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Items: 1 to 50 of 364

1.

Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi.

De Araújo JS, da Silva PB, Batista MM, Peres RB, Cardoso-Santos C, Kalejaiye TD, Munday JC, De Heuvel E, Sterk GJ, Augustyns K, Salado IG, Matheeussen A, De Esch I, De Koning HP, Leurs R, Maes L, Soeiro MNC.

J Antimicrob Chemother. 2019 Dec 20. pii: dkz516. doi: 10.1093/jac/dkz516. [Epub ahead of print]

PMID:
31860098
2.

Covalent Inhibition of the Histamine H3 Receptor.

Wágner G, Mocking TAM, Kooistra AJ, Slynko I, Ábrányi-Balogh P, Keserű GM, Wijtmans M, Vischer HF, de Esch IJP, Leurs R.

Molecules. 2019 Dec 11;24(24). pii: E4541. doi: 10.3390/molecules24244541.

3.

Identification of Phenylphthalazinones as a New Class of Leishmania infantum Inhibitors.

Sijm M, de Heuvel E, Matheeussen A, Caljon G, Maes L, Sterk GJ, de Esch IJP, Leurs R.

ChemMedChem. 2020 Jan 17;15(2):219-227. doi: 10.1002/cmdc.201900538. Epub 2019 Dec 9.

PMID:
31756285
4.

A toolbox of molecular photoswitches to modulate the CXCR3 chemokine receptor with light.

Gómez-Santacana X, de Munnik SM, Mocking TAM, Hauwert NJ, Sun S, Vijayachandran P, de Esch IJP, Vischer HF, Wijtmans M, Leurs R.

Beilstein J Org Chem. 2019 Oct 23;15:2509-2523. doi: 10.3762/bjoc.15.244. eCollection 2019.

5.

The Landscape of Atypical and Eukaryotic Protein Kinases.

Kanev GK, de Graaf C, de Esch IJP, Leurs R, Würdinger T, Westerman BA, Kooistra AJ.

Trends Pharmacol Sci. 2019 Nov;40(11):818-832. doi: 10.1016/j.tips.2019.09.002. Epub 2019 Oct 31. Review.

6.

4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity.

Wágner G, Mocking TAM, Arimont M, Provensi G, Rani B, Silva-Marques B, Latacz G, Da Costa Pereira D, Karatzidou C, Vischer HF, Wijtmans M, Kieć-Kononowicz K, de Esch IJP, Leurs R.

J Med Chem. 2019 Dec 12;62(23):10848-10866. doi: 10.1021/acs.jmedchem.9b01462. Epub 2019 Nov 20.

7.

Modulators of CXCR4 and CXCR7/ACKR3 Function.

Adlere I, Caspar B, Arimont M, Dekkers S, Visser K, Stuijt J, de Graaf C, Stocks M, Kellam B, Briddon S, Wijtmans M, de Esch I, Hill S, Leurs R.

Mol Pharmacol. 2019 Dec;96(6):737-752. doi: 10.1124/mol.119.117663. Epub 2019 Sep 23.

PMID:
31548340
8.

The human cytomegalovirus-encoded G protein-coupled receptor UL33 exhibits oncomodulatory properties.

van Senten JR, Bebelman MP, Fan TS, Heukers R, Bergkamp ND, van Gasselt P, Langemeijer EV, Slinger E, Lagerweij T, Rahbar A, Stigter-van Walsum M, Maussang D, Leurs R, Musters RJP, van Dongen GAMS, Söderberg-Nauclér C, Würdinger T, Siderius M, Smit MJ.

J Biol Chem. 2019 Nov 1;294(44):16297-16308. doi: 10.1074/jbc.RA119.007796. Epub 2019 Sep 13.

PMID:
31519750
9.

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).

de Heuvel E, Singh AK, Boronat P, Kooistra AJ, van der Meer T, Sadek P, Blaazer AR, Shaner NC, Bindels DS, Caljon G, Maes L, Sterk GJ, Siderius M, Oberholzer M, de Esch IJP, Brown DG, Leurs R.

Bioorg Med Chem. 2019 Sep 15;27(18):4013-4029. doi: 10.1016/j.bmc.2019.06.026. Epub 2019 Jul 5.

