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Rob Leurs

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Mounir Andaloussi; Iwan J P De Esch; Rob Leurs; Herman D Lim; Chris B M Poulie; Maarten Sijm; Tiffany van der Meer; Rogier A Smits
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.
Chris de Graaf; Gerdien E de Kloe; Paul J England; Albert J Kooistra; Martien Kuijer; Rob Leurs; Saskia Nijmeijer; Jacqueline van Muijlwijk-Koezen; Mark H P Verheij; Henry Vischer; Iwan J P De Esch
Small and colorful stones make beautiful mosaics: fragment-based chemogenomics.
A O Watts; Guido J R Zaman; Rob Leurs; Marco Siderius; M van Zwam; J Vinet; H W G M Boddeke; W C Jaeger; K D G Pfleger; R M Seeber; M J Smit; M M C van der Lee; M M H van Lipzig; H F Vischer
Identification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes.

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All Publications

2013: Mounir Andaloussi; Iwan J P De Esch; Rob Leurs; Herman D Lim; Chris B M Poulie; Maarten Sijm; Tiffany van der Meer; Rogier A Smits
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 2013;23(9):2663-70.
2013: Chris de Graaf; Gerdien E de Kloe; Paul J England; Albert J Kooistra; Martien Kuijer; Rob Leurs; Saskia Nijmeijer; Jacqueline van Muijlwijk-Koezen; Mark H P Verheij; Henry Vischer; Iwan J P De Esch
Small and colorful stones make beautiful mosaics: fragment-based chemogenomics.
Drug discovery today 2013;18(7-8):323-30.
2013: A O Watts; Guido J R Zaman; Rob Leurs; Marco Siderius; M van Zwam; J Vinet; H W G M Boddeke; W C Jaeger; K D G Pfleger; R M Seeber; M J Smit; M M C van der Lee; M M H van Lipzig; H F Vischer
Identification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes.
British journal of pharmacology 2013;168(7):1662-74.
2013: Chimed Jansen; Hengming Ke; Albert J Kooistra; Kristina M Orrling; Thomas Seebeck; Hermann Tenor; Huanchen Wang; David Bailey; Iwan J P De Esch; Chris de Graaf; Rob Leurs
Discovery of novel Trypanosoma brucei phosphodiesterase B1 inhibitors by virtual screening against the unliganded TbrPDEB1 crystal structure.
Journal of medicinal chemistry 2013;56(5):2087-96.
2013: Anne O Watts; Guido J R Zaman; Martien Kuijer; Rob Leurs; Martine J Smit; Claudia A W Timmerman; Miranda M C van der Lee; Lambertus H C J van Lith; Jody van Offenbeek; Folkert Verkaar; Henry Vischer
β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.
The Journal of biological chemistry 2013;288(10):7169-81.
2013: Albert J Kooistra; Rob Leurs; Luc Roumen; Iwan J P De Esch; Chris de Graaf
From heptahelical bundle to hits from the Haystack: structure-based virtual screening for GPCR ligands.
Methods in enzymology 2013;522():279-336.
2013: Sabine Schultes; Obbe P Zuiderveld; Iwan J P De Esch; Harald Engelhardt; Eric E J Haaksma; Rob Leurs; Luc Roumen; Chris de Graaf
Combining quantum mechanical ligand conformation analysis and protein modeling to elucidate GPCR-ligand binding modes.
ChemMedChem 2013;8(1):49-53.
2012: Maikel Wijtmans; Meritxell Canals; Hans Custers; Iwan J P De Esch; Chris de Graaf; Frans J J de Kanter; Marjolein Glas; Luc Roumen; Danny J Scholten; Martine J Smit; Marlies C A Vreeker; Rob Leurs
Chemical subtleties in small-molecule modulation of peptide receptor function: the case of CXCR3 biaryl-type ligands.
Journal of medicinal chemistry 2012;55(23):10572-83.
2012: Saskia Nijmeijer; Anders F Rudebeck; Henry Vischer; David Falck; Frank Fleurbaaij; Rob Leurs; Wilfried M A Niessen; Jeroen Kool
Development of a profiling strategy for metabolic mixtures by combining chromatography and mass spectrometry with cell-based GPCR signaling.
Journal of biomolecular screening 2012;17(10):1329-38.
2012: Mark H P Verheij; Rob Leurs; Sarah C R Lummis; Andrew J Thompson; Jacqueline van Muijlwijk-Koezen; Iwan J P De Esch
Design, synthesis, and structure-activity relationships of highly potent 5-HT₃ receptor ligands.
Journal of medicinal chemistry 2012;55(20):8603-14.
2012: Kristina M Orrling; Thomas Seebeck; Anitha Shanmugham; Geert Jan Sterk; Andrea C van de Stolpe; Erika van den Bogaart; Johan Veerman; Xuan Lan Vu; Stèphanie Zorg; Emily Adams; David Bailey; Vreni Balmer; Patrick Bregy; Eric Chatelain; Paul Cos; Iwan J P De Esch; Paul England; Jean-Robert Ioset; Chimed Jansen; Louis Maes; Rob Leurs
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Journal of medicinal chemistry 2012;55(20):8745-56.
2012: Oscar P J van Linden; Maikel Wijtmans; Rob Leurs; Lonneke Rotteveel; Luc Roumen; Iwan J P De Esch
Regiochemistry of the condensation of 2-aroyl-cyclohexanones and 2-cyanoacetamide: 13C-labeling studies and semiempirical MO calculations.
The Journal of organic chemistry 2012;77(17):7355-63.
2012: Harald Engelhardt; Eric E J Haaksma; Daniel Kuhn; Sebastian Lips; Moriz Mayer; Dirk Scharn; Rogier A Smits; Obbe P Zuiderveld; Heribert Arnhof; Iwan J P De Esch; Julia Dobler; Rob Leurs
Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.
European journal of medicinal chemistry 2012;54():660-8.
2012: D J Scholten; Dennis Verzijl; Maikel Wijtmans; Iwan J P De Esch; M J Smit; H F Vischer; M Canals; S de Munnik; P Nguyen; Rob Leurs
Pharmacological characterization of a small-molecule agonist for the chemokine receptor CXCR3.
British journal of pharmacology 2012;166(3):898-911.
2012: Maikel Wijtmans; David Maussang; Azra Mujić-Delić; Danny J Scholten; Francesco Sirci; Martine J Smit; Meritxell Canals; Kristell L S Chatalic; Milagros Chong; Hans Custers; Iwan J P De Esch; Chris de Graaf; Elwin Janssen; Rob Leurs
Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists.
European journal of medicinal chemistry 2012;51():184-92.
2012: Anne O Watts; Laura H Heitman; Danny J Scholten; Henry Vischer; Rob Leurs
Label-free impedance responses of endogenous and synthetic chemokine receptor CXCR3 agonists correlate with Gi-protein pathway activation.
Biochemical and biophysical research communications 2012;419(2):412-8.
2012: D J Scholten; Maikel Wijtmans; M J Smit; H F Vischer; M Canals; C de Graaf; D Maussang; L Roumen; Rob Leurs
Pharmacological modulation of chemokine receptor function.
British journal of pharmacology 2012;165(6):1617-43.
2012: Ewald Edink; Chimed Jansen; Rob Leurs; August B Smit; Jacqueline van Muijlwijk-Koezen; Obbe Zuiderveld; René van Elk; Atilla Akdemir; Frans J J de Kanter; Iwan J P De Esch
Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.
