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Rob Leurs

This is a preview profile on BiomedExperts - the first literature-based scientific social network. It brings the right researchers together and allows them to collaborate online. Collexis and Dell provide the BiomedExperts network of +1.5 Million pre-calculated profiles free of charge to researchers worldwide.

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Publications

TOP 3
Maussang David; Vischer Henry F; Leurs Rob; Smit Martine J
Herpesvirus-encoded G protein-coupled receptors as modulators of cellular function.
Engelhardt Harald; Smits Rogier A; Leurs Rob; Haaksma Eric; de Esch Iwan J P
A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic.
Mariottini Chiara; Scartabelli Tania; Bongers Gerold; Arrigucci Silvia; Nosi Daniele; Leurs Rob; Chiarugi Alberto; Blandina Patrizio; Pellegrini-Giampietro Domenico E; Beatrice Passani Maria
Activation of the histaminergic H3 receptor induces phosphorylation of the Akt/GSK-3 beta pathway in cultured cortical neurons and protects against neurotoxic insults.

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All Publications

2009: Maussang David; Vischer Henry F; Leurs Rob; Smit Martine J
Herpesvirus-encoded G protein-coupled receptors as modulators of cellular function.
Molecular pharmacology 2009;76(4):692-701.
2009: Engelhardt Harald; Smits Rogier A; Leurs Rob; Haaksma Eric; de Esch Iwan J P
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: Mariottini Chiara; Scartabelli Tania; Bongers Gerold; Arrigucci Silvia; Nosi Daniele; Leurs Rob; Chiarugi Alberto; Blandina Patrizio; Pellegrini-Giampietro Domenico E; Beatrice Passani Maria
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: Smits Rogier A; Leurs Rob; de Esch Iwan J P
Major advances in the development of histamine H4 receptor ligands.
Drug discovery today 2009;14(15-16):745-53.
2009: de Kloe Gerdien E; Bailey David; Leurs Rob; de Esch Iwan J P
Transforming fragments into candidates: small becomes big in medicinal chemistry.
Drug discovery today 2009;14(13-14):630-46.
2009: Célanire Sylvain; Wijtmans Maikel; Christophe Bernard; Collart Philippe; de Esch Iwan; Dassesse Donald; Delaunoy Christel; Denonne Frédéric; Durieu Véronique; Gelens Edith; Gillard Michel; Lallemand Bénédicte; Lamberty Yves; Lebon Florence; Nicolas Jean-Marie; Quéré Luc; Snip Erwin; Vanbellinghen Alain; Van Houtvin Nathalie; Verbois Valérie; Timmerman Henk; Talaga Patrice; Leurs Rob; Provins Laurent
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: Lim Herman D; Istyastono Enade P; van de Stolpe Andrea; Romeo Giuseppe; Gobbi Silvia; Schepers Marjo; Lahaye Roger; Menge Wiro M B P; Zuiderveld Obbe P; Jongejan Aldo; Smits Rogier A; Bakker Remko A; Haaksma Eric E J; Leurs Rob; de Esch Iwan J P
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: Lim Herman D; Adami Maristella; Guaita Elena; Werfel Thomas; Smits Rogier A; de Esch Iwan J P; Bakker Remko A; Gutzmer Ralf; Coruzzi Gabriella; Leurs Rob
Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430.
British journal of pharmacology 2009;157(1):34-43.
2009: Leurs Rob; Chazot Paul L; Shenton Fiona C; Lim Herman D; de Esch Iwan J P
Molecular and biochemical pharmacology of the histamine H4 receptor.
British journal of pharmacology 2009;157(1):14-23.
2009: de Kruijf Petra; van Heteren Jane; Lim Herman D; Conti Paolo G M; van der Lee Miranda M C; Bosch Leontien; Ho Koc-Kan; Auld Douglas; Ohlmeyer Michael; Smit Martin J; Wijkmans Jac C H M; Zaman Guido J R; Smit Martine J; Leurs Rob
Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor.
The Journal of pharmacology and experimental therapeutics 2009;329(2):783-90.
