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
Sala, Luca, Yu, Zhiyi, Ward‐van Oostwaard, Dorien, Veldhoven, Jacobus PD, Moretti, Alessandra, Laugwitz, Karl‐Ludwig, Mummery, Christine L, IJzerman, Adriaan P, Bellin, Milena
Published in EMBO molecular medicine (01.09.2016)
Published in EMBO molecular medicine (01.09.2016)
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Journal Article
Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2
Ortiz Zacarías, Natalia V, van Veldhoven, Jacobus P. D, Portner, Laura, van Spronsen, Eric, Ullo, Salviana, Veenhuizen, Margo, van der Velden, Wijnand J. C, Zweemer, Annelien J. M, Kreekel, Roy M, Oenema, Kenny, Lenselink, Eelke B, Heitman, Laura H, IJzerman, Adriaan P
Published in Journal of medicinal chemistry (25.10.2018)
Published in Journal of medicinal chemistry (25.10.2018)
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Journal Article
Structure–Affinity Relationships and Structure–Kinetics Relationships of Pyrido[2,1‑f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists
Xia, Lizi, Burger, Wessel A. C, van Veldhoven, Jacobus P. D, Kuiper, Boaz J, van Duijl, Tirsa T, Lenselink, Eelke B, Paasman, Ellen, Heitman, Laura H, IJzerman, Adriaan P
Published in Journal of medicinal chemistry (14.09.2017)
Published in Journal of medicinal chemistry (14.09.2017)
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Journal Article
Predicting Binding Affinities for GPCR Ligands Using Free-Energy Perturbation
Lenselink, Eelke B, Louvel, Julien, Forti, Anna F, van Veldhoven, Jacobus P. D, de Vries, Henk, Mulder-Krieger, Thea, McRobb, Fiona M, Negri, Ana, Goose, Joseph, Abel, Robert, van Vlijmen, Herman W. T, Wang, Lingle, Harder, Edward, Sherman, Woody, IJzerman, Adriaan P, Beuming, Thijs
Published in ACS omega (31.08.2016)
Published in ACS omega (31.08.2016)
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Journal Article
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A2A Receptor
Amelia, Tasia, van Veldhoven, Jacobus P. D, Falsini, Matteo, Liu, Rongfang, Heitman, Laura H, van Westen, Gerard J. P, Segala, Elena, Verdon, Grégory, Cheng, Robert K. Y, Cooke, Robert M, van der Es, Daan, IJzerman, Adriaan P
Published in Journal of medicinal chemistry (08.04.2021)
Published in Journal of medicinal chemistry (08.04.2021)
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Journal Article
Label-free detection of prostaglandin transporter (SLCO2A1) function and inhibition: insights by wound healing and TRACT assays
Mocking, Tamara A M, van Oostveen, Wieke M, van Veldhoven, Jacobus P D, Minnee, Hugo, Fehres, Cynthia M, Whitehurst, Charles E, IJzerman, Adriaan P, Heitman, Laura H
Published in Frontiers in pharmacology (09.05.2024)
Published in Frontiers in pharmacology (09.05.2024)
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Journal Article
Development of subtype-selective covalent ligands for the adenosine A2B receptor by tuning the reactive group
Beerkens, Bert L. H., Wang, Xuesong, Avgeropoulou, Maria, Adistia, Lisa N., van Veldhoven, Jacobus P. D., Jespers, Willem, Liu, Rongfang, Heitman, Laura H., IJzerman, Adriaan P., van der Es, Daan
Published in MedChemComm (20.07.2022)
Published in MedChemComm (20.07.2022)
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Journal Article
False Positives in a Reporter Gene Assay: Identification and Synthesis of Substituted N-Pyridin-2-ylbenzamides as Competitive Inhibitors of Firefly Luciferase
Heitman, Laura H, van Veldhoven, Jacobus P. D, Zweemer, Annelien M, Ye, Kai, Brussee, Johannes, IJzerman, Adriaan P
Published in Journal of medicinal chemistry (14.08.2008)
Published in Journal of medicinal chemistry (14.08.2008)
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Journal Article
Species differences and mechanism of action of A3 adenosine receptor allosteric modulators
Du, Lili, Gao, Zhan-Guo, Paoletta, Silvia, Wan, Tina C., Gizewski, Elizabeth T., Barbour, Samantha, van Veldhoven, Jacobus P. D., IJzerman, Adriaan P., Jacobson, Kenneth A., Auchampach, John A.
