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  • R. Leurs
2020

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

De Araújo, J. S., da Silva, P. B., Batista, M. M., Peres, R. B., Cardoso-Santos, C., Kalejaiye, T. D., Munday, J. C., De Heuvel, E., Sterk, G. J., Augustyns, K., Salado, I. G., Matheeussen, A., De Esch, I., De Koning, H. P., Leurs, R., Maes, L. & Soeiro, M. D. N. C., 1 Apr 2020, In : The Journal of antimicrobial chemotherapy. 75, 4, p. 958-967 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

2019

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, T. A. M., Arimont, M., Provensi, G., Rani, B., Silva-Marques, B., Latacz, G., Da Costa Pereira, D., Karatzidou, C., Vischer, H. F., Wijtmans, M., Kieć-Kononowicz, K., De Esch, I. J. P. & Leurs, R., 1 Nov 2019, In : Journal of Medicinal Chemistry. 62, 23, p. 10848-10866 19 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors

de Heuvel, E., Singh, A. K., Edink, E., van der Meer, T., van der Woude, M., Sadek, P., Krell-Jørgensen, M. P., van den Bergh, T., Veerman, J., Caljon, G., Kalejaiye, T. D., Wijtmans, M., Maes, L., de Koning, H. P., Jan Sterk, G., Siderius, M., de Esch, I. J. P., Brown, D. G. & Leurs, R., 15 Sep 2019, In : Bioorganic and Medicinal Chemistry. 27, 18, p. 3998-4012 15 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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

de Heuvel, E., Singh, A. K., Boronat, P., Kooistra, A. J., van der Meer, T., Sadek, P., Blaazer, A. R., Shaner, N. C., Bindels, D. S., Caljon, G., Maes, L., Sterk, G. J., Siderius, M., Oberholzer, M., de Esch, I. J. P., Brown, D. G. & Leurs, R., 15 Sep 2019, In : Bioorganic and Medicinal Chemistry. 27, 18, p. 4013-4029

Research output: Contribution to JournalArticleAcademicpeer-review

A Photoswitchable Agonist for the Histamine H 3 Receptor, a Prototypic Family A G-Protein-Coupled Receptor

Hauwert, N. J., Mocking, T. A. M., Da Costa Pereira, D., Lion, K., Huppelschoten, Y., Vischer, H. F., De Esch, I. J. P., Wijtmans, M. & Leurs, R., 26 Mar 2019, In : Angewandte Chemie - International Edition. 58, 14, p. 4531-4535 5 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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

Gómez-Santacana, X., De Munnik, S. M., Mocking, T. A. M., Hauwert, N. J., Sun, S., Vijayachandran, P., De Esch, I. J. P., Vischer, H. F., Wijtmans, M. & Leurs, R., 23 Oct 2019, In : Beilstein Journal of Organic Chemistry. 15, p. 2509-2523 15 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Open Access

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

Arimont, M., Hoffmann, C., de Graaf, C. & Leurs, R., 1 Dec 2019, In : Molecular pharmacology. 96, 6, p. 765-777 13 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

Covalent inhibition of the histamine H3 receptor

Wágner, G., Mocking, T. A. M., Kooistra, A. J., Slynko, I., Ábrányi-Balogh, P., Keser u, G. M., Wijtmans, M., Vischer, H. F., de Esch, I. J. P. & Leurs, R., 11 Dec 2019, In : Molecules. 24, 24, p. 1-19 19 p., 4541.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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 H 3 receptor antagonists

Staszewski, M., Stasiak, A., Karcz, T., McNaught Flores, D., Fogel, W. A., Kieć-Kononowicz, K., Leurs, R. & Walczyński, K., Feb 2019, In : MedChemComm. 10, 2, p. 234-251 18 p.

