66: 413-63. PMID 7494855 DOI: 10.1016/0163-7258(95)00006-3 |
0.847 |
|
| 1995 |
LEURS R, KATHMANN M, VOLLINGA R, MENGE W, SCHLICKER E, TIMMERMAN H. The histamine analogue impentamine discriminates between peripheral and brain histamine H3 receptors Pharmacological Research. 31: 272-272. DOI: 10.1016/1043-6618(95)87347-3 |
0.522 |
|
| 1995 |
Jansen FP, Mochizuki T, Macyama K, Leurs R, Timmerman H. Characterization of histamine H3-receptors in mouse brain using the H3-antagonist [125I]-iodophenpropit Pharmacological Research. 31: 271-271. DOI: 10.1016/1043-6618(95)87343-0 |
0.547 |
|
| 1994 |
Vollinga RC, de Koning JP, Jansen FP, Leurs R, Menge WM, Timmerman H. A new potent and selective histamine H3 receptor agonist, 4-(1H-imidazol-4-ylmethyl)piperidine. Journal of Medicinal Chemistry. 37: 332-3. PMID 8308858 DOI: 10.1021/Jm00029A002 |
0.733 |
|
| 1994 |
Leurs R, Traiffort E, Arrang JM, Tardivel-Lacombe J, Ruat M, Schwartz JC. Guinea pig histamine H1 receptor. II. Stable expression in Chinese hamster ovary cells reveals the interaction with three major signal transduction pathways. Journal of Neurochemistry. 62: 519-27. PMID 8294914 DOI: 10.1046/J.1471-4159.1994.62020519.X |
0.373 |
|
| 1994 |
Traiffort E, Leurs R, Arrang JM, Tardivel-Lacombe J, Diaz J, Schwartz JC, Ruat M. Guinea pig histamine H1 receptor. I. Gene cloning, characterization, and tissue expression revealed by in situ hybridization. Journal of Neurochemistry. 62: 507-18. PMID 8294913 DOI: 10.1046/J.1471-4159.1994.62020507.X |
0.505 |
|
| 1994 |
Leurs R, Smit MJ, Tensen CP, Ter Laak AM, Timmerman H. Site-directed mutagenesis of the histamine H1-receptor reveals a selective interaction of asparagine207 with subclasses of H1-receptor agonists. Biochemical and Biophysical Research Communications. 201: 295-301. PMID 8198587 DOI: 10.1006/Bbrc.1994.1701 |
0.856 |
|
| 1994 |
Yokoyama H, Onodera K, Maeyama K, Sakurai E, Iinuma K, Leurs R, Timmerman H, Watanabe T. Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. European Journal of Pharmacology. 260: 23-8. PMID 7957622 DOI: 10.1016/0014-2999(94)90005-1 |
0.746 |
|
| 1994 |
Leurs R, Smit MJ, Menge WM, Timmerman H. Pharmacological characterization of the human histamine H2 receptor stably expressed in Chinese hamster ovary cells. British Journal of Pharmacology. 112: 847-54. PMID 7921611 DOI: 10.1111/J.1476-5381.1994.Tb13157.X |
0.854 |
|
| 1994 |
Smit MJ, Leurs R, Shukrula SR, Bast A, Timmerman H. Rapid desensitization of the histamine H2 receptor on the human monocytic cell line U937. European Journal of Pharmacology. 288: 17-25. PMID 7705464 DOI: 10.1016/0922-4106(94)90005-1 |
0.86 |
|
| 1994 |
van der Goot H, Eriks JC, Leurs R, Timmerman H. Amselamine, a new selective histamine H2-receptor agonist Bioorganic & Medicinal Chemistry Letters. 4: 1913-1916. DOI: 10.1016/S0960-894X(01)80533-3 |
0.57 |
|
| 1993 |
Bloemers SM, Leurs R, Smit MJ, Verheule S, Tertoolen LG, Timmerman H, de Laat SW. Mouse P19 embryonal carcinoma cells express functional histamine H1-receptors. Biochemical and Biophysical Research Communications. 191: 118-25. PMID 8447817 DOI: 10.1006/Bbrc.1993.1192 |
0.818 |
|
| 1993 |
Ruat M, Traiffort E, Leurs R, Tardivel-Lacombe J, Diaz J, Arrang JM, Schwartz JC. Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. Proceedings of the National Academy of Sciences of the United States of America. 90: 8547-51. PMID 8397408 DOI: 10.1073/Pnas.90.18.8547 |
0.383 |
|
| 1993 |