2009: Maussang David; Langemeijer Ellen; Fitzsimons Carlos P; Stigter-van Walsum Marijke; Dijkman Remco; Borg Martin K; Slinger Erik; Schreiber Andreas; Michel Detlef; Tensen Cornelis P; van Dongen Guus A M S; Leurs Rob; Smit Martine J
The human cytomegalovirus-encoded chemokine receptor US28 promotes angiogenesis and tumor formation via cyclooxygenase-2.
Cancer research 2009;69(7):2861-9.
2009: Wijtmans Maikel; Verzijl Dennis; van Dam Cindy M E; Bosch Leontien; Smit Martine J; Leurs Rob; de Esch Iwan J P
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.
2008: Vischer Henry F; Nijmeijer Saskia; Smit Martine J; Leurs Rob
Viral hijacking of human receptors through heterodimerization.
Biochemical and biophysical research communications 2008;377(1):93-7.
2008: Lim Herman D; Jongejan Aldo; Bakker Remko A; Haaksma Eric; de Esch Iwan J P; Leurs Rob
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: Jiang Wen; Lim Herman D; Zhang Mai; Desai Pragnya; Dai Heng; Colling Patricia M; Leurs Rob; Thurmond Robin L
Cloning and pharmacological characterization of the dog histamine H4 receptor.
European journal of pharmacology 2008;592(1-3):26-32.
2008: van Rijn Richard M; van Marle André; Chazot Paul L; Langemeijer Ellen; Qin Yongjun; Shenton Fiona C; Lim Herman D; Zuiderveld Obbe P; Sansuk Kamonchanok; Dy Michel; Smit Martine J; Tensen Cornelis P; Bakker Remko A; Leurs Rob
Cloning and characterization of dominant negative splice variants of the human histamine H4 receptor.
The Biochemical journal 2008;414(1):121-31.
2008: Wijtmans Maikel; Verzijl Dennis; Leurs Rob; de Esch Iwan J P; Smit Martine J
Towards small-molecule CXCR3 ligands with clinical potential.
ChemMedChem 2008;3(6):861-72.
2008: Wijtmans Maikel; Celanire Sylvain; Snip Erwin; Gillard Michel R; Gelens Edith; Collart Philippe P; Venhuis Bastiaan J; Christophe Bernard; Hulscher Saskia; van der Goot Henk; Lebon Florence; Timmerman Henk; Bakker Remko A; Lallemand Bénédicte I L F; Leurs Rob; Talaga Patrice E; de Esch Iwan J P
4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
Journal of medicinal chemistry 2008;51(10):2944-53.
2008: Verzijl Dennis; Storelli Stefania; Scholten Danny J; Bosch Leontien; Reinhart Todd A; Streblow Daniel N; Tensen Cornelis P; Fitzsimons Carlos P; Zaman Guido J R; Pease James E; de Esch Iwan J P; Smit Martine J; Leurs Rob
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: Smits Rogier A; Lim Herman D; Hanzer Agnes; Zuiderveld Obbe P; Guaita Elena; Adami Maristella; Coruzzi Gabriella; Leurs Rob; de Esch Iwan J P
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; Balog Crina I A; van der Does Anne M; Booth Raymond; de Grip Willem J; Deelder André M; Bakker Remko A; Leurs Rob; Hensbergen Paul J
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: Bakker Remko A; Jongejan Aldo; Sansuk Kamonchanok; Hacksell Uli; Timmerman Henk; Brann Mark R; Weiner Dave M; Pardo Leonardo; Leurs Rob
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.
2008: Booth R G; 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.] 2008;57 Suppl 1():S43-4.
2007: Kool Jeroen; van Marle André; Hulscher Saskia; Selman Maurice; van Iperen Dick J; van Altena Klaas; Gillard Michel; Bakker Remko A; Irth Hubertus; Leurs Rob; Vermeulen Nico P E
A flow-through fluorescence polarization detection system for measuring GPCR-mediated modulation of cAMP production.
Journal of biomolecular screening : the official journal of the Society for Biomolecular Screening 2007;12(8):1074-83.