Research output: Contribution to JournalArticleAcademicpeer-review

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

Sebastián-Pérez, V., Schroeder, S., Munday, J. C., Van Der Meer, T., Zaldívar-Díez, J., Siderius, M., De Koning, H. P., Brown, D., Martínez, A., Campillo, N. E., Leurs, R. & Gil, C., 1 Jan 2019, In : Future Medicinal Chemistry. 11, 14, p. 1703-1720 18 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Identification of Key Structural Motifs Involved in 7 Transmembrane Signaling of Adhesion GPCRs

Arimont Segura, M., van der Woude, M., Leurs, R., Vischer, H. F., de Graaf, C. & Nijmeijer, S., 21 Jan 2019, In : ACS Pharmacology & Translational Science. 2, 2, p. 101-113 13 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Identification of Phenylphthalazinones as a New Class of Leishmania infantum Inhibitors

Sijm, M., de Heuvel, E., Matheeussen, A., Caljon, G., Maes, L., Sterk, G. J., de Esch, I. J. P. & Leurs, R., 22 Nov 2019, In : ChemMedChem. 15, 2, p. 1-10 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

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, I. J. P., de Nazaré Correia Soeiro, M., Sterk, G. J. & Leurs, R., 1 Jan 2019, In : ChemMedChem. 14, 18, p. 1662-1668 7 p.

Research output: Contribution to JournalArticleAcademicpeer-review

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., 1 Dec 2019, In : Molecular pharmacology. 96, 6, p. 737-752 16 p.

Research output: Contribution to JournalShort surveyAcademicpeer-review

Open Access

Phenyldihydropyrazolones as Novel Lead Compounds Against Trypanosoma cruzi

Sijm, M., Siciliano De Araújo, J., Kunz, S., Schroeder, S., Edink, E., Orrling, K. M., Matheeussen, A., Van De Meer, T., Sadek, P., Custers, H., Cotillo, I., Martin, J. J., Siderius, M., Maes, L., Brown, D. G., De Nazaré Correia Soeiro, M., Sterk, G. J., De Esch, I. J. P. & Leurs, R., 10 Apr 2019, In : ACS Omega. 4, 4, p. 6585-6596 12 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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

Bosma, R., Stoddart, L. A., Georgi, V., Bouzo-Lorenzo, M., Bushby, N., Inkoom, L., Waring, M. J., Briddon, S. J., Vischer, H. F., Sheppard, R. J., Fernández-Montalván, A., Hill, S. J. & Leurs, R., 1 Dec 2019, In : Scientific Reports. 9, 1, 7906.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

Route to prolonged residence time at the histamine H1 receptor: Growing from desloratadine to rupatadine

Bosma, R., Wang, Z., Kooistra, A. J., Bushby, N., Kuhne, S., Van Den Bor, J., Waring, M. J., De Graaf, C., De Esch, I. J., Vischer, H. F., Sheppard, R. J., Wijtmans, M. & Leurs, R., 25 Jul 2019, In : Journal of Medicinal Chemistry. 62, 14, p. 6630-6644 15 p.

Research output: Contribution to JournalArticleAcademicpeer-review

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

Botros, S. S., William, S., Sabra, A. N. A., El-Lakkany, N. M., Seif el-Din, S. H., García-Rubia, A., Sebastián-Pérez, V., Blaazer, A. R., de Heuvel, E., Sijm, M., Zheng, Y., Salado, I. G., Munday, J. C., Maes, L., de Esch, I. J. P., Sterk, G. J., Augustyns, K., Leurs, R., Gil, C. & De Koning, H. P., Apr 2019, In : International Journal for Parasitology: Drugs and Drug Resistance. 9, p. 35-43 9 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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 Perpiñá, C., Caspar, B., Arimont, M., Bebelman, J. P., Briddon, S. J., Hoffmann, C., Hill, S. J., Smit, M. J., Vischer, H. F., Wijtmans, M., de Graaf, C., de Esch, I. J. P. & Leurs, R., 15 Jan 2019, In : European Journal of Medicinal Chemistry. 162, p. 631-649 19 p.

Research output: Contribution to JournalArticleAcademicpeer-review

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

Van Senten, J. R., Bebelman, M. P., Fan, T. S., Heukers, R., Bergkamp, N. D., Van Gasselt, P., Langemeijer, E. V., Slinger, E., Lagerweij, T., Rahbar, A., Van Walsum, M. S., Maussang, D., Leurs, R., Musters, R. J. P., Van Dongen, G. A. M. S., Söderberg-Nauclér, C., Würdinger, T., Siderius, M. & Smit, M. J., 1 Nov 2019, In : Journal of Biological Chemistry. 294, 44, p. 16297-16308 12 p.

