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Items: 1 to 50 of 347

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.

Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity.

Botros SS, William S, Sabra AA, El-Lakkany NM, Seif El-Din SH, García-Rubia A, Sebastián-Pérez V, Blaazer AR, de Heuvel E, Sijm M, Zheng Y, Salado IG, Munday JC, Maes L, de Esch IJP, Sterk GJ, Augustyns K, Leurs R, Gil C, De Koning HP.

Int J Parasitol Drugs Drug Resist. 2019 Jan 14;9:35-43. doi: 10.1016/j.ijpddr.2019.01.001. [Epub ahead of print]

3.

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
4.

Aminergic GPCR-Ligand Interactions: A Chemical and Structural Map of Receptor Mutation Data.

Vass M, Podlewska S, de Esch IJP, Bojarski AJ, Leurs R, Kooistra AJ, de Graaf C.

J Med Chem. 2018 Nov 27. doi: 10.1021/acs.jmedchem.8b00836. [Epub ahead of print]

PMID:
30351004
5.

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
6.

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.

7.

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
8.

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.

9.

Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.

Blaazer AR, Singh AK, de Heuvel E, Edink E, Orrling KM, Veerman JJN, van den Bergh T, Jansen C, Balasubramaniam E, Mooij WJ, Custers H, Sijm M, Tagoe DNA, Kalejaiye TD, Munday JC, Tenor H, Matheeussen A, Wijtmans M, Siderius M, de Graaf C, Maes L, de Koning HP, Bailey DS, Sterk GJ, de Esch IJP, Brown DG, Leurs R.

J Med Chem. 2018 May 10;61(9):3870-3888. doi: 10.1021/acs.jmedchem.7b01670. Epub 2018 May 1.

10.
11.

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.

12.

Non-Imidazole Histamine H₃ Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines.

Guryn R, Staszewski M, Stasiak A, McNaught Flores D, Fogel WA, Leurs R, Walczyński K.

Molecules. 2018 Feb 3;23(2). pii: E326. doi: 10.3390/molecules23020326.

13.

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.

14.

3D-e-Chem: Structural Cheminformatics Workflows for Computer-Aided Drug Discovery.

Kooistra AJ, Vass M, McGuire R, Leurs R, de Esch IJP, Vriend G, Verhoeven S, de Graaf C.

ChemMedChem. 2018 Mar 20;13(6):614-626. doi: 10.1002/cmdc.201700754. Epub 2018 Feb 14.

15.

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.

16.

The single cyclic nucleotide-specific phosphodiesterase of the intestinal parasite Giardia lamblia represents a potential drug target.

Kunz S, Balmer V, Sterk GJ, Pollastri MP, Leurs R, Müller N, Hemphill A, Spycher C.

PLoS Negl Trop Dis. 2017 Sep 15;11(9):e0005891. doi: 10.1371/journal.pntd.0005891. eCollection 2017 Sep.

17.

The Future of Drug Development for Neglected Tropical Diseases: How the European Commission Can Continue to Make a Difference.

Pierce RJ, MacDougall J, Leurs R, Costi MP.

Trends Parasitol. 2017 Aug;33(8):581-583. doi: 10.1016/j.pt.2017.04.007. Epub 2017 May 18.

PMID:
28529130
18.

The clinical pharmacology of non-sedating antihistamines.

Yanai K, Yoshikawa T, Yanai A, Nakamura T, Iida T, Leurs R, Tashiro M.

Pharmacol Ther. 2017 Oct;178:148-156. doi: 10.1016/j.pharmthera.2017.04.004. Epub 2017 Apr 27. Review.

PMID:
28457804
19.

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time.

Schuetz DA, de Witte WEA, Wong YC, Knasmueller B, Richter L, Kokh DB, Sadiq SK, Bosma R, Nederpelt I, Heitman LH, Segala E, Amaral M, Guo D, Andres D, Georgi V, Stoddart LA, Hill S, Cooke RM, De Graaf C, Leurs R, Frech M, Wade RC, de Lange ECM, IJzerman AP, Müller-Fahrnow A, Ecker GF.

Drug Discov Today. 2017 Jun;22(6):896-911. doi: 10.1016/j.drudis.2017.02.002. Epub 2017 Apr 13. Review.

PMID:
28412474
20.

Structural Analysis of Chemokine Receptor-Ligand Interactions.

Arimont M, Sun SL, Leurs R, Smit M, de Esch IJP, de Graaf C.

J Med Chem. 2017 Jun 22;60(12):4735-4779. doi: 10.1021/acs.jmedchem.6b01309. Epub 2017 Mar 10. Review.

21.

3D-e-Chem-VM: Structural Cheminformatics Research Infrastructure in a Freely Available Virtual Machine.

McGuire R, Verhoeven S, Vass M, Vriend G, de Esch IJ, Lusher SJ, Leurs R, Ridder L, Kooistra AJ, Ritschel T, de Graaf C.

J Chem Inf Model. 2017 Feb 27;57(2):115-121. doi: 10.1021/acs.jcim.6b00686. Epub 2017 Feb 14.

