Research Topics
| Jeroen KoolSummaryAffiliation: Vrije Universiteit Country: The Netherlands Publications
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Detail Information
Publications
High throughput screening methodologies classified for major drug target classes according to target signaling pathwaysJeroen Kool
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Science, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, Amsterdam, The Netherlands
Comb Chem High Throughput Screen 13:548-61. 2010..Furthermore, special attention is paid to less traditional (non-platereader based) state-of-the-art screening approaches such as LC-MS, microarrays, microfluidics and sensor based technologies...
Nanofractionation spotter technology for rapid contactless and high-resolution deposition of LC eluent for further off-line analysisJeroen Kool
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, and FMI Bèta VU, ELE Bèta VU Mechanical and Electronic Engineering, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, 1081HV Amsterdam, The Netherlands
Anal Chem 83:125-32. 2011....
Advances in mass spectrometry-based post-column bioaffinity profiling of mixturesJeroen Kool
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, The Netherlands
Anal Bioanal Chem 399:2655-68. 2011..Furthermore, off-line screening is discussed briefly with the on-line and at-line approaches...- Online fluorescence enhancement assay for the acetylcholine binding protein with parallel mass spectrometric identificationJeroen Kool
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, 1081HV Amsterdam, The Netherlands
J Med Chem 53:4720-30. 2010..This led to the possibility of affinity ranking of ligands in mixtures with parallel high-resolution mass spectrometry for compound identification... - High-resolution bioactivity profiling of mixtures toward the acetylcholine binding protein using a nanofractionation spotter technologyJeroen Kool
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, Amsterdam, The Netherlands
J Biomol Screen 16:917-24. 2011.... - Development of a microfluidic confocal fluorescence detection system for the hyphenation of nano-LC to on-line biochemical assaysFerry Heus
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
Anal Bioanal Chem 398:3023-32. 2010..Finally, coupling of the detection system to gradient reversed-phase nano-LC allowed analysis of mixtures in order to identify the bioactive compounds present by injecting 10 nL of each mixture... - Targeted LC-MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBAMark Eggink
Section of Biomolecular Analysis, Faculty of Science, VU University Amsterdam, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands
Anal Bioanal Chem 397:665-75. 2010.... - Development of three parallel cytochrome P450 enzyme affinity detection systems coupled on-line to gradient high-performance liquid chromatographyJeroen Kool
Vrije Universiteit, Department of Pharmacochemistry, LACDR Division of Molecular Toxicology, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
Drug Metab Dispos 35:640-8. 2007..The triple parallelized P450-EAD system was shown to enable rapid profiling of individual components in complex mixtures for inhibitory activity to three different P450s... - Online biochemical detection of glutathione-S-transferase P1-specific inhibitors in complex mixturesJeroen Kool
LACDR Division of Molecular Toxicology, Department of Pharmacochemistry, Vrije Universiteit, Amsterdam, The Netherlands
J Biomol Screen 12:396-405. 2007..It is concluded that the present online gradient HPLC-based HRS screening technology offers new perspectives for sensitive and simultaneous screening of general cGSTs and specific GST P1 inhibitors in mixtures... - On-line electrochemistry-bioaffinity screening with parallel HR-LC-MS for the generation and characterization of modified p38α kinase inhibitorsDavid Falck
Division of BioMolecular Analysis, Faculty of Sciences, VU University Amsterdam, Amsterdam, The Netherlands
Anal Bioanal Chem 403:367-75. 2012..Both products were detected in the p38α bioaffinity assay, which indicates binding to the p38α kinase... - Determination and identification of estrogenic compounds generated with biosynthetic enzymes using hyphenated screening assays, high resolution mass spectrometry and off-line NMRJon S B de Vlieger
LACDR Division of Biomolecular Analysis, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
J Chromatogr B Analyt Technol Biomed Life Sci 878:667-74. 2010..g. metabolism studies and compound-library screening... - Reversed-phase liquid chromatography coupled on-line to estrogen receptor bioaffinity detection based on fluorescence polarizationJelle Reinen
Department of Chemistry and Pharmaceutical Sciences, LACDR Division of Molecular Toxicology, Vrije Universiteit, De Boelelaan 1083, 1081 HV, Amsterdam, The Netherlands
Anal Bioanal Chem 390:1987-98. 2008..It is concluded that the on-line FP-based bioassay can be used to screen for the affinity of compounds without the disturbing occurrence of autofluorescence... - Rapid on-line profiling of estrogen receptor binding metabolites of tamoxifenJeroen Kool
