Adriaan IJzerman

Professor emeritus Pharmacochemistry

Name: Prof.dr. A.P. IJzerman
Telephone: +31 71 527 2727
E-mail: ijzerman@lacdr.leidenuniv.nl
ORCID iD: 0000-0002-1182-2259

Ad IJzerman is Professor of Medicinal Chemistry and Head of the Medicinal Chemistry group at the Division of Drug Discovery & Safety. His research interests are linked to G protein-coupled receptors (GPCRs).

More information about Adriaan IJzerman

PhD Candidates

News

Former PhD candidates

I studied pharmacy at Utrecht University. In 1979 I graduated with a specialization in pharmaceutical chemistry and one year later I qualified as a pharmacist. Rather than opening a drug store I continued my research education, leading to the defense of my PhD thesis from the Vrije Universiteit in Amsterdam in 1985, on a subject in the area of receptor research. I was appointed assistant, associate and full professor of medicinal chemistry in Leiden in 1985, 1992 and 2000, respectively.

My research interests have always been linked to G protein-coupled receptors (GPCRs). In particular the molecular mechanisms of drug action are at the core of my research 'business'. One cannot study all (800?) GPCRs at the time, so my main attention is focussed on adenosine receptors. Every now and then I allow myself to diverge a little bit, lately to study nicotinic acid and chemokine CCR2 receptors. All this has led to a scientific 'output' of over 260 articles, quite a few reviews and book chapters, a dozen or so patents, and some 20 accepted PhD theses. You will find references to recent work at this website.

Duties as a professor include teaching, which I like very much. If you're interested why not watch a weblecture called "Breaking and Making. The art of medicinal chemistry", in which I explain and discus some principles and issues in medicinal chemistry

( https://av-media.vu.nl/VUMedia/Play/3687b568049643f1aa671c8d59c1361c1d).

My hope and dream is that once I will be able to show my students the wonder world of drug - receptor interactions through some sort of 'molecular microscope' Next to these teaching efforts other 'obligations' are the membership of the editorial boards of the Journal of Medicinal Chemistry, ChemMedChem, Purinergic Signalling, Chemistry & Biodiversity, Drug Development Research, Molecular Informatics, and Molecules. I happily contribute to the IUPHAR adenosine receptor, GnRH, and nicotinic acid receptor nomenclature committees, and manage(d) quite a number of receptor-related research programs funded by Dutch scientific bodies such as the Top Institute Pharma, and by the European Union (most prominently and recently the 2012-2017 IMI consortium on drug target kinetics). I also served as chairman to FIGON, the Dutch federation for innovative drug research ( www.figon.nl).

