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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. 19 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Histamine H3 Receptors
Histamine Agonists
Amines
Central Nervous System
Cytochrome P-450 Enzyme System

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., 18 Jun 2019, In : Bioorganic and Medicinal Chemistry. p. 1-15 15 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Trypanosoma brucei brucei
Phosphoric Diester Hydrolases
Parasites
Cyclic Nucleotides
Cytotoxicity

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 17 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Phosphodiesterase Inhibitors
Parasites
African Trypanosomiasis
Trypanosoma brucei brucei
Trypanosomiasis

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
Histamine Agonists
G-Protein-Coupled Receptors
Histamine
Proteins
Chemical activation

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
Chemokine Receptors
Switches
Ligands
Halogens
Chemokines
Open Access
Histamine H3 Receptors
histamines
Bioluminescence
bioluminescence
Energy Transfer

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
Chemokine Receptors
Drug Discovery
G-Protein-Coupled Receptors
Immune System Diseases
Pathologic Processes

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
Histamine H3 Receptors
histamines
Scaffolds
Ligands
reactivity

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

Guanidines
Histamine
Guanidine
Rats
Histamine Receptors

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

Schistosoma mansoni
Schistosomiasis
Phosphoric Diester Hydrolases
Small Molecule Libraries
Cyclic Nucleotides

Drug-receptor binding kinetics in drug discovery: Sticking around at the histamine H1 receptor

Bosma, R., 2019, 177 p.

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

Open Access
File

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

G-Protein-Coupled Receptors
Physiological Phenomena
Drug Design
Molecular Dynamics Simulation
Site-Directed Mutagenesis

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. p. 1-10 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Leishmania infantum
Triazoles
Leishmania
Cytotoxicity
Scaffolds

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

Trypanosoma cruzi
Dimers
Nifurtimox
Chagas Disease
Libraries

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
CXC Chemokines
Chemokine Receptors
Ligands
G-Protein-Coupled Receptors
Chemokines

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

Lead compounds
Phosphoric Diester Hydrolases
Pharmaceutical Preparations
Phosphodiesterase 4 Inhibitors
Enzyme inhibition

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
G-Protein-Coupled Receptors
Rate constants
Ligands
Kinetics
Kinetic parameters

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

Histamine H1 Receptors
Pharmaceutical Preparations
Amines
Ligands
rupatadine

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
Imidazoles
Eggs
Libraries
Praziquantel
Schistosoma mansoni

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

CXCR4 Receptors
Quantitative Structure-Activity Relationship
Chemokine Receptors
Screening
Pharmacology

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

G-Protein-Coupled Receptors
Cytomegalovirus
Glioblastoma
Cell signaling
Tumors

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
Protein Kinases
Phosphotransferases
Spine
Single Nucleotide Polymorphism
Tumors
2018

4-Hydroxypiperidines and their flexible 3-(amino)propyloxy analogues as non-imidazole histamine H3 receptor antagonist: Further structure-activity relationship exploration and in vitro and in vivo pharmacological evaluation

Olszewska, B., Stasiak, A., McNaught Flores, D., Fogel, W. A., Leurs, R. & Walczyński, K., Apr 2018, In : International Journal of Molecular Sciences. 19, p. 1-19 19 p., 1243.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Histamine H3 Antagonists
Histamine H3 Receptors
histamines
Structure-Activity Relationship
Rats

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. 56 p.

Research output: Contribution to JournalArticleAcademicpeer-review

G-Protein-Coupled Receptors
Ligands
Mutation
Drug Discovery
Site-Directed Mutagenesis

Design and synthesis of tool compounds to probe GPCRs

Kuhne, S., 2018, 248 p.

Research output: PhD ThesisPhD Thesis - Research VU, graduation VUAcademic

Open Access
File

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 JournalArticleAcademicpeer-review

Open Access
Histamine H1 Antagonists
Histamine H1 Receptors
Cells
Ligands
Kinetics

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 JournalArticleAcademicpeer-review

Histamine H3 Receptors
Ligands
Histamine Receptors
Energy Transfer
Membranes

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 JournalArticleAcademicpeer-review

Open Access
Histamine H3 Receptors
histamines
Histamine
Rats
Piperazines

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 JournalArticleAcademicpeer-review

Ligands
Molecules
Chemical activation
Electrophysiology
Proteins

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 JournalArticleAcademicpeer-review

Open Access
Histamine H3 Receptors
G-Protein-Coupled Receptors
Ligands
Proteins
Electrophysiology

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 othersMaes, 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 JournalArticleAcademicpeer-review

Open Access
Phosphodiesterase Inhibitors
Phosphoric Diester Hydrolases
Parasites
African Trypanosomiasis
Trypanosoma brucei brucei

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, p. 1-12 12 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Chemokine Receptors
Glioblastoma
Cytomegalovirus
Single-Domain Antibodies
Growth
Open Access
Non-Sedating Histamine H1 Antagonists
Histamine H1 Receptors
fexofenadine
Pharmaceutical Preparations
Pyrilamine
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

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Workflow
Drug Discovery
Ligands
Computer-Aided Design
Proteins

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
Ligands
workflow
infrastructure
Proteins
interaction

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 othersFrech, 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

Drug Industry
Drug Discovery
Pharmaceutical Preparations
Decision Making
Industry

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

Histamine Receptors
Ligands
Pharmaceutical Preparations
Histamine Antagonists

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

Histamine Receptors
Pharmacology
Ligands
Animal Disease Models
Drug Discovery

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
Chemokine Receptors
Ligands
Molecular Models
Structure-Activity Relationship
Site-Directed Mutagenesis

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

Clinical Pharmacology
Histamine Antagonists
Histamine H1 Antagonists
Histamine H1 Receptors
Hypnotics and Sedatives

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

Neglected Diseases
Pharmaceutical Preparations
Clinical Trials
Lead

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
Giardia
Giardia lamblia
Cyclic Nucleotides
Phosphoric Diester Hydrolases
Parasites
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

Immunology
Allergy and Immunology
Leukocytes
Adhesion
Membranes

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

Histamine H1 Receptors
Histamine Antagonists
Histamine
Ligands
Pharmaceutical Preparations

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
G-Protein-Coupled Receptors
Screening
Ligands
Molecular interactions
Histamine

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
Phosphotransferases
Databases
Ligands
Dermatoglyphics
Protein Kinases

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

Dermatoglyphics
Drug Discovery
G-Protein-Coupled Receptors
Ligands
Polypharmacology