Bioorganic & medicinal chemistry letters 2012;22(3):1448-54.
2012: Ellen V Langemeijer; Rob Leurs; David Maussang; Andreas Schreiber; Marco Siderius; Erik Slinger; Folkert Verkaar; Henry Vischer; Sabrina de Munnik; Martine J Smit
Constitutive β-catenin signaling by the viral chemokine receptor US28.
PloS one 2012;7(11):e48935.
2012: Saskia Nijmeijer; Chris de Graaf; Rob Leurs; Henry Vischer
Molecular pharmacology of histamine H4 receptors.
Frontiers in bioscience : a journal and virtual library 2012;17():2089-106.
2012: Maristella Adami; Simone Bertini; Anna Maria Cantoni; Iwan J P De Esch; Rob Leurs; Alessandro Menozzi; Benedetta Passeri; Cristina Pozzoli; Rogier Smits; Gabriella Coruzzi
Effects of histamine H4 receptor ligands in a mouse model of gastric ulceration.
Pharmacology 2012;89(5-6):287-94.
2012: Meritxell Canals; Sabrina de Munnik; Mitchell K L Han; Danny J Scholten; Martine J Smit; Rob Leurs
Ubiquitination of CXCR7 controls receptor trafficking.
PloS one 2012;7(3):e34192.
2012: Oscar P J van Linden; Maikel Wijtmans; Willem H Zoutman; Carine Farenc; Liesbeth Hameetman; Rob Leurs; Gregg Siegal; Cornelis P Tensen; Iwan J P De Esch
Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase.
European journal of medicinal chemistry 2012;47(1):493-500.
2011: Chris de Graaf; So Iwata; Vsevolod Katritch; Albert J Kooistra; Martien Kuijer; Tatsuro Shimamura; Mitsunori Shiroishi; Raymond C Stevens; Henry Vischer; Iwan J P De Esch; Rob Leurs
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.
Journal of medicinal chemistry 2011;54(23):8195-206.
2011: Enade P Istyastono; Albert J Kooistra; Rob Leurs; Herman D Lim; Saskia Nijmeijer; Luc Roumen; Andrea C van de Stolpe; Henry Vischer; Iwan J P De Esch; Chris de Graaf
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 2011;54(23):8136-47.
2011: Sebastiaan Kuhne; Rob Leurs; Herman D Lim; Maikel Wijtmans; Iwan J P De Esch
Several down, a few to go: histamine H3 receptor ligands making the final push towards the market?
Expert opinion on investigational drugs 2011;20(12):1629-48.
2011: Petra de Kruijf; Douglas S Auld; Chris de Graaf; Herman D Lim; Véronique A Renjaän; Luc Roumen; Martine J Smit; Maria L Webb; Jac C H M Wijkmans; Guido J R Zaman; Jiuqiao Zhao; Rob Leurs
Identification of a novel allosteric binding site in the CXCR2 chemokine receptor.
Molecular pharmacology 2011;80(6):1108-18.
2011: Gabriella Coruzzi; Iwan J P De Esch; Cristina Pozzoli; Rogier Smits; Maristella Adami; Rob Leurs
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 2011;669(1-3):121-7.
2011: Atilla Akdemir; Daniel Bertrand; Sonia Bertrand; Chris de Graaf; Aldo Jongejan; Rob Leurs; Prakash Rucktooa; Titia K Sixma; August B Smit; Rene van Elk; Iwan J P De Esch
Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors.
Bioorganic & medicinal chemistry 2011;19(20):6107-19.
2011: Mark H P Verheij; Henry Vischer; Obbe P Zuiderveld; Chris de Graaf; Gerdien E de Kloe; Saskia Hulscher; Rob Leurs; Sarah C R Lummis; Saskia Nijmeijer; Linda Silvestri; Rogier A Smits; Andrew J Thompson; Jacqueline van Muijlwijk-Koezen; Iwan J P De Esch
Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.
Bioorganic & medicinal chemistry letters 2011;21(18):5460-4.
2011: Jeroen Kool; Rob Leurs; Henk Lingeman; Iwan J P De Esch; Gerdien de Kloe; Ewald Edink; Ferry Heus; Hubertus Irth; August B Smit; Wilfried M A Niessen
High-resolution bioactivity profiling of mixtures toward the acetylcholine binding protein using a nanofractionation spotter technology.
Journal of biomolecular screening 2011;16(8):917-24.
2011: Maikel Wijtmans; Dennis Verzijl; Serge Bergmans; Michael Lai; Leontien Bosch; Martine J Smit; Iwan J P De Esch; Rob Leurs
CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors.
Bioorganic & medicinal chemistry 2011;19(11):3384-93.
2011: Henry F Vischer; Anne O Watts; Saskia Nijmeijer; Rob Leurs
G protein-coupled receptors: walking hand-in-hand, talking hand-in-hand?
British journal of pharmacology 2011;163(2):246-60.
2011: Ewald Edink; Prakash Rucktooa; Kim Retra; Atilla Akdemir; Tariq Nahar; Obbe Zuiderveld; René Van Elk; Elwin Janssen; Pim Van Nierop; Jacqueline van Muijlwijk-Koezen; August B Smit; Titia K Sixma; Rob Leurs; Iwan J P De Esch
Fragment growing induces conformational changes in acetylcholine-binding protein: a structural and thermodynamic analysis.
Journal of the American Chemical Society 2011;133(14):5363-71.
2011: Rob Leurs; Henry Vischer; Maikel Wijtmans; Iwan J P De Esch
En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family.
Trends in pharmacological sciences 2011;32(4):250-7.
2011: Lindsay B Hough; Julia W Nalwalk; Jun Yang; Jennie L Conroy; Melissa A VanAlstine; Weizhu Yang; Joseph Gargano; Zhixing Shan; Shao-Zhong Zhang; Mark P Wentland; James G Phillips; Brian I Knapp; Jean M Bidlack; Obbe P Zuiderveld; Rob Leurs; Xinxin Ding
Brain P450 epoxygenase activity is required for the antinociceptive effects of improgan, a nonopioid analgesic.
Pain 2011;152(4):878-87.
2011: Maikel Wijtmans; Chris de Graaf; Gerdien de Kloe; Enade P Istyastono; Judith Smit; Herman Lim; Ratchanok Boonnak; Saskia Nijmeijer; Rogier A Smits; Aldo Jongejan; Obbe Zuiderveld; Iwan J P De Esch; Rob Leurs
Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity.
Journal of medicinal chemistry 2011;54(6):1693-703.
2011: Kamonchanok Sansuk; Xavier Deupi; Ivan Rodriguez Torrecillas; Aldo Jongejan; Saskia Nijmeijer; Remko A Bakker; Leonardo Pardo; Rob Leurs
A structural insight into the reorientation of transmembrane domains 3 and 5 during family A G protein-coupled receptor activation.
Molecular pharmacology 2011;79(2):262-9.
2011: Enade P Istyastono; Chris de Graaf; Iwan J P De Esch; Rob Leurs
Molecular determinants of selective agonist and antagonist binding to the histamine H₄ receptor.
Current topics in medicinal chemistry 2011;11(6):661-79.
2011: Jeroen Kool; Gerdien de Kloe; Arnoud D Denker; Klaas Van Altena; Marek Smoluch; Dick van Iperen; Tariq T Nahar; Rob J Limburg; Wilfried M A Niessen; Henk Lingeman; Rob Leurs; Iwan J P De Esch; August B Smit; Hubertus Irth
Nanofractionation spotter technology for rapid contactless and high-resolution deposition of LC eluent for further off-line analysis.