Professor emeritus Pharmacochemistry

Science
Leiden Academic Centre for Drug Research
LACDR/Medicinal Chemistry

Contact

Hollander L.S. den, Béquignon O.J.M., Wang X., Wezel K. van, Broekhuis J.D., Gorostiola Gonzalez M., Visser K.E. de, IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2023), Corrigendum to "Impact of cancer-associated mutations in CC chemokine receptor 2 on receptor function and antagonism" [Biochem. Pharmacol. 208 (2023) 115399], Biochemical Pharmacology 209: 115540 (115450). article in magazine/newspaper
Bongers B.J., Sijben H.J., Hartog P.B.R., Tarnovskiy A., IJzerman A.P., Heitman L.H. & Westen G.J.P. van (2023), Proteochemometric modeling identifies chemically diverse norepinephrine transporter inhibitors, Journal of Chemical Information and Modeling 63(6): 1745-1755. article in journal: refereed
Liu X., Ye K., Vlijmen H. van, IJzerman A.P. & Westen G.J.P. van (2023), DrugEx v3: scaffold-constrained drug design with graph transformer-based reinforcement learning, Journal of Cheminformatics 15(1): 24. article in journal: refereed
Béquignon O.J.M., Bongers B.J., Jespers W., IJzerman A.P., Water B. van de & Westen G.J.P. van (2023), Papyrus: a large-scale curated dataset aimed at bioactivity predictions, Journal of cheminformatics 15(1): 3. article in journal: refereed
Hollander L.S. den, Béquignon O.J.M., Wang X., Wezel K. van, Broekhuis J., Gorostiola González M., Visser K.E. de, IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2022), Impact of cancer-associated mutations in CC chemokine receptor 2 on receptor function and antagonism, Biochemical Pharmacology 208: 115399. article in journal: refereed
Bongers B.J., Gorostiola González M., Wang X., Vlijmen H. van, Jespers W., Gutiérrez-de-Terán H., Ye K., IJzerman A.P., Heitman L.H. & Westen G.J.P. van (2022), Pan-cancer functional analysis of somatic mutations in G protein-coupled receptors, Scientific Reports 12(1): 21534. article in journal: refereed
Beerkens B.L.H., Koc C., Liu R., Florea B.I., Le Dévédec S.E., Heitman L.H., IJzerman A.P. & Es D. van der (2022), A chemical biological approach to study G protein-coupled receptors: labeling the adenosine A1 receptor using an electrophilic covalent probe, ACS Chemical Biology 17(11): 3131-3139. article in journal: refereed
Wang X., Westen G.J.P. van, IJzerman A.P. & Heitman L.H. (2022), G protein-coupled receptors and their mutations in cancer: a focus on adenosine receptors. In: Gilchrist A. (Ed.) GPCRs as therapeutic targets.: John Wiley & Sons. 631-676. book chapter
Gorostiola Gonzalez M., Janssen A.P.A., IJzerman A.P., Heitman L.H. & Westen G.J.P. van (2022), Oncological drug discovery: AI meets structure-based computational research, Drug Discovery Today 27(6): 1661-1670. article in journal: refereed
Vlachodimou A., Vries H. de, Pasoli M., Goudswaard M., Kim S.A., Kim Y.C., Scortichini M., Marshall M., Linden J., Heitman L.H., Jacobson K.A. & IJzerman A.P. (2022), Kinetic profiling and functional characterization of 8-phenylxanthine derivatives as A2B adenosine receptor antagonists, Biochemical Pharmacology 200: 115027. article in journal: refereed
Wang X., Jespers W., Wolff K.A.N., Buytelaar J., IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2022), Cancer-related somatic mutations in transmembrane helices alter adenosine A1 receptor pharmacology, Molecules 27(12): 3742. article in journal: refereed
Wang X., Jespers W., Waal J.J. de, Wolff K.A.N., Uden L. van, IJzerman A.P., Westen G.J.P. van & Heitman L.H. (2022), Cancer-related somatic mutations alter adenosine A1 receptor pharmacology: a focus on mutations in the loops and C- terminus, The FASEB Journal 36(6): e22358. article in journal: refereed
Sijben H.J., Dall’ Acqua L., Liu R., Jarret A., Christodoulaki E., Onstein S., Wolf G., Verburgt S.J., Le Dévédec S.E., Wiedmer T., Superti-Furga G., IJzerman A.P. & Heitman L.H. (2022), Impedance-based phenotypic readout of transporter function: a case for glutamate transporters, Frontiers in Pharmacology 13: 872335. article in journal: refereed
IJzerman A.P., Jacobson K.A., Müller C.E., Cronstein B.N. & Cunha R.A. (2022), International Union of Basic and Clinical Pharmacology. CXII: adenosine receptors: a further update, Pharmacological Reviews 74(2): 340-372. article in journal: refereed
Sijben H.J., Superti-Furga G., IJzerman A.P. & Heitman L.H. (2022), Targeting solute carriers to modulate receptor-ligand interactions, Trends in Pharmacological Sciences 43(5): 358-361. article in journal: refereed
Mocking T.A.M., Sijben H.J., Vermeulen Y., IJzerman A.P. & Heitman L.H. (2022), MPP+-induced changes in cellular impedance as a measure for organic cation transporter (SLC22A1-3) activity and inhibition, International Journal of Molecular Sciences 23(3): 1203. article in journal: refereed
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. article in journal: refereed
Liu X., IJzerman A.P. & Westen G.J.P. van (2021), Computational Approaches for De Novo Drug Design: Past, Present, and Future. In: Cartwright H. (Ed.), Artificial Neural Networks. Methods in Molecular Biology no. 2190. New York, NY, U.S.A.: Humana Press. 139-165.
Jespers W., Heitman L.H., IJzerman A.P., Sotelo E., Westen G.J.P. van, Aqvist J. & Gutiérrez-de-Terán H. (2021), Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations, PLoS Computational Biology 17(11): e1009152. article in journal: refereed
Liu X., Ye K., Vlijmen H.W.T. van, Emmerich M.T.M., IJzerman A.P. & Westen G.J.P. van (2021), DrugEx v2: de novo design of drug molecules by pareto-based multi-objective reinforcement learning in polypharmacology, Journal of Cheminformatics 13(1): 85. article in journal: refereed
Dvorakm V., Wiedmer T., Ingles-Prieto A., Altermatt P., Batoulis H, Bärenz F., Bender E., Digles D., Dürrenberger F., Heitman L.H., IJzerman A.P., Kell D.B., Kickinger S., Körzö D., Leippe P., Licher T., Manolova V., Rizzetto R., Sassone F., Scarabottolo L., Schlessinger A., Schneider V., Sijben H.J., Steck A.L., Sundström H., Tremolada S., Wilhelm M., Wright Muelas M., Zindel D., Steppan C.M. & Superti-Furga G. (2021), An overview of cell-based assay platforms for the solute carrier family of transporters, Frontiers in Pharmacology 12: 722889. article in journal: refereed
Wang X., Jespers W., Prieto-Díaz R., Majellaro M., IJzerman A.P., Westen G.J.P. van, Sotelo E. & Heitman L.H. (2021), Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition, Scientific Reports 11. article in journal: refereed
Sijben H.J., Oostveen W.M. van, Hartog P.B.R., Stucchi L., Rossignoli A., Maresca G., Scarabottolo. L., IJzerman A.P. & Heitman L.H. (2021), Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors, Scientific Reports 11. article in journal: refereed
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. article in journal: refereed
Zhou X., Carbo-Bague I., Siegler M.A., Hilgendorf J., Basu U., Ott I., Liu R., Zhang L., Vadde R., IJzerman A.P. & Bonnet S.A. (2021), Rollover cyclometalation vs nitrogen coordination in Tetrapyridyl Anticancer Gold(III) complexes: effect on protein interaction and toxicity, JACS AU 1(4): 380-395. article in journal: refereed
Ortiz Zacarías N.V., Chahal K.K., Šimková T., Horst C. van der, Zheng Y., Inoue A., Theunissen E., Mallee L., Es D. van der, Louvel J., IJzerman A.P., Handel T.M., Kufareva I. & Heitman L.H. (2021), Design and characterization of an intracellular covalent ligand for CC chemokine receptor 2, Journal of Medicinal Chemistry 64(5): 2608-2621. article in journal: refereed
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. article in journal: refereed
Sijben H.J., Berg J.E. van den, Broekhuis J.D., IJzerman A.P. & Heitman L.H. (2021), A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery, Scientific Reports 11. article in journal: refereed
Wang X., Westen G.J.P. van, Heitman L.H. & IJzerman A.P. (2021), G protein-coupled receptors expressed and studied in yeast. The adenosine receptor as a prime example, Biochemical Pharmacology 187: 114370.
Yang X., Heitman L.H., IJzerman A.P. & Es D. van der (2021), Molecular probes for the human adenosine receptors, Purinergic Signalling 17: 85-108.
Burggraaff L., Veen A. van, Lam C.C., Vlijmen H.W.T., IJzerman A.P. & Westen G.J.P. van (2020), Annotation of Allosteric Compounds to Enhance Bioactivity Modeling for Class A GPCRs, Journal of Chemical Information and Modeling 60(10): 4664-4672.
Superti-Furga G., Lackner D., Wiedmer T., Ingles-Prieto A., Barbosa B., Girardi E., Goldmann U., Gürtl B., Klavins K., Klimek C., Lindinger S., Liñeiro-Retes E., Müller A.C., Onstein S., Redinger G., Reil D., Sedlyarov V., Wolf G., Crawford M., Everley R., Hepworth D., Liu S., Noell S., Piotrowski M., Stanton R., Zhang H., Corallino S., Faedo A., Insidioso M., Maresca G., Redaelli L., Sassone F., Scarabottolo L., Stucchi M., Tarroni P., Tremolada S., Batoulis H., Becker A., Bender E., Chang Y.N., Ehrmann A., Müller-Fahrnow A., Pütter V., Zindel D., Hamilton B., Lenter M., Santacruz D., Viollet C., Whitehurst C., Johnsson K., Leippe P., Baumgarten B., Chang L., Ibig Y., Pfeifer M., Reinhardt J., Schönbett J., Selzer P., Seuwen K., Bettembourg C., Biton B., Czech J., de Foucauld H., Didier M., Licher T., Mikol V., Pommereau A., Puech F., Yaligara V., Edwards A., Bongers B.J., Heitman L.H., Ijzerman A.P., Sijben H.J., Westen G.J.P. van, Grixti J., Kell D.B., Mughal F., Swainston N., Wright-Muelas M., Bohstedt T., Burgess-Brown N., Carpenter L., Dürr K., Hansen J., Scacioc A., Banci G., Colas C., Digles D., Ecker G., Füzi B., Gamsjäger V., Grandits M., Martini R., Troger F., Altermatt P., Doucerain C., Dürrenberger F., Manolova V., Steck A.L., Sundström H., Wilhelm M. & Steppan C.M. (2020), The RESOLUTE consortium: unlocking SLC transporters for drug discovery, Nature Reviews Drug Discovery 19(7): 429-430.
Wang X. Jespers W. Bongers B.J. Habben Jansen M.C.C. Stangenberger C.M. Dilweg M.A. Gutiérrez-de-Terán H. IJzerman A.P. Heitman L.H. Westen G.J.P. van (2020), Characterization of cancer-related somatic mutations in the adenosine A2B receptor, European Journal of Pharmacology 880: 173126.
Qile M., Ji Y., Golden T.D., Houtman M.J.C., Romunde F., Fransen D., Ham W.B. van, IJzerman A.P., January C.T., Heitman L.H., Stary-Weinzinger A., Delisle B.P. & Heyden M.A.G. van der (2020), LUF7244 plus Dofetilide Rescues Aberrant Kv11.1 Trafficking and Produces Functional IKv11.1, Molecular Pharmacology 97(6): 355-364.
Yang X. Dilweg M.A. Osemwengie D. Burggraaff L. Es D. van der Heitman L.H. IJzerman A.P. (2020), Design and pharmacological profile of a novel covalent partial agonist for the adenosine A1 receptor, Biochemical Pharmacology 180: 114144.
Burggraaff L. Lenselink E.B. Jespers W. Engelen J. van Bongers B.J. Gorostiola Gonzalez M. Liu R. Hoos H.H. Vlijmen H. van IJzerman A.P. Westen G.J.P. van (2020), Successive statistical and structure-based modeling to identify chemically novel kinase inhibitors, Journal of Chemical Information and Modeling 60(9): 4283-4295.
