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Items: 1 to 50 of 75

1.

A Photoswitchable Agonist for the Histamine H3 Receptor, a prototypic family A G protein-coupled receptor.

Hauwert NJ, Mocking TAM, Da Costa Pereira D, Lion K, Huppelschoten Y, Vischer HF, De Esch IJP, Wijtmans M, Leurs R.

Angew Chem Int Ed Engl. 2019 Feb 8. doi: 10.1002/anie.201813110. [Epub ahead of print]

PMID:
30735597
2.

Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.

Adlere I, Sun S, Zarca A, Roumen L, Gozelle M, Viciano CP, Caspar B, Arimont M, Bebelman JP, Briddon SJ, Hoffmann C, Hill SJ, Smit MJ, Vischer HF, Wijtmans M, de Graaf C, de Esch IJP, Leurs R.

Eur J Med Chem. 2019 Jan 15;162:631-649. doi: 10.1016/j.ejmech.2018.10.060. Epub 2018 Oct 30.

PMID:
30476826
3.

Homogeneous, Real-Time NanoBRET Binding Assays for the Histamine H3 and H4 Receptors on Living Cells.

Mocking TAM, Verweij EWE, Vischer HF, Leurs R.

Mol Pharmacol. 2018 Dec;94(6):1371-1381. doi: 10.1124/mol.118.113373. Epub 2018 Sep 24.

PMID:
30249614
4.

The long duration of action of the second generation antihistamine bilastine coincides with its long residence time at the histamine H1 receptor.

Bosma R, van den Bor J, Vischer HF, Labeaga L, Leurs R.

Eur J Pharmacol. 2018 Nov 5;838:107-111. doi: 10.1016/j.ejphar.2018.09.011. Epub 2018 Sep 7.

5.

Photoswitching the Efficacy of a Small-Molecule Ligand for a Peptidergic GPCR: from Antagonism to Agonism.

Gómez-Santacana X, de Munnik SM, Vijayachandran P, Da Costa Pereira D, Bebelman JPM, de Esch IJP, Vischer HF, Wijtmans M, Leurs R.

Angew Chem Int Ed Engl. 2018 Sep 3;57(36):11608-11612. doi: 10.1002/anie.201804875. Epub 2018 Aug 6.

PMID:
29926530
6.

The constitutive activity of the virally encoded chemokine receptor US28 accelerates glioblastoma growth.

Heukers R, Fan TS, de Wit RH, van Senten JR, De Groof TWM, Bebelman MP, Lagerweij T, Vieira J, de Munnik SM, Smits-de Vries L, van Offenbeek J, Rahbar A, van Hoorick D, Söderberg-Naucler C, Würdinger T, Leurs R, Siderius M, Vischer HF, Smit MJ.

Oncogene. 2018 Jul;37(30):4110-4121. doi: 10.1038/s41388-018-0255-7. Epub 2018 Apr 30.

7.

Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology.

Hauwert NJ, Mocking TAM, Da Costa Pereira D, Kooistra AJ, Wijnen LM, Vreeker GCM, Verweij EWE, De Boer AH, Smit MJ, De Graaf C, Vischer HF, de Esch IJP, Wijtmans M, Leurs R.

J Am Chem Soc. 2018 Mar 28;140(12):4232-4243. doi: 10.1021/jacs.7b11422. Epub 2018 Mar 14.

8.

Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells.

Stoddart LA, Vernall AJ, Bouzo-Lorenzo M, Bosma R, Kooistra AJ, de Graaf C, Vischer HF, Leurs R, Briddon SJ, Kellam B, Hill SJ.

Sci Rep. 2018 Jan 25;8(1):1572. doi: 10.1038/s41598-018-19714-2.

9.

The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor.

Bosma R, Witt G, Vaas LAI, Josimovic I, Gribbon P, Vischer HF, Gul S, Leurs R.

Front Pharmacol. 2017 Sep 25;8:667. doi: 10.3389/fphar.2017.00667. eCollection 2017.

10.

CXCR4-Specific Nanobodies as Potential Therapeutics for WHIM syndrome.

de Wit RH, Heukers R, Brink HJ, Arsova A, Maussang D, Cutolo P, Strubbe B, Vischer HF, Bachelerie F, Smit MJ.