10.

Discovery of novel Schistosoma mansoni PDE4A inhibitors as potential agents against schistosomiasis.

Sebastián-Pérez V, Schroeder S, Munday JC, van der Meer T, Zaldívar-Díez J, Siderius M, de Koning HP, Brown D, Martínez A, Campillo NE, Leurs R, Gil C.

Future Med Chem. 2019 Jul;11(14):1703-1720. doi: 10.4155/fmc-2018-0592. Epub 2019 Aug 2.

PMID:
31370708
11.

Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H3 Receptor.

Mocking TAM, Buzink MCML, Leurs R, Vischer HF.

Int J Mol Sci. 2019 Jul 30;20(15). pii: E3724. doi: 10.3390/ijms20153724.

12.

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.

de Heuvel E, Singh AK, Edink E, van der Meer T, van der Woude M, Sadek P, Krell-Jørgensen MP, van den Bergh T, Veerman J, Caljon G, Kalejaiye TD, Wijtmans M, Maes L, de Koning HP, Jan Sterk G, Siderius M, de Esch IJP, Brown DG, Leurs R.

Bioorg Med Chem. 2019 Sep 15;27(18):3998-4012. doi: 10.1016/j.bmc.2019.06.027. Epub 2019 Jun 18.

13.

Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents.

Sijm M, Siciliano de Araújo J, Ramos Llorca A, Orrling K, Stiny L, Matheeussen A, Maes L, de Esch IJP, de Nazaré Correia Soeiro M, Sterk GJ, Leurs R.

ChemMedChem. 2019 Sep 18;14(18):1662-1668. doi: 10.1002/cmdc.201900370. Epub 2019 Aug 23.

14.

Route to Prolonged Residence Time at the Histamine H1 Receptor: Growing from Desloratadine to Rupatadine.

Bosma R, Wang Z, Kooistra AJ, Bushby N, Kuhne S, van den Bor J, Waring MJ, de Graaf C, de Esch IJ, Vischer HF, Sheppard RJ, Wijtmans M, Leurs R.

J Med Chem. 2019 Jul 25;62(14):6630-6644. doi: 10.1021/acs.jmedchem.9b00447. Epub 2019 Jul 5.

15.

Chemokine Receptor Crystal Structures: What Can Be Learned from Them?

Arimont M, Hoffmann C, de Graaf C, Leurs R.

Mol Pharmacol. 2019 Dec;96(6):765-777. doi: 10.1124/mol.119.117168. Epub 2019 Jul 2.

PMID:
31266800
16.

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor.

Bosma R, Stoddart LA, Georgi V, Bouzo-Lorenzo M, Bushby N, Inkoom L, Waring MJ, Briddon SJ, Vischer HF, Sheppard RJ, Fernández-Montalván A, Hill SJ, Leurs R.

Sci Rep. 2019 May 27;9(1):7906. doi: 10.1038/s41598-019-44025-5.

17.

Design, synthesis, and in vitro and in vivo characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H3 receptor antagonists.

Staszewski M, Stasiak A, Karcz T, McNaught Flores D, Fogel WA, Kieć-Kononowicz K, Leurs R, Walczyński K.

Medchemcomm. 2019 Jan 11;10(2):234-251. doi: 10.1039/c8md00527c. eCollection 2019 Feb 1.

18.

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 Mar 26;58(14):4531-4535. doi: 10.1002/anie.201813110. Epub 2019 Feb 27.

19.

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 Apr;9:35-43. doi: 10.1016/j.ijpddr.2019.01.001. Epub 2019 Jan 14.

20.

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
21.

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. 2019 Apr 25;62(8):3784-3839. doi: 10.1021/acs.jmedchem.8b00836. Epub 2018 Nov 27.

PMID:
30351004
22.

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
23.

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.

24.

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
25.

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.

26.

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.

27.
28.

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.

29.

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.

30.

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.

31.

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.

32.

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.

33.

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.

34.

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
35.

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
36.

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
37.

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.

38.

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.

39.

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
40.

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
41.

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
42.

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.

43.

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
44.

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
45.

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
46.

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
47.

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
48.

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
49.

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.

50.

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.

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