Vlachodimou A., Konstantinopoulou K., IJzerman A.P. & Heitman L.H. (2020), Affinity, binding kinetics and functional characterization of draflazine analogues for human equilibrative nucleoside transporter 1 (SLC29A1), Biochemical Pharmacology 172: 113747.
Bouma M.J., Freund C., IJzerman A.P., Boomsma D.I., Mummery C.L. & Raymond K. (2019), Lymphoblast-derived hiPS cell lines generated from four individuals of a family of genetically unrelated parents and their female monozygotic twins, Stem Cell Research 41: 101654.
Burggraaff L., Vlijmen H.W.T. van., IJzerman A.P. & Westen G.J.P. van (2020), Quantitative prediction of selectivity between the A1 and A2A adenosine receptors, Journal of Cheminformatics 12: 33.
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.
IJzerman A.P. & Guo D. (2019), Drug-Target Association Kinetics in Drug Discovery, Trends in Biochemical Sciences 44(10): 861-871.
Qile M., Beekman H.D.M., Sprenkeler D.J., Houtman M.J.C., Ham W.B. van, Stary-Weinzinger A., Beyl S., Hering S., Berg D.J. van den, Lange E.C.M. de, Heitman L.H., IJzerman A.P., Vos M.A. & Heyden M.A.G. van der (2019), LUF7244, an allosteric modulator/activator of Kv11.1 channels, counteracts dofetilide‐induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model, British Journal of Pharmacology 176(19): 3871-3885.
Vlachodimou A., IJzerman A.P. & Heitman L.H. (2019), Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1, Scientific Reports 9(1): 13802.
Massink A., Amelia T., Karamychev A. & IJzerman A.P. (2019), Allosteric modulation of G protein-coupled receptors by amiloride and its derivatives. Perspectives for drug discovery?, Medicinal Research Reviews 40(2): 683-708.
Oranje P., Gouka R., Burggraaff L., Vermeer M., Chalet C., Duchateau G., Pijl P. van der, Geldof M., Roo N. de, Clauwaert F., Vanpaeschen T., Nicolai J., Bruyn T. de, Annaert P., IJzerman A.P. & Westen G.J.P. van (2019), Novel natural and synthetic inhibitors of solute carriers SGLT1 and SGLT2, Pharmacology Research and Perspectives 7(4): e00504.
Bouzo-Lorenzo M., Stoddart L.A., Xia L., IJzerman A.P., Heitman L.H., Briddon S.J. & Hill S.J. (2019), A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A(3) receptor, Purinergic Signalling 15(2): 139-153.
Liu X., Ye K., Vlijmen H.W.T. van, IJzerman A.P. & Westen G.J.P. van (2019), An exploration strategy improves the diversity of de novo ligands using deep reinforcement learning: a case for the adenosine A2A receptor, Journal of Cheminformatics 11: 35.
Putten C. van der, Veth J., Sukurova L., Zuiderwijk-Sick E.A., Simonetti E., Koenen H.J.P.M., Burm S.M., Noort J.M. van, IJzerman A.P., Hijum S.A.F.T. van, Divavatopoulos D. & Bajramovi J.J. (2019), TLR-Induced IL-12 and CCL2 Production by Myeloid Cells Is Dependent on Adenosine A(3) Receptor-Mediated Signaling, Journal of Immunology 202(8): 2421-2430.
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.
Rouquette M., Lepetre-Mouelhi S., Dufrancais O., Yang X., Mougin J., Pieters G., Garcia-Argote S., IJzerman A.P. & Couvreur P. (2019), Squalene-Adenosine Nanoparticles: Ligands of Adenosine Receptors or Adenosine Prodrug?, Journal of Pharmacology and Experimental Therapeutics 369(1): 144-151.
Yun Y., Chen J., Liu R., Chen W., Liu C., Wang R., Hou Z., Yu Z., Sun Y., IJzerman A.P., Heitman L.H., Yin X. & Guo D. (2019), Long residence time adenosine A1 receptor agonists produce sustained wash-resistant antilipolytic effect in rat adipocytes, Biochemical Pharmacology 164: 45-52.
Sydow D., Burggraaff L., Szengel A., Vlijmen H. van, IJzerman A.P., Westen G.J.P. van & Volkamer A. (2019), Advances and Challenges in Computational Target Prediction, Journal of Chemical Information and Modeling 59(5): 1728-1742.
Burggraaff L., Oranje P., Gouka R., Pijl P. van der, Geldof M., Vlijmen H.W.T. van, IJzerman A.P. & Westen G.J.P. van (2019), Identification of novel small molecule inhibitors for solute carrier SGLT1 using proteochemometric modeling, Journal of Cheminformatics 11: 15.
Bongers B.J., IJzerman A.P. & Westen G.J.P. (2019), Proteochemometrics – recent developments in bioactivity and selectivity modeling, Drug Discovery Today: Technologies 32-33: 89-98. article in journal: refereed
Guo D. & IJzerman A.P. (2018), Molecular Basis of Ligand Dissociation from G Protein-Coupled Receptors and Predicting Residence Time. Methods in Molecular Biology no. 1705. New York: Springer.
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.
Rouquette M., Lepetre-Mouelhi S., Roux K.S.L., Polrot M., Cailleau C., Yang X., Ijzerman A. & Couvreur P. (2018), Adenosine delivery via squalene-adenosine nanoparticles to treat ischemic diseases: liver versus brain, New Biotechnology 44(Supplelment): S12-S12.
Yevseyeva I., Lenselink E.B., Vries A. de, IJzerman A.P., Deutz A.H. & Emmerich M.T.M. (2019), Application of portfolio optimization to drug discovery, Information Sciences 475: 29-43.
Yang X., Michiels T.J.M., Jong C. de, Soethoudt M., Dekker N., Gordon E., Stelt M. van der, Heitman L.H., Es D. van der & IJzerman A.P. (2018), An Affinity-Based Probe for the Human Adenosine A(2A) Receptor, Journal of Medicinal Chemistry 61(17): 7892-7901.
Doornbos M.L.J., Vermond S.C., Lavreysen H., Tresadern G., IJzerman A.P. & Heitman L.H. (2018), Impact of allosteric modulation: exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2, Biochemical Pharmacology 155: 356-365.
Doornbos M.L.J., Linden I. van der, Vereyken L., Tresadern G., IJzerman A.P., Lavreysen H. & Heitman L.H. (2018), Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor, Biochemical Pharmacology 152: 201-210.
Guo D., Peletier L.A., Bridge L., Keur W., Vries H. de, Zweemer J.M., Heitman L.H. & IJzerman A.P. (2018), A two-state model for the kinetics of competitive radioligand binding, British Journal of Pharmacology 175(10): 1719-1730.
Xia L., Vries H. de, Yang X., Lenselink E.B., Kyrizaki A., Barth F., Louvel J., Dreyer M.K., Es D. van der, IJzerman A.P. & Heitman L.H. (2018), Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure-kinetics relationships (SKR) and implications for insurmountable antagonism, Biochemical Pharmacology 151: 166-179.
Muller S., Ackloo S., Arrowsmith C.H., Bauser M., Baryza J.L., Blagg J., Bottcher J., Bountra C., Brown P.J., Bunnage M.E., Carter A.J., Damerell D., Dotsch V., Drewry D.H., Edwards A.M., Edwards J., Elkins J.M., Fischer C., Frye S.V., Gollner A., Grimshaw C.E., IJzerman A.P., Hanke T., Hartung I.V., Hitchcock S., Howe T., Hughes T.V., Laufer S., Li V.M.J., Liras S., Marsden B.D., Matsui H., Mathias J., O'Hagan R.C., Owen D.R., Pande V., Rauh D., Rossenberg S.H., Roth B.L., Schneider N.S., Scholten C., Saikatendu K.S., Simeonov A., Takizawa M., Tse C., Thompson P.R., Treiber D.K., Viana A.Y., Wells C.I., Willson T.M., Zuercher W.J., Knapp S., Mueller-Fahrnow A. & Mueller-Fahrnow A. (2018), Donated chemical probes for open science, eLife 7: e34311.
Ortiz Zacarías N.V., Lenselink E.B., IJzerman A.P., Handel T.M. & Heitman L.H. (2018), Intracellular Receptor Modulation: Novel Approach to Target GPCRs, Trends in Pharmacological Sciences 39(6): 547-559.
Doornbos M.L.J., Wang X., Vermond S.C., Peeters L., Pérez-Benito L., Trabanco A.A., Lavreysen H., Cid J.M., Heitman L.H., Tresadern G. & IJzerman A.P. (2019), Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization, Journal of Medicinal Chemistry 62(1): 223-233.
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.
Soethoudt M., Stolze S.C., Westphal M.V., Stralen L. van, Martella A., Rooden E.J. van, Guba W., Varga Z.V., Deng H., Kasteren S.I. van, Grether U., IJzerman A.P., Pacher P., Carreira E.M., Overkleeft H.S., Heitman L.H., Ioan-Facsinay A. & Stelt M. van der (2018), A selective photoaffinity probe that enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells, Journal of the American Chemical Society 140(19): 6067-6075.
Xia L.Z., Kyrizaki A., Tosh D.K., Duijl T.T. van, Roorda J.C., Jacobson K.A., IJzerman A.P. & Heitman L.H. (2018), A binding kinetics study of human adenosine A(3) receptor agonists, Biochemical Pharmacology 153: 248-259.
Hilger J.M., Lieuw W.L., Heitman L.H. & IJzerman A.P. (2017), Label-free technology and patient cells: from early drug development to precision medicine, Drug Discovery Today 22(12): 1808-1815.
Xia L., Vries H. de, Lenselink E.B., Louvel J.A., Waring M.J., Cheng L., Pahlen S., Petersson M.J., Schell P., Olsson R.I., Heitman L.H., Sheppard R.J. & IJzerman A.P. (2017), Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists, Journal of Medicinal Chemistry 60(23): 9545-9564.
Alexander S.P.H., Kelly E., Marrion N.V., Peters J.A., Faccenda E., Harding S.D., Pawson A.J., Sharman J.L., Southan C., Buneman O.P., Cidlowski J.A., Christopoulos A., Davenport A.P., Fabbro D., Spedding M., Striessnig J., Davies J.A. & IJzerman A.P. (2017), The concise guide to pharmacology 2017/18: Overview, British Journal of Pharmacology 174: S1-S16.
Donkers J.M., Zehnder B., Westen G.J.P. van, Kwakkenbos M.J., IJzerman A.P., Oude Elferink R.P.J., Beuers U., Urban S. & Graaf S.F.J. van de (2017), Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP, Scientific Reports 7: 15307.
Lowe P.T., Dall'Angelo S., Mulder-Krieger T., IJzerman A.P., Zanda M. & O'Hagan D. (2017), A New Class of Fluorinated A(2A) Adenosine Receptor Agonist with Application to Last-Step Enzymatic [F-18]Fluorination for PET Imaging, ChemBioChem 18(21): 2156-2164.
Nederpelt I., Kuzikov M., Witte W.E.A. de, Schnider P., Tuijt B., Gul S., IJzerman A.P., Lange E.C.M. de & Heitman L.H. (2017), From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action, Scientific Reports 7: 14169.
Martella A., Sijben H.J., Rufer A.C., Grether U., Fingerle J., Ullmer C., Hartung T., IJzerman A.P., Stelt M. van der & Heitman L.H. (2017), A novel selective inverse agonist of the CB2 receptor as a radiolabeled tool compound for kinetic binding studies, Molecular Pharmacology 92(4): 389-400.
Saxena P., Hortigon-Vinagre M.P., Beyl S., Baburin I., Andranovits S., Iqbal S.M., Costa A., IJzerman A.P., Kuegler P., Timin E., Smith G.L. & Hering S. (2017), Correlation between human ether-a-go-go-related gene channel inhibition and action potential prolongation, British Journal of Pharmacology 174(18): 3081-3093.
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.
Doornbos M.L.J., Cid J.M., Haubrich J., Nunes A.G., Sande J.W. van de, Vermond S.C., Mulder T., Trabanco A.A., Ahnaou A., Drinkenburg W.H., Lavreysen H., Heitman L.H., IJzerman A.P. & Tresadern G. (2017), Discovery and Kinetic Profiling of 7‑Aryl-1,2,4-triazolo[4,3‑a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2, Journal of Medicinal Chemistry 60(15): 6704–6720.
Yang X., Dong G., Michiels T.J.M., Lenselink E.B., Heitman L.H., Louvel J.A. & IJzerman A.P. (2017), A covalent antagonist for the human adenosine A_2A receptor, Purinergic Signalling 13(2): 191-201.