J Pharmacol Exp Ther. 2017 Oct;363(1):35-44. doi: 10.1124/jpet.117.242735. Epub 2017 Aug 2.

PMID:
28768817
11.

Identification of Ligand Binding Hot Spots of the Histamine H1 Receptor following Structure-Based Fragment Optimization.

Kuhne S, Kooistra AJ, Bosma R, Bortolato A, Wijtmans M, Vischer HF, Mason JS, de Graaf C, de Esch IJ, Leurs R.

J Med Chem. 2016 Oct 13;59(19):9047-9061. Epub 2016 Sep 27.

PMID:
27643714
12.

BRET-based β-arrestin2 recruitment to the histamine H1 receptor for investigating antihistamine binding kinetics.

Bosma R, Moritani R, Leurs R, Vischer HF.

Pharmacol Res. 2016 Sep;111:679-687. doi: 10.1016/j.phrs.2016.07.034. Epub 2016 Jul 26.

PMID:
27468652
13.

Function-specific virtual screening for GPCR ligands using a combined scoring method.

Kooistra AJ, Vischer HF, McNaught-Flores D, Leurs R, de Esch IJ, de Graaf C.

Sci Rep. 2016 Jun 24;6:28288. doi: 10.1038/srep28288.

14.

Adhesion GPCRs in immunology.

Nijmeijer S, Vischer HF, Leurs R.

Biochem Pharmacol. 2016 Aug 15;114:88-102. doi: 10.1016/j.bcp.2016.04.013. Epub 2016 Apr 27. Review.

PMID:
27131861
15.

The viral G protein-coupled receptor ORF74 unmasks phospholipase C signaling of the receptor tyrosine kinase IGF-1R.

de Munnik SM, van der Lee R, Velders DM, van Offenbeek J, Smits-de Vries L, Leurs R, Smit MJ, Vischer HF.

Cell Signal. 2016 Jun;28(6):595-605. doi: 10.1016/j.cellsig.2016.02.017. Epub 2016 Feb 27.

PMID:
26931381
16.

Molecular Pharmacology of Chemokine Receptors.

de Wit RH, de Munnik SM, Leurs R, Vischer HF, Smit MJ.

Methods Enzymol. 2016;570:457-515. doi: 10.1016/bs.mie.2015.12.002. Epub 2016 Jan 19.

PMID:
26921959
17.

Ligand Residence Time at G-protein-Coupled Receptors-Why We Should Take Our Time To Study It.

Hoffmann C, Castro M, Rinken A, Leurs R, Hill SJ, Vischer HF.

Mol Pharmacol. 2015 Sep;88(3):552-60. doi: 10.1124/mol.115.099671. Epub 2015 Jul 7. Review.

PMID:
26152198
18.

G Protein-Coupled Receptor Multimers: A Question Still Open Despite the Use of Novel Approaches.

Vischer HF, Castro M, Pin JP.

Mol Pharmacol. 2015 Sep;88(3):561-71. doi: 10.1124/mol.115.099440. Epub 2015 Jul 2. Review.

PMID:
26138074
19.

The Viral G Protein-Coupled Receptor ORF74 Hijacks β-Arrestins for Endocytic Trafficking in Response to Human Chemokines.

de Munnik SM, Kooistra AJ, van Offenbeek J, Nijmeijer S, de Graaf C, Smit MJ, Leurs R, Vischer HF.

PLoS One. 2015 Apr 20;10(4):e0124486. doi: 10.1371/journal.pone.0124486. eCollection 2015.

20.

Combinatorial Consensus Scoring for Ligand-Based Virtual Fragment Screening: A Comparative Case Study for Serotonin 5-HT(3)A, Histamine H(1), and Histamine H(4) Receptors.

Schultes S, Kooistra AJ, Vischer HF, Nijmeijer S, Haaksma EE, Leurs R, de Esch IJ, de Graaf C.

J Chem Inf Model. 2015 May 26;55(5):1030-44. doi: 10.1021/ci500694c. Epub 2015 Apr 23.

PMID:
25815783
21.