2007: Bongers Gerold; Krueger Kathleen M; Miller Thomas R; Baranowski John L; Estvander Brian R; Witte David G; Strakhova Marina I; van Meer Peter; Bakker Remko A; Cowart Marlon D; Hancock Arthur A; Esbenshade Timothy A; Leurs Rob
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: Cannon Keri E; Leurs Rob; Hough Lindsay B
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: Hough L B; Menge W M P B; van de Stolpe A C; Nalwalk J W; Leurs R; de Esch I J P
Antinociceptive activity of furan-containing congeners of improgan and ranitidine.
Bioorganic & medicinal chemistry letters 2007;17(20):5715-9.
2007: Bongers Gerold; Sallmen Tina; Passani Maria Beatrice; Mariottini Chiara; Wendelin Dominique; Lozada Adrian; Marle André van; Navis Marjon; Blandina Patrizio; Bakker Remko A; Panula Pertti; Leurs Rob
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: Wijtmans Maikel; Leurs Rob; de Esch Iwan
Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas.
Expert opinion on investigational drugs 2007;16(7):967-85.
2007: Bakker R A; Nicholas M W; Smith T T; Burstein E S; Hacksell U; Timmerman H; Leurs R; Brann M R; Weiner D M
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: Storelli Stefania; Verzijl Dennis; Al-Badie Jawad; Elders Niels; Bosch Leontien; Timmerman Henk; Smit Martine J; De Esch Iwan J P; Leurs Rob
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: Coruzzi Gabriella; Adami Maristella; Guaita Elena; de Esch Iwan J P; Leurs Rob
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: Hulsman Niels; Medema Jan Paul; Bos Carina; Jongejan Aldo; Leurs Rob; Smit Martine J; de Esch Iwan J P; Richel Dick; Wijtmans Maikel
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: Bongers Gerold; Bakker Remko A; Leurs Rob
Molecular aspects of the histamine H3 receptor.
Biochemical pharmacology 2007;73(8):1195-204.
2007: Ratnala Venkata R P; Kiihne Suzanne R; Buda Francesco; Leurs Rob; de Groot Huub J M; DeGrip Willem J
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: Smit Martine J; Vischer Henry F; Bakker Remko A; Jongejan Aldo; Timmerman Henk; Pardo Leonardo; Leurs Rob
Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity.
Annual review of pharmacology and toxicology 2007;47():53-87.
2006: Lim Herman D; Smits Rogier A; Bakker Remko A; van Dam Cindy M E; de Esch Iwan J P; Leurs Rob
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: Verzijl Dennis; Pardo Leonardo; van Dijk Marie; Gruijthuijsen Yvonne K; Jongejan Aldo; Timmerman Henk; Nicholas John; Schwarz Mario; Murphy Philip M; Leurs Rob; Smit Martine J
Helix 8 of the viral chemokine receptor ORF74 directs chemokine binding.
The Journal of biological chemistry 2006;281(46):35327-35.
2006: Hulshof Janneke W; Vischer Henry F; Verheij Mark H P; Fratantoni Silvina A; Smit Martine J; de Esch Iwan J P; Leurs Rob
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: Hough Lindsay B; de Esch Iwan J P; Janssen Elwin; Phillips James; Svokos Konstantina; Kern Brian; Trachler Jennifer; Abood Mary E; Leurs Rob; Nalwalk Julia W
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: Maussang David; Verzijl Dennis; van Walsum Marijke; Leurs Rob; Holl Jens; Pleskoff Olivier; Michel Detlef; van Dongen Guus A M S; Smit Martine J
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: van Rijn Richard M; Chazot Paul L; Shenton Fiona C; Sansuk Kamonchanok; Bakker Remko A; Leurs Rob
Oligomerization of recombinant and endogenously expressed human histamine H(4) receptors.
Molecular pharmacology 2006;70(2):604-15.