Hillger J.M., Roy B. le, Wang Z., Mulder-Krieger T., Boomsma D.I., Slagboom P.E., Danen E.H.J., IJzerman A.P. & Heitman L.H. (2017), Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype, Biochemical Pharmacology 130: 60-70.
Schuetz D.A., Witte W.E.A. de, Wong Y.C, Knasmueller B., Richter L., Kokh D.B., Sadiq S.K., Bosma R., Nederpelt I., Heitman L.H., Segala E., Amaral M., Guo D., Andres D., Georgi V., Stoddart L.A., Hill S., Cooke R.M., Graaf C. de, Leurs R., Frech M., Wade R.C., Lange E.C.M. de, IJzerman A.P., Mueller-Fahrnow A. & Ecker G.F. (2017), Kinetics for Drug Discovery: an industry-driven effort to target drug residence time, Drug Discovery Today 22(6): 896-911.
Bot I., Ortiz Zacarias N.V., Witte W.E. de, Vries H. de, Santbrink P.J. van, Velden D. van der, Kroener M.J., Berg D.J. van den, Stamos D., Lange E.C.M. de, Kuiper J., IJzerman A.P. & Heitman L.H. (2017), A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy, Scientific Reports 2017(7): 52.
Meer B.J. van, Vries H. de, Firth K.S.A., Weerd J. van, Tertoolen L.G.J., Karperien H.B.J., Jonkheijm P., Denning C., IJzerman A.P. & Mummery C.L. (2017), Small molecule absorption by PDMS in the context of drug response bioassays, Biochemical and Biophysical Research Communications 482(2): 323-328.
Alachouzos G., Lenselink E.B., Mulder-Krieger T., Vries H. de, IJzerman A.P. & Louvel J. (2017), Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A(1) receptor antagonists, European Journal of Medicinal Chemistry 125: 586-602.
Lenselink E.B., Dijke N. ten, Bongers B.J., Papadatos G., Vlijmen H. van, Kowalczyk W.J., IJzerman A.P. & Westen G.J.P. van (2017), Beyond the Hype: Deep Neural Networks Outperform Established Methods Using A ChEMBL Bioactivity Benchmark Set, Journal of Cheminformatics 9(1): 45.
Hothersall J.D., Guo D., Sarda S., Sheppard R.J., Chen H.M., Keur W., Waring M.J., IJzerman A.P., Hill S.J., Dale I.L. & Rawlins P.B. (2017), Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics, Molecular Pharmacology 91(1): 25-38.
Zheng Y., Qin L., Ortiz Zacarias N.V., Vries H. de, Han G.W., Gustavsson M., Dabros M., Zhao C., Cherney R.J., Carter P., Stamos D., Abagyan R., Cherezov V., Stevens R.C., IJzerman A.P., Heitman L.H., Tebben A., Kufareva I. & Handel T.M. (2016), Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists, Nature 540(7633): 458-461.
Lenselink E.B., Jespers W., Vlijmen H.W.T. van, IJzerman A.P. & Westen G.J.P. van (2016), Interacting with GPCRs: Using Interaction Fingerprints for Virtual Screening, Journal of Chemical Information and Modeling 56(10): 2053-2060.
Paricharak S.A., Méndez-Lucio O., Chavan Ravindranath A., Bender A., IJzerman A.P. & Westen G.J. van (2018), Data-driven approaches used for compound library design, hit triage and bioactivity modeling in high-throughput screening, Briefings in Bioinformatics 19(2): 277-285.
Nederpelt I., Bleeker D., Tuijt B., IJzerman A.P. & Heitman L.H. (2016), Kinetic binding and activation profiles of endogenous tachykinins targeting the NK1 receptor, Biochemical Pharmacology 118: 88-95.
Guo D., Heitman L.H. & IJzerman A.P. (2016), The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery, Acs Medicinal Chemistry Letters 7(9): 819-821.
Hillger J.M., Diehl C., Spronsen E. van, Boomsma D.I., Slagboom P.E., Heitman L.H. & Ijzerman A.P. (2016), Getting personal: Endogenous adenosine receptor signaling in lymphoblastoid cell lines, Biochemical Pharmacology 115: 114-122.
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. article in journal: refereed
Liu R., Wong W. & IJzerman A.P. (2016), Human G protein-coupled receptor studies in Saccharomyces cerevisiae, Biochemical Pharmacology 114: 103-115.
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. article in journal: refereed
Segala E., Guo D., Cheng R.K.Y., Bortolato A., Deflorian F., Dore A.S., Errey J.C., Heitman L.H., IJzerman A.P., Marshall F.H. & Cooke R.M. (2016), Controlling the dissociation of ligands from the adenosine A(2A) receptor through modulation of salt bridge strength, Journal of Medicinal Chemistry 59(13): 6470-6479.
Guo D., Pan A.C., Dror R.O., Mocking T., Liu R., Heitman L.H., Shaw D.E. & IJzerman A.P. (2016), Molecular Basis of Ligand Dissociation from the Adenosine A(2A) Receptor, Molecular Pharmacology 89(5): 485-491.
Nederpelt I., Vergroesen R.D., IJzerman A.P. & Heitman L.H. (2016), Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology, Biosensors and Bioelectronics 79: 721-727.
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.
Guo D., Heitman L.H. & IJzerman A.P. (2017), Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors, Chemical Reviews 117(1): 38-66.
Guo D., Dijksteel G.S., Duijl T. van, Heezen M., Heitman L.H. & IJzerman A.P. (2016), Equilibrium and kinetic selectivity profiling on the human adenosine receptors, Biochemical Pharmacology 105: 34-41.
Doornbos M.L.J., Perez-Benito L., Tresadern G., Mulder T., Biesmans I., Trabanco A.A., Cid M.J., Lavreysen H., IJzerman A.P. & Heitman L.H. (2016), Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222, British Journal of Pharmacology 173(3): 588-600.
Paricharak S., IJzerman A.P., Bender A. & Nigsch F. (2016), Analysis of Iterative Screening with Stepwise Compound Selection Based on Novartis In-house HTS Data, ACS Chemical Biology 11: 1255-1264.
Nederpelt I., Georgi V., Schiele F., Nowak-Reppel K., Fernández-Montalván A.E., IJzerman A.P. & Heitman L.H. (2016), Characterization of 12 GnRH peptide agonists : a kinetic perspective, British Journal of Pharmacology 173(1): 128-141.
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.
Nederpelt I., Bunnik J., IJzerman A.P. & Heitman L.H. (2016), Kinetic profile of neuro-peptide-receptor interactions, Trends in Neurosciences 39: 830.
Peeters M.C., Fokkelman M., Boogaard B., Egerod K.L., Water B. van de, IJzerman A.P. & Schwartz T.W. (2015), The adhesion G protein-coupled receptor G2 (ADGRG2/GPR64) constitutively activates SRE and NFκB and is involved in cell adhesion and migration, Cellular Signalling 27(12): 2579-2588.
Hillger J.M., Schoop J., Boomsma D.I., Slagboom P.E., IJzerman A.P. & Heitman L.H. (2015), Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines, Biosensors and Bioelectronics 74: 233-42.
Xia L., Vries H. de, IJzerman A.P. & Heitman L.H. (2016), Scintillation proximity assay (SPA) as a new approach to determine a ligand's kinetic profile. A case in point for the adenosine A1 receptor, Purinergic Signalling 12(1): 115-126.
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.
Vilums M., Heuberger J., Heitman L.H. & IJzerman A.P. (2015), Indanes--Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors, Medicinal Research Reviews 35(6): 1097-1126.
Guo D., Heitman L.H. & IJzerman A.P. (2015), The Role of Target Binding Kinetics in Drug Discovery, ChemMedChem 10(11): 1793-6.
Massink A., Holzheimer M., Hölscher A., Louvel J., Guo D., Spijksma G., Hankemeier T. & IJzerman A.P. (2015), Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors, Purinergic Signalling 11(4): 581-594.
Louvel J., Guo D., Soethoudt M., Mocking T.A.M., Lenselink E.B., Mulder-Krieger T., Heitman L.H. & Ijzerman A.P. (2015), Structure-kinetics relationships of Capadenoson derivatives as adenosine A(1) receptor agonists, European Journal of Medicinal Chemistry 101: 681-691.
Romagnoli R., Baraldi P.G., Lopez-Cara C., Cruz-Lopez O., Moorman A.R., Massink A., IJzerman A.P., Vincenzi F., Borea P.A. & Varani K. (2015), Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study, European Journal of Medicinal Chemistry 101: 185-204.
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.
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.
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.
Liu R., Nahon D., Roy B. le, Lenselink E.B. & IJzerman A.P. (2015), Scanning mutagenesis in a yeast system delineates the role of the NPxxY(x)(5,6)F motif and helix 8 of the adenosine A(2B) receptor in G protein coupling, Biochemical Pharmacology 95(4): 290-300.
Paricharak S., Cortés-Ciriano I., IJzerman A.P., Malliavin T.E. & Bender A. (2015), Proteochemometric modelling coupled to in silico target prediction:: an integrated approach for the simultaneous prediction of polypharmacology and binding affinity/potency of small molecules, Journal of Cheminformatics 7: 15.
Guo D., IJzerman A.P. & Heitman L.H. (2015), Importance of drug-target residence time at G protein-coupled receptors - a case for the adenosine receptors. In: Keseru G., Swinney D.C., Mannhold R., Kubinyi H. & Folkers G. (Eds.), Thermodynamics and Kinetics of Drug Binding. Methods and Principles in Medicinal Chemistry. Dusseldorf: Wiley. 360.
Vilums M., Zweemer A.J., Barmare F., Gracht A.M. van der, Bleeker D.C.T., Yu Z., Vries H. de, Gross R., Clemens J., Krenitsky P., Brussee H., Stamos D., Saunders J., Heitman L.H. & IJzerman A.P. (2015), When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists, European Journal of Medicinal Chemistry 93: 121-34.
Yu Z., IJzerman A.P. & Heitman L.H. (2015), Kv11.1 (hERG)-induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypical Kv11.1 (hERG) inhibitors, British Journal of Pharmacology 172(3): 940-955.
Li P., Rial D., Canas P.M., Yoo J.-H., Li W., Zhou X., Wang Y., Westen G.J.P. van, Payen M.-P., Augusto E., Gonçalves N., Tomé A.R., Li Z., Wu Z., Hou X., Zhou Y., IJzerman A.P., Boyden E.S., Cunha R.A., Qu J. & Chen J.-.F. (2015), Optogenetic activation of intracellular adenosine A2A receptor signaling in the hippocampus is sufficient to trigger CREB phosphorylation and impair memory, Molecular Psychiatry 20: 1339–1349.
Massink A., Gutiérrez-de-Terán H., Lenselink E.B., Ortiz Zacarías N.V., Xia L., Heitman L.H., Katritch V., Stevens R.C. & IJzerman A.P. (2015), Sodium Ion Binding Pocket Mutations and Adenosine A2A Receptor Function, Molecular Pharmacology 87(2): 305-13.
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, Venhorst Suzanne N., Massink Arnault, Van Veldhoven Jacobus P.D., Vauquelin Georges, IJzerman Adriaan P. & Heitman Laura H. (2014), Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A(1) adenosine receptor, British Journal of Pharmacology 171(23): 5295-5312.
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.
Vilums M., Zweemer A.J.M., Dekkers S., Askar Y., Vries H. de, Saunders J., Stamos D., Brussee J., Heitman L.H. & IJzerman A.P. (2014), Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives, Bioorganic and Medicinal Chemistry Letters 24(23): 5377-5380.
Van Diepen Hester C., Lucassen Eliane A., Yasenkov Roman, Groenen Inske, Ijzerman Adriaan P., Meijer Johanna H. & Deboer Tom (2014), Caffeine increases light responsiveness of the mouse circadian pacemaker, European Journal of Neuroscience 40(10): 3504-3511.
Bansal M., Yang J., Karan C ., Menden M.P., Costello J.C., Tang H., Xiao G., Li Y., Allen J., Zhong R., Chen B., Kim M., Wang T., Heiser L.M., Realubit R., Mattioli M., Alvarez M.J., Shen Y., Westen G.J.P. van., IJzerman A.P., Lenselink E.B., Vlijmen H.W.T. van, Wegner J.K., Gallahan D., Singer D., Saez-Rodriguezc J., Xie Y., Stolovitzky G. & Califano A. (2014), A community computational challenge to predict the activity of pairs of compounds, Nature Biotechnology 32: 1213–1222.