Modulation of cellular signaling by herpesvirus-encoded G protein-coupled receptors.

de Munnik SM, Smit MJ, Leurs R, Vischer HF.

Front Pharmacol. 2015 Mar 9;6:40. doi: 10.3389/fphar.2015.00040. eCollection 2015. Review.

22.

Chemokine cooperativity is caused by competitive glycosaminoglycan binding.

Verkaar F, van Offenbeek J, van der Lee MMC, van Lith LHCJ, Watts AO, Rops ALWMM, Aguilar DC, Ziarek JJ, van der Vlag J, Handel TM, Volkman BF, Proudfoot AEI, Vischer HF, Zaman GJR, Smit MJ.

J Immunol. 2014 Apr 15;192(8):3908-3914. doi: 10.4049/jimmunol.1302159. Epub 2014 Mar 17.

23.

Herpesvirus-encoded GPCRs: neglected players in inflammatory and proliferative diseases?

Vischer HF, Siderius M, Leurs R, Smit MJ.

Nat Rev Drug Discov. 2014 Feb;13(2):123-39. doi: 10.1038/nrd4189. Epub 2014 Jan 21. Review.

PMID:
24445563
24.

Llama-derived single variable domains (nanobodies) directed against chemokine receptor CXCR7 reduce head and neck cancer cell growth in vivo.

Maussang D, Mujić-Delić A, Descamps FJ, Stortelers C, Vanlandschoot P, Stigter-van Walsum M, Vischer HF, van Roy M, Vosjan M, Gonzalez-Pajuelo M, van Dongen GA, Merchiers P, van Rompaey P, Smit MJ.

J Biol Chem. 2013 Oct 11;288(41):29562-72. doi: 10.1074/jbc.M113.498436. Epub 2013 Aug 26.

25.

Bispyrimidines as potent histamine H(4) receptor ligands: delineation of structure-activity relationships and detailed H(4) receptor binding mode.

Engelhardt H, Schultes S, de Graaf C, Nijmeijer S, Vischer HF, Zuiderveld OP, Dobler J, Stachurski K, Mayer M, Arnhof H, Scharn D, Haaksma EE, de Esch IJ, Leurs R.

J Med Chem. 2013 Jun 13;56(11):4264-76. doi: 10.1021/jm301886t. Epub 2013 May 28.

PMID:
23668417
26.

Detailed analysis of biased histamine H₄ receptor signalling by JNJ 7777120 analogues.

Nijmeijer S, Vischer HF, Sirci F, Schultes S, Engelhardt H, de Graaf C, Rosethorne EM, Charlton SJ, Leurs R.

Br J Pharmacol. 2013 Sep;170(1):78-88. doi: 10.1111/bph.12117.

27.

Design and pharmacological characterization of VUF14480, a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor.

Nijmeijer S, Engelhardt H, Schultes S, van de Stolpe AC, Lusink V, de Graaf C, Wijtmans M, Haaksma EE, de Esch IJ, Stachurski K, Vischer HF, Leurs R.

Br J Pharmacol. 2013 Sep;170(1):89-100. doi: 10.1111/bph.12113.

28.

β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.

Watts AO, Verkaar F, van der Lee MM, Timmerman CA, Kuijer M, van Offenbeek J, van Lith LH, Smit MJ, Leurs R, Zaman GJ, Vischer HF.

J Biol Chem. 2013 Mar 8;288(10):7169-81. doi: 10.1074/jbc.M112.406108. Epub 2013 Jan 22.

29.

Small and colorful stones make beautiful mosaics: fragment-based chemogenomics.

de Graaf C, Vischer HF, de Kloe GE, Kooistra AJ, Nijmeijer S, Kuijer M, Verheij MH, England PJ, van Muijlwijk-Koezen JE, Leurs R, de Esch IJ.

Drug Discov Today. 2013 Apr;18(7-8):323-30. doi: 10.1016/j.drudis.2012.12.003. Epub 2012 Dec 22.

PMID:
23266367
30.

Identification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes.

Watts AO, van Lipzig MM, Jaeger WC, Seeber RM, van Zwam M, Vinet J, van der Lee MM, Siderius M, Zaman GJ, Boddeke HW, Smit MJ, Pfleger KD, Leurs R, Vischer HF.