2006: Smits Rogier A; Lim Herman D; Stegink Bart; Bakker Remko A; de Esch Iwan J P; Leurs Rob
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: Govoni Marinella; Lim Herman D; El-Atmioui Dris; Menge Wiro M P B; Timmerman Henk; Bakker Remko A; Leurs Rob; De Esch Iwan J P
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: Bakker Remko A; Lozada Adrian Flores; van Marle André; Shenton Fiona C; Drutel Guillaume; Karlstedt Kaj; Hoffmann Marcel; Lintunen Minnamaija; Yamamoto Yumiko; van Rijn Richard M; Chazot Paul L; Panula Pertti; Leurs Rob
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: Fitzsimons Carlos P; Gompels Ursula A; Verzijl Dennis; Vischer Henry F; Mattick Claire; Leurs Rob; Smit Martine J
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: Gelens E; De Kanter F J J; Schmitz R F; Sliedregt L A J M; Van Steen B J; Kruse Chris G; Leurs R; Groen M B; Orru R V A
Efficient library synthesis of imidazoles using a multicomponent reaction and microwave irradiation.
Molecular diversity 2006;10(1):17-22.
2006: Vischer Henry F; Leurs Rob; Smit Martine J
HCMV-encoded G-protein-coupled receptors as constitutively active modulators of cellular signaling networks.
Trends in pharmacological sciences 2006;27(1):56-63.
2006: Vischer H F; Hulshof J W; de Esch I J P; Smit M J; 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 2006;(2):187-209.
2006: Lim Herman D; Smits Rogier A; Leurs Rob; De Esch Iwan J P
The emerging role of the histamine H4 receptor in anti-inflammatory therapy.
Current topics in medicinal chemistry 2006;6(13):1365-73.
2005: Celanire Sylvain; Wijtmans Maikel; Talaga Patrice; Leurs Rob; de Esch Iwan J P
Keynote review: histamine H3 receptor antagonists reach out for the clinic.
Drug discovery today 2005;10(23-24):1613-27.
2005: Kitbunnadaj Ruengwit; Hoffmann Marcel; Fratantoni Silvina A; Bongers Gerold; Bakker Remko A; Wieland Kerstin; el Jilali Ahmed; De Esch Iwan J P; Menge Wiro M P B; Timmerman Henk; Leurs Rob
New high affinity H3 receptor agonists without a basic side chain.
Bioorganic & medicinal chemistry 2005;13(23):6309-23.
2005: Hulshof Janneke W; Casarosa Paola; Menge Wiro M P B; Kuusisto Leena M S; van der Goot Henk; Smit Martine J; de Esch Iwan J P; Leurs Rob
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: Bruysters Martijn; Jongejan Aldo; Akdemir Atilla; Bakker Remko A; Leurs Rob
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: de Esch Iwan J P; Thurmond Robin L; Jongejan Aldo; Leurs Rob
The histamine H4 receptor as a new therapeutic target for inflammation.
Trends in pharmacological sciences 2005;26(9):462-9.
2005: Lim Herman D; van Rijn Richard M; Ling Ping; Bakker Remko A; Thurmond Robin L; Leurs Rob
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: Pleskoff Olivier; Casarosa Paola; Verneuil Laurence; Ainoun Fadela; Beisser Patrick; Smit Martine; Leurs Rob; Schneider Pascal; Michelson Susan; Ameisen Jean Claude
The human cytomegalovirus-encoded chemokine receptor US28 induces caspase-dependent apoptosis.
The FEBS journal 2005;272(16):4163-77.
2005: Jongejan Aldo; Bruysters Martijn; Ballesteros Juan A; Haaksma Eric; Bakker Remko A; Pardo Leonardo; Leurs Rob
Linking agonist binding to histamine H1 receptor activation.
Nature chemical biology 2005;1(2):98-103.
2005: Jongejan Aldo; Leurs Rob
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: Storelli Stefania; Verdijk Pauline; Verzijl Dennis; Timmerman Henk; van de Stolpe Andrea C; Tensen Cornelis P; Smit Martine J; De Esch Iwan J P; Leurs Rob
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: Bruysters Martijn; Jongejan Aldo; Gillard Michel; van de Manakker Frank; Bakker Remko A; Chatelain Pierre; Leurs Rob
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: Kitbunnadaj Ruengwit; Hashimoto Takeshi; Poli Enzo; Zuiderveld Obbe P; Menozzi Alessandro; Hidaka Ryoko; de Esch Iwan J P; Bakker Remko A; Menge Wiro M P B; Yamatodani Atsushi; Coruzzi Gabriella; Timmerman Henk; Leurs Rob
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: Nalwalk J W; Svokos K; Leurs R; Hough L B
Absence of 5-HT3 and cholinergic mechanisms in improgan antinociception.