Peeters Miriam C., Li Qilan, Elands Rachel, Van Westen Gerard J.P., Lenselink Eelke B., Mueller Christa E. & IJzerman Adriaan P. (2014), Domains for activation and inactivation in G protein-coupled receptors - A mutational analysis of constitutive activity of the adenosine A(2B) receptor, Biochemical Pharmacology 92(2): 348-357.
Zweemer Annelien J.M., Bunnik Julia, Veenhuizen Margo, Miraglia Fabiana, Lenselink Eelke B., Vilums Maris, De Vries Henk, Gibert Arthur, Thiele Stefanie, Rosenkilde Mette M., IJzerman Adriaan P. & Heitman Laura H. (2014), Discovery and Mapping of an Intracellular Antagonist Binding Site at the Chemokine Receptor CCR2, Molecular Pharmacology 86(4): 358-368.
Cortes-Ciriano I., Ul Ain Q., Subramanian V., Lenselink E.B., Mendez-Lucio O., IJzerman A.P., Wohlfahrt G., Prusis P., Malliavin T.E., Westen G.J.P. van & Bender A. (2014), Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospects, MedChemComm 6(1): 24-50.
Liu R., Groenewoud N.J.A., Peeters M.C., Lenselink E.B. & IJzerman A.P. (2014), A yeast screening method to decipher the interaction between the adenosine A2B receptor and the C-terminus of different G protein α-subunits, Purinergic Signalling 10(3): 441-453.
Romagnoli Romeo, Baraldi Pier Giovanni, IJzerman Adriaan P., Massink Arnault, Cruz-Lopez Olga, Lopez-Cara Luisa Carlota, Saponaro Giulia, Preti Delia, Tabrizi Mojgan Aghazadeh, Baraldi Stefania, Moorman Allan R., Vincenzi Fabrizio, Borea Pier Andrea & Varani Katia (2014), Synthesis and Biological Evaluation of Novel Allosteric Enhancers of the A(1) Adenosine Receptor Based on 2-Amino-3-(4 '-Chlorobenzoyl)-4-Substituted-5-Arylethynyl Thiophene, Journal of Medicinal Chemistry 57(18): 7673-7686.
Guo D., Hillger J.M., IJzerman A.P. & Heitman L.H. (2014), Drug-Target Residence Time-A Case for G Protein-Coupled Receptors, Medicinal Research Reviews 34(4): 856-892.
Zweemer A.J.M., Toraskar J., Heitman L.H. & IJzerman A.P. (2014), Bias in chemokine receptor signalling, Trends in Immunology 35(6): 243-252.
Lenselink Eelke B., Beuming Thijs, Sherman Woody, Van Vlijmen Herman W.T. & IJzerman Adriaan P. (2014), Selecting an Optimal Number of Binding Site Waters To Improve Virtual Screening Enrichments Against the Adenosine A(2A) Receptor, Journal of Chemical Information and Modeling 54(6): 1737-1746.
Costello J.C., Heiser L.M., Georgii E., Gönen M., Menden M.P., Wang N.J., Bansal M., Ammad-ud-din M., Hintsanen P., Khan S.A., Mpindi J-P., Kallioniemi O., Honkela A., Aittokallio T., Wennerberg K., Westen G.J.P van, Lenselink E.B., IJzerman A.P., Vlijmen H.W.T. van, Collins J.J., Gallahan D., Singer D., Saez-Rodriguez J., Kaski S., Gray J.W. & Stolovitzky G. (2014), A community effort to assess and improve drug sensitivity prediction algorithms, Nature Biotechnology 32: 1202–1212.
Louvel J.A., Guo D., Agliardi M., Mocking T.A.M., Kars R., Xia L., Vries H. de, Brussee J., Heitman L.H. & IJzerman A.P. (2014), Agonists for the adenosine A(1) receptor with tunable residence time: a case for nonribose 4-Amino-6-aryl-5-cyano-2-thiopyrimidines, Journal of Medicinal Chemistry 57(8): 3213-3222.
Yu Z., Klaasse E., Heitman L.H. & IJzerman A.P. (2014), Allosteric modulators of the hERG K+ channel Radioligand binding assays reveal allosteric characteristics of dofetilide analogs, Toxicology and Applied Pharmacology 274(1): 78-86.
Louvel J.A., Carvalho J.F.S., Yu Z., Soethoudt M., Lenselink E.B., Klaasse E., Brussee J. & IJzerman A.P. (2013), Removal of Human Ether-a-go-go Related Gene (hERG) K+ Channel Affinity through Rigidity: A Case of Clofilium Analogues, Journal of Medicinal Chemistry 56(23): 9427-9440.
Gutlerrez-de-Teran Hugo, Massink Arnault, Rodriguez David, Liu Wei, Han Gye Won, Joseph Jeremiah S., Katritch Ilia, Heitman Laura H., Xia Lizi, IJzerman Adriaan P., Cherezov Vadim, Katritch Vsevolod & Stevens Raymond C. (2013), The Role of a Sodium Ion Binding Site in the Allosteric Modulation of the A(2A) Adenosine G Protein-Coupled Receptor, Structure Fold Design 21(12): 2175-2185.
Koutsoukas A., Paricharak S., Galloway W.R.J.D., Spring D.R., IJzerman A.P., Glen R.C., Marcus D. & Bender A. (2014), How Diverse Are Diversity Assessment Methods? A Comparative Analysis and Benchmarking of Molecular Descriptor Space, Journal of Chemical Information and Modeling 54(1): 230-242.
Chen D., Ranganathan A., IJzerman A.P., Siegal G. & Carlsson J. (2013), Complementarity between in Silico and Biophysical Screening Approaches in Fragment-Based Lead Discovery against the A(2A) Adenosine Receptor, Journal of Chemical Information and Modeling 53(10): 2701-2714.
Zweemer Annelien J.M., Nederpelt Indira, Vrieling Hilde, Hafith Sarah, Doornbos Maarten L.J., De Vries Henk, Abt Jeffrey, Gross Raymond, Stamos Dean, Saunders John, Smit Martine J., IJzerman Adriaan P. & Heitman Laura H. (2013), Multiple Binding Sites for Small-Molecule Antagonists at the CC Chemokine Receptor 2, Molecular Pharmacology 84(4): 551-561.
Vilums Maris, Zweemer Annelien J.M., Yu Zhiyi, De Vries Henk, Hillger Julia M., Wapenaar Hannah, Bollen Ilse A.E., Barmare Farhana, Gross Raymond, Clemens Jeremy, Krenitsky Paul, Brussee Johannes, Stamos Dean, Saunders John, Heitman Laura H. & IJzerman Adriaan P. (2013), Structure-Kinetic Relationships-An Overlooked Parameter in Hit-to-Lead Optimization: A Case of Cyclopentylamines as Chemokine Receptor 2 Antagonists, Journal of Medicinal Chemistry 56(19): 7706-7714.
Westen G.J.P. van, Swier R.F., Wegner J.K., IJzerman A.P., Vlijmen H. van & Bender A. (2013), Benchmarking of protein descriptor sets in proteochemometric modeling (part 1): comparative study of 13 amino acid descriptor sets, Journal of Cheminformatics 5: 41.
Varkevisser R., Houtman M.J.C., Linder T., De Git K.C.G., Beekman H.D.M., Tidwell R.R., IJzerman A.P., Stary-Weinzinger A., Vos M.A. & Van der Heyden M.A.G. (2013), Structure-activity relationships of pentamidine-affected ion channel trafficking and dofetilide mediated rescue, British Journal of Pharmacology 169(6): 1322-1334.
De Bruyn Tom, Van Westen Gerard J.P., IJzerman Adriaan P., Stieger Bruno, De Witte Peter, Augustijns Patrick F. & Annaert Pieter P. (2013), Structure-Based Identification of OATP1B1/3 Inhibitors, Molecular Pharmacology 83(6): 1257-1267.
Carvalho J.F.S., Louvel J.A., Doornbos M.L.J., Klaasse E., Yu Z., Brussee H. & IJzerman A.P. (2013), Strategies To Reduce hERG K+ Channel Blockade. Exploring Heteroaromaticity and Rigidity in Novel Pyridine Analogues of Dofetilide, Journal of Medicinal Chemistry 56(7): 2828-2840.
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.
Langemeijer Ellen V., Verzijl Dennis, Dekker Stefan J. & IJzerman Ad P. (2013), Functional selectivity of adenosine A(1) receptor ligands?, 9(1): 91-100.
Westen G.J.P. van, Hendriks A., Wegner J.K., IJzerman A.P., Vlijmen H.W.T. van & Bender A. (2013), Significantly Improved HIV Inhibitor Efficacy Prediction Employing Proteochemometric Models Generated From Antivirogram, PLoS Computational Biology 9(2): e1002899.
Li Zhaosha, Blad Clara C., Van der Sluis Ronald J., De Vries Henk, Van Berkel Theo J.C., IJzerman Adriaan P. & Hoekstra Menno (2012), Effects of pyrazole partial agonists on HCA2-mediated flushing and VLDL-triglyceride levels in mice, British Journal of Pharmacology 167(4): 818-825.
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.
Van Westen Gerard J.P., Van den Hoven Olaf O., Van der Pijl Rianne, Mulder-Krieger Thea, De Vries Henk, Wegner Jorg K., Ijzerman Adriaan P., Van Vlijmen Herman W.T. & Bender Andreas (2012), Identifying Novel Adenosine Receptor Ligands by Simultaneous Proteochemometric Modeling of Rat and Human Bioactivity Data, Journal of Medicinal Chemistry 55(16): 7010-7020.
Guo Dong, Mulder-Krieger Thea, IJzerman Adriaan P. & Heitman Laura H. (2012), Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time, British Journal of Pharmacology 166(6): 1846-1859.
Liu Wei, Chun Eugene, Thompson Aaron A., Chubukov Pavel, Xu Fei, Katritch Vsevolod, Han Gye Won, Roth Christopher B., Heitman Laura H., IJzerman Adriaan P., Cherezov Vadim & Stevens Raymond C. (2012), Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions, Science 337(6091): 232-236.
Peeters M.C., Wisse L.E., Dinaj A., Vroling B., Vriend G. & IJzerman A.P. (2012), The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation, Biochemical Pharmacology 84(1): 76-87.
Bot I., Vries H. de, Bot M., Berkel T.J.C. van, IJzerman A.P. & Kuiper J. (2012), Adenosine A(2B) receptor agonism inhibits vascular smooth muscle cell proliferation and intimal hyperplasia in ApoE deficient mice, Vascular Pharmacology 56(5-6): 349-350.
Sanders Marijn P.A., Roumen Luc, Van der Horst Eelke, Lane J. Robert, Vischer Henry F., Van Offenbeek Jody, De Vries Henk, Verhoeven Stefan, Chow Ken Y., Verkaar Folkert, Beukers Margot W., McGuire Ross, Leurs Rob, IJzerman Adriaan P., De Vlieg Jacob, De Esch Iwan J.P., Zaman Guido J.R., Klomp Jan P.G., Bender Andreas & De Graaf Chris (2012), A Prospective Cross-Screening Study on G-Protein-Coupled Receptors: Lessons Learned in Virtual Compound Library Design, Journal of Medicinal Chemistry 55(11): 5311-5325.
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.
Heitman Laura H., Kleinau Gunnar, Brussee Johannes, Krause Gerd & Ijzerman Adriaan P. (2012), Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands, Molecular and Cellular Endocrinology 351(2): 326-336.
Lane J. Robert, Herenbrink Carmen Klein, Van Westen Gerard J.P., Spoorendonk Jelle A., Hoffmann Carsten & IJzerman Adriaan P. (2012), A Novel Nonribose Agonist, LUF5834, Engages Residues That Are Distinct from Those of Adenosine-Like Ligands to Activate the Adenosine A(2a) Receptor, Molecular Pharmacology 81(3): 475-487.
Peeters M.C. & IJzerman A.P. (2012), Mutational analysis of adenosine receptors, 8(1): 120-120.
Guo D., Heitman L.H. & IJzerman A.P. (2012), The relationship between binding kinetics and functional efficacy of adenosine A(2A) receptor agonists, 8(1): 172-173.
Peeters M.C., Li Q., Westen G.J.P. van & IJzerman A.P. (2012), Three "hotspots" important for adenosine A(2B) receptor activation: a mutational analysis of transmembrane domains 4 and 5 and the second extracellular loop, Purinergic Signalling 8(1): 23-38.
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.
Vilums M., Overman J., Klaasse E., Scheel O., Brussee J. & IJzerman A.P. (2012), Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E-4031 Analogues, ChemMedChem 7(1): 107-113.
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, The Journal of pharmacology and experimental therapeutics 340(1): 210-217.
Chen D., Errey J.C., Heitman L.H., Marshall F.H., IJzerman A.P. & Siegal G. (2012), Fragment Screening of GPCRs Using Biophysical Methods: Identification of Ligands of the Adenosine A(2A) Receptor with Novel Biological Activity, ACS Chemical Biology 7(12): .
