Research Output 1985 2019

Filter
Article
2019
Arabidopsis
Salts
Agricultural Crops
Cathode ray tubes
Level control

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

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

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

Inhibition of autotransporter biogenesis by small molecules

Steenhuis, M., Luirink, S., Jong, W. S. P., van Ulsen, J. P., Wijtmans, M., van den Berg van Saparoea, H. B., Sterk, G. J., Kuhne, S., de Munnik, S. M., Abdallah, A. M., van der Wel, N. N., Wagner, S. & Westerhausen, S., 28 Mar 2019, In : Molecular Microbiology. p. 1-18 18 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Membrane Proteins
Virulence Factors
Libraries
Hemoglobins
Peptide Hydrolases

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

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

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

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
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

Correction: Quantifying exosome secretion from single cells reveals a modulatory role for GPCR signaling

Verweij, F. J., Bebelman, M. P., Jimenez, C. R., Garcia-Vallejo, J. J., Janssen, H., Neefjes, J., Knol, J. C., de Goeij-de Haas, R., Piersma, S. R., Baglio, S. R., Verhage, M., Middeldorp, J. M., Zomer, A., van Rheenen, J., Coppolino, M. G., Hurbain, I., Raposo, G., Smit, M. J., Toonen, R. F. G., van Niel, G. & 1 othersPegtel, D. M., 23 Jan 2018, In : Journal of Cell Biology.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

CXCR4-targeting nanobodies differentially inhibit CXCR4 function and HIV entry

Van Hout, A., Klarenbeek, A., Bobkov, V., Doijen, J., Arimont, M., Zhao, C., Heukers, R., Rimkunas, R., de Graaf, C., Verrips, T., van der Woning, B., de Haard, H., Rucker, J. B., Vermeire, K., Handel, T., Van Loy, T., Smit, M. J. & Schols, D., 1 Dec 2018, In : Biochemical Pharmacology. 158, p. 402-412 11 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Single-Domain Antibodies
HIV
HIV Receptors
Calcium-Sensing Receptors
Anti-HIV Agents

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

Dynamic tuneable G protein-coupled receptor monomer-dimer populations

Dijkman, P. M., Castell, O. K., Goddard, A. D., Munoz-Garcia, J. C., De Graaf, C., Wallace, M. I. & Watts, A., 1 Dec 2018, In : Nature Communications. 9, 1, 1710.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
G-Protein-Coupled Receptors
Dimers
monomers
Monomers
dimers

Heterogeneity assessment of antibody-derived therapeutics at the intact and middle-up level by low-flow sheathless capillary electrophoresis-mass spectrometry

Haselberg, R., De Vijlder, T., Heukers, R., Smit, M. J., Romijn, E. P., Somsen, G. W. & Domínguez-Vega, E., 1 Jan 2018, (Accepted/In press) In : Analytica Chimica Acta. 1044, p. 181-190

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Capillary electrophoresis
Capillary Electrophoresis
low flow
antibody
Mass spectrometry

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

Nanobody-Fc constructs targeting chemokine receptor CXCR4 potently inhibit signaling and CXCR4-mediated HIV-entry and induce antibody effector functions

Bobkov, V., Zarca, A. M., Van Hout, A., Arimont, M., Doijen, J., Bialkowska, M., Toffoli, E., Klarenbeek, A., van der Woning, B., van der Vliet, H. J., Van Loy, T., de Haard, H., Schols, D., Heukers, R. & Smit, M. J., Dec 2018, In : Biochemical Pharmacology. 158, p. 413-424 12 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Single-Domain Antibodies
Chemokine Receptors
HIV
Antibodies
Molecules

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

Quantifying exosome secretion from single cells reveals a modulatory role for GPCR signaling

Verweij, F. J., Bebelman, M. P., Jimenez, C. R., Garcia-Vallejo, J. J., Janssen, H., Neefjes, J., Knol, J. C., de Goeij-de Haas, R., Piersma, S. R., Baglio, S. R., Verhage, M., Middeldorp, J. M., Zomer, A., van Rheenen, J., Coppolino, M. G., Hurbain, I., Raposo, G., Smit, M. J., Toonen, R. F. G., van Niel, G. & 1 othersPegtel, D. M., 5 Mar 2018, In : Journal of Cell Biology. 217, 3, p. 1129-1142 14 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Exosomes
Multivesicular Bodies
Membrane Fusion
Cell Membrane
Qa-SNARE Proteins

Salinity tolerance of two potato cultivars (Solanum tuberosum) correlates with differences in vacuolar transport activity

Jaarsma, R. & de Boer, A. H., 5 Jun 2018, In : Frontiers in Plant Science. 9, 737.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Solanum tuberosum
potatoes
salinity
proton pump
cultivars

Structural analysis of the interaction between the bacterial cell division proteins FTSQ and FTSB