Pharmacology, biochemistry, and behavior 2005;80(3):505-10.
2005: de Ligt Rianne A F; Rivkees Scott A; Lorenzen Anna; Leurs Rob; IJzerman Ad P
A "locked-on," constitutively active mutant of the adenosine A1 receptor.
European journal of pharmacology 2005;510(1-2):1-8.
2005: Leurs Rob; Bakker Remko A; Timmerman Henk; de Esch Iwan J P
The histamine H3 receptor: from gene cloning to H3 receptor drugs.
Nature reviews. Drug discovery 2005;4(2):107-20.
2005: Casarosa Paola; Waldhoer Maria; LiWang Patricia J; Vischer Henry F; Kledal Thomas; Timmerman Henk; Schwartz Thue W; Smit Martine J; Leurs Rob
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: Beisser Patrick S; Verzijl Dennis; Gruijthuijsen Yvonne K; Beuken Erik; Smit Martine J; Leurs Rob; Bruggeman Cathrien A; Vink Cornelis
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.
2005: Jongejan Aldo; de Graaf Chris; Vermeulen Nico P E; Leurs Rob; de Esch Iwan J P
The role and application of in silico docking in chemical genomics research.
Methods in molecular biology (Clifton, N.J.) 2005;310():63-91.
2005: Lozada A; Munyao N; Sallmen T; Lintunen M; Leurs R; Lindsberg P J; Panula P
Postischemic regulation of central histamine receptors.
Neuroscience 2005;136(1):371-9.
2004: Terzioglu Nalan; van Rijn Richard M; Bakker Remko A; De Esch Iwan J P; Leurs Rob
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: Bakker Remko A; Dees Guido; Carrillo Juan J; Booth Raymond G; López-Gimenez Juan F; Milligan Graeme; Strange Philip G; Leurs Rob
Domain swapping in the human histamine H1 receptor.
The Journal of pharmacology and experimental therapeutics 2004;311(1):131-8.
2004: Klaasse Elisabeth; de Ligt Rianne A F; Roerink Sophie F; Lorenzen Anna; Milligan Graeme; Leurs Rob; IJzerman Ad P
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: Nalwalk J W; Svokos K; Taraschenko O; Leurs R; Timmerman H; Hough L B
Activation of brain stem nuclei by improgan, a non-opioid analgesic.
Brain research 2004;1021(2):248-55.
2004: Ratnala Venkata R P; Swarts Herman G P; VanOostrum Jenny; Leurs Rob; DeGroot Huub J M; Bakker Remko A; DeGrip Willem J
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: Kitbunnadaj Ruengwit; Zuiderveld Obbe P; Christophe Bernard; Hulscher Saskia; Menge Wiro M P B; Gelens Edith; Snip Erwin; Bakker Remko A; Celanire Sylvain; Gillard Michel; Talaga Patrice; Timmerman Henk; Leurs Rob
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: Gruijthuijsen Yvonne K; Beuken Erik V H; Smit Martine J; Leurs Rob; Bruggeman Cathrien A; Vink Cornelis
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: Verzijl Dennis; Fitzsimons Carlos P; Van Dijk Marie; Stewart James P; Timmerman Henk; Smit Martine J; Leurs Rob
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: Hensbergen Paul J; Verzijl Dennis; Balog Crina I A; Dijkman Remco; van der Schors Roel C; van der Raaij-Helmer Elizabeth M H; van der Plas Mariena J A; Leurs Rob; Deelder André M; Smit Martine J; Tensen Cornelis P
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: Poli E; Menozzi A; Pozzoli C; Coruzzi G; Kitbunnadaj R; Timmermann H; Leurs R
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: Hough L B; Nalwalk J W; Svokos K; Leurs R; Timmermann H
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: Bruysters Martijn; Pertz Heinz H; Teunissen Aloys; Bakker Remko A; Gillard Michel; Chatelain Pierre; Schunack Walter; Timmerman Henk; Leurs Rob
Mutational analysis of the histamine H1-receptor binding pocket of histaprodifens.