Br J Pharmacol. 2013 Apr;168(7):1662-74. doi: 10.1111/bph.12064.

31.

Virtual fragment screening: discovery of histamine H3 receptor ligands using ligand-based and protein-based molecular fingerprints.

Sirci F, Istyastono EP, Vischer HF, Kooistra AJ, Nijmeijer S, Kuijer M, Wijtmans M, Mannhold R, Leurs R, de Esch IJ, de Graaf C.

J Chem Inf Model. 2012 Dec 21;52(12):3308-24. doi: 10.1021/ci3004094. Epub 2012 Dec 3.

PMID:
23140085
32.

Inhibition of CXCR3-mediated chemotaxis by the human chemokine receptor-like protein CCX-CKR.

Vinet J, van Zwam M, Dijkstra IM, Brouwer N, van Weering HR, Watts A, Meijer M, Fokkens MR, Kannan V, Verzijl D, Vischer HF, Smit MJ, Leurs R, Biber K, Boddeke HW.

Br J Pharmacol. 2013 Mar;168(6):1375-87. doi: 10.1111/bph.12042.

33.

Analysis of multiple histamine H₄ receptor compound classes uncovers Gαi protein- and β-arrestin2-biased ligands.

Nijmeijer S, Vischer HF, Rosethorne EM, Charlton SJ, Leurs R.

Mol Pharmacol. 2012 Dec;82(6):1174-82. doi: 10.1124/mol.112.080911. Epub 2012 Sep 12.

PMID:
22973061
34.

Development of a profiling strategy for metabolic mixtures by combining chromatography and mass spectrometry with cell-based GPCR signaling.

Nijmeijer S, Vischer HF, Rudebeck AF, Fleurbaaij F, Falck D, Leurs R, Niessen WM, Kool J.

J Biomol Screen. 2012 Dec;17(10):1329-38. doi: 10.1177/1087057112451922. Epub 2012 Jun 26.

PMID:
22740245
35.

Molecular pharmacology of histamine H4 receptors.

Nijmeijer S, de Graaf C, Leurs R, Vischer HF.

Front Biosci (Landmark Ed). 2012 Jun 1;17:2089-106. Review.

PMID:
22652766
36.

A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design.

Sanders MP, Roumen L, van der Horst E, Lane JR, Vischer HF, van Offenbeek J, de Vries H, Verhoeven S, Chow KY, Verkaar F, Beukers MW, McGuire R, Leurs R, Ijzerman AP, de Vlieg J, de Esch IJ, Zaman GJ, Klomp JP, Bender A, de Graaf C.

J Med Chem. 2012 Jun 14;55(11):5311-25. doi: 10.1021/jm300280e. Epub 2012 May 23.

PMID:
22563707
37.

High-resolution metabolic profiling towards G protein-coupled receptors: rapid and comprehensive screening of histamine H₄ receptor ligands.

Kool J, Rudebeck AF, Fleurbaaij F, Nijmeijer S, Falck D, Smits RA, Vischer HF, Leurs R, Niessen WM.

J Chromatogr A. 2012 Oct 12;1259:213-20. doi: 10.1016/j.chroma.2012.03.052. Epub 2012 Mar 22.

PMID:
22520160
38.

Label-free impedance responses of endogenous and synthetic chemokine receptor CXCR3 agonists correlate with Gi-protein pathway activation.

Watts AO, Scholten DJ, Heitman LH, Vischer HF, Leurs R.

Biochem Biophys Res Commun. 2012 Mar 9;419(2):412-8. doi: 10.1016/j.bbrc.2012.02.036. Epub 2012 Feb 13.

PMID:
22349504
39.

Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.

de Graaf C, Kooistra AJ, Vischer HF, Katritch V, Kuijer M, Shiroishi M, Iwata S, Shimamura T, Stevens RC, de Esch IJ, Leurs R.

J Med Chem. 2011 Dec 8;54(23):8195-206. doi: 10.1021/jm2011589. Epub 2011 Nov 7.

40.

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.