Analytical chemistry 2011;83(1):125-32.
2010: Sven Jähnichen; Christophe Blanchetot; David Maussang; Maria Gonzalez-Pajuelo; Ken Y Chow; Leontien Bosch; Sindi De Vrieze; Benedikte Serruys; Hans Ulrichts; Wesly Vandevelde; Michael Saunders; Hans J De Haard; Dominique Schols; Rob Leurs; Peter Vanlandschoot; Theo Verrips; Martine J Smit
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 2010;107(47):20565-70.
2010: Gerdien E de Kloe; Kim Retra; Matthis Geitmann; Per Kallblad; Tariq Nahar; René Van Elk; August B Smit; Jacqueline van Muijlwijk-Koezen; Rob Leurs; Hubertus Irth; Helena Danielson; Iwan J P De Esch
Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptor α7 ligands.
Journal of medicinal chemistry 2010;53(19):7192-201.
2010: Saskia Nijmeijer; Rob Leurs; Martine J Smit; Henry Vischer
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 2010;285(38):29632-41.
2010: Petra de Kruijf; Herman D Lim; Saskia A Overbeek; Guido J R Zaman; Aletta D Kraneveld; Gert Folkerts; Rob Leurs; Martine J Smit
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 2010;643(1):29-33.
2010: Jeroen Kool; Gerdien E de Kloe; Ben Bruyneel; Jon S B de Vlieger; Kim Retra; Maikel Wijtmans; Rene van Elk; August B Smit; Rob Leurs; Henk Lingeman; Iwan J P De Esch; Hubertus Irth
Online fluorescence enhancement assay for the acetylcholine binding protein with parallel mass spectrometric identification.
Journal of medicinal chemistry 2010;53(12):4720-30.
2010: Herman D Lim; Chris de Graaf; Wen Jiang; Payman Sadek; Patricia M McGovern; Enade P Istyastono; Remko A Bakker; Iwan J P De Esch; Robin Thurmond; Rob Leurs
Molecular determinants of ligand binding to H4R species variants.
Molecular pharmacology 2010;77(5):734-43.
2010: Rogier A Smits; Maristella Adami; Enade P Istyastono; Obbe P Zuiderveld; Cindy M E van Dam; Frans J J de Kanter; Aldo Jongejan; Gabriella Coruzzi; Rob Leurs; Iwan J P De Esch
Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists.
Journal of medicinal chemistry 2010;53(6):2390-400.
2010: Jennie L Conroy; Cheng Fang; Jun Gu; Scott O Zeitlin; Weizhu Yang; Jun Yang; Melissa A VanAlstine; Julia W Nalwalk; Phillip J Albrecht; Joseph E Mazurkiewicz; Abigail Snyder-Keller; Zhixing Shan; Shao-Zhong Zhang; Mark P Wentland; Melissa Behr; Brian I Knapp; Jean M Bidlack; Obbe P Zuiderveld; Rob Leurs; Xinxin Ding; Lindsay B Hough
Opioids activate brain analgesic circuits through cytochrome P450/epoxygenase signaling.
Nature neuroscience 2010;13(3):284-6.
2010: Henry Vischer; Janneke W Hulshof; Saskia Hulscher; Silvina A Fratantoni; Mark H P Verheij; Jane Victorina; Martine J Smit; Iwan J P De Esch; Rob Leurs
Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.
Bioorganic & medicinal chemistry 2010;18(2):675-88.
2010: Gerold Bongers; Iwan J P De Esch; Rob Leurs
Molecular pharmacology of the four histamine receptors.
Advances in experimental medicine and biology 2010;709():11-9.
2010: Maristella Adami; Cristina Pozzoli; Rob Leurs; Holger Stark; Gabriella Coruzzi
Histamine H(3) receptors are involved in the protective effect of ghrelin against HCl-induced gastric damage in rats.
Pharmacology 2010;86(5-6):259-66.
2009: David Maussang; Henry Vischer; Rob Leurs; Martine J Smit
Herpesvirus-encoded G protein-coupled receptors as modulators of cellular function.
Molecular pharmacology 2009;76(4):692-701.
2009: Harald Engelhardt; Rogier A Smits; Rob Leurs; Eric Haaksma; Iwan J P De Esch
A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic.
Current opinion in drug discovery & development 2009;12(5):628-43.
2009: Chiara Mariottini; Tania Scartabelli; Gerold Bongers; Silvia Arrigucci; Daniele Nosi; Rob Leurs; Alberto Chiarugi; patrizio blandina; Domenico E Pellegrini-Giampietro; Maria Beatrice Passani
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 2009;110(5):1469-78.
2009: Rogier A Smits; Rob Leurs; Iwan J P De Esch
Major advances in the development of histamine H4 receptor ligands.
Drug discovery today 2009;14(15-16):745-53.
2009: Gerdien E de Kloe; David Bailey; Rob Leurs; Iwan J P De Esch
Transforming fragments into candidates: small becomes big in medicinal chemistry.
Drug discovery today 2009;14(13-14):630-46.
2009: Sylvain Célanire; Maikel Wijtmans; bernard christophe; Philippe Collart; Iwan de Esch; Donald Dassesse; Christel Delaunoy; Frédéric Denonne; Véronique Durieu; Edith Gelens; Michel Gillard; Bénédicte Lallemand; Yves Lamberty; Florence Lebon; Jean-Marie Nicolas; Luc Quéré; Erwin Snip; Alain Vanbellinghen; Nathalie Van Houtvin; Valérie Verbois; Henk Timmerman; Patrice Talaga; Rob Leurs; Laurent Provins
Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists.
ChemMedChem 2009;4(7):1063-8.
2009: Herman D Lim; Enade P Istyastono; Andrea van de Stolpe; Giuseppe Romeo; Silvia Gobbi; Marjo Schepers; Roger Lahaye; Wiro M P B Menge; Obbe P Zuiderveld; Aldo Jongejan; Rogier A Smits; Remko A Bakker; Eric E J Haaksma; Rob Leurs; Iwan J P De Esch
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
Bioorganic & medicinal chemistry 2009;17(11):3987-94.
2009: Herman D Lim; Maristella Adami; Elena Guaita; Thomas Werfel; Rogier A Smits; Iwan J P De Esch; Remko A Bakker; Ralf Gutzmer; Gabriella Coruzzi; Rob Leurs
Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430.
British journal of pharmacology 2009;157(1):34-43.
2009: Rob Leurs; Paul L Chazot; Fiona C Shenton; Herman D Lim; Iwan J P De Esch
Molecular and biochemical pharmacology of the histamine H4 receptor.
British journal of pharmacology 2009;157(1):14-23.
2009: Petra de Kruijf; Jane van Heteren; Herman D Lim; Paolo G M Conti; Miranda M C van der Lee; Leontien Bosch; Koc-Kan Ho; Douglas Auld; Michael Ohlmeyer; Martine J Smit; Jac C H M Wijkmans; Guido J R Zaman; Martine J Smit; Rob Leurs
Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor.
The Journal of pharmacology and experimental therapeutics 2009;329(2):783-90.
2009: Maikel Wijtmans; Dennis Verzijl; Cindy M E van Dam; Leontien Bosch; Martine J Smit; Rob Leurs; Iwan J P De Esch
Exploring a pocket for polycycloaliphatic groups in the CXCR3 receptor with the aid of a modular synthetic strategy.