Leiden Amsterdam Center for Drug Research/Division of Molecular Toxicology, Department of Chemistry and Pharmacochemistry, Vrije Universiteit, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
J Med Chem 49:3287-92. 2006..Most of the 14 metabolites detected exhibited affinity for the ERalpha. The HRS methodology shows great potential for metabolite bio-affinity profiling and application in drug discovery and development... - Screening of protein-ligand interactions using dynamic protein-affinity chromatography solid-phase extraction-liquid chromatography-mass spectrometryNiels Jonker
VU University Amsterdam, Faculty of Sciences, Department of Chemistry, Biomolecular Analysis Group, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
J Chromatogr A 1205:71-7. 2008..The weakest binder that can be identified is norethindrone (approximately K(d)=0.1-1mM). The same setup also provides the possibilities to measure EC50 curves of both weak and strong binders... - Cytochrome P450 bio-affinity detection coupled to gradient HPLC: on-line screening of affinities to cytochrome P4501A2 and 2D6Jeroen Kool
LACDR Division of Molecular Toxicology, Department of Pharmacochemistry, Vrije Universiteit, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
J Chromatogr B Analyt Technol Biomed Life Sci 858:49-58. 2007..Finally, the on-line CYP2D6 EAD system was used to screen for the inhibitory activities of stereoisomers of a mixture of five methylenedioxy-alkylamphetamines (XTC analogs) on a chiral analytical column... - Development of surface plasmon resonance biosensor assays for primary and secondary screening of acetylcholine binding protein ligandsKim Retra
Leiden Amsterdam Center for Drug Research, Division of BioMolecular Analysis, Faculty of Sciences, Vrije Universiteit Amsterdam, 1081 HV Amsterdam, The Netherlands
Anal Biochem 407:58-64. 2010..96. Using both assays, we identified the compound tacrine as a ligand for AChBP... - Online magnetic bead based dynamic protein affinity selection coupled to LC-MS for the screening of acetylcholine binding protein ligandsLionel Pochet
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, 1081HV Amsterdam, The Netherlands
J Chromatogr B Analyt Technol Biomed Life Sci 879:1781-8. 2011..The results obtained with AChBP as target protein demonstrated reliable discrimination between binders with pK(i) values ranging from at least 6.26 to 8.46 and non-binders... - Metabolic profiling of endocrine-disrupting compounds by on-line cytochrome p450 bioreaction coupled to on-line receptor affinity screeningSebastiaan M van Liempd
LACDR Division of Molecular Toxicology, Department of Chemistry and Pharmaceutical Sciences, Vrije Universiteit, Amsterdam, The Netherlands
Chem Res Toxicol 20:1825-32. 2007..The hyphenated P450-bioreactor-SPE-HPLC-HRS-ERAD methodology presented here will be of great interest in on-line research of metabolic activation of endocrine-disrupting compounds... - High temperature liquid chromatography hyphenated with ESI-MS and ICP-MS detection for the structural characterization and quantification of halogen containing drug metabolitesJon S B de Vlieger
Biomolecular Analysis Group, Faculty of Sciences, VU University Amsterdam, The Netherlands
Anal Chim Acta 698:69-76. 2011..The importance of these kinds of quantification strategies is stressed by the observation that the difference of the position of one oxygen atom in a structure can greatly affect its response in ESI-MS and UV detection... - Development of an on-line weak-cation exchange liquid chromatography-tandem mass spectrometric method for screening aldehyde products in biological matricesMark Eggink
VU University Amsterdam, Faculty of Science, Section of Analytical Chemistry and Applied Spectroscopy, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
J Chromatogr B Analyt Technol Biomed Life Sci 877:3937-45. 2009..An in vitro model shows how derivatized aldehydes in human and rat plasma are detected. Finally, plasma treated with radical inducer shows elevated aldehyde species compared to untreated plasma... - An on-line post-column detection system for the detection of reactive-oxygen-species-producing compounds and antioxidants in mixturesJeroen Kool
LACDR Division of Molecular Toxicology, Department of Pharmacochemistry, Vrije Universiteit, Amsterdam, The Netherlands
Anal Bioanal Chem 388:871-9. 2007..The resulting high-resolution screening technology was able to separate mixtures of ROS-producing compounds and antioxidants, allowing each species to be characterized rapidly and sensitively... - Recent developments in protein-ligand affinity mass spectrometryNiels Jonker
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, The Netherlands
Anal Bioanal Chem 399:2669-81. 2011..The review addresses the principles of each of the methods discussed, with a focus on developments in recent years, and the applicability of the methods to lead generation and development in drug discovery... - Development of an online p38α mitogen-activated protein kinase binding assay and integration of LC-HR-MSDavid Falck
LACDR Division of Biomolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, VU University Amsterdam, 1081 HV Amsterdam, The Netherlands