Published in Purinergic signalling (01.03.2018)
Published in Purinergic signalling (01.03.2018)
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Journal Article
Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor
Yang, Xue, van Veldhoven, Jacobus P. D, Offringa, Jelle, Kuiper, Boaz J, Lenselink, Eelke B, Heitman, Laura H, van der Es, Daan, IJzerman, Adriaan P
Published in Journal of medicinal chemistry (11.04.2019)
Published in Journal of medicinal chemistry (11.04.2019)
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Journal Article
Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor
Vilums, Maris, Zweemer, Annelien J. M., Dilanchian, Arian, van Veldhoven, Jacobus P. D., de Vries, Henk, Brussee, Johannes, Saunders, John, Stamos, Dean, Heitman, Laura H., IJzerman, Adriaan P.
Published in ChemMedChem (01.07.2015)
Published in ChemMedChem (01.07.2015)
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Journal Article
Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics
Guo, Dong, van Dorp, Erika J H, Mulder-Krieger, Thea, van Veldhoven, Jacobus P D, Brussee, Johannes, Ijzerman, Adriaan P, Heitman, Laura H
Published in Journal of biomolecular screening (01.03.2013)
Published in Journal of biomolecular screening (01.03.2013)
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Journal Article
Novel 3,6,7-Substituted Pyrazolopyrimidines as Positive Allosteric Modulators for the Hydroxycarboxylic Acid Receptor 2 (GPR109A)
Blad, Clara C, van Veldhoven, Jacobus P. D, Klopman, Corné, Wolfram, Dieter R, Brussee, Johannes, Lane, J. Robert, IJzerman, Adriaan P
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
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Journal Article
Binding Kinetics of ZM241385 Derivatives at the Human Adenosine A2A Receptor
Guo, Dong, Xia, Lizi, van Veldhoven, Jacobus P. D., Hazeu, Marc, Mocking, Tamara, Brussee, Johannes, IJzerman, Adriaan P., Heitman, Laura H.
Published in ChemMedChem (01.04.2014)
Published in ChemMedChem (01.04.2014)
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Journal Article
A new generation of adenosine receptor antagonists: From di- to trisubstituted aminopyrimidines
van Veldhoven, Jacobus P.D., Chang, Lisa C.W., von Frijtag Drabbe Künzel, Jacobien K., Mulder-Krieger, Thea, Struensee-Link, Regina, Beukers, Margot W., Brussee, Johannes, IJzerman, Adriaan P.
Published in Bioorganic & medicinal chemistry (15.03.2008)
Published in Bioorganic & medicinal chemistry (15.03.2008)
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Journal Article
Labeling of CC Chemokine Receptor 2 with a Versatile Intracellular Allosteric Probe
den Hollander, Lisa S., Beerkens, Bert L.H., Dekkers, Sebastian, van Veldhoven, Jacobus P.D., Ortiz Zacarías, Natalia V., van der Horst, Cas, Sieders, Elisabeth G., de Valk, Bert, Wang, Jianhui, IJzerman, Adriaan P., van der Es, Daan, Heitman, Laura H.
Published in ACS chemical biology (20.09.2024)
Published in ACS chemical biology (20.09.2024)
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Journal Article
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5
Zacarias, Natalia V. Ortiz, van Veldhoven, Jacobus P. D., den Hollander, Lisa S., Dogan, Burak, Openy, Joseph, Hsiao, Ya-Yun, Lenselink, Eelke B., Heitman, Laura H., IJzerman, Adriaan P.
Published in Journal of medicinal chemistry (26.12.2019)
Published in Journal of medicinal chemistry (26.12.2019)
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Journal Article
Exploring novel dilazep derivatives as hENT1 inhibitors and potentially covalent molecular tools
Dilweg, Majlen A, Gorostiola González, Marina, de Ruiter, Martijn D, Meijboom, Nadine J, van Veldhoven, Jacobus P D, Liu, Rongfang, Jespers, Willem, van Westen, Gerard J P, Heitman, Laura H, IJzerman, Adriaan P, van der Es, Daan
Published in Purinergic signalling (15.06.2024)
Published in Purinergic signalling (15.06.2024)
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Journal Article
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A 2A Receptor
Amelia, Tasia, van Veldhoven, Jacobus P D, Falsini, Matteo, Liu, Rongfang, Heitman, Laura H, van Westen, Gerard J P, Segala, Elena, Verdon, Grégory, Cheng, Robert K Y, Cooke, Robert M, van der Es, Daan, IJzerman, Adriaan P
Published in Journal of medicinal chemistry (08.04.2021)
Published in Journal of medicinal chemistry (08.04.2021)
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Journal Article
Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor
Guo, Dong, Venhorst, Suzanne N, Massink, Arnault, Veldhoven, Jacobus P D, Vauquelin, Georges, IJzerman, Adriaan P, Heitman, Laura H
Published in British journal of pharmacology (01.12.2014)
Published in British journal of pharmacology (01.12.2014)
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