Research output: Contribution to JournalArticleAcademicpeer-review

The Landscape of Atypical and Eukaryotic Protein Kinases

Kanev, G. K., de Graaf, C., de Esch, I. J. P., Leurs, R., Würdinger, T., Westerman, B. A. & Kooistra, A. J., Nov 2019, In : Trends in Pharmacological Sciences. 40, 11, p. 818-832 15 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

Open Access
2017

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

Kooistra, A. J., Vass, M., Mcguire, R., Leurs, R., deEsch, I. J. P., Vriend, G., Verhoeven, S. & deGraaf, C., 1 Jan 2017, (Accepted/In press) In : ChemMedChem. 13, 6, p. 614-626 13 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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

McGuire, R., Verhoeven, S., Vass, M., Vriend, G., De Esch, I. J. P., Lusher, S. J., Leurs, R., Ridder, L., Kooistra, A. J., Ritschel, T. & de Graaf, C., 27 Feb 2017, In : Journal of Chemical Information and Modeling. 57, 2, p. 115-121 7 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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

Schuetz, D. A., de Witte, W. E. A., Wong, Y. C., Knasmueller, B., Richter, L., Kokh, D. B., Sadiq, S. K., Bosma, R., Nederpelt, I., Heitman, L. H., Segala, E., Amaral, M., Guo, D., Andres, D., Georgi, V., Stoddart, L. A., Hill, S., Cooke, R. M., de Graaf, C., Leurs, R. & 6 others, Frech, M., Wade, R. C., de Lange, E. C. M., IJzerman, A. P., Müller-Fahrnow, A. & Ecker, G. F., 1 Jun 2017, In : Drug Discovery Today. 22, 6, p. 896-911 16 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

Ligand-binding kinetics on histamine receptors

Bosma, R., Mocking, T. A. M., Leurs, R. & Vischer, H. F., 2017, Histamine receptors as drug targets. Humana Press, p. 115-155 (Methods in pharmacology and toxicology).

Research output: Chapter in Book / Report / Conference proceedingChapterAcademicpeer-review

Methods to study the molecular pharmacology of the histamine H4 receptor

Verweij, E. W. E., Leurs, R. & Vischer, H. F., 2017, Histamine receptors as drug targets. Humana Press, p. 157-181 (Methods in pharmacology and toxicology).

Research output: Chapter in Book / Report / Conference proceedingChapterAcademicpeer-review

Structural Analysis of Chemokine Receptor-Ligand Interactions

Arimont, M., Sun, S-L., Leurs, R., Smit, M., De Esch, I. J. P. & de Graaf, C., 22 Jun 2017, In : Journal of Medicinal Chemistry. 60, 12, p. 4735-4779 45 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

Open Access

The clinical pharmacology of non-sedating antihistamines

Yanai, K., Yoshikawa, T., Yanai, A., Nakamura, T., Iida, T., Leurs, R. & Tashiro, M., 1 Oct 2017, In : Pharmacology and Therapeutics. 178, p. 148-156 9 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

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

Pierce, R. J., MacDougall, J., Leurs, R. & Costi, M. P., 1 Aug 2017, In : Trends in Parasitology. 33, 8, p. 581-583 3 p.

Research output: Contribution to JournalShort surveyAcademicpeer-review

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

Kunz, S., Balmer, V., Sterk, G. J., Pollastri, M. P., Leurs, R., Müller, N., Hemphill, A. & Spycher, C., 15 Sep 2017, In : PLoS Neglected Tropical Diseases. 11, 9, e0005891.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
2016

Adhesion CPCRs in immunology

Nijmeijer, S., Vischer, H. F. & Leurs, R., 2016, In : Biochemical Pharmacology. 114, p. 88-102

Research output: Contribution to JournalArticleAcademicpeer-review

BRET-based beta-arrestin2 recruitmanet to the histamine H1 receptor for investigating antihistamine binding kinetics.