Smit MJ, Leurs R, Bloemers SM, Tertoolen LG, Bast A, De Laat SW, Timmerman H. Extracellular ATP elevates cytoplasmatic free Ca2+ in HeLa cells by the interaction with a 5'-nucleotide receptor. European Journal of Pharmacology. 247: 223-6. PMID 8282011 DOI: 10.1016/0922-4106(93)90082-K |
0.757 |
|
| 1993 |
Leurs R, Timmerman H. The histamine H3-receptor: a target for developing new drugs. Progress in Drug Research. Fortschritte Der Arzneimittelforschung. Progres Des Recherches Pharmaceutiques. 39: 127-65. PMID 1335582 DOI: 10.1007/978-3-0348-7144-0_4 |
0.396 |
|
| 1992 |
Smit MJ, Bloemers SM, Leurs R, Tertoolen LG, Bast A, de Laat SW, Timmerman H. Short-term desensitization of the histamine H1 receptor in human HeLa cells: involvement of protein kinase C dependent and independent pathways. British Journal of Pharmacology. 107: 448-55. PMID 1422591 DOI: 10.1111/J.1476-5381.1992.Tb12766.X |
0.78 |
|
| 1992 |
Traiffort E, Ruat M, Arrang JM, Leurs R, Piomelli D, Schwartz JC. Expression of a cloned rat histamine H2 receptor mediating inhibition of arachidonate release and activation of cAMP accumulation. Proceedings of the National Academy of Sciences of the United States of America. 89: 2649-53. PMID 1313563 DOI: 10.1073/Pnas.89.7.2649 |
0.607 |
|
| 1992 |
Leurs R, Brozius MM, Jansen W, Bast A, Timmerman H. Desensitization of histamine H1 receptor-mediated cyclic GMP production in guinea-pig lung. European Journal of Pharmacology. 225: 137-41. PMID 1312939 DOI: 10.1016/0922-4106(92)90093-B |
0.57 |
|
| 1991 |
Leurs R, Smit MJ, Bast A, Timmerman H. Different profiles of desensitization dynamics in guinea-pig jejunal longitudinal smooth muscle after stimulation with histamine and methacholine. British Journal of Pharmacology. 101: 881-8. PMID 2085711 DOI: 10.1111/J.1476-5381.1990.Tb14175.X |
0.784 |
|
| 1991 |
Ruat M, Traiffort E, Arrang JM, Leurs R, Schwartz JC. Cloning and tissue expression of a rat histamine H2-receptor gene. Biochemical and Biophysical Research Communications. 179: 1470-8. PMID 1930188 DOI: 10.1016/0006-291X(91)91738-X |
0.385 |
|
| 1991 |
Beusenberg FD, Leurs R, van Schaik A, van Amsterdam JG, Bonta IL. Sensitization enhances the adenylyl cyclase responsiveness in alveolar macrophages. Changes induced at post-receptor level. Biochemical Pharmacology. 42: 485-90. PMID 1907147 DOI: 10.1016/0006-2952(91)90309-S |
0.425 |
|
| 1991 |
Leurs R, Bast A, Timmerman H. Fluoride is a contractile agent of guinea pig airway smooth muscle. General Pharmacology. 22: 631-6. PMID 1657687 DOI: 10.1016/0306-3623(91)90068-H |
0.662 |
|
| 1991 |
Leurs R, Smit MJ, Bast A, Timmerman H. Homologous histamine H1 receptor desensitization results in reduction of H1 receptor agonist efficacy. European Journal of Pharmacology. 196: 319-22. PMID 1654256 DOI: 10.1016/0014-2999(91)90446-W |
0.854 |
|
| 1991 |
Leurs R, Brozius MM, Jansen W, Bast A, Timmerman H. Histamine H1-receptor-mediated cyclic GMP production in guinea-pig lung tissue is an L-arginine-dependent process. Biochemical Pharmacology. 42: 271-7. PMID 1650206 DOI: 10.1016/0006-2952(91)90713-F |
0.665 |
|
| 1991 |
Leurs R, Smit MJ, Brozius MM, Jansen W, Bast A, Timmerman H. Is protein kinase C involved in histamine H1-receptor desensitization? Agents and Actions. Supplements. 33: 393-402. PMID 1647131 |
0.817 |
|
| 1991 |
Leurs R, Brozius MM, Smit MJ, Bast A, Timmerman H. Effects of histamine H1-, H2- and H3-receptor selective drugs on the mechanical activity of guinea-pig small and large intestine. British Journal of Pharmacology. 102: 179-85. PMID 1646056 DOI: 10.1111/J.1476-5381.1991.Tb12150.X |
0.837 |
|
| 1991 |