Kureisaite-Ciziene, D., Varadajan, A., McLaughlin, S. H., Glas, M., Silva, A. M., Luirink, R., Mueller, C., Blaauwen, T. D., Grossmann, T. N., Luirink, J. & Löwe, J., 11 Sep 2018, In : mBio. 9, 5, p. 1-17 17 p., e01346-18.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Cell Division
Proteins
Bacteria
Periplasm
Membrane Proteins

Structural insights into serotonin receptor ligands polypharmacology

Podlewska, S., Kafel, R., Lacivita, E., Satała, G., Kooistra, A. J., Vass, M., de Graaf, C., Leopoldo, M., Bojarski, A. J. & Mordalski, S., 10 May 2018, In : European Journal of Medicinal Chemistry. 151, p. 797-814 18 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Polypharmacology
Serotonin Receptors
Ligands
Illegitimacy
Mutagenesis

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 Arabidopsis GORK K+-channel is phosphorylated by calcium-dependent protein kinase 21 (CPK21), which in turn is activated by 14-3-3 proteins

van Kleeff, P. J. M., Gao, J., Mol, S., Zwart, N., Zhang, H., Li, K. W. & de Boer, A. H., Apr 2018, In : Plant Physiology and Biochemistry. 125, p. 219-231 13 p.

Research output: Contribution to JournalArticleAcademicpeer-review

14-3-3 Proteins
potassium channels
Arabidopsis
protein kinases
phosphorylation

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

When fragments link: a bibliometric perspective on the development of fragment-based drug discovery

Romasanta, A. K. S., van der Sijde, P., Hellsten, I., Hubbard, R. E., Keseru, G. M., van Muijlwijk-Koezen, J. & de Esch, I. J. P., Sep 2018, In : Drug Discovery Today. 23, 9, p. 1596-1609

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Bibliometrics
Drug Discovery
Industry
Authorship
Pharmaceutical Chemistry
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

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

Antibodies targeting G protein-coupled receptors: Recent advances and therapeutic challenges

Ayoub, M. A., Crépieux, P., Koglin, M., Parmentier, M., Pin, J. P., Poupon, A., Reiter, E., Smit, M., Steyaert, J., Watier, H. & Wilkinson, T., 4 Jul 2017, In : mAbs. 9, 5, p. 735-741 7 p.

Research output: Contribution to JournalArticleAcademicpeer-review

G-Protein-Coupled Receptors
Single-Domain Antibodies
Antibodies
Therapeutics
Pharmacology

Cold stress increases salt tolerance of the extremophytes Eutrema salsugineum (Thellungiella salsuginea) and Eutrema (Thellungiella) botschantzevii

Shamustakimova, A. O., Leonova, G., Taranov, V. V., de Boer, A. H. & Babakov, A. V., 1 Jan 2017, In : Journal of Plant Physiology. 208, January, p. 128-138 11 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Eutrema
Salt-Tolerance
cold stress
salt tolerance
Acclimatization

CXCR4-Specific Nanobodies as Potential Therapeutics for WHIM syndrome

de Wit, R. H., Heukers, R., Brink, H. J., Arsova, A., Maussang, D., Cutolo, P., Strubbe, B., Vischer, H. F., Bachelerie, F. & Smit, M. J., Oct 2017, In : The Journal of Pharmacology and Experimental Therapeutics. 363, 1, p. 35-44 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Single-Domain Antibodies
Therapeutics
Leukocytes
WHIM syndrome
Antibodies

Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators

Galambos, J., Bielik, A., Wágner, G., Domány, G., Kóti, J., Béni, Z., Szigetvári, Á., Sánta, Z., Orgován, Z., Bobok, A., Kiss, B., Mikó-Bakk, M. L., Vastag, M., Sághy, K., Krasavin, M., Gál, K., Greiner, I., Szombathelyi, Z. & Keserű, G. M., 1 Jan 2017, In : European Journal of Medicinal Chemistry. 133, p. 240-254 15 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Metabotropic Glutamate 5 Receptor
Morpholinos
Modulators
Anxiety
Central Nervous System Diseases

Human cytomegalovirus-encoded receptor US28 is expressed in renal allografts and facilitates viral spreading in vitro.

Lollinga, W. T., de Wit, R. H., Rahbar, A., Vasse, G. F., Davoudi, B., Diepstra, A., Riezebos-Brilman, A., Harmsen, M. C., Hillebrands, J-L., Söderberg-Naucler, C., van Son, W. J., Smit, M. J., Sanders, J-S. & van den Born, J., Mar 2017, In : Transplantation. 101, 3, p. 531-540 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Cytomegalovirus
Allografts
Kidney
Vascular Smooth Muscle
Smooth Muscle Myocytes

Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators

Song, G., Yang, D., Wang, Y., de Graaf, C., Zhou, Q., Jiang, S., Liu, K., Cai, X., Dai, A., Lin, G., Liu, D., Wu, F., Wu, Y., Zhao, S., Ye, L., Han, G. W., Lau, J., Wu, B., Hanson, M. A., Liu, Z. J. & 2 othersWang, M. W. & Stevens, R. C., 8 Jun 2017, In : Nature. 546, 7657, p. 312-315 4 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Glucagon Receptors
G-Protein-Coupled Receptors
Insulin
Glucose
Secretin

Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype

Hillger, J. M., le Roy, B., Wang, Z., Mulder-Krieger, T., Boomsma, D. I., Slagboom, P. E., Danen, E. H. J., IJzerman, A. P. & Heitman, L. H., 15 Apr 2017, In : Biochemical Pharmacology. 130, p. 60-70 11 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Cannabinoid Receptors
Cannabinoids
Screening
Genotype
Ligands

Structure and Function of Peptide-Binding G Protein-Coupled Receptors

Wu, F., Song, G., de Graaf, C. & Stevens, R. C., 2017, (Accepted/In press) In : Journal of Molecular Biology.

Research output: Contribution to JournalArticleAcademicpeer-review

G-Protein-Coupled Receptors
Carrier Proteins
Peptides
Pharmaceutical Preparations
Ligands

Structure of the full-length glucagon class B G-protein-coupled receptor

Zhang, H., Qiao, A., Yang, D., Yang, L., Dai, A., de Graaf, C., Reedtz-Runge, S., Dharmarajan, V., Zhang, H., Han, G. W., Grant, T. D., Sierra, R. G., Weierstall, U., Nelson, G., Liu, W., Wu, Y., Ma, L., Cai, X., Lin, G., Wu, X. & 13 othersGeng, Z., Dong, Y., Song, G., Griffin, P. R., Lau, J., Cherezov, V., Yang, H., Hanson, M. A., Stevens, R. C., Zhao, Q., Jiang, H., Wang, M. W. & Wu, B., 8 Jun 2017, In : Nature. 546, 7657, p. 259-264 6 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
G-Protein-Coupled Receptors
Glucagon
Glucagon Receptors
Deuterium
Molecular Dynamics Simulation

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

The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

Bosma, R., Witt, G., Vaas, L. A. I., Josimovic, I., Gribbon, P., Vischer, H. F., Gul, S. & Leurs, R., 2017, In : Frontiers in Pharmacology. 8, p. 667

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Histamine H1 Receptors
Histamine Antagonists
GTP-Binding Proteins
Pharmaceutical Preparations
Competitive Binding
2016

4,6-diphenylpyridines as promising novel anti-influenza agents targeting the PA-PB1 protein-protein interaction: structure-activity relationships.

Trist, I. M., Nannetti, G., Tintori, C., Fallacara, A. L., Deodato, D., Mercorrelli, B., Palu, G., Wijtmans, M., Gospodova, T., Edink, E. S., Verheij, M. H. P., de Esch, I. J. P., Viteva, L., Loregian, A. & Botta, M., 2016, In : Journal of Medicinal Chemistry. 59, 6, p. 2688-2703

Research output: Contribution to JournalArticleAcademicpeer-review

Structure-Activity Relationship
Human Influenza
Antiviral Agents
Proteins
Pyridines

4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate

Galambos, J., Domány, G., Nógrádi, K., Wágner, G., Keseru, G. M., Bobok, A., Kolok, S., Mikó-Bakk, M. L., Vastag, M., Sághy, K., Kóti, J., Szakács, Z., Béni, Z., Gál, K., Szombathelyi, Z. & Greiner, I., 15 Feb 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 4, p. 1249-1252 4 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Quinolines
Modulators
Libraries
Screening
Throughput

7TM Domain structure of adhesion GPCRs.

Nijmeijer, S., Wolf, S., Ernst, O. P. & de Graaf, C., 2016, In : Handbook of Experimental Pharmacology. 234, p. 43-55

Research output: Contribution to JournalArticleAcademicpeer-review

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

Application of a cocktail approach to screen cytochrome P450 BM3 libraries for metabolic activity and diversity.

Reinen, J. R., Postma, G., Tump, C., Bloemberg, T., Engel, J., Vermeulen, N. P. E., Commandeur, J. N. M. & Honing, M., 2016, In : Analytical and Bioanalytical Chemistry. 408, 5, p. 1425-1443 19 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access

Auxin effects on ion transport in Chara corallina

Zhang, S., de Boer, A. H. & van Duijn, B., 2016, In : Journal of Plant Physiology. 193, p. 37-44

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

Histamine H1 Receptors
Histamine Antagonists
Histamine
Ligands
Pharmaceutical Preparations

Classification, nomenclature, and structural aspects of adhesion GPCRs.

Krishnan, A., Nijmeijer, S., de Graaf, C. & Schioth, H. B., 2016, In : Handbook of Experimental Pharmacology. 234, p. 15-41

Research output: Contribution to JournalArticleAcademicpeer-review