Anal Bioanal Chem 398:1771-80. 2010..8, which is suitable for semi-quantitative affinity measurements and applicable to various binding modes. Furthermore, the integrated approach gives affinity data on individual compounds instead of averaged ones for mixtures... - Production and on-line acetylcholinesterase bioactivity profiling of chemical and biological degradation products of tacrineLygia Azevedo Marques
VU University Amsterdam, Faculty of Sciences, Section of Biomolecular Analysis, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
J Pharm Biomed Anal 53:609-16. 2010..Furthermore, chemical degradation can be used to produce conveniently and in relatively large quantities clean mixtures of compounds that are also produced during metabolic incubations... - Development of a selective ESI-MS derivatization reagent: synthesis and optimization for the analysis of aldehydes in biological mixturesMark Eggink
Leiden Amsterdam Center for Drug Research, Faculty of Sciences, Department of Chemistry, Section of Analytical Chemistry and Applied Spectroscopy, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
Anal Chem 80:9042-51. 2008..Finally, of all aldehydes, pentanal and hexanal were detected at elevated levels in pooled healthy human urine samples... - Microfractionation revisited: a 1536 well high resolution screening assayMartin Giera
Biomolecular Analysis Group, Department of Chemistry, Faculty of Sciences, VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
Anal Chem 81:5460-6. 2009..Furthermore, it allows coupling of a microbore HPLC with a biochemical screening assay without compromising resolution and overcomes problems associated with the 1536 well format... - Development of a profiling strategy for metabolic mixtures by combining chromatography and mass spectrometry with cell-based GPCR signalingSaskia Nijmeijer
Medicinal Chemistry, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University, Amsterdam, The Netherlands
J Biomol Screen 17:1329-38. 2012.... - An efficient analytical platform for on-line microfluidic profiling of neuroactive snake venoms towards nicotinic receptor affinityFerry Heus
AIMMS Division of BioMolecular Analysis, Faculty of Sciences, De Boelelaan 1083, 1081 HV Amsterdam, VU University Amsterdam, The Netherlands
Toxicon 61:112-24. 2013..Our methodology has the potential to aid the field of profiling complex animal venoms for drug discovery... - Studying protein-protein affinity and immobilized ligand-protein affinity interactions using MS-based methodsJeroen Kool
BioMolecular Analysis, Department of Chemistry and Pharmaceutical Sciences, Faculty of Sciences, VU University Amsterdam, Amsterdam, The Netherlands
Anal Bioanal Chem 401:1109-25. 2011..The review focuses on the analysis of bioaffinity interactions of proteins with other proteins and with ligands, where the proteins are considered as the bioactives analyzed by MS... - Online screening of homogeneous catalyst performance using reaction detection mass spectrometryCornelius T Martha
Department of Analytical Chemistry and Applied Spectroscopy, Faculty of Sciences, Vrije Universiteit Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands
Anal Chem 80:7121-7. 2008.... - A flow-through fluorescence polarization detection system for measuring GPCR-mediated modulation of cAMP productionJeroen Kool
LACDR Division of Molecular Toxicology, Department of Chemistry and Pharmaceutical Sciences, Vrije Universiteit Amsterdam, The Netherlands
J Biomol Screen 12:1074-83. 2007.... - Development of a novel cytochrome p450 bioaffinity detection system coupled online to gradient reversed-phase high-performance liquid chromatographyJeroen Kool
LACDR-Division of Molecular Toxicology, Department of Pharmacochemistry, Vrije Universiteit, Amsterdam, The Netherlands
J Biomol Screen 10:427-36. 2005..It is concluded that this novel screening technology offers new perspectives for rapid and sensitive screening of individual compounds in mixtures exhibiting affinity for liver microsomal Cyt P450s... - The chemical interaction between the estrogen receptor and monohydroxybenzo[a]pyrene derivatives studied by fluorescence line-narrowing spectroscopyArjen N Bader
Department of Analytical Chemistry and Applied Spectroscopy, Laser Centre, Amsterdam, The Netherlands
Chem Res Toxicol 18:1405-12. 2005..Furthermore, the spectra indicated a pi-pi stacking aromatic interaction for 9-OH-BaP with PHE404. These results are in line with molecular modeling studies published earlier... - Development and validation of a microsomal online cytochrome P450 bioreactor coupled to solid-phase extraction and reversed-phase liquid chromatographySebastiaan M van Liempd
LACDR-Division of Molecular Toxicology, Department of Pharmacochemistry, Vrije Universiteit, De Boelelaan 1083, 1081 HVAmsterdam, The Netherlands
J Chromatogr A 1075:205-12. 2005..66 +/- 0.08 microM and 6.4 +/- 0.2 nmol/min/mg protein respectively. In conclusion the newly developed analytical method can be used effectively and at a microliter scale for online generation, extraction and separation of metabolites...