Jaco van Veldhoven
Health, safety and environmental expert
- Name
- Ing. J.P.D. van Veldhoven
- Telephone
- +31 71 527 4333
- j.van.veldhoven@science.leidenuniv.nl
I studied organic chemistry at the Hogeschool Rotterdam and as part of this I did a 6 months internship at AltanaPharma, Konstanz, Germany. The following 3 years, I synthesized screening compounds and building blocks at Specs and BioSpecs, two services companies based in Delft, The Netherlands. Because of my interest in Medicinal Chemistry I joined Prof. IJzerman's group as a research technician in March 2005.
My part of the research on adenosine receptors is the synthesis of new ligands. I am particular interested in labeling already known ligands with a photo affinity probe. This photo affinity probe attached to the ligands can be activated by UV light and will form a covalent bond with the binding pocket of the receptor. Hopefully this research can teach us more about the location of the binding pocket on the receptor and in particular which amino acids are involved in this process.
Health, safety and environmental expert
- Science
- Bedrijfsvoering
- Arbo- en milieudienst
- Beerkens B.L.H., Wang X., Avgeropoulou M., Adistia L.N., Veldhoven J.P.D. van, Jespers W., Liu R., Heitman L.H., IJzerman A.P. & Es D. van der (2022), Development of subtype-selective covalent ligands for the adenosine A2B receptor by tuning the reactive group, RSC Medicinal Chemistry 13(7): 850-856.
- Amelia T., Veldhoven J.P.D. van, Falsini M., Liu R., Heitman L.H., Westen G.J.P. van, Segala E., Verdon G., Cheng R.K.Y., Cooke R.M., Es D. van der & IJzerman A.P. (2021), Crystal structure and subsequent ligand design of a nonriboside partial agonist bound to the adenosine A2A receptor, Journal of Medicinal Chemistry 64(7): 3827-3842.
- Veldhoven J.P.D. van, Campostrini G., Gessel C.J.E. van, Ward-van Oostwaard D., Liu R., Mummery C.L., Bellin M. & IJzerman A.P. (2021), Targeting the Kv11.1 (hERG) channel with allosteric modulators. Synthesis and biological evaluation of three novel series of LUF7346 derivatives, European Journal of Medicinal Chemistry 212: 113033.
- Mever M. van, Willacey C.C.W., Zhang W., Drouin N.F.P., Christina A.E., Lindenburg P.W., Veldhoven J.P. D. van, Es D. van der, Harms A.C., Hankemeier T. & Ramautar R. (2021), Profiling acidic metabolites by capillary electrophoresis‐mass spectrometry in low numbers of mammalian cells using a novel chemical derivatization approach, Analytical Science Advances 3(1-2): 3-13.
- Yang X., Veldhoven J.P.D. van, Offringa J., Kuiper B.J., Lenselink E.B., Heitman L.H., Es D. van der & IJzerman A.P. (2019), Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor, Journal of Medicinal Chemistry 62(7): 3539-3552.
- Ortiz Zacarías N.V., Veldhoven J.P.D. van, Hollander L.S. den, Dogan B., Openy J., Hsiao Y.Y., Lenselink E.B., Heitman L.H. & IJzerman A.P. (2019), Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5, Journal of Medicinal Chemistry 62(24): 11035-11053.
- Du L., Gao Z.G., Paoletta S., Wan T.C., Gizewski E.T., Barbour S., Veldhoven J.P.D. van, IJzerman A.P., Jacobson K.A. & Auchampach J.A. (2018), Species differences and mechanism of action of A(3) adenosine receptor allosteric modulators, Purinergic Signalling 14(1): 59-71.
- Zacarias N.V.O., Veldhoven J.P.D. van, Portner L., Spronsen E. van, Ullo S, Veenhuizen M., Velden W.J.C. van der, Zweemer A.J.M., Kreekel R.M., Oenema K., Lenselink E.B., Heitman L.H.I & IJzerman A.P. (2018), Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2, Journal of Medicinal Chemistry 61(20): 9146-9161.