Leurs R, Goot HVD, Timmerman H. Histaminergic Agonists and Antagonists Recent Developments Advances in Drug Research. 20: 217-304. DOI: 10.1016/B978-0-12-013320-8.50008-3 |
0.408 |
|
| 1990 |
Leurs R, Bast A, Timmerman H. Essential thiol and disulphide groups in the histamine H1-receptor signal transfer of guinea-pig parenchymal lung strips. Agents and Actions. 30: 169-73. PMID 2371919 DOI: 10.1007/Bf01969029 |
0.74 |
|
| 1990 |
Leurs R, Bast A, Timmerman H. Labelling of non-H1-receptor binding sites by [3H]-mepyramine on the rat liver plasma membrane. Agents and Actions. 30: 157-60. PMID 2371917 DOI: 10.1007/Bf01969026 |
0.715 |
|
| 1990 |
Haaksma EE, Leurs R, Timmerman H. Histamine receptors: subclasses and specific ligands. Pharmacology & Therapeutics. 47: 73-104. PMID 2195558 DOI: 10.1016/0163-7258(90)90046-5 |
0.779 |
|
| 1990 |
Leurs R, Bast A, Timmerman H. Ebselen inhibits contractile responses of guinea-pig parenchymal lung strips. European Journal of Pharmacology. 179: 193-9. PMID 2114294 DOI: 10.1016/0014-2999(90)90418-6 |
0.321 |
|
| 1990 |
Leurs R, Beusenberg FD, Bast A, Van Amsterdam JG, Timmerman H. Identification of beta 2-adrenoceptors on guinea pig alveolar macrophages using (-)-3-[125I]iodocyanopindolol. Inflammation. 14: 421-6. PMID 1974244 DOI: 10.1007/Bf00914093 |
0.608 |
|
| 1990 |
Brozius M, Leurs R, Bast A, Timmerman H. Relaxations of the guinea-pig intestinal smooth muscle by histetmine H2-receptor agonists are not related to H2-receptor stimulation European Journal of Pharmacology. 183: 1552-1553. DOI: 10.1016/0014-2999(90)94714-9 |
0.748 |
|
| 1990 |
Smit M, Leurs R, Bast A, Timmerman H. Homologous and heterologous desensitisation of histamine H1-receptor mediated contractions of guinea-pig jejunum European Journal of Pharmacology. 183: 2428-2429. DOI: 10.1016/0014-2999(90)94002-F |
0.854 |
|
| 1990 |
Leurs R, Jansen W, Bast A, Timmerman H. Desensitisation off histamine H1-receptor mediated cyclic-GMP production in guinea-pig lung slices European Journal of Pharmacology. 183: 2167. DOI: 10.1016/0014-2999(90)93693-K |
0.712 |
|
| 1989 |
Leurs R, Go JN, Bast A, Timmerman H. Involvement of protein kinase C in the histamine H1-receptor mediated contraction of guinea-pig lung parenchymal strips. Agents and Actions. 27: 180-3. PMID 2750590 DOI: 10.1007/Bf02222233 |
0.696 |
|
| 1989 |
Leurs R, Donnell D, Timmerman H, Bast A. Interaction of nefopam and orphenadrine with the cytochrome P-450 and the glutathione system in rat liver. The Journal of Pharmacy and Pharmacology. 41: 388-93. PMID 2570834 DOI: 10.1111/J.2042-7158.1989.Tb06483.X |
0.574 |
|
| 1989 |
Leurs R, Bast A, Timmerman H. High affinity, saturable [3H]mepyramine binding sites on rat liver plasma membrane do not represent histamine H1-receptors. A warning. Biochemical Pharmacology. 38: 2175-80. PMID 2567596 DOI: 10.1016/0006-2952(89)90073-7 |
0.724 |
|
| 1988 |
Leurs R, Donnell D, Timmerman H, Bast A. Cytochrome P450 metabolic intermediate complex of nefopam. The Journal of Pharmacy and Pharmacology. 39: 835-7. PMID 2891822 DOI: 10.1111/J.2042-7158.1987.Tb05127.X |
0.556 |
|
| 1987 |
Bast A, Leurs R, Timmerman H. Cyclandelate as a calcium modulating agent in rat cerebral cortex. Drugs. 67-74. PMID 3040372 DOI: 10.2165/00003495-198700332-00012 |
0.624 |
|
| 1986 |
Leurs R, Rademaker B, Kramer K, Timmerman H, Bast A. The effects of 4-hydroxy-2,3-trans-nonenal on beta-adrenoceptors of rat lung membranes. Chemico-Biological Interactions. 59: 211-8. PMID 3021348 DOI: 10.1016/S0009-2797(86)80067-9 |
0.577 |
|
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