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.
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.
Jacobson K.A., Gao Z.G., Goblyos A. & IJzerman A.P. (2011), Allosteric modulation of purine and pyrimidine receptors, Advances in pharmacology 61: .
Blad C.C., Ahmed K., IJzerman A.P. & Offermanns S. (2011), Biological and pharmacological roles of HCA receptors, Advances in pharmacology 62: .
Van der Horst E., Peironcely J.E., Van Westen G.J.P., Van den Hoven O.O., Galloway W.R.J.D., Spring D.R., Wegner J.K., Van Vlijmen H.W.T., IJzerman A.P., Overington J.P. & Bender A. (2011), Chemogenomics Approaches for Receptor Deorphanization and Extensions of the Chemogenomics Concept to Phenotypic Space, Current Topics in Medicinal Chemistry 11(15): 1964-1977.
Gao Z.G., Verzijl D., Zweemer A., Ye K., Goblyos A., IJzerman A.P. & Jacobson K.A. (2011), Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers, Biochemical Pharmacology 82(6): .
Verzijl D. & IJzerman A.P. (2011), Functional selectivity of adenosine receptor ligands, 7(2): .
Peeters M.C., Van Westen G.J., Guo D., Wisse L.E., Muller C.E., Beukers M.W. & IJzerman A.P. (2011), GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor, The FASEB Journal 25(2): 632-643.
Gomes I., IJzerman A.P., Ye K., Maillet E.L. & Devi L.A. (2011), G Protein-Coupled Receptor Heteromerization: A Role in Allosteric Modulation of Ligand Binding, Molecular Pharmacology 79(6): .
Fruh V., IJzerman A.P. & Siegal G. (2011), How to Catch a Membrane Protein in Action: A Review of Functional Membrane Protein Immobilization Strategies and Their Applications, Chemical Reviews 111(2): 640-656.
Peeters M.C., Van Westen G.J.P., Li Q. & IJzerman A.P. (2011), Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation, Trends in Pharmacological Sciences 32(1): 35-42.
Offermanns S., Colletti S.L., Lovenberg T.W., Semple G., Wise A. & IJzerman A.P. (2011), International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B), Pharmacological Reviews 63(2): .
Fredholm B.B., IJzerman A.P., Jacobson K.A., Linden J. & Muller C.E. (2011), International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors-An Update, Pharmacological Reviews 63(1): .
Du L., Gao Z.G., Nithipatikom K., IJzerman A.P., Van Veldhoven J.P., Jacobson K.A., Gross G.J. & Auchampach J.A. (2011), Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A3 adenosine receptor, The Journal of pharmacology and experimental therapeutics 340(1): 210-217.
Van Westen G.J.P., Wegner J.K., IJzerman A.P., Van Vlijmen H.W.T. & Bender A. (2011), Proteochemometric modeling as a tool to design selective compounds and for extrapolating to novel targets, MedChemComm 2(1): 16-30.
Blad C.C., Frijtag Drabbe Kunzel J.K. von, De Vries H., Mulder-Krieger T., Bar-Yehuda S., Fishman P. & IJzerman A.P. (2011), Putative role of the adenosine A(3) receptor in the antiproliferative action of N (6)-(2-isopentenyl)adenosine, 7(4): 453-462.
Van der Horst E., Van der Pijl R., Mulder-Krieger T., Bender A. & IJzerman A.P. (2011), Substructure-Based Virtual Screening for Adenosine A(2A) Receptor Ligands, ChemMedChem 6(12): .
Lane J.R., Jaakola V.P. & IJzerman A.P. (2011), The structure of the adenosine receptors: implications for drug discovery, Advances in pharmacology 61: .
Vilums M., Overman J., Klaasse E., Scheel O., Brussee J. & IJzerman A.P. (2011), Understanding of Molecular Substructures that Contribute to hERG K(+) Channel Blockade: Synthesis and Biological Evaluation of E-4031 Analogues, ChemMedChem : .
Westen G.J.P. van, Wegner J.K., Geluykens P., Kwanten L., Vereycken I., Peeters A., IJzerman A.P., Vlijmen H. van & Bender A. (2011), Which compound to select in lead optimization? Prospectively validated proteochemometric models guide preclinical development, PLoS ONE 6(11): e27518.
Jaakola V.P., Lane J.R., Lin J.Y., Katritch V., IJzerman A.P. & Stevens R.C. (2010), Ligand Binding and Subtype Selectivity of the Human A2A Adenosine Receptor: Identification and Characterization of Essential Amino Acid Residues, Journal of Biological Chemistry 285(17): 13032-13044.
Horst E. van der, Peironcely Julio E., IJzerman A.P., Beukers M.W., Lane J.R., Vlijmen H. van, Emmerich M.T.M., Okuno Yasushi & Bender A. (2010), A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization, BMC Bioinformatics 11: 316.
Lane J.R., Klaasse E., Lin J., Van Bruchem J., Beukers M.W. & IJzerman A.P. (2010), Characterization of [H-3]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor, Biochemical Pharmacology 80(8): .
Doddareddy M.R., Westen G.J.P. van, Horst Eelke van der, Peironcely Julio E., Corthals Frans, IJzerman A.P., Emmerich Michael T.M., Jenkins Jeremy L. & Bender Andreas (2010), Chemogenomics: Looking at biology through the lens of chemistry, Statistical Analysis and Data Mining 2(3): 149-160.
Eelke H. van der, Kruisselbrink J.W., Aleman A., Emmerich M.T.M., Bender A. & IJzerman A.P. (2010), Evolutionary Design of Selective Adenosine Receptor Ligands [poster], Journal of Cheminformatics 2: 1-1.
Narlawar R., Lane J.R., Doddareddy M., Lin J.D., Brussee J. & IJzerman A.P. (2010), Hybrid Ortho/Allosteric Ligands for the Adenosine A1 Receptor, Journal of Medicinal Chemistry 53(8): .
Van Westen G.J.P., Wegner J.K., Bender A., IJzerman A.P. & Van Vlijmen H.W.T. (2010), Mining protein dynamics from sets of crystal structures using "consensus structures", Protein Science 19(4): 742-752.
Doddareddy M.R., Klaasse E.C., Shagufta, IJzerman A.P. & Bender A. (2010), Prospective Validation of a Comprehensive In silico hERG Model and its Applications to Commercial Compound and Drug Databases, ChemMedChem 5(5): .
Willems L.I. & IJzerman A.P. (2010), Small Molecule Antagonists for Chemokine CCR3 Receptors, Medicinal Research Reviews 30(5): .
Katritch V., Jaakola V.P., Lane J.R., Lin J., IJzerman A.P., Yeager M., Kufareva I., Stevens R.C. & Abagyan R. (2010), Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists, Journal of Medicinal Chemistry 53(4): .
Jaakola V.P. & IJzerman A.P. (2010), The crystallographic structure of the human adenosine A2A receptor in a high-affinity antagonist-bound state: implications for GPCR drug screening and design, Current Opinion in Structural Biology 20(4): .
Lane J.R., Beukers M.W., Mulder-Krieger T. & IJzerman A.P. (2010), The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor, Biochemical Pharmacology 79(1): 48-56.
Putten C. van der, Zuiderwijk-Sick E.A., Straalen L. van, Geus E.D. de, Boven L.A., Kondova I., IJzerman A.P. & Bajramovic J.J. (2009), Differential expression of adenosine A3 receptors controls adenosine A2A receptor-mediated inhibition of toll-like receptor responses in microglia, Glia 57(13): S132-S132.
Lane J.R., Mulder T., Beukers M.W. & IJzerman A.P. (2009), The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A_3 adenosine receptor, Naunyn-Schmiedeberg's Archives of Pharmacology 380(3): 264-265.
Doddareddy M.R., Westen G.J.P. van, Horst E. van der, Peironcely J., Corthals F., IJzerman A.P., Emmerich M.T.M., Jenkins J.L. & Bender A. (2009), Chemogenomics: Looking at biology through the lens of chemistry, Statistical Analysis and Data Mining 2(3): 149-160.
Yuliana N.D., Khatib A., Link-Struensee A.M.R., IJzerman A.P., Choi Y.H. & Verpoorte R. (2009), Adenosine A1 Receptor Antagonist Activity of Methoxy Flavonoids from Orthosiphon stamineus, Planta Medica 75(2): 132-136.
Göblyös Anikó & IJzerman Ad P. (2009), Allosteric modulation of adenosine receptors, 5(1): 51-61.
Emmerich Michael T.M., Li B.V.Y., Bender Andreas, Faddiev E., Kruisselbrink J.W., Deutz A.H., Horst Eelke van der, IJzerman Adriaan P. & Bäck T.H.W. (2009), Analyzing Molecular Landscapes using Random walks and Information Theory [poster], Chemistry Central Journal 3(Suppl. 1): .
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.
Kruisselbrink J.W., Emmerich M.T.M., Bäck T.H.W., Bender A., IJzerman A.P. & Horst E. van der (2009), Combining Aggregation with Pareto Optimization: A Case Study in Evolutionary Molecular Design. Ehrgott M., Fonseca C.M., Gandibleux X., Hao J.K. & Sevaux M. (Eds.), Evolutionary Multi-Criterion Optimization. EMO 2009. EMO: International Conference on Evolutionary Multi-Criterion Optimization 7 April 2009 - 10 April 2009 no. LNCS 5467. Berlin / Heidelberg: Springer. 453-467.
Van der Putten Celine, Zuiderwijk-Sick Ella A., Van Straalen Linda, De Geus Eveline D., Boven Leonie A., Kondova Ivanela, IJzerman Ad P. & Bajramovic Jeffrey J. (2009), Differential Expression of Adenosine A3 Receptors Controls Adenosine A2A Receptor-Mediated Inhibition of TLR Responses in Microglia, Journal of Immunology 182(12): 7603-7612.
Kruisselbrink J.W., Aleman A., Emmerich Michael T.M., IJzerman A.P., Bender A., Bäck T.H.W. & Horst E. van der (2009), Enhancing search space diversity in multi-objective evolutionary drug molecule design using niching, Proceedings of the 11th Annual conference on Genetic and Evolutionary Computation (GECCO). . New York: ACM. 217-224.
Shagufta, Guo Dong, Klaasse Elisabeth, De Vries Henk, Brussee Johannes, Nalos Lukáscaron, Rook Martin B., Vos Marc A., Van der Heyden Marcel A.G. & Ijzerman Adriaan P. (2009), Exploring Chemical Substructures Essential for hERG K+ Channel Blockade by Synthesis and Biological Evaluation of Dofetilide Analogues, ChemMedChem 4(10): 1722-1732.
Kim Yoonkyung, De Castro Sonia, Gao Zhan-Guo, IJzerman Adriaan P. & Jacobson Kenneth A. (2009), Novel 2- and 4-Substituted 1H-Imidazo[4,5-c]quinolin-4-amine Derivatives as Allosteric Modulators of the A3 Adenosine Receptor, Journal of Medicinal Chemistry 52(7): 2098-2108.
Heitman Laura H., Narlawar Rajeshwar, De Vries Henk, Willemsen Milou N., Wolfram Dieter, Brussee Johannes & IJzerman Adriaan P. (2009), Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor, Journal of Medicinal Chemistry 52(7): 2036-2042.
Emmerich Michael T.M., Li B.V.Y., Bender A., Faddiev E., Kruisselbrink J.W., Deutz A.H., Horst E. van der, IJzerman A.P. & Bäck T.H.W. (2008), Analysing Molecular Landscapes Using Random Walks and Information Theory, German Conference on Chemoinformatics. 4th German Conference on Chemoinformatics 10 November 2008 - 12 November 2008. Goslar 73.
Lane J.R., Beukers M.W. & IJzerman A. (2008), The endocannabinoids anandamide and 2-arachidonylglycerol are negative allosteric modulators of ligand binding at the human A3 adenosine receptor, Fundamental Clinical Pharmacology 22: 28-28.
Chang L.C.W., Brussee J. & IJzerman A.P. (2008), 2,6,8-Trisubstituted 1-deazapurines and their different uses and preparation. [patent].
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.
Heitman L.H., Oosterom J., Bonger K.M., Timmers C., Wiegerinck P. & IJzerman A.P. (2008), [3H]Org 43553, the first low molecular weight agonistic and allosteric radioligand for the human luteinizing hormone receptor, Molecular Pharmacology 73(2): 518-524.
Heitman L.H., Ye K., Oosterom J. & IJzerman A.P. (2008), Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor, Molecular Pharmacology 73(6): 1808-1815.