- Xia L., Burger W.A.C., Veldhoven J.P.D. van, Kuiper B.J., Duijl T.T. van, Lenselink E.B., Paasman E., Heitman L.H. & IJzerman A.P. (2017), Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A(3) Receptor Antagonists, Journal of Medicinal Chemistry 60(17): 7555-7568.
- Liu R., Veldhoven J.P.D. van & IJzerman A.P. (2016), The role of the C-terminus of the human hydroxycarboxylic acid receptors 2 and 3 in G protein activation using Gα-engineered yeast cells, European Journal of Pharmacology 2016(770): 70-77.
- Lenselink E.B., Louvel J.A., Forti A.F., Veldhoven J.P.D. van, Vries H. de, Mulder-Krieger T., McRobb F.M., Negri A., Goose J., Abel R., Vlijmen H.W.T. van, Wang L., Harder E., Sherman W., IJzerman A.P. & Beuming T. (2016), Predicting binding affinities for GPCR ligands using free-energy perturbation, ACS Omega 1(2): 293-304.
- Sala L., Yu Z., Ward-van Oostwaard D., Veldhoven J.P.D. van, Moretti A., Laugwitz K.L., Mummery C.L., IJzerman A.P. & Bellin M. (2016), A new hERG allosteric modulator rescues genetic and drug‐induced long‐QT syndrome phenotypes in cardiomyocytes from isogenic pairs of patient induced pluripotent stem cells, EMBO Molecular Medicine 8(9): 1065-1081.
- Yu Z., Liu J., Veldhoven J.P.D. van, IJzerman A.P., Schalij M.J., Pijnappels D.A., Heitman L.H. & Vries A.A.F. de (2016), Allosteric modulation of K(v)11.1 (hERG) channels protects against drug-induced ventricular arrhythmias, Circulation: Arrhythmia and Electrophysiology 9(4): e003439.
- Veldhoven J.P.D. van, Liu R., Thee S.A., Wouters Y., Verhoork S.J.M., Mooiman C., Louvel J. & IJzerman A.P. (2015), Affinity and kinetics study of anthranilic acids as HCA(2) receptor agonists, Bioorganic & Medicinal Chemistry 23(14): 4013-4025.
- Vilums M., Zweemer A.J.M., Dilanchian A., Veldhoven J.P.D., Vries H. de, Brussee J., Saunders J., Stamos D., Heitman L.H. & IJzerman A.P. (2015), Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor, ChemMedChem 10(7): 1249-1258.
- Zhiyi Y., Veldhoven J.P.D. van, Louvel J.A., Hart I.M.E. 't, Rook M.B., Heyden M.A.G. van der, Heitman L.H. & IJzerman A.P. (2015), Structure-affinity relationships (SARs) and structure-kinetics relationships (SKRs) of Kv11.1 blockers, Journal of Medicinal Chemistry 58(15): 5916-5929.
- Yu Z., Veldhoven J.P.D. van, Hart I.M. 't, Kopf A.H., Heitman L.H. & IJzerman A.P. (2015), Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel, European Journal of Medicinal Chemistry 106: 50-9.
- Du L., Gao Z.-G., Paoletta S., Wan T., Veldhoven J.P.D. van, IJzerman A.P., Jacobson K. & Auchampach J. (2014), Species differences and molecular mechanism of action of A(3) adenosine receptor allosteric modulators, 10(4): 755-755.
- Guo D., Xia L., Veldhoven J.P.D. van, Hazeu M.D., Mocking T., Brussee J.M., IJzerman A.P. & Heitman L.H. (2014), Binding kinetics of ZM241385 derivatives at the human adenosine A(2A) receptor, ChemMedChem 9(4): 752-761.
- Guo Dong, Van Dorp Erika J.H., Mulder-Krieger Thea, Van Veldhoven Jacobus P.D., Brussee Johannes, IJzerman Adriaan P. & Heitman Laura H. (2013), Dual-Point Competition Association Assay: A Fast and High-Throughput Kinetic Screening Method for Assessing Ligand-Receptor Binding Kinetics, Journal of Biomolecular Screening 18(3): 309-320.