Bioorganic & medicinal chemistry letters 2009;19(8):2252-7.
2009: David Maussang; Ellen Langemeijer; Carlos P Fitzsimons; Marijke Stigter-van Walsum; Remco Dijkman; Martin K Borg; Erik Slinger; Andreas Schreiber; Detlef Michel; Cornelis P Tensen; Guus A M S van Dongen; Rob Leurs; Martine J Smit
The human cytomegalovirus-encoded chemokine receptor US28 promotes angiogenesis and tumor formation via cyclooxygenase-2.
Cancer research 2009;69(7):2861-9.
2008: Henry Vischer; Saskia Nijmeijer; Martine J Smit; Rob Leurs
Viral hijacking of human receptors through heterodimerization.
Biochemical and biophysical research communications 2008;377(1):93-7.
2008: Herman D Lim; Aldo Jongejan; Remko A Bakker; Eric Haaksma; Iwan J P De Esch; Rob Leurs
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 2008;327(1):88-96.
2008: Wendy Jiang; Herman D Lim; Mai Zhang; Pragnya Desai; Heng Dai; Patricia M Colling; Rob Leurs; Robin Thurmond
Cloning and pharmacological characterization of the dog histamine H4 receptor.
European journal of pharmacology 2008;592(1-3):26-32.
2008: Richard M van Rijn; André van Marle; Paul L Chazot; Ellen Langemeijer; Yongjun Qin; Fiona C Shenton; Herman D Lim; Obbe P Zuiderveld; Kamonchanok Sansuk; Michel Dy; Martine J Smit; Cornelis P Tensen; Remko A Bakker; Rob Leurs
Cloning and characterization of dominant negative splice variants of the human histamine H4 receptor.
The Biochemical journal 2008;414(1):121-31.
2008: Maikel Wijtmans; Dennis Verzijl; Rob Leurs; Iwan J P De Esch; Martine J Smit
Towards small-molecule CXCR3 ligands with clinical potential.
ChemMedChem 2008;3(6):861-72.
2008: Maikel Wijtmans; Sylvain Celanire; Erwin Snip; Michel Gillard; Edith Gelens; Philippe P Collart; Bastiaan J Venhuis; Bernard Christophe; Saskia Hulscher; Henk van der Goot; Florence Lebon; Henk Timmerman; Remko A Bakker; Bénédicte I L F Lallemand; Rob Leurs; Patrice Talaga; Iwan J P De Esch
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
Journal of medicinal chemistry 2008;51(10):2944-53.
2008: Dennis Verzijl; Stefania Storelli; Danny J Scholten; Leontien Bosch; Todd A Reinhart; Daniel N Streblow; Cornelis P Tensen; Carlos P Fitzsimons; Guido J R Zaman; James E Pease; Iwan J P De Esch; Martine J Smit; Rob Leurs
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 2008;325(2):544-55.
2008: Rogier A Smits; Herman D Lim; Agnes Hanzer; Obbe P Zuiderveld; Elena Guaita; Maristella Adami; Gabriella Coruzzi; Rob Leurs; Iwan J P De Esch
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
Journal of medicinal chemistry 2008;51(8):2457-67.
2008: Kamonchanok Sansuk; Crina I A Balog; Anne M van der Does; Raymond G Booth; Willem J De Grip; André M Deelder; Remko A Bakker; Rob Leurs; Paul J Hensbergen
GPCR proteomics: mass spectrometric and functional analysis of histamine H1 receptor after baculovirus-driven and in vitro cell free expression.
Journal of proteome research 2008;7(2):621-9.
2008: Raymond G Booth; L Fang; Andrzej Wilczynski; S Sivendren; Z Sun; S Travers; M Bruysters; K Sansuk; Rob Leurs
Molecular determinants of ligand-directed signaling for the histamine H1 receptor.
Inflammation research : official journal of the European Histamine Research Society ... [et al.] 2008;57 Suppl 1():S43-4.
2008: Remko A Bakker; Aldo Jongejan; Kamonchanok Sansuk; Uli Hacksell; Henk Timmerman; Mark R Brann; David M Weiner; Leonardo Pardo; Rob Leurs
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 2008;73(1):94-103.
2007: Jeroen Kool; André van Marle; Saskia Hulscher; Maurice Selman; Dick J van Iperen; Klaas Van Altena; Michel Gillard; Remko A Bakker; Hubertus Irth; Rob Leurs; Nico P E Vermeulen
A flow-through fluorescence polarization detection system for measuring GPCR-mediated modulation of cAMP production.
Journal of biomolecular screening 2007;12(8):1074-83.
2007: Gerold Bongers; Kathleen M Krueger; Thomas R Miller; John L Baranowski; Brian R Estvander; David G Witte; Marina I Strakhova; Peter Van Meer; Remko A Bakker; Marlon D Cowart; Arthur A Hancock; Timothy A Esbenshade; Rob Leurs
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 2007;323(3):888-98.
2007: Keri E Cannon; Rob Leurs; Lindsay B Hough
Activation of peripheral and spinal histamine H3 receptors inhibits formalin-induced inflammation and nociception, respectively.
Pharmacology, biochemistry, and behavior 2007;88(1):122-9.
2007: Lindsay B Hough; Wiro M P B Menge; Andrea C van de Stolpe; Julia W Nalwalk; Rob Leurs; Iwan J P De Esch
Antinociceptive activity of furan-containing congeners of improgan and ranitidine.
Bioorganic & medicinal chemistry letters 2007;17(20):5715-9.
2007: Gerold Bongers; Tina Sallmen; Maria Beatrice Passani; Chiara Mariottini; Dominique Wendelin; Adrian F Lozada; André van Marle; Marjon Navis; patrizio blandina; Remko A Bakker; Pertti Panula; Rob Leurs
The Akt/GSK-3beta axis as a new signaling pathway of the histamine H(3) receptor.
Journal of neurochemistry 2007;103(1):248-58.
2007: Maikel Wijtmans; Rob Leurs; Iwan J P De Esch
Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas.
Expert opinion on investigational drugs 2007;16(7):967-85.
2007: Remko A Bakker; M W Nicholas; T T Smith; Ethan S Burstein; Uli Hacksell; Henk Timmerman; Rob Leurs; Mark R Brann; David M Weiner
In vitro pharmacology of clinically used central nervous system-active drugs as inverse H(1) receptor agonists.
The Journal of pharmacology and experimental therapeutics 2007;322(1):172-9.
2007: Stefania Storelli; Dennis Verzijl; Jawad Al-Badie; Niels Elders; Leontien Bosch; Henk Timmerman; Martine J Smit; Iwan J P De Esch; Rob Leurs
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 2007;340(6):281-91.
2007: Gabriella Coruzzi; Maristella Adami; Elena Guaita; Iwan J P De Esch; Rob Leurs
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 2007;563(1-3):240-4.
2007: Niels Hulsman; Jan Paul Medema; Carina Bos; Aldo Jongejan; Rob Leurs; Martine J Smit; Iwan J P De Esch; Dick Richel; Maikel Wijtmans
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 2007;50(10):2424-31.
2007: Gerold Bongers; Remko A Bakker; Rob Leurs
Molecular aspects of the histamine H3 receptor.
Biochemical pharmacology 2007;73(8):1195-204.
2007: Venkata R P Ratnala; Suzanne Kiihne; Francesco Buda; Rob Leurs; Huub J M de Groot; Willem J Degrip
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 2007;129(4):867-72.