22.

Molecular interaction fingerprint approaches for GPCR drug discovery.

Vass M, Kooistra AJ, Ritschel T, Leurs R, de Esch IJ, de Graaf C.

Curr Opin Pharmacol. 2016 Oct;30:59-68. doi: 10.1016/j.coph.2016.07.007. Epub 2016 Jul 29. Review.

PMID:
27479316
23.

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
24.

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
25.

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.

26.

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
27.

Surface plasmon resonance biosensor assay for the analysis of small-molecule inhibitor binding to human and parasitic phosphodiesterases.

Siderius M, Shanmugham A, England P, van der Meer T, Bebelman JP, Blaazer AR, de Esch IJ, Leurs R.

Anal Biochem. 2016 Jun 15;503:41-9. doi: 10.1016/j.ab.2016.03.013. Epub 2016 Mar 28.

PMID:
27033007
28.

Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.

Veerman J, van den Bergh T, Orrling KM, Jansen C, Cos P, Maes L, Chatelain E, Ioset JR, Edink EE, Tenor H, Seebeck T, de Esch I, Leurs R, Sterk GJ.

Bioorg Med Chem. 2016 Apr 1;24(7):1573-81. doi: 10.1016/j.bmc.2016.02.032. Epub 2016 Feb 26.

PMID:
26935942
29.

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
30.

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
31.

PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.

Jansen C, Kooistra AJ, Kanev GK, Leurs R, de Esch IJ, de Graaf C.

J Med Chem. 2016 Aug 11;59(15):7029-65. doi: 10.1021/acs.jmedchem.5b01813. Epub 2016 Mar 18.

PMID:
26908025
32.

Combined CXCR3/CXCR4 measurements are of high prognostic value in chronic lymphocytic leukemia due to negative co-operativity of the receptors.

Ganghammer S, Gutjahr J, Hutterer E, Krenn PW, Pucher S, Zelle-Rieser C, Jöhrer K, Wijtmans M, Leurs R, Smit MJ, Gattei V, Greil R, Hartmann TN.

Haematologica. 2016 Mar;101(3):e99-102. doi: 10.3324/haematol.2015.133470. Epub 2015 Nov 20. No abstract available.

33.

KLIFS: a structural kinase-ligand interaction database.

Kooistra AJ, Kanev GK, van Linden OP, Leurs R, de Esch IJ, de Graaf C.

Nucleic Acids Res. 2016 Jan 4;44(D1):D365-71. doi: 10.1093/nar/gkv1082. Epub 2015 Oct 22.

34.

Metabolic profiling of ligands for the chemokine receptor CXCR3 by liquid chromatography-mass spectrometry coupled to bioaffinity assessment.

Mladic M, Scholten DJ, Wijtmans M, Falck D, Leurs R, Niessen WM, Smit MJ, Kool J.

Anal Bioanal Chem. 2015 Sep;407(23):7067-81. doi: 10.1007/s00216-015-8867-z. Epub 2015 Jul 12.

35.

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
36.

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.

Panula P, Chazot PL, Cowart M, Gutzmer R, Leurs R, Liu WL, Stark H, Thurmond RL, Haas HL.

Pharmacol Rev. 2015 Jul;67(3):601-55. doi: 10.1124/pr.114.010249. Review.

37.

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.

38.

Structure-Based Prediction of G-Protein-Coupled Receptor Ligand Function: A β-Adrenoceptor Case Study.

Kooistra AJ, Leurs R, de Esch IJ, de Graaf C.

J Chem Inf Model. 2015 May 26;55(5):1045-61. doi: 10.1021/acs.jcim.5b00066. Epub 2015 May 1.

PMID:
25848966
39.

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
40.

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.

41.

Pharmacological characterization of [3H]VUF11211, a novel radiolabeled small-molecule inverse agonist for the chemokine receptor CXCR3.

Scholten DJ, Wijtmans M, van Senten JR, Custers H, Stunnenberg A, de Esch IJ, Smit MJ, Leurs R.

Mol Pharmacol. 2015 Apr;87(4):639-48. doi: 10.1124/mol.114.095265. Epub 2015 Jan 9.

PMID:
25576486
42.

Fragment-based screening in tandem with phenotypic screening provides novel antiparasitic hits.

Blaazer AR, Orrling KM, Shanmugham A, Jansen C, Maes L, Edink E, Sterk GJ, Siderius M, England P, Bailey D, de Esch IJ, Leurs R.

J Biomol Screen. 2015 Jan;20(1):131-40. doi: 10.1177/1087057114549735. Epub 2014 Sep 17.

PMID:
25231971
43.

The Concise Guide to PHARMACOLOGY 2013/14: overview.