European journal of pharmacology 2004;487(1-3):55-63.
2004: Bakker R A; Weiner D M; ter Laak T; Beuming T; Zuiderveld O P; Edelbroek M; Hacksell U; Timmerman H; Brann M R; Leurs R
8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist.
Molecular pharmacology 2004;65(3):538-49.
2004: Bakker Remko A; Casarosa Paola; Timmerman Henk; Smit Martine J; Leurs Rob
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: Govoni Marinella; Bakker Remko A; van de Wetering Ineke; Smit Martine J; Menge Wiro M B P; Timmerman Henk; Elz Sigurd; Schunack Walter; Leurs Rob
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
Journal of medicinal chemistry 2003;46(26):5812-24.
2003: Kitbunnadaj Ruengwit; Zuiderveld Obbe P; De Esch Iwan J P; Vollinga Roeland C; Bakker Remko; Lutz Martin; Spek Anthony L; Cavoy Emile; Deltent Marie-France; Menge Wiro M P B; Timmerman Henk; Leurs Rob
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Journal of medicinal chemistry 2003;46(25):5445-57.
2003: Casarosa Paola; Gruijthuijsen Yvonne K; Michel Detlef; Beisser Patrick S; Holl Jens; Fitzsimons Carlos P; Verzijl Dennis; Bruggeman Cathrien A; Mertens Thomas; Leurs Rob; Vink Cornelis; Smit Martine J
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: Smit Martine J; Verdijk Pauline; van der Raaij-Helmer Elisabeth M H; Navis Marjon; Hensbergen Paul J; Leurs Rob; Tensen Cornelis P
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: Hashimoto Takeshi; Harusawa Shinya; Araki Lisa; Zuiderveld Obbe P; Smit Martine J; Imazu Tomonari; Takashima Seiichiroh; Yamamoto Yumiko; Sakamoto Yasuhiko; Kurihara Takushi; Leurs Rob; Bakker Remko A; Yamatodani Atsushi
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: Smit M J; Vink C; Verzijl D; Casarosa P; Bruggeman C A; Leurs R
Virally encoded G protein-coupled receptors: targets for potentially innovative anti-viral drug development.
Current drug targets 2003;4(5):431-41.
2003: Izadi Mobarakeh Jalal; Nalwalk Julia W; Watanabe Takeshi; Sakurada Shinobu; Hoffman Marcel; Leurs Rob; Timmerman Henk; Silos-Santiago Immaculada; Yanai Kazuhiko; Hough Lindsay B
Improgan antinociception does not require neuronal histamine or histamine receptors.
Brain research 2003;974(1-2):146-52.
2003: Waldhoer Maria; Casarosa Paola; Rosenkilde Mette M; Smit Martine J; Leurs Rob; Whistler Jennifer L; Schwartz Thue W
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: Casarosa Paola; Menge Wiro M; Minisini Rosalba; Otto Claas; van Heteren Jane; Jongejan Aldo; Timmerman Henk; Moepps Barbara; Kirchhoff Frank; Mertens Thomas; Smit Martine J; Leurs Rob
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: Sallmen Tina; Lozada Adrian F; Anichtchik Oleg V; Beckman Alexander L; Leurs Rob; Panula Pertti
Changes in hippocampal histamine receptors across the hibernation cycle in ground squirrels.
Hippocampus 2003;13(6):745-54.