2007: Martine J Smit; Henry Vischer; Remko A Bakker; Aldo Jongejan; Henk Timmerman; Leonardo Pardo; Rob Leurs
Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity.
Annual review of pharmacology and toxicology 2007;47():53-87.
2006: Dennis Verzijl; Leonardo Pardo; Marie Van Dijk; Yvonne K Gruijthuijsen; Aldo Jongejan; Henk Timmerman; John Nicholas; Mario Schwarz; Philip M Murphy; Rob Leurs; Martine J Smit
Helix 8 of the viral chemokine receptor ORF74 directs chemokine binding.
The Journal of biological chemistry 2006;281(46):35327-35.
2006: Herman D Lim; Rogier A Smits; Remko A Bakker; Cindy M E van Dam; Iwan J P De Esch; Rob Leurs
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
Journal of medicinal chemistry 2006;49(23):6650-1.
2006: Janneke W Hulshof; Henry Vischer; Mark H P Verheij; Silvina A Fratantoni; Martine J Smit; Iwan J P De Esch; Rob Leurs
Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28.
Bioorganic & medicinal chemistry 2006;14(21):7213-30.
2006: Lindsay B Hough; Iwan J P De Esch; Elwin Janssen; James Phillips; Konstantina Svokos; Brian Kern; Jennifer Trachler; Mary E Abood; Rob Leurs; Julia W Nalwalk
Antinociceptive activity of chemical congeners of improgan: optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic.
Neuropharmacology 2006;51(3):447-56.
2006: David Maussang; Dennis Verzijl; Marijke van Walsum; Rob Leurs; Jens Michael Holl; Olivier Pleskoff; Detlef Michel; Guus A M S van Dongen; Martine J Smit
Human cytomegalovirus-encoded chemokine receptor US28 promotes tumorigenesis.
Proceedings of the National Academy of Sciences of the United States of America 2006;103(35):13068-73.
2006: Richard M van Rijn; Paul L Chazot; Fiona C Shenton; Kamonchanok Sansuk; Remko A Bakker; Rob Leurs
Oligomerization of recombinant and endogenously expressed human histamine H(4) receptors.
Molecular pharmacology 2006;70(2):604-15.
2006: Rogier A Smits; Herman D Lim; Bart Stegink; Remko A Bakker; Iwan J P De Esch; Rob Leurs
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
Journal of medicinal chemistry 2006;49(15):4512-6.
2006: Marinella Govoni; Herman D Lim; Dris El-Atmioui; Wiro M P B Menge; Henk Timmerman; Remko A Bakker; Rob Leurs; Iwan J P De Esch
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 2006;49(8):2549-57.
2006: Remko A Bakker; Adrian F Lozada; André van Marle; Fiona C Shenton; Guillaume Drutel; Kaj Karlstedt; Marcel Hoffmann; Minnamaija Lintunen; Yumiko Yamamoto; Richard M van Rijn; Paul L Chazot; Pertti Panula; Rob Leurs
Discovery of naturally occurring splice variants of the rat histamine H3 receptor that act as dominant-negative isoforms.
Molecular pharmacology 2006;69(4):1194-206.
2006: Carlos P Fitzsimons; Ursula A Gompels; Dennis Verzijl; Henry Vischer; Claire Mattick; Rob Leurs; Martine J Smit
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 2006;69(3):888-98.
2006: Edith Gelens; Frans J J de Kanter; Rob F Schmitz; Leo A J M Sliedregt; Bart J van Steen; Chris G Kruse; Rob Leurs; Marinus B Groen; Romano V A Orru
Efficient library synthesis of imidazoles using a multicomponent reaction and microwave irradiation.
Molecular diversity 2006;10(1):17-22.
2006: Henry Vischer; Janneke W Hulshof; Iwan J P De Esch; Martine J Smit; Rob Leurs
Virus-encoded G-protein-coupled receptors: constitutively active (dys)regulators of cell function and their potential as drug target.
Ernst Schering Foundation symposium proceedings 2006;(2):187-209.
2006: Herman D Lim; Rogier A Smits; Rob Leurs; Iwan J P De Esch
The emerging role of the histamine H4 receptor in anti-inflammatory therapy.
Current topics in medicinal chemistry 2006;6(13):1365-73.
2006: Henry Vischer; Rob Leurs; Martine J Smit
HCMV-encoded G-protein-coupled receptors as constitutively active modulators of cellular signaling networks.
Trends in pharmacological sciences 2006;27(1):56-63.
2005: Sylvain Celanire; Maikel Wijtmans; Patrice Talaga; Rob Leurs; Iwan J P De Esch
Keynote review: histamine H3 receptor antagonists reach out for the clinic.
Drug discovery today 2005;10(23-24):1613-27.
2005: Ruengwit Kitbunnadaj; Marcel Hoffmann; Silvina A Fratantoni; Gerold Bongers; Remko A Bakker; Kerstin Wieland; Ahmed el Jilali; Iwan J P De Esch; Wiro M P B Menge; Henk Timmerman; Rob Leurs
New high affinity H3 receptor agonists without a basic side chain.
Bioorganic & medicinal chemistry 2005;13(23):6309-23.
2005: Martijn Bruysters; Aldo Jongejan; Atilla Akdemir; Remko A Bakker; Rob Leurs
A G(q/11)-coupled mutant histamine H(1) receptor F435A activated solely by synthetic ligands (RASSL).
The Journal of biological chemistry 2005;280(41):34741-6.
2005: Janneke W Hulshof; Paola Casarosa; Wiro M P B Menge; Leena M S Kuusisto; Henk van der Goot; Martine J Smit; Iwan J P De Esch; Rob Leurs
Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.
Journal of medicinal chemistry 2005;48(20):6461-71.
2005: Iwan J P De Esch; Robin Thurmond; Aldo Jongejan; Rob Leurs
The histamine H4 receptor as a new therapeutic target for inflammation.
Trends in pharmacological sciences 2005;26(9):462-9.
2005: Herman D Lim; Richard M van Rijn; Ping Ling; Remko A Bakker; Robin Thurmond; Rob Leurs
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 2005;314(3):1310-21.
2005: Olivier Pleskoff; Paola Casarosa; Laurence Verneuil; Fadela Ainoun; Patrick S Beisser; Martine Smit; Rob Leurs; Pascal Schneider; Susan Michelson; Jean-Claude Ameisen
The human cytomegalovirus-encoded chemokine receptor US28 induces caspase-dependent apoptosis.
The FEBS journal 2005;272(16):4163-77.
2005: Aldo Jongejan; Martijn Bruysters; Juan A Ballesteros; Eric Haaksma; Remko A Bakker; Leonardo Pardo; Rob Leurs
Linking agonist binding to histamine H1 receptor activation.
Nature chemical biology 2005;1(2):98-103.
2005: Stefania Storelli; Pauline Verdijk; Dennis Verzijl; Henk Timmerman; Andrea C van de Stolpe; Cornelis P Tensen; Martine J Smit; Iwan J P De Esch; Rob Leurs
Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.
Bioorganic & medicinal chemistry letters 2005;15(11):2910-3.
2005: Aldo Jongejan; Rob Leurs
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 2005;338(5-6):248-59.
2005: Martijn Bruysters; Aldo Jongejan; Michel Gillard; Frank van de Manakker; Remko A Bakker; Pierre Chatelain; Rob Leurs
Pharmacological differences between human and guinea pig histamine H1 receptors: Asn84 (2.61) as key residue within an additional binding pocket in the H1 receptor.