Istyastono EP, Nijmeijer S, Lim HD, van de Stolpe A, Roumen L, Kooistra AJ, Vischer HF, de Esch IJ, Leurs R, de Graaf C.

J Med Chem. 2011 Dec 8;54(23):8136-47. doi: 10.1021/jm201042n. Epub 2011 Nov 7.

PMID:
22003888
41.

Pharmacological characterization of a small-molecule agonist for the chemokine receptor CXCR3.

Scholten DJ, Canals M, Wijtmans M, de Munnik S, Nguyen P, Verzijl D, de Esch IJ, Vischer HF, Smit MJ, Leurs R.

Br J Pharmacol. 2012 Jun;166(3):898-911. doi: 10.1111/j.1476-5381.2011.01648.x.

42.

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.

Verheij MH, de Graaf C, de Kloe GE, Nijmeijer S, Vischer HF, Smits RA, Zuiderveld OP, Hulscher S, Silvestri L, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5460-4. doi: 10.1016/j.bmcl.2011.06.123. Epub 2011 Jul 2.

43.

Pharmacological modulation of chemokine receptor function.

Scholten DJ, Canals M, Maussang D, Roumen L, Smit MJ, Wijtmans M, de Graaf C, Vischer HF, Leurs R.

Br J Pharmacol. 2012 Mar;165(6):1617-1643. doi: 10.1111/j.1476-5381.2011.01551.x. Review.

44.

En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family.

Leurs R, Vischer HF, Wijtmans M, de Esch IJ.

Trends Pharmacol Sci. 2011 Apr;32(4):250-7. doi: 10.1016/j.tips.2011.02.004. Epub 2011 Mar 15. Review. Erratum in: Trends Pharmacol Sci. 2012 Jan;33(1):49.

PMID:
21414671
45.

G protein-coupled receptors: walking hand-in-hand, talking hand-in-hand?

Vischer HF, Watts AO, Nijmeijer S, Leurs R.

Br J Pharmacol. 2011 May;163(2):246-60. doi: 10.1111/j.1476-5381.2011.01229.x. Review.

46.

Constitutive activity of the histamine H(1) receptor.

Nijmeijer S, Leurs R, Vischer HF.

Methods Enzymol. 2010;484:127-47. doi: 10.1016/B978-0-12-381298-8.00007-1.

PMID:
21036230
47.

The cytomegalovirus-encoded chemokine receptor US28 promotes intestinal neoplasia in transgenic mice.

Bongers G, Maussang D, Muniz LR, Noriega VM, Fraile-Ramos A, Barker N, Marchesi F, Thirunarayanan N, Vischer HF, Qin L, Mayer L, Harpaz N, Leurs R, Furtado GC, Clevers H, Tortorella D, Smit MJ, Lira SA.

J Clin Invest. 2010 Nov;120(11):3969-78. doi: 10.1172/JCI42563. Epub 2010 Oct 11.

48.

The Epstein-Barr virus-encoded G protein-coupled receptor BILF1 hetero-oligomerizes with human CXCR4, scavenges Gαi proteins, and constitutively impairs CXCR4 functioning.

Nijmeijer S, Leurs R, Smit MJ, Vischer HF.

J Biol Chem. 2010 Sep 17;285(38):29632-41. doi: 10.1074/jbc.M110.115618. Epub 2010 Jul 9.

49.

Herpesvirus-encoded GPCRs rewire cellular signaling.

Slinger E, Langemeijer E, Siderius M, Vischer HF, Smit MJ.

Mol Cell Endocrinol. 2011 Jan 15;331(2):179-84. doi: 10.1016/j.mce.2010.04.007. Epub 2010 Apr 14. Review.

PMID:
20398729
50.

The G-protein coupled receptor associated sorting protein GASP-1 regulates the signalling and trafficking of the viral chemokine receptor US28.

Tschische P, Moser E, Thompson D, Vischer HF, Parzmair GP, Pommer V, Platzer W, Schwarzbraun T, Schaider H, Smit MJ, Martini L, Whistler JL, Waldhoer M.

Traffic. 2010 May;11(5):660-74. doi: 10.1111/j.1600-0854.2010.1045.x.

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