Research Output 1985 2020

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2020

Real-time imaging of multivesicular body–plasma membrane fusion to quantify exosome release from single cells

Bebelman, M. P., Bun, P., Huveneers, S., van Niel, G., Pegtel, D. M. & Verweij, F. J., Jan 2020, In : Nature Protocols. 15, 1, p. 102-121 20 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Exosomes
Membrane Fusion
Fusion reactions
Multivesicular Bodies
Membranes
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

Analysis of Arabidopsis thaliana HKT1 and Eutrema salsugineum/botschantzevii HKT1;2 Promoters in Response to Salt Stress in Athkt1:1 Mutant

Nawaz, I., Iqbal, M., Hakvoort, H. W. J., de Boer, A. H. & Schat, H., 1 Jun 2019, In : Molecular Biotechnology. 61, 6, p. 442-450 9 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Arabidopsis
Salts
Agricultural Crops
Cathode ray tubes
Level control

Antibodies Targeting Chemokine Receptors CXCR4 and ACKR3

Bobkov, V., Arimont, M., Zarca, A., De Groof, T. W. M., van der Woning, B., de Haard, H. & Smit, M. J., 1 Dec 2019, In : Molecular pharmacology. 96, 6, p. 753-764 12 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Single-Domain Antibodies
Chemokine Receptors
G-Protein-Coupled Receptors
Monoclonal Antibodies
Immunoglobulin Fragments

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

Atypical chemokine receptor 3 (ACKR3): A comprehensive overview of its expression and potential roles in the immune system

Koenen, J., Bachelerie, F., Balabanian, K., Schlecht-Louf, G. & Gallego, C., 1 Dec 2019, In : Molecular pharmacology. 96, 6, p. 809-818 10 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Chemokine Receptors
Immune System
CXC Chemokines
Ligands
Inflammation
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

Community assessment to advance computational prediction of cancer drug combinations in a pharmacogenomic screen

AstraZeneca-Sanger Drug Combination DREAM Consortium, 1 Dec 2019, In : Nature Communications. 10, 1, 2674.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Pharmacogenetics
Drug Combinations
drugs
cancer
predictions

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

CXCR4/AckR3 phosphorylation and recruitment of interacting proteins: Key mechanisms regulating their functional status

Fumagalli, A., Zarca, A., Neves, M., Caspar, B., Hill, S. J., Mayor, F., Smit, M. J. & Marin, P., 1 Dec 2019, In : Molecular pharmacology. 96, 6, p. 794-808 15 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
CXC Chemokines
Chemokine Receptors
G-Protein-Coupled Receptors
Phosphorylation
Post Translational Protein Processing

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

From Insight to Modulation of CXCR4 and ACKR3 (CXCR7) Function

Smit, M. J. & van Muijlwijk-Koezen, J. E., 1 Dec 2019, In : Molecular pharmacology. 96, 6, p. 735-736 2 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Chemokine Receptors
Immunologic Receptors
Neoplasms
G-Protein-Coupled Receptors
Phosphorylation

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

Inhibition of autotransporter biogenesis by small molecules

Steenhuis, M., Abdallah, A. M., de Munnik, S. M., Kuhne, S., Sterk, G. J., van den Berg van Saparoea, B., Westerhausen, S., Wagner, S., van der Wel, N. N., Wijtmans, M., van Ulsen, P., Jong, W. S. P. & Luirink, J., Jul 2019, In : Molecular Microbiology. 112, 1, p. 81-98 18 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Membrane Proteins
Virulence Factors
Libraries
Hemoglobins
Peptide Hydrolases

Interrogating the essential bacterial cell division protein FtsQ with fragments using target immobilized NMR screening (TINS)

Glas, M., Eiso, A. B., Hollander, J., Siegal, G., Luirink, J. & de Esch, I., 1 Aug 2019, In : International Journal of Molecular Sciences. 20, 15, 3684.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
cell division
Cell Division
affinity
Screening
screening

Nanobody-Targeted Photodynamic Therapy Selectively Kills Viral GPCR-Expressing Glioblastoma Cells

De Groof, T. W. M., Mashayekhi, V., Fan, T. S., Bergkamp, N. D., Toraño, J. S., Van Senten, J. R., Heukers, R., Smit, M. J. & Oliveira, S., 1 Jan 2019, In : Molecular Pharmaceutics.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Single-Domain Antibodies
Photochemotherapy
Viral Proteins
Glioblastoma
G-Protein-Coupled Receptors

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 role of ACKR3 in breast, lung, and brain cancer

Neves, M., Fumagalli, A., van den Bor, J., Marin, P., Smit, M. J. & Mayor, F., 1 Dec 2019, In : Molecular pharmacology. 96, 6, p. 819-825 7 p.

Research output: Contribution to JournalArticleAcademicpeer-review

Open Access
Chemokine Receptors
Brain Neoplasms
Lung Neoplasms
Breast Neoplasms
Neoplasms
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

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
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