Molecular pharmacology 2005;67(4):1045-52.
2005: Ruengwit Kitbunnadaj; Takeshi Hashimoto; Enzo Poli; Obbe P Zuiderveld; Alessandro Menozzi; Ryoko Hidaka; Iwan J P De Esch; Remko A Bakker; Wiro M P B Menge; Atsushi Yamatodani; Gabriella Coruzzi; Henk Timmerman; Rob Leurs
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
Journal of medicinal chemistry 2005;48(6):2100-7.
2005: Rianne A F de Ligt; Scott A Rivkees; Anna Lorenzen; Rob Leurs; Adriaan P IJzerman
A "locked-on," constitutively active mutant of the adenosine A1 receptor.
European journal of pharmacology 2005;510(1-2):1-8.
2005: Julia W Nalwalk; Konstantina Svokos; Rob Leurs; Lindsay B Hough
Absence of 5-HT3 and cholinergic mechanisms in improgan antinociception.
Pharmacology, biochemistry, and behavior 2005;80(3):505-10.
2005: Paola Casarosa; Maria Waldhoer; Patricia J LiWang; Henry Vischer; Thomas N Kledal; Henk Timmerman; Thue W Schwartz; Martine J Smit; Rob Leurs
CC and CX3C chemokines differentially interact with the N terminus of the human cytomegalovirus-encoded US28 receptor.
The Journal of biological chemistry 2005;280(5):3275-85.
2005: Rob Leurs; Remko A Bakker; Henk Timmerman; Iwan J P De Esch
The histamine H3 receptor: from gene cloning to H3 receptor drugs.
Nature reviews. Drug discovery 2005;4(2):107-20.
2005: Aldo Jongejan; Chris de Graaf; Nico P E Vermeulen; Rob Leurs; Iwan J P De Esch
The role and application of in silico docking in chemical genomics research.
Methods in molecular biology (Clifton, N.J.) 2005;310():63-91.
2005: Adrian F Lozada; N Munyao; Tina Sallmen; Minnamaija Lintunen; Rob Leurs; P J Lindsberg; Pertti Panula
Postischemic regulation of central histamine receptors.
Neuroscience 2005;136(1):371-9.
2005: Patrick S Beisser; Dennis Verzijl; Yvonne K Gruijthuijsen; Erik Beuken; Martine J Smit; Rob Leurs; Cathrien A Bruggeman; Cornelis Vink
The Epstein-Barr virus BILF1 gene encodes a G protein-coupled receptor that inhibits phosphorylation of RNA-dependent protein kinase.
Journal of virology 2005;79(1):441-9.
2004: Nalan Terzioglu; Richard M van Rijn; Remko A Bakker; Iwan J P De Esch; Rob Leurs
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
Bioorganic & medicinal chemistry letters 2004;14(21):5251-6.
2004: Remko A Bakker; Guido Dees; Juan J Carrillo; Raymond G Booth; Juan F López-Gimenez; Graeme Milligan; Philip G Strange; Rob Leurs
Domain swapping in the human histamine H1 receptor.
The Journal of pharmacology and experimental therapeutics 2004;311(1):131-8.
2004: Julia W Nalwalk; Konstantina Svokos; Olga D Taraschenko; Rob Leurs; Henk Timmerman; Lindsay B Hough
Activation of brain stem nuclei by improgan, a non-opioid analgesic.
Brain research 2004;1021(2):248-55.
2004: Elisabeth C Klaasse; Rianne A F de Ligt; Sophie F Roerink; Anna Lorenzen; Graeme Milligan; Rob Leurs; Adriaan P IJzerman
Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits.
European journal of pharmacology 2004;499(1-2):91-8.
2004: Venkata R P Ratnala; Herman G P Swarts; Jenny VanOostrum; Rob Leurs; Huub J M DeGroot; Remko A Bakker; Willem J Degrip
Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor.
European journal of biochemistry / FEBS 2004;271(13):2636-46.
2004: Ruengwit Kitbunnadaj; Obbe P Zuiderveld; Bernard Christophe; Saskia Hulscher; Wiro M P B Menge; Edith Gelens; Erwin Snip; Remko A Bakker; Sylvain Celanire; Michel Gillard; Patrice Talaga; Henk Timmerman; Rob Leurs
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 2004;47(10):2414-7.
2004: Paul J Hensbergen; Dennis Verzijl; Crina I A Balog; Remco Dijkman; Roel C Van Der Schors; Elisabeth M H van der Raaij-Helmer; Mariena J A van der Plas; Rob Leurs; André M Deelder; Martine J Smit; Cornelis P Tensen
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 2004;279(14):13402-11.
2004: Yvonne K Gruijthuijsen; Erik Beuken; Martine J Smit; Rob Leurs; Cathrien A Bruggeman; Cornelis Vink
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 2004;85(Pt 4):897-909.
2004: Dennis Verzijl; Carlos P Fitzsimons; Marie Van Dijk; James P Stewart; Henk Timmerman; Martine J Smit; Rob Leurs
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 2004;78(7):3343-51.
2004: Martijn Bruysters; Heinz H Pertz; Aloys Teunissen; Remko A Bakker; Michel Gillard; Pierre Chatelain; Walter Schunack; Henk Timmerman; Rob Leurs
Mutational analysis of the histamine H1-receptor binding pocket of histaprodifens.
European journal of pharmacology 2004;487(1-3):55-63.
2004: Enzo Poli; Alessandro Menozzi; Cristina Pozzoli; Gabriella Coruzzi; Ruengwit Kitbunnadaj; H Timmermann; Rob Leurs
Functional characterisation of the novel histamine H(3) receptor agonist, VUF 5810, on the guinea-pig isolated ileum.
Inflammation research : official journal of the European Histamine Research Society ... [et al.] 2004;53 Suppl 1():S77-8.
2004: Lindsay B Hough; Julia W Nalwalk; Konstantina Svokos; Rob Leurs; H Timmermann
Pain-relieving drugs and the brain histaminergic system: multiple analgesic mechanisms from histamine, improgan and cimetidine.
Inflammation research : official journal of the European Histamine Research Society ... [et al.] 2004;53 Suppl 1():S43-4.
2004: Remko A Bakker; David M Weiner; Antonius Marinus ter Laak; T Beuming; Obbe P Zuiderveld; M Edelbroek; Uli Hacksell; Henk Timmerman; Mark R Brann; Rob Leurs
8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist.
Molecular pharmacology 2004;65(3):538-49.
2004: Remko A Bakker; Paola Casarosa; Henk Timmerman; Martine J Smit; Rob Leurs
Constitutively active Gq/11-coupled receptors enable signaling by co-expressed G(i/o)-coupled receptors.
The Journal of biological chemistry 2004;279(7):5152-61.
2003: Marinella Govoni; Remko A Bakker; Ineke van de Wetering; Martine J Smit; Wiro M P B Menge; Henk Timmerman; Sigurd Elz; Walter Schunack; Rob Leurs
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
Journal of medicinal chemistry 2003;46(26):5812-24.
2003: Paola Casarosa; Yvonne K Gruijthuijsen; Detlef Michel; Patrick S Beisser; Jens Michael Holl; Carlos P Fitzsimons; Dennis Verzijl; Cathrien A Bruggeman; Thomas Mertens; Rob Leurs; Cornelis Vink; Martine J Smit
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 2003;278(50):50010-23.
