Research Output 1985 2019

2019

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

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
Open Access
Histamine H3 Receptors
histamines
Bioluminescence
bioluminescence
Energy Transfer

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

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

Differential Salt Sensitivity in Potato Cultivars: The Role of Na+ Tissue Distribution and Vacuolar Na+ Sequestration

Jaarsma, R., 2019, 113 p.

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

Open Access
File

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 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.

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., 1 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

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

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

Nanobodies: New avenues for imaging, stabilizing and modulating GPCRs

De Groof, T. W. M., Bobkov, V., Heukers, R. & Smit, M. J., 15 Mar 2019, In : Molecular and Cellular Endocrinology. 484, p. 15-24 10 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

Open Access
Single-Domain Antibodies
G-Protein-Coupled Receptors
Imaging techniques
Immunoglobulin Fragments
Antibodies

Nanobodies detecting and modulating GPCRs outside in and inside out

Heukers, R., De Groof, T. W. M. & Smit, M. J., 1 Apr 2019, In : Current Opinion in Cell Biology. 57, p. 115-122 8 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

Single-Domain Antibodies
G-Protein-Coupled Receptors
Immunoglobulin Fragments
Physiological Phenomena
Drug Discovery

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

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
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

A Structural Framework for GPCR Chemogenomics: What’s In a Residue Number?

Vass, M., Kooistra, A. J., Verhoeven, S., Gloriam, D., de Esch, I. J. P. & de Graaf, C., 2018, Computational Methods for GPCR Drug Discovery. Heifetz, A. (ed.). Humana Press Inc, p. 73-113 41 p. (Methods in Molecular Biology; vol. 1705).

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

G-Protein-Coupled Receptors
Binding Sites
Ligands
Workflow
Mutation

Biogenesis and function of extracellular vesicles in cancer

Bebelman, M. P., Smit, M. J., Pegtel, D. M. & Baglio, S. R., Aug 2018, In : Pharmacology and Therapeutics. 188, p. 1-11 11 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

Open Access
Exosomes
Neoplasms
Biological Phenomena
Endosomes
Growth

Chemical Diversity in the G Protein-Coupled Receptor Superfamily

Vass, M., Kooistra, A. J., Yang, D., Stevens, R. C., Wang, M. W. & de Graaf, C., 1 May 2018, In : Trends in Pharmacological Sciences. 39, 5, p. 494-512 19 p.

Research output: Contribution to JournalReview articleAcademicpeer-review

G-Protein-Coupled Receptors
Ligands
Cell signaling
Chemical compounds
Modulators

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., 1 Mar 2018, In : Journal of Cell Biology. 217, 3, p. 1157 1 p.

Research output: Contribution to JournalComment / Letter to the editorAcademic

Open Access
File

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

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

Diagnostic accuracy of diagnostic imaging for lumbar disc herniation in adults with low back pain or sciatica is unknown; a systematic review

Kim, J-H., van Rijn, R. M., van Tulder, M. W., Koes, B. W., de Boer, M. R., Ginai, A. Z., Ostelo, R. W. G. J., van der Windt, D. A. M. W. & Verhagen, A. P., 2018, In : Chiropractic and Manual Therapies. 26, p. 37

Research output: Contribution to JournalReview articleAcademicpeer-review

Open Access
Sciatica
Myelography
Diagnostic Imaging
Low Back Pain
Tomography

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
Authorship
Pharmaceutical Chemistry
Physics
2017

1.15 - Structural Chemogenomics Databases to Navigate Protein–Ligand Interaction Space

Kanev, G. K., Kooistra, A. J., de Esch, I. J. P. & de Graaf, C., 2017, 1.15 - Structural Chemogenomics Databases to Navigate Protein–Ligand Interaction Space. Comprehensive Medicinal Chemistry III ed. Elsvier, Vol. 1. p. 444-471

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

Ligands
Proteins
Proteome
Bioactivity
Data mining

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