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.
Emmerich Michael T.M., Kruisselbrink J.W., Horst E. van der, IJzerman A.P., Bender A. & Bäck T.H.W. (2008), Combined Interactive and Automated Adaptive Search for Molecular Design, Proceedings of Adaptive Computing in Design and Manufacture 2008. : IPCC.
Kruisselbrink J.W., Bäck T.H.W., IJzerman A.P. & Horst E. van der (2008), Evolutionary Algorithms for Automated Drug Design Towards Target Molecule Properties, Proceedings of GECCO 2008. . Atlanta: ACM Press.
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.
Kazius J., Wurdinger K., Iterson M. van, Kok J.N., Bäck T.H.W. & IJzerman A.P. (2008), GPCR NaVa database: Natural variants in human G protein-coupled receptors, Human Mutation 29(1): 39-44.
Heitman L.H. & IJzerman A.P. (2008), G Protein-Coupled Receptors of the Hypothalamic-Pituitary-Gonadal Axis: A Case for GnRH, LH, FSH, and GPR54 Receptor Ligands, Medical Research Reviews 28(6): 975-1011.
Biber K.P., Pinto-Duarte A., Wittendorp M.C., Dolga A.M., Fernandes C.C., Frijtag Drabbe Kűnzel J.K. von , Keijser J.N., Vries R. de, IJzerman A.P., Ribeiro J.A., Eisel U., Sebastião A.M. & Boddeke H.W. (2008), Interleukin-6 Upregulates Neuronal Adenosine A(1) Receptors: Implications for Neuromodulation and Neuroprotection, Neuropsychopharmacology 33(9): 2237-2250.
Klaasse E.C., IJzerman A.P., Grip W.J. de & Beukers M.W. (2008), Internalization and desensitization of adenosine receptors, Purinergic Signalling 4(1): 21-37.
Ye K., Feenstra K.A., Heringa J.R., IJzerman A.P. & Marchiori E. (2008), Multi-RELIEF: a method to recognize specificity determining residues from multiple sequence alignments using a machine learning approach for feature weighting, BIOINFORMATICS 24(1): 18-25.
Bonger K.M., Berg R.J.B.H.N. van den, Knijnenburg A.D., Heitman L.H., IJzerman A.P., Oosterom J., Timmers C.M., Overkleeft H.S. & Marel G.A. van der (2008), Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core, Bioorganic & Medicinal Chemistry 16(7): 3744-3758.
Jaakola V.-P., Griffith M.T., Hanson M.A., Cherezov V., Chien E.Y.T., Lane J.R., IJzerman A.P. & Stevens R.C. (2008), The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist, Science 322(5905): 1211-1217.
Peeters M.C., Beukers M.W. & IJzerman A.P. (2008), The second extracellular loop plays an important role in GPCR activation. The adenosine A2B receptor as a point in case, Fundamental Clinical Pharmacology 22: 60.
Ye K., Vriend G. & IJzerman A.P. (2008), Tracing evolutionary pressure, BIOINFORMATICS 24(7): 908-915.
Chang L.C.W., Frijtag Drabbe Künzel J.K. von , Mulder-Krieger T., Westerhout J., Spangenberg T., Brussee J. & IJzerman A.P. (2007), 2,6,8-Trisubstituted 1-deazapurines as adenosine receptor antagonists, Journal of Medicinal Chemistry 50(4): 828-834.
Ye K., Kosters W.A. & IJzerman A.P. (2007), An efficient, versatile and scalable pattern growth approach to mine frequent patterns in unaligned protein sequences, BIOINFORMATICS 23(6): 687-693.
Samsonova E., Krause P., Bäck T.H.W. & IJzerman A.P. (2007), Characteristic amino acid combinations in olfactory G protein-coupled receptors, Proteins, Structure, Function and Bioinformatics 67(1): 154-166.
Lameijer E.M.W., Tromp R.A., Spanjersberg R.F., Brussee J. & IJzerman A.P. (2007), Designing active template molecules by combining computational de novo design and human chemist's expertise, Journal of Medicinal Chemistry 50(8): 1925-1932.
Soudijn W., Wijngaarden I. van & IJzerman A.P. (2007), Nicotinic acid receptor subtypes and their ligands, Medicinal Research Reviews 27(3): 417-433.
Priego E.M., Pérez-Pérez M.J., Frijtag Drabbe Künzel J.K. von, Vries H. de, IJzerman A.P., Camarasa M.J. & Martin-Santamaria S. (2007), Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding, ChemMedChem 3(1): 111-119.
Bonger K.M., Berg R.J.B.H.N. van den, Heitman L.H., IJzerman A.P., Oosterom J., Timmers C.M., Overkleeft H.S. & Marel G.A. van der (2007), Synthesis and evaluation of homo-bivalent GnRHR ligands, Bioorganic & Medicinal Chemistry 15(14): 4841-4856.
Ye K., Kosters W.A. & IJzerman A.P. (2007), Versatile and Scalable Pattern Growth Approach to Mine Frequent Patterns in Unaligned Protein Sequences, BIOINFORMATICS 23: 687-693.
Li Q., Ye K., Blad C.C., Dulk H. den, Brouwer J., IJzerman A.P. & Beukers M.W. (2007), ZM241385, DPCPX and MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor, Journal of Pharmacology and Experimental Therapeutics 320: 637-645.
Li Q., Ye K., Blad C.C., Dulk H. den, Brouwer J., IJzerman A.P. & Beukers M.W. (2007), ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor, Journal of Pharmacology and Experimental Therapeutics 320(2): 637-645.
Biber K., Pinto-Duarte A., Dolga A.M., Femandes C.C., IJzerman A.P., Eisel U., Sebastiao A.M. & Boddeke H.W.G.M. (2006), The role of adenosine receptors in IL-6-dependent neuroprotection, Journal of Neuroimmunology 178(178/S1): 131-131.
Chang L.C.W., Spanjersberg R.F., Frijtag Drabbe Künzel J.K. von , Mulder-Krieger T., Brussee J. & IJzerman A.P. (2006), 2,6-Disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists, Journal of Medicinal Chemistry 49: 2861-2867.
Heitman L.H., Mulder-Krieger T., Spanjersberg R.F., Frijtag Drabbe Künzel J.K. von, Dalpiaz A. & IJzerman A.P. (2006), Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist, British Journal of Pharmacology 147(5): 533-541.
Ye K., Lameijer E.M.W., Beukers M.W. & IJzerman A.P. (2006), A two-entropies analysis to identify functional positions in the transmembrane region of class A G protein-coupled receptors, Proteins, Structure, Function and Bioinformatics 63: 1018-1030.
Lameijer E.M.W., Kok J.N., Bäck T.H.W. & IJzerman A.P. (2006), Mining a chemical database for fragment co-occurrence: discovery of "chemical clichés", Journal of Chemical Information and Modeling 46(2): 553-562.
Bond R.A. & IJzerman A.P. (2006), Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery, Trends in Pharmacological Sciences 27: 92-96.
Göblyös A., Gao Z.-G., Brussee J., Connestari R., Santiago S.N., Ye K., IJzerman A.P. & Jacobson K.A. (2006), Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor, Journal of Medicinal Chemistry 49: 2861-2867.
Beukers M.W., Meurs I. & IJzerman A.P. (2006), Structure-affinity relationships of adenosine A2B receptor ligands, Medicinal Research Reviews 26: 667-698.
Kazius J., Nijssen S., Kok J.N., Bäck T.H.W. & IJzerman A.P. (2006), Substructure mining using elaborate chemical representation, Journal of Chemical Information and Modeling 46: 597-605.
Lameijer E.M.W., Kok J.N., Bäck T.H.W. & IJzerman A.P. (2006), The Molecule Evoluator. An interactive evolutionary algorithm for the design of drug-like molecules, Journal of Chemical Information and Modeling 46: 545-552.
Samsonova E., Kok J.N. & IJzerman A.P. (2006), TreeSOM: Cluster analysis in the self-organizing map, Cromohs (Firenze) 19: 935-949.
Gao Z.-G., Kim S-K., IJzerman A.P. & Jacobson K.A. (2005), Allosteric modulation of the adenosine family of receptors, Mini-Reviews in Medicinal Chemistry 5: 545-553.
Klaasse E.C., Hout G. van den, Roerink S.F., Grip W.J. de, IJzerman A.P. & Beukers M.W. (2005), Allosteric modulators affect the internalization of human adenosine A1 receptors, European Journal of Pharmacology 522(1-3): 1-8.
Ligt R.A.F. de, Rivkees S.A., Lorenzen A., Leurs R. & IJzerman A.P. (2005), A locked-on, constitutively active mutant of the adenosine A1 receptor, European Journal of Pharmacology 510: 1-8.
Chang L.C.W., Frijtag Drabbe Künzel J.K. von , Mulder-Krieger T., Spanjersberg R.F., Roerink S.F., Hout G. van den, Beukers M.W., Brussee J. & IJzerman A.P. (2005), A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor, Journal of Medicinal Chemistry 48: 2045-2053.
Schaddelee M.P., Read K.D., Cleypool C.G., IJzerman A.P., Danhof M. & Boer A.G. de (2005), Brain penetration of synthetic adenosine A1 receptor agonists in situ: role of the rENT1 nucleoside transporter and binding to blood constituents, European Journal of Pharmaceutical Sciences 24(1): 59-66.
Lameijer E.M.W., Bäck T.H.W., Kok J.N. & IJzerman A.P. (2005), Evolutionary algorithms in drug design, Natural computing 4: 177-243.
Tromp R.A., Spanjersberg R.F., Frijtag Drabbe Künzel J.K. von & IJzerman A.P. (2005), Inhibition of nucleoside transport proteins by C8-alkylamine substituted purines, Journal of Medicinal Chemistry 48: 321-329.
Schaddelee M.P., Collins S.D., DeJongh J., Boer A.G. de, IJzerman A.P. & Danhof M. (2005), Pharmacokinetic/pharmacodynamic modelling of the anti-hyperalgesic and anti-nociceptive effect of adenosine A1 receptor partial agonists in neuropathic pain, European Journal of Pharmaceutical Sciences 514(2-3): 131-140.
Samsonova E., Bäck T.H.W., Kok J.N. & IJzerman A.P. (2005), Reliable hierarchical clustering with the self-organizing map, Proceedings of the 6th International Symposium on Intelligent Data Analysis (IDA 2005). 385-396.
Soudijn M., Wijngaarden I. van & IJzerman A.P. (2005), Structure-activity relationships of inverse agonists for G-protein-coupled receptors, Medicinal Research Reviews 25: 398-426.
Göblyös A., Neves Santiago S., Pietra D., Mulder-Krieger T., Frijtag Drabbe Künzel J.K. von, Brussee J. & IJzerman A.P. (2005), Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors. Lack of effect of 2-aminothiazoles as allosteric enhancers, Bioorganic & Medicinal Chemistry 13: 2079-2087.
Göblyös A., Vries H. de, Brussee J. & IJzerman A.P. (2005), Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action, Journal of Medicinal Chemistry 48: 1145-1151.
Beukers M.W. & IJzerman A.P. (2005), Techniques: how to boost GPCR mutagenesis studies using yeast, Trends in Pharmacological Sciences 26: 533-539.
Lameijer E.M.W., IJzerman A.P. & Bäck T.H.W. (2005), The Molecule Evoluator: an interactive evolutionary algorithm for designing drug molecules. Beyer H.-G. & O'Reilly U.-M. (Eds.), Proceedings of the 7th Annual Genetic and Evolutionary Computation Conference (GECCO-2005). . New York: ACM. 1969-1976.
Samsonova E., Kok J.H. & IJzerman A.P. (2005), TreeSOM: cluster analysis in the Self-Organizing Map, 5th Workshop on Self-Organizing Maps (WSOM). 429-438.
Lameijer E.M.W., IJzerman A.P. & Kok J.N. (2005), Using data mining to improve mutation in a tool for molecular evolution, Proceedings of the 2005 IEEE Congress on Evolutionary Computation (CEC 2005). .
Nieuwendijk A.M.C.H. van den, Pietra D., Heitman L.H., Göblyös A. & IJzerman A.P. (2004), Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors, Journal of Medicinal Chemistry 47(3): 663-672.
Chang L.C.W., Spanjersberg R.F., Frijtag Drabbe Kunzel J.K. von , Mulder-Krieger T., Hout G. van den, Beukers M.W., Brussee J. & IJzerman A.P. (2004), 2, 4, 6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists, Journal of Medicinal Chemistry 47: 6529-6540.
Klaasse E.C., Ligt R.A.F. de, Roerink S.F., Milligan G., Leurs R. & IJzerman A.P. (2004), Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi-subunits, European Journal of Pharmacology 499: 91-98.