2003: Ruengwit Kitbunnadaj; Obbe P Zuiderveld; Iwan J P De Esch; Roeland C Vollinga; Remko A Bakker; Martin Lutz; Anthony L Spek; Emile Cavoy; Marie-France Deltent; Wiro M P B Menge; Henk Timmerman; Rob Leurs
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Journal of medicinal chemistry 2003;46(25):5445-57.
2003: Martine J Smit; Pauline Verdijk; Elisabeth M H van der Raaij-Helmer; Marjon Navis; Paul J Hensbergen; Rob Leurs; Cornelis P Tensen
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 2003;102(6):1959-65.
2003: Takeshi Hashimoto; Shinya Harusawa; Lisa Araki; Obbe P Zuiderveld; Martine J Smit; Tomonari Imazu; Seiichiroh Takashima; Yumiko Yamamoto; Yasuhiko Sakamoto; Takushi Kurihara; Rob Leurs; Remko A Bakker; Atsushi Yamatodani
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 2003;46(14):3162-5.
2003: Martine J Smit; Cornelis Vink; Dennis Verzijl; Paola Casarosa; Cathrien A Bruggeman; Rob Leurs
Virally encoded G protein-coupled receptors: targets for potentially innovative anti-viral drug development.
Current drug targets 2003;4(5):431-41.
2003: Jalal Izadi Mobarakeh; Julia W Nalwalk; Takeshi Watanabe; Shinobu Sakurada; Marcel Hoffman; Rob Leurs; Henk Timmerman; Inmaculada Silos-Santiago; Kazuhiko Yanai; Lindsay B Hough
Improgan antinociception does not require neuronal histamine or histamine receptors.
Brain research 2003;974(1-2):146-52.
2003: Maria Waldhoer; Paola Casarosa; Mette M Rosenkilde; Martine J Smit; Rob Leurs; Jennifer L Whistler; Thue W Schwartz
The carboxyl terminus of human cytomegalovirus-encoded 7 transmembrane receptor US28 camouflages agonism by mediating constitutive endocytosis.
The Journal of biological chemistry 2003;278(21):19473-82.
2003: Paola Casarosa; Wiro M P B Menge; Rosalba Minisini; Claas Otto; Jane van Heteren; Aldo Jongejan; Henk Timmerman; Barbara Moepps; Frank Kirchhoff; Thomas Mertens; Martine J Smit; Rob Leurs
Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G protein-coupled receptor.
The Journal of biological chemistry 2003;278(7):5172-8.
2003: Tina Sallmen; Adrian F Lozada; Oleg V Anichtchik; Alexander L Beckman; Rob Leurs; Pertti Panula
Changes in hippocampal histamine receptors across the hibernation cycle in ground squirrels.
Hippocampus 2003;13(6):745-54.
2002: Lindsay B Hough; Julia W Nalwalk; Rebecca Stadel; Henk Timmerman; Rob Leurs; B C Paria; X Wang; S K Dey
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 2002;303(1):314-22.
2002: Raymond G Booth; Nader H Moniri; Remko A Bakker; Neepa Y Choksi; William B Nix; Henk Timmerman; Rob Leurs
A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors.
The Journal of pharmacology and experimental therapeutics 2002;302(1):328-36.
2002: Rob Leurs; M K Church; M Taglialatela
H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects.
Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology 2002;32(4):489-98.
2002: Martine J Smit; Dennis Verzijl; Paola Casarosa; Marjon Navis; Henk Timmerman; Rob Leurs
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 2002;76(4):1744-52.
2002: Yvonne K Gruijthuijsen; Paola Casarosa; Suzanne J F Kaptein; Jos L V Broers; Rob Leurs; Cathrien A Bruggeman; Martine J Smit; Cornelis Vink
The rat cytomegalovirus R33-encoded G protein-coupled receptor signals in a constitutive fashion.
Journal of virology 2002;76(3):1328-38.
2002: Remko A Bakker; Henk Timmerman; Rob Leurs
Histamine receptors: specific ligands, receptor biochemistry, and signal transduction.
Clinical allergy and immunology 2002;17():27-64.
2002: Rob Leurs; Marcel Hoffmann; Astrid E Alewijnse; Martine J Smit; Henk Timmerman
Methods to determine the constitutive activity of histamine H2 receptors.
Methods in enzymology 2002;343():405-16.
2001: Konstantina Svokos; Julia W Nalwalk; Rob Leurs; Wiro M P B Menge; Henk Timmerman; Lindsay B Hough
A role for spinal, but not supraspinal, alpha(2) adrenergic receptors in the actions of improgan, a powerful, non-opioid analgesic.
Brain research 2001;923(1-2):12-9.
2001: Kerstin Wieland; Gerold Bongers; Yumiko Yamamoto; Takeshi Hashimoto; Atsushi Yamatodani; Wiro M P B Menge; Henk Timmerman; T W Lovenberg; Rob Leurs
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
The Journal of pharmacology and experimental therapeutics 2001;299(3):908-14.
2001: Remko A Bakker; S B Schoonus; Martine J Smit; Henk Timmerman; Rob Leurs
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 2001;60(5):1133-42.
2001: A Alves-Rodrigues; S Lemstra; Roeland C Vollinga; Wiro M P B Menge; Henk Timmerman; Rob Leurs
Pharmacological analysis of immepip and imetit homologues. Further evidence for histamine H(3) receptor heterogeneity?
Behavioural brain research 2001;124(2):121-7.
2001: Marcel Hoffmann; Dennis Verzijl; Kenneth Lundstrom; Urs Simmen; Astrid E Alewijnse; Henk Timmerman; Rob Leurs
Recombinant Semliki Forest virus for over-expression and pharmacological characterisation of the histamine H(2) receptor in mammalian cells.
European journal of pharmacology 2001;427(2):105-14.
2001: Iwan J P De Esch; JE Mills; TD Perkins; Giuseppe Romeo; Marcel Hoffmann; Kerstin Wieland; Rob Leurs; Wiro M P B Menge; PH Nederkoorn; Philip M Dean; Henk Timmerman
Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.
Journal of medicinal chemistry 2001;44(11):1666-74.
2001: Lindsay B Hough; Julia W Nalwalk; Rob Leurs; Wiro M P B Menge; Henk Timmerman
Significance of GABAergic systems in the action of improgan, a non-opioid analgesic.
Life sciences 2001;68(24):2751-7.
2001: Minnamaija Lintunen; Petri Hyytiä; Tina Sallmen; Kaj Karlstedt; Leena Tuomisto; Rob Leurs; Kalervo Kiianmaa; Esa R Korpi; Pertti Panula
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 2001;15(6):1074-6.
2001: Paola Casarosa; Remko A Bakker; Dennis Verzijl; Marjon Navis; Henk Timmerman; Rob Leurs; Martine J Smit
Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28.
The Journal of biological chemistry 2001;276(2):1133-7.
2001: Guillaume Drutel; Nina Peitsaro; Kaj Karlstedt; Kerstin Wieland; Martine J Smit; Henk Timmerman; Pertti Panula; Rob Leurs
Identification of rat H3 receptor isoforms with different brain expression and signaling properties.
Molecular pharmacology 2001;59(1):1-8.
2000: M S Rodriguez-Pena; Henk Timmerman; Rob Leurs
Modulation of histamine H(2) receptor signalling by G-protein-coupled receptor kinase 2 and 3.
British journal of pharmacology 2000;131(8):1707-15.