Alexander SP, Benson HE, Faccenda E, Pawson AJ, Sharman JL, McGrath JC, Catterall WA, Spedding M, Peters JA, Harmar AJ; CGTP Collaborators, Abul-Hasn N, Anderson CM, Anderson CM, Araiksinen MS, Arita M, Arthofer E, Barker EL, Barratt C, Barnes NM, Bathgate R, Beart PM, Belelli D, Bennett AJ, Birdsall NJ, Boison D, Bonner TI, Brailsford L, Bröer S, Brown P, Calo G, Carter WG, Catterall WA, Chan SL, Chao MV, Chiang N, Christopoulos A, Chun JJ, Cidlowski J, Clapham DE, Cockcroft S, Connor MA, Cox HM, Cuthbert A, Dautzenberg FM, Davenport AP, Dawson PA, Dent G, Dijksterhuis JP, Dollery CT, Dolphin AC, Donowitz M, Dubocovich ML, Eiden L, Eidne K, Evans BA, Fabbro D, Fahlke C, Farndale R, Fitzgerald GA, Fong TM, Fowler CJ, Fry JR, Funk CD, Futerman AH, Ganapathy V, Gaisnier B, Gershengorn MA, Goldin A, Goldman ID, Gundlach AL, Hagenbuch B, Hales TG, Hammond JR, Hamon M, Hancox JC, Hauger RL, Hay DL, Hobbs AJ, Hollenberg MD, Holliday ND, Hoyer D, Hynes NA, Inui KI, Ishii S, Jacobson KA, Jarvis GE, Jarvis MF, Jensen R, Jones CE, Jones RL, Kaibuchi K, Kanai Y, Kennedy C, Kerr ID, Khan AA, Klienz MJ, Kukkonen JP, Lapoint JY, Leurs R, Lingueglia E, Lippiat J, Lolait SJ, Lummis SC, Lynch JW, MacEwan D, Maguire JJ, Marshall IL, May JM, McArdle CA, McGrath JC, Michel MC, Millar NS, Miller LJ, Mitolo V, Monk PN, Moore PK, Moorhouse AJ, Mouillac B, Murphy PM, Neubig RR, Neumaier J, Niesler B, Obaidat A, Offermanns S, Ohlstein E, Panaro MA, Parsons S, Pwrtwee RG, Petersen J, Pin JP, Poyner DR, Prigent S, Prossnitz ER, Pyne NJ, Pyne S, Quigley JG, Ramachandran R, Richelson EL, Roberts RE, Roskoski R, Ross RA, Roth M, Rudnick G, Ryan RM, Said SI, Schild L, Sanger GJ, Scholich K, Schousboe A, Schulte G, Schulz S, Serhan CN, Sexton PM, Sibley DR, Siegel JM, Singh G, Sitsapesan R, Smart TG, Smith DM, Soga T, Stahl A, Stewart G, Stoddart LA, Summers RJ, Thorens B, Thwaites DT, Toll L, Traynor JR, Usdin TB, Vandenberg RJ, Villalon C, Vore M, Waldman SA, Ward DT, Willars GB, Wonnacott SJ, Wright E, Ye RD, Yonezawa A, Zimmermann M.

Br J Pharmacol. 2013 Dec;170(8):1449-58. doi: 10.1111/bph.12444.

44.

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
45.

Identification of overlapping but differential binding sites for the high-affinity CXCR3 antagonists NBI-74330 and VUF11211.

Scholten DJ, Roumen L, Wijtmans M, Verkade-Vreeker MC, Custers H, Lai M, de Hooge D, Canals M, de Esch IJ, Smit MJ, de Graaf C, Leurs R.

Mol Pharmacol. 2014 Jan;85(1):116-26. doi: 10.1124/mol.113.088633. Epub 2013 Oct 30.

PMID:
24174496
46.

From three-dimensional GPCR structure to rational ligand discovery.

Kooistra AJ, Leurs R, de Esch IJ, de Graaf C.

Adv Exp Med Biol. 2014;796:129-57. doi: 10.1007/978-94-007-7423-0_7. Review.

PMID:
24158804
47.

KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space.

van Linden OP, Kooistra AJ, Leurs R, de Esch IJ, de Graaf C.

J Med Chem. 2014 Jan 23;57(2):249-77. doi: 10.1021/jm400378w. Epub 2013 Sep 20.

PMID:
23941661
48.

Neutralizing nanobodies targeting diverse chemokines effectively inhibit chemokine function.

Blanchetot C, Verzijl D, Mujić-Delić A, Bosch L, Rem L, Leurs R, Verrips CT, Saunders M, de Haard H, Smit MJ.

J Biol Chem. 2013 Aug 30;288(35):25173-82. doi: 10.1074/jbc.M113.467969. Epub 2013 Jul 8.

49.

A structural chemogenomics analysis of aminergic GPCRs: lessons for histamine receptor ligand design.

Kooistra AJ, Kuhne S, de Esch IJ, Leurs R, de Graaf C.

Br J Pharmacol. 2013 Sep;170(1):101-26. doi: 10.1111/bph.12248.

50.

A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H₃ receptor stably expressed in CHO-K1 cells.

Flores-Clemente C, Osorio-Espinoza A, Escamilla-Sánchez J, Leurs R, Arias JM, Arias-Montaño JA.

Br J Pharmacol. 2013 Sep;170(1):127-35. doi: 10.1111/bph.12257.

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