Bosma, R., Moritani, R., Leurs, R. & Vischer, H. F., 2016, In : Pharmacological Research. 111, p. 679-687

Research output: Contribution to JournalArticleAcademicpeer-review

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, P. W., Pucher, S., Zelle-Rieser, C., Johrer, K., Wijtmans, M., Leurs, R., Smit, M. J., Gattei, V., Greil, R. & Hartmann, T. N., 2016, In : Haematologica. 101, 3, p. 99-102 101 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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

Kooistra, A. J., Vischer, H. F., McNaught-Flores, D., Leurs, R., de Esch, I. J. P. & de Graaf, C., 2016, In : Scientific Reports. 2016, 6, 28288.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

Identification of ligand binding hot spots of the histamine H1 receptor following structure-based fragment optimization.

Kuhne, S., Kooistra, A. J., Bosma, R., Bortolato, A., Wijtmans, M., Vischer, H. F., Mason, J. S., de Graaf, C., de Esch, I. J. P. & Leurs, R., 2016, In : Journal of Medicinal Chemistry. 59, 19, p. 9047-9061

Research output: Contribution to JournalArticleAcademicpeer-review

KLIFS: a structural kinase-ligand interaction database.

Kooistra, A. J., Kanev, G. K., van Linden, O. P. J., Leurs, R., de Esch, I. J. P. & de Graaf, C., 2016, In : Nucleic Acids Research. 44, D1, p. D365-D371

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

Molecular Aspects of Histamine Receptors

Mocking, T., Bosma, R., Rahman, S. N., Verweij, E. W. E., McNaught-Flores, D. A., Vischer, H. F. & Leurs, R., 2016, Histamine Receptors. Preclinical and clinical aspects.. Blandina, P. & Passani, M. B. (eds.). Humana Press, p. 1-49 (The Receptors; no. 28).

Research output: Chapter in Book / Report / Conference proceedingChapterAcademicpeer-review

Molecular interaction fingerprints approaches for GPCR drug discovery.

Vass, M., Kooistra, A. J., Ritschel, T., Leurs, R., de Esch, I. J. P. & de Graaf, C., 2016, In : Current Opinion in Pharmacology. 30, p. 59-68

Research output: Contribution to JournalArticleAcademicpeer-review

Molecular pharmocology of chemokine receptors.

de Wit, R. H., de Munnik, S. M., Leurs, R., Vischer, H. F. & Smit, M. J., 2016, In : Methods in Enzymology. 570, p. 457-515

Research output: Contribution to JournalArticleAcademicpeer-review

PDEStrIAn: A phosphodiesterase structure and ligan interaction annotated database as a tool for structure-based drug design.

Jansen, C. J. W., Kooistra, A. J., Kanev, G. K., Leurs, R., de Esch, I. J. P. & de Graaf, C., 2016, In : Journal of Medicinal Chemistry. 59, 15, p. 7029-7065

Research output: Contribution to JournalArticleAcademicpeer-review

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

Siderius, M. H., Shanmugham, A., England, P., van der Meer, T. K., Bebelman, J. P., Blaazer, A. R., de Esch, I. J. P. & Leurs, R., 2016, In : Analytical Biochemistry. 503, p. 41-49

Research output: Contribution to JournalArticleAcademicpeer-review

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, K. M., Jansen, C. J. W., Cos, P., Maes, L., Chatelain, E., Ioset, J. R., Edink, E. S. E., Tenor, H., Seebeck, T., de Esch, I. J. P., Leurs, R. & Sterk, G. J., 2016, In : Bioorganic and Medicinal Chemistry. 24, 7, p. 1573-1581

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

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

de Munnik, S. M., van der Lee, R., Velders, D. M., van Offenbeek, J., Smits-de Vries, L., Leurs, R., Smit, M. J. & Vischer, H. F., 2016, In : Cellular Signalling. 28, 6, p. 595-605

Research output: Contribution to JournalArticleAcademicpeer-review