2000: Lindsay B Hough; Julia W Nalwalk; Y Chen; A Schuller; Y Zhu; J Zhang; Wiro M P B Menge; Rob Leurs; Henk Timmerman; John E Pintar
Improgan, a cimetidine analog, induces morphine-like antinociception in opioid receptor-knockout mice.
Brain research 2000;880(1-2):102-8.
2000: Frank Jansen; T Mochizuki; K Maeyama; Rob Leurs; Henk Timmerman
Characterization of histamine H3 receptors in mouse brain using the H3 antagonist [125I]iodophenpropit.
Naunyn-Schmiedeberg's archives of pharmacology 2000;362(1):60-7.
2000: Albert D Windhorst; Henk Timmerman; E A Worthington; GJ Bijloo; PH Nederkoorn; Wiro M P B Menge; Rob Leurs; J D M Herscheid
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 2000;43(9):1754-61.
2000: Astrid E Alewijnse; Henk Timmerman; Edwin H Jacobs; Martine J Smit; E Roovers; S Cotecchia; Rob Leurs
The effect of mutations in the DRY motif on the constitutive activity and structural instability of the histamine H(2) receptor.
Molecular pharmacology 2000;57(5):890-8.
2000: Rob Leurs; M S Rodriguez Pena; R A Bakker; Astrid E Alewijnse; Henk Timmerman
Constitutive activity of G protein coupled receptors and drug action.
Pharmaceutica acta Helvetiae 2000;74(2-3):327-31.
2000: Martine J Smit; Henk Timmerman; Dennis Verzijl; Rob Leurs
Viral-encoded G-protein coupled receptors: new targets for drug research?
Pharmaceutica acta Helvetiae 2000;74(2-3):299-304.
2000: Remko A Bakker; Kerstin Wieland; Henk Timmerman; Rob Leurs
Constitutive activity of the histamine H(1) receptor reveals inverse agonism of histamine H(1) receptor antagonists.
European journal of pharmacology 2000;387(1):R5-7.
2000: Lindsay B Hough; Julia W Nalwalk; W G Barnes; Rob Leurs; Wiro M P B Menge; Henk Timmerman; Mark P Wentland
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 2000;909():25-40.
2000: Lindsay B Hough; Julia W Nalwalk; Rob Leurs; Wiro M P B Menge; Henk Timmerman
Antinociceptive activity of derivatives of improgran and burimamide.
Pharmacology, biochemistry, and behavior 2000;65(1):61-6.
2000: Rob Leurs; Marcel Hoffmann; Kerstin Wieland; Henk Timmerman
H3 receptor gene is cloned at last.
Trends in pharmacological sciences 2000;21(1):11-2.
1999: Kerstin Wieland; Antonius Marinus ter Laak; Martine J Smit; R Kühne; Henk Timmerman; Rob Leurs
Mutational analysis of the antagonist-binding site of the histamine H(1) receptor.
The Journal of biological chemistry 1999;274(42):29994-30000.
1999: Albert D Windhorst; Henk Timmerman; Rob P Klok; Wiro M P B Menge; Rob Leurs; J D M Herscheid
Evaluation of [18F]VUF 5000 as a potential PET ligand for brain imaging of the histamine H3 receptor.
Bioorganic & medicinal chemistry 1999;7(9):1761-7.
1999: Albert D Windhorst; Henk Timmerman; Rob P Klok; F G Custers; Wiro M P B Menge; Rob Leurs; Holger Stark; Walter Schunack; E G Gielen; M J van Kroonenburgh; J D M Herscheid
Radiosynthesis and biodistribution of 123I-labeled antagonists of the histamine H3 receptor as potential SPECT ligands.
Nuclear medicine and biology 1999;26(6):651-9.
1999: Cornelis P Tensen; Jacoba Flier; Elisabeth M H van der Raaij-Helmer; SC Sampat-Sardjoepersad; Roel C Van Der Schors; Rob Leurs; Rik J Scheper; Dick M Boorsma; Rein Willemze
Human IP-9: A keratinocyte-derived high affinity CXC-chemokine ligand for the IP-10/Mig receptor (CXCR3).
The Journal of investigative dermatology 1999;112(5):716-22.
1999: Iwan J P De Esch; Roeland C Vollinga; Kees Goubitz; Henk Schenk; U Appelberg; Uli Hacksell; S Lemstra; Obbe P Zuiderveld; Marcel Hoffmann; Rob Leurs; Wiro M P B Menge; Henk Timmerman
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 1999;42(7):1115-22.
1999: Lindsay B Hough; Julia W Nalwalk; Rob Leurs; Wiro M P B Menge; Henk Timmerman
Antinociceptive activity of impentamine, a histamine congener, after CNS administration.
Life sciences 1999;64(5):PL79-86.
1998: M D Bannoura; Julia W Nalwalk; Y Tang; M Carlile; Rob Leurs; Wiro M P B Menge; Henk Timmerman; Lindsay B Hough
Absence of antinociceptive tolerance to improgan, a cimetidine analog, in rats.
Brain research 1998;814(1-2):218-21.
1998: Rob Leurs; Martine J Smit; Astrid E Alewijnse; Henk Timmerman
Agonist-independent regulation of constitutively active G-protein-coupled receptors.
Trends in biochemical sciences 1998;23(11):418-22.
1998: Cornelis P Tensen; KJ Cox; Julian Burke; Rob Leurs; Roel C Van Der Schors; Wijnand P M Geraerts; E Vreugdenhil; H Heerikhuizen
Molecular cloning and characterization of an invertebrate homologue of a neuropeptide Y receptor.
The European journal of neuroscience 1998;10(11):3409-16.
1998: Astrid E Alewijnse; Martine J Smit; Marcel Hoffmann; Dennis Verzijl; Henk Timmerman; Rob Leurs
Constitutive activity and structural instability of the wild-type human H2 receptor.
Journal of neurochemistry 1998;71(2):799-807.
1998: Rob Leurs; patrizio blandina; C Tedford; Henk Timmerman
Therapeutic potential of histamine H3 receptor agonists and antagonists.
Trends in pharmacological sciences 1998;19(5):177-83.
1998: A Alves-Rodrigues; Henk Timmerman; E Willems; S Lemstra; Obbe P Zuiderveld; Rob Leurs
Pharmacological characterisation of the histamine H3 receptor in the rat hippocampus.
Brain research 1998;788(1-2):179-86.
1998: Martine J Smit; Henk Timmerman; Astrid E Alewijnse; Rob Leurs
From histamine H2 receptor regulation to reclassification of H2 antagonists; inverse agonism as the basis for H2 receptor upregulation.
Receptors & channels 1998;5(2):99-102.
1997: Astrid E Alewijnse; Martine J Smit; M S Rodriguez Pena; Dennis Verzijl; Henk Timmerman; Rob Leurs
Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active G(S)-coupled receptors.
FEBS letters 1997;419(2-3):171-4.
1997: Lindsay B Hough; Julia W Nalwalk; B Y Li; Rob Leurs; Wiro M P B Menge; Henk Timmerman; M E Carlile; C Cioffi; Mark P Wentland
Novel qualitative structure-activity relationships for the antinociceptive actions of H2 antagonists, H3 antagonists and derivatives.
The Journal of pharmacology and experimental therapeutics 1997;283(3):1534-43.
1997: Margot W Beukers; Corné Klaassen; Willem J De Grip; Dennis Verzijl; Henk Timmerman; Rob Leurs
Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
British journal of pharmacology 1997;122(5):867-74.