2002: Hough L B; Nalwalk J W; Stadel R; Timmerman H; Leurs R; Paria B C; Wang X; Dey S K
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: Booth Raymond G; Moniri Nader H; Bakker Remko A; Choksi Neepa Y; Nix William B; Timmerman Henk; Leurs Rob
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: Leurs R; Church M K; Taglialatela M
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: Smit Martine J; Verzijl Dennis; Casarosa Paola; Navis Marjon; Timmerman Henk; Leurs Rob
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: Gruijthuijsen Yvonne K; Casarosa Paola; Kaptein Suzanne J F; Broers Jos L V; Leurs Rob; Bruggeman Cathrien A; Smit Martine J; Vink Cornelis
The rat cytomegalovirus R33-encoded G protein-coupled receptor signals in a constitutive fashion.
Journal of virology 2002;76(3):1328-38.
2002: Bakker Remko A; Timmerman Hendrik; Leurs Rob
Histamine receptors: specific ligands, receptor biochemistry, and signal transduction.
Clinical allergy and immunology 2002;17():27-64.
2002: Leurs Rob; Hoffmann Marcel; Alewijnse Astrid E; Smit Martine J; Timmerman Henk
Methods to determine the constitutive activity of histamine H2 receptors.
Methods in enzymology 2002;343():405-16.
2001: Svokos K; Nalwalk J W; Leurs R; Menge W M; Timmerman H; Hough L B
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: Wieland K; Bongers G; Yamamoto Y; Hashimoto T; Yamatodani A; Menge W M; Timmerman H; Lovenberg T W; Leurs R
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: Bakker R A; Schoonus S B; Smit M J; 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 2001;60(5):1133-42.
2001: Alves-Rodrigues A; Lemstra S; Vollinga R C; Menge W M; Timmerman H; Leurs R
Pharmacological analysis of immepip and imetit homologues. Further evidence for histamine H(3) receptor heterogeneity?
Behavioural brain research 2001;124(2):121-7.
2001: Hoffmann M; Verzijl D; Lundstrom K; Simmen U; Alewijnse A E; 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 2001;427(2):105-14.
2001: Hough L B; Nalwalk J W; Leurs R; Menge W M; Timmerman H
Significance of GABAergic systems in the action of improgan, a non-opioid analgesic.
Life sciences 2001;68(24):2751-7.
2001: De Esch I J; Mills J E; Perkins T D; Romeo G; Hoffmann M; Wieland K; Leurs R; Menge W M; Nederkoorn P H; Dean P M; Timmerman H
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: Lintunen M; Hyytiä P; Sallmen T; Karlstedt K; Tuomisto L; Leurs R; Kiianmaa K; Korpi E R; Panula P
Increased brain histamine in an alcohol-preferring rat line and modulation of ethanol consumption by H(3) receptor mechanisms.
The FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2001;15(6):1074-6.
2001: Drutel G; Peitsaro N; Karlstedt K; Wieland K; Smit M J; Timmerman H; Panula P; Leurs R
Identification of rat H3 receptor isoforms with different brain expression and signaling properties.
Molecular pharmacology 2001;59(1):1-8.
2001: Casarosa P; Bakker R A; Verzijl D; Navis M; Timmerman H; Leurs R; Smit M J
Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28.
The Journal of biological chemistry 2001;276(2):1133-7.
2000: Rodriguez-Pena M S; Timmerman H; Leurs R
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: Hough L B; Nalwalk J W; Chen Y; Schuller A; Zhu Y; Zhang J; Menge W M; Leurs R; Timmerman H; Pintar J E
Improgan, a cimetidine analog, induces morphine-like antinociception in opioid receptor-knockout mice.
Brain research 2000;880(1-2):102-8.
2000: Jansen F P; 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 2000;362(1):60-7.
2000: Windhorst A D; Timmerman H; Worthington E A; Bijloo G J; Nederkoorn P H; Menge W M; Leurs R; Herscheid J D
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: Alewijnse A E; Timmerman H; Jacobs E H; Smit M J; Roovers E; Cotecchia S; Leurs R
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: Leurs R; Rodriguez Pena M S; Bakker R A; Alewijnse A E; Timmerman H
Constitutive activity of G protein coupled receptors and drug action.
Pharmaceutica acta Helvetiae 2000;74(2-3):327-31.
2000: Smit M J; Timmerman H; Verzijl D; Leurs R
Viral-encoded G-protein coupled receptors: new targets for drug research?
