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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 JournalArticle

2018
Open Access

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

Vass, M., Podlewska, S., De Esch, I. J. P., Bojarski, A. J., Leurs, R., Kooistra, A. J. & De Graaf, C., 17 Oct 2018, In : Journal of Medicinal Chemistry. 62, 8, p. 3784-3839 56 p.

Research output: Contribution to JournalArticle

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

Stoddart, L. A., Vernall, A. J., Bouzo-Lorenzo, M., Bosma, R., Kooistra, A. J., De Graaf, C., Vischer, H. F., Leurs, R., Briddon, S. J., Kellam, B. & Hill, S. J., 1 Dec 2018, In : Scientific Reports. 8, 1, 1572.

Research output: Contribution to JournalArticle

Open Access

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

Mocking, T. A. M., Verweij, E. W. E., Vischer, H. F. & Leurs, R., Dec 2018, In : Molecular pharmacology. 94, 6, p. 1371-1381 11 p.

Research output: Contribution to JournalArticle

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, W. A., Leurs, R. & Walczynski, K., 3 Feb 2018, In : Molecules. 23, 2, p. 1-20 20 p., 326.

Research output: Contribution to JournalArticle

Open Access

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

Gómez-Santacana, X., de Munnik, S. M., Vijayachandran, P., Da Costa Pereira, D., Bebelman, J. P. M., de Esch, I. J. P., Vischer, H. F., Wijtmans, M. & Leurs, R., 3 Sep 2018, In : Angewandte Chemie - International Edition. 57, 36, p. 11608-11612 5 p.

Research output: Contribution to JournalArticle

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

Hauwert, N. J., Mocking, T. A. M., Da Costa Pereira, D., Kooistra, A. J., Wijnen, L. M., Vreeker, G. C. M., Verweij, E. W. E., De Boer, A. H., Smit, M. J., De Graaf, C., Vischer, H. F., De Esch, I. J. P., Wijtmans, M. & Leurs, R., 28 Mar 2018, In : Journal of the American Chemical Society. 140, 12, p. 4232-4243 12 p.

Research output: Contribution to JournalArticle

Open Access

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

Blaazer, A. R., Singh, A. K., De Heuvel, E., Edink, E., Orrling, K. M., Veerman, J. J. N., Van Den Bergh, T., Jansen, C., Balasubramaniam, E., Mooij, W. J., Custers, H., Sijm, M., Tagoe, D. N. A., Kalejaiye, T. D., Munday, J. C., Tenor, H., Matheeussen, A., Wijtmans, M., Siderius, M., De Graaf, C. & 7 others, Maes, L., De Koning, H. P., Bailey, D. S., Sterk, G. J., De Esch, I. J. P., Brown, D. G. & Leurs, R., 10 May 2018, In : Journal of Medicinal Chemistry. 61, 9, p. 3870-3888 19 p.

Research output: Contribution to JournalArticle

Open Access

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

Heukers, R., Fan, T. S., de Wit, R. H., van Senten, J. R., de Groof, T. W. M., Bebelman, M. P., Lagerweij, T., Vieira, J., de Munnik, S. M., Smits-de Vries, L., van Offenbeek, J., Rahbar, A., van Hoorick, D., Söderberg-Naucler, C., Würdinger, T., Leurs, R., Siderius, M., Vischer, H. F. & Smit, M. J., 30 Apr 2018, In : Oncogene. 2018, 30, p. 1-12 12 p.

Research output: Contribution to JournalArticle

Open Access
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 JournalArticle

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 JournalArticle

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 article

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 article

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 article

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 survey

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle

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 JournalArticle