- Du Lili, Gao Zhan-Guo, Nithipatikom Kasem, IJzerman Adriaan P., Van Veldhoven Jacobus P.D., Jacobson Kenneth A., Gross Garrett J. & Auchampach John A. (2012), Protection from Myocardial Ischemia/Reperfusion Injury by a Positive Allosteric Modulator of the A(3) Adenosine Receptor, Journal of Pharmacology and Experimental Therapeutics 340(1): 210-217.
- Blad Clara C., Van Veldhoven Jacobus P.D., Klopman Corne, Wolfram Dieter R., Brussee Johannes, Lane J. Robert & IJzerman Adriaan P. (2012), Novel 3,6,7-Substituted Pyrazolopyrimidines as Positive Allosteric Modulators for the Hydroxycarboxylic Acid Receptor 2 (GPR109A), Journal of Medicinal Chemistry 55(7): 3563-3567.
- Horst Eelke van der, Marques-Gallego P., Mulder-Krieger Thea, Veldhoven J.P.D. van, Kruisselbrink J.W., Aleman A., Emmerich Michael T.M., Brussee J., Bender Andreas & IJzerman A.P. (2012), Multi-Objective Evolutionary Design of Adenosine Receptor Ligands, Journal of Chemical Information and Modeling 52(7): 1713-1721.
- Bot I., Vries H. de, Korporaal S.J.A., Foks A.C., Bot M., Veldhoven J.P.D., Borg M.N.D. ter, Santbrink P.J. van, Berkel T.J. van.C., Kuiper J. & Ijzerman A.P. (2012), Adenosine A(2B) Receptor Agonism Inhibits Neointimal Lesion Development After Arterial Injury in Apolipoprotein E-Deficient Mice, Arteriosclerosis, Thrombosis, and Vascular Biology 32(9): 2197-2205.
- Du L.L., Gao Z.G., Veldhoven J.P.D. van, IJzerman A.P., Jacobson K.A. & Auchampach J.A. (2012), Activity of LUF6000 and LUF6096 as positive allosteric modulators (PAMs) for the A3 adenosine receptor (AR) is species-dependent, 340(1): 210-217.
- Veldhoven J.P.D. van, Blad C.C., Artsen C.M., Klopman C., Wolfram D.R., Abdelkadir M.J., Lane J.R., Brussee J. & IJzerman A.P. (2011), Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A), Bioorganic and Medicinal Chemistry Letters 21(9): 2736-2739.
- Heitman L.H., Göblyös A., Zweemer A.M., Bakker R., Mulder-Krieger T., Veldhoven J.P.D. van, Vries H. de, Brussee J. & IJzerman A.P. (2009), A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A(3) receptor, Journal of Medicinal Chemistry 52(4): 926-931.
- Heitman L.H., Veldhoven J.P.D. van, Zweemer A.M., Ye K., Brussee J. & IJzerman A.P. (2008), False Positives in a Reporter Gene Assay: Identification and Synthesis of Substituted N-Pyridin-2-yl-benzamides as Competitive Inhibitors of Firefly Luciferase, Journal of Medicinal Chemistry 51(15): 4724-4729.
- Mantri M., Graaf O. de, Veldhoven J.P.D. van, Göblyös A., Frijtag Drabbe Künzel J.K. von, Mulder-Krieger T., Link R., Vries H. de, Beukers M.W., Brussee J. & IJzerman A.P. (2008), 2-Amino-6-furan-2-yl-4-substituted-nicotinonitriles as A2A adenosine receptor antagonists, Journal of Medicinal Chemistry 51(15): 4449-4455.
- Veldhoven J.P.D. van, Chang L.C.W., Frijtag Drabbe Kűnzel J.K. von, Mulder-Krieger T., Struensee-Link R., Beukers M.W., Brussee J. & IJzerman A.P. (2008), A new generation of adenosine receptor antagonists: From di- to trisubstituted aminopyrimidines, Bioorganic & Medicinal Chemistry 16(6): 2741-2752.