Pharmaceutica acta Helvetiae 2000;74(2-3):299-304.
2000: Hough L B; Nalwalk J W; Leurs R; Menge W M; Timmerman H
Antinociceptive activity of derivatives of improgran and burimamide.
Pharmacology, biochemistry, and behavior 2000;65(1):61-6.
2000: Leurs R; Hoffmann M; Wieland K; Timmerman H
H3 receptor gene is cloned at last.
Trends in pharmacological sciences 2000;21(1):11-2.
2000: Bakker R A; 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 2000;387(1):R5-7.
2000: Hough L B; Nalwalk J W; Barnes W G; Leurs R; Menge W M; 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 2000;909():25-40.
1999: Wieland K; Laak A M; Smit M J; Kühne R; Timmerman H; Leurs R
Mutational analysis of the antagonist-binding site of the histamine H(1) receptor.
The Journal of biological chemistry 1999;274(42):29994-30000.
1999: Windhorst A D; Timmerman H; Klok R P; Menge W M; Leurs R; Herscheid J D
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: Windhorst A D; Timmerman H; Klok R P; Custers F G; Menge W M; Leurs R; Stark H; Schunack W; Gielen E G; van Kroonenburgh M J; Herscheid J D
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: Tensen C P; Flier J; Van Der Raaij-Helmer E M; Sampat-Sardjoepersad S; Van Der Schors R C; Leurs R; Scheper R J; Boorsma D M; 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 1999;112(5):716-22.
1999: De Esch I J; Vollinga R C; Goubitz K; Schenk H; Appelberg U; Hacksell U; Lemstra S; Zuiderveld O P; Hoffmann M; Leurs R; Menge W M; 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 1999;42(7):1115-22.
1999: Hough L B; Nalwalk J W; Leurs R; Menge W M; Timmerman H
Antinociceptive activity of impentamine, a histamine congener, after CNS administration.
Life sciences 1999;64(5):PL79-86.
1998: Bannoura M D; Nalwalk J W; Tang Y; Carlile M; Leurs R; Menge W M; Timmerman H; Hough L B
Absence of antinociceptive tolerance to improgan, a cimetidine analog, in rats.
Brain research 1998;814(1-2):218-21.
1998: Leurs R; Smit M J; Alewijnse A E; Timmerman H
Agonist-independent regulation of constitutively active G-protein-coupled receptors.
Trends in biochemical sciences 1998;23(11):418-22.
1998: Tensen C P; Cox K J; Burke J F; Leurs R; van der Schors R C; Geraerts W P; Vreugdenhil E; Heerikhuizen H
Molecular cloning and characterization of an invertebrate homologue of a neuropeptide Y receptor.
The European journal of neuroscience 1998;10(11):3409-16.
1998: Alewijnse A E; Smit M J; Hoffmann M; Verzijl D; Timmerman H; Leurs R
Constitutive activity and structural instability of the wild-type human H2 receptor.
Journal of neurochemistry 1998;71(2):799-807.
1998: Leurs R; Blandina P; Tedford C; Timmerman H
Therapeutic potential of histamine H3 receptor agonists and antagonists.
Trends in pharmacological sciences 1998;19(5):177-83.
1998: Alves-Rodrigues A; Timmerman H; Willems E; Lemstra S; Zuiderveld O P; Leurs R
Pharmacological characterisation of the histamine H3 receptor in the rat hippocampus.
Brain research 1998;788(1-2):179-86.
1998: Smit M J; Timmerman H; Alewijnse A E; Leurs R
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: Alewijnse A E; Smit M J; Rodriguez Pena M S; Verzijl D; Timmerman H; Leurs R
Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active G(S)-coupled receptors.
FEBS letters 1997;419(2-3):171-4.
1997: Hough L B; Nalwalk J W; Li B Y; Leurs R; Menge W M; Timmerman H; Carlile M E; Cioffi C; Wentland M
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: Beukers M W; Klaassen C H; De Grip W J; Verzijl D; Timmerman H; Leurs R
Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
British journal of pharmacology 1997;122(5):867-74.

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