Soudijn W., Wijngaarden I. van & IJzerman A.P. (2004), Allosteric modulation of G protein-coupled receptors. Perspectives and recent developments, Drug Discovery Today 9: 752-758.
Cordeaux Y., IJzerman A.P. & Hill S.J. (2004), Coupling of the human A1 adenosine receptor to different heterotrimeric G proteins; evidence for agonist-specific G protein activation, British Journal of Pharmacology 143: 705-714.
Tromp R.A., Ameijde S. van, Pütz C., Sundermann C., Sundermann B., Frijtag Drabbe Kunzel J.K. von & IJzerman A.P. (2004), Inhibition of nucleoside transport by new analogs of 4-nitrobenzylthioinosine (NBTI): replacement of the ribose moiety by substituted benzyl groups, Journal of Medicinal Chemistry 47: 5441-5550.
Beukers M.W., Chang L.C.W., Frijtag Drabbe Kunzel J.K. von, Mulder-Krieger T., Spanjersberg R.F., Brussee J. & IJzerman A.P. (2004), New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine, Journal of Medicinal Chemistry 47: 3707-3709.
Chang L.C.W., Brussee J. & IJzerman A.P. (2004), Non-xanthine antagonists for the adenosine A1 receptor, Chemistry and Biodiversity 1: 1591-1626.
Schaddelee M.P., Groenendaal D., DeJongh J., Cleypool C.G., IJzerman A.P., Boer A.G. de & Danhof M. (2004), Population pharmacokinetic modeling of blood-brain barrier transport of synthetic adenosine A1 receptor agonists, Journal of Pharmacology and Experimental Therapeutics 311: 1138-1146.
Schaddelee M.P., DeJongh J., Collins S.D., Boer A.G. de, IJzerman A.P. & Danhof M. (2004), Population pharmacokinetic-pharmacodynamic modelling of the anti-hyperalgesic effect of 5'deoxy-N6-cylopentyladenosine in the mononeuropathic rat, European Journal of Pharmacology 504: 7-15.
Beukers M.W., Oppenraaij J. van, Hoorn P.P.W. van der, Blad C.C., Dulk H. den, Brouwer J. & IJzerman A.P. (2004), Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations, Molecular Pharmacology 65: 702-710.
Ligt R.A.F. de, Klein P.A. van der, Frijtag Drabbe Kunzel J.K. von , Lorenzen A., Ait El Maate F., Fujikawa S., Westhoven R. van, Hoven T. van den, Brussee J. & IJzerman A.P. (2004), Synthesis and biological evaluation of disubstituted N6-cyclopentyladenine analogues: the search for a neutral antagonist with high affinity for the adenosine A1 receptor, Bioorganic & Medicinal Chemistry 12: 139-149.
Wittendorp M.C., Frijtag Drabbe Kunzel J.K. von, IJzerman A.P., Boddeke H.W. & biber K. (2004), The mouse brain adenosine A1 receptor: functional expression and pharmacology, European Journal of Pharmacology 487: 73-79.
Ligt R.A.F. de, Lorenzen A. & Ijzerman A.P. (2003), Inverse agonism at adenosine A(1) receptors, International Congress Series 1249: 87-99.
Herk T. van, Brussee J.M., Nieuwendijk A.M.C.H. van den, Klein P.A.M. van der, IJzerman A.P., Stannek C., Burmeister A. & Lorenzen A. (2003), Pyrazole derivatives as partial Agonists for the nicotinic acid receptor, Journal of Medicinal Chemistry 46(18): 3945-3951.
Deghati P.Y.F., Borghini A., Nieuwendijk A.M.C.H. van den, Dissen-de Groote M. & IJzerman A.P. (2003), Inhibition of nucleoside transport by new analogues of nitrobenzylthioinosine, Bioorganic & Medicinal Chemistry 11(6): 899-908.
Tilburg E.W. van, Gremmen M., Frijtag Drabbe Kuenzel J.K. von, Groote M. de & IJzerman A.P. (2003), 2,8-Disubstituted adenosine derivatives as partial agonists for the adenosine A2A receptor, Bioorganic & Medicinal Chemistry 11: 2183-2192.
Bueters T.J.H., Joosen M.J.A., Helden H.P.M., IJzerman A.P. & Danhof M. (2003), Adenosine A1 receptor agonist N6-cyclopentyladenosine affects the inactivation of acetylcholinesterase in blood and brain by sarin, Journal of Pharmacology and Experimental Therapeutics 304: 1307-1313.
Schaddelee M.P., Voorwinden H.L., Groenendaal D., Hersey A., IJzerman A.P., Danhof M. & Boer A.G. de (2003), Blood-Brain Barrier transport of Synthetic adenosine A1 receptor agonists in vitro: structure transport relationships, European Journal of Pharmaceutical Sciences 20: 347-356.
Bueters T.J.H., IJzerman A.P., Helden H.P.M. & Danhof M. (2003), Characterization of the pharmacokinetics, brain distribution, and therapeutic efficacy of the adenosine A1 receptor partial agonist 2'-deoxy-N6-cyclopentyladenosine in sarin-poisoned rats, Toxicology and Applied Pharmacology 192: 86-94.
Samsonova E., Bäck T.H.W., Beukers M.W., IJzerman A.P. & Kok J.N. (2003), Combining and comparing cluster methods in a receptor database, 2810: 342-351.
Bueters T.J.H., Duivenvoorde L.M. van, Danhof M., IJzerman A.P. & Helden H.P. van (2003), Cyclopentyladenosine and some of its low-efficacy derivatives inhibit striatal synaptosomal release of acetylcholine to a similar degree, European Journal of Pharmacology 481: 141-146.
Gao Z.G., Melman N., Erdmann A., Kim S.G., Mueller C., IJzerman A.P. & Jacobson K.A. (2003), Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A1 and A3 adenosine receptors, Biochemical Pharmacology 64: 525-534.
Soudijn W., Wijngaarden I. van & IJzerman A.P. (2003), Enantioselectivity in Drug-Receptor interactions. In: Eichelbaum Michel F., Testa Bernard & Somogyi Andrew (Eds.), Handbook of Experimental Pharmacology (Stereochemical aspects of drug action and disposition). Handbook of Experimental Pharmacology. Berlin: Springer Verlag. 161-182.
Boer A.G. de (2003), Functional role of adenosine receptor subtypes in the regulation of blood-brain barrier permeability: possible implications for the design of synthetic adenosine derivatives, European Journal of Pharmaceutical Sciences 19: 13-22.
IJzerman A.P. (2003), Inverse Agonism. Amsterdam: Elsevier.
IJzerman A.P. (2003), Inverse Agonism. In: IJzerman A.P. (Ed.), Esteve Foundation Symposia. Amsterdam: Elsevier.
Bueters T.J.H., Helden H.P. van, IJzerman A.P. & Danhof M. (2003), Low efficacy adenosine A1 agonists inhibit striatal acetylcholine release in rats improving central selectivity of action, Neuroscience Letters 343: 57-61.
Schaddelee M.P., Voorwinden H.L., Tilburg E.W. van, Pateman T.J., IJzerman A.P., Danhof M., Soudijn W. & Wijngaarden I. van (2003), Medicinal chemistry of adenosine A1 receptor ligands, Current Topics in Medicinal Chemistry 3: 355-367.
Beukers M.W., Wanner M.J., Frijtag Drabbe Kuenzel J.K. von, Klaasse E.C., IJzerman A.P. & Koomen G.J. (2003), N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor, Journal of Medicinal Chemistry 46: 1492-1503.
Harrison P.K., Bueters T.J.H., IJzerman A.P., Helden H.P. van & Tattersall J.E. (2003), Partial adenosine A1 receptor agonists inhibit sarin-induced epileptiform activity in the hippocampal slice, European Journal of Pharmacology 471: 97-104.
Herk T. van, Brussee J., Nieuwendijk A.M.C.H. van den, Klein P.A. van der, IJzerman A.P., Stannek C., Burmeister A. & Lorenzen A. (2003), Pyrazole derivatives as partial agonists for the nicotinic acid receptor, Journal of Medicinal Chemistry 46: 3945-3951.
Herk T. van, Brussee J., Nieuwendijk A.M.C.H. van den, Klein P.A.M. van der, IJzerman A.P., Stannek C., Burmeister A. & Lorenzen A. (2003), Pyrazole derivatives as partial agonists for the nicotinic receptor, Journal of Medicinal Chemistry 46: 3945-3951.
Soudijn W., Wijngaarden I. van & IJzerman A.P. (2003), Stereoselectivity of drug-receptor interactions, IDrugs 6: 43-56.
Calenbergh S. van, Link A., Fujikawa S., Ligt R.A.F. de, Vanheusden V., Golisade A., Blaton N.M., Rozenski J., IJzerman A.P. & Herdewijn P. (2002), 5’-Deoxy congeners of 9-(3-amido-3-deoxy-β-D-xylofuranosyl)-N6-cyclopentyladenine: new adenosine A1 receptor antagonists and inverse agonists, Journal of Medicinal Chemistry 45: 1845-1852.
Soudijn W., Wijngaarden I. van & IJzerman A.P. (2002), Allosteric modulation of G protein-coupled receptors, Curr. Opin. DrugDisc. Dev. 5: 748-755.
Schrier S.M., Florea B.I., Mulder G.J., Nagelkerke J.F. & IJzerman A.P. (2002), Apoptosis induced by extracellular ATP in the mouse neuroblastoma cell line N1E-115:studies on involvement of P2 receptors and adenosine, Biochemical Pharmacology 63: 1119-1126.
Schrier S.M., Florea B.I., Mulder G.J., Nagelkerke J.F. & IJzerman A.P. (2002), Apoptosis induced by extracellular ATP in the neuroblastoma cell line NIE-115: studies on involvement of P2 receptors and adenosine, Biochemical Pharmacology 63: 1119-1126.
Bueters T.J.H., Helden H.P.M., Danhof M. & IJzerman A.P. (2002), Effects of the adenosine A1 receptor allosteric modulators PD81,723 and LUF5484 on the striatal acetylcholine release, European Journal of Pharmacology 454: 177-182.
Tilburg E.W. van, Frijtag Drabbe Künzel J. von, Groote M. de & IJzerman A.P. (2002), Evaluation of C2,5'-disubstituted adenosine derivatives: selectivity and efficacy for the adenosine A1, A2A and A3 receptor, Journal of Medicinal Chemistry 45: 420-429.
Haan J.M.M. den, Mutis T., Blokland E., IJzerman A.P. & Goulmy E.A.J.M. (2002), General T-cell receptor antagonists to immunomodulate HLA-A2-restricted minor histocompatibility antigen HA-1-specific T-cell responses, Blood 99: 985-992.
Haan J.M.M. den, Mutis T., Blokland E., IJzerman A.P. & Goulmy E.A.J.M. (2002), General T-cell receptor antagonist to immunomodulate HLA-A2-restricted minor histocompatibility antigen HA-1 specific T cell responses, Blood 99(3): 985-992.
Deghati P.Y.F., Borghini A., Nieuwendijk A.M.C.H. van den, Dissen-de Groote M. & IJzerman A.P. (2002), Inhibition of nucleoside transport by new analogs of nitrobenzylthioinosine, Bioorganic & Medicinal Chemistry 11: 899-908.
Ligt A.F. de & IJzerman A.P. (2002), Intrinsic activity at adenosine A1 receptors: partial and inverse agonism, Current Pharmaceutical Design 8: 2333-2344.
Lorenzen A., Beukers M.W., Graaf P.H. van der, Lang H., Muijlwijk-Koezen J.E. van, Groote M. de, Menge W., Schwabe U. & IJzerman A.P. (2002), Modulation of agonist responses at the A1 adenosine receptor by an irreversible antagonist, receptor-G protein uncoupling and by the G protein activation state, Biochemical Pharmacology 64: 1251-1265.
Carmine R. del, Amrosio C., Sbraccia M., Cotecchia S., IJzerman A.P. & Costa T. (2002), Mutations inducing divergent shifts of constitutive activity reveal different modes of binding among catecholamine analogues to the beta2-adrenergic receptor, British Journal of Pharmacology 135: 1715-1722.
Priego E.M., Frijtag Drabbe Künzel J.K. von , IJzerman A.P., Camarasa M.J. & Perez-Perez M.J. (2002), Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A3 adenosine receptor antagonists, Journal of Medicinal Chemistry 45: 3337-3344.
Gao Z.-G., Kim S.G., Soltysiak K.A., Melman N., IJzerman A.P. & Jacobson K.A. (2002), Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives, Molecular Pharmacology 62: 81-89.
Dalpiaz A., Pavan B., Ngo F., Franchetti P. & IJzerman A.P. (2002), Temperature dependence of the affinity enhancement of selective adenosine A1 receptor agonism: a thermodynamic analysis, European Journal of Pharmacology 448: 123-131.
Bueters T.J.H., Groen B., Danhof M., IJzerman A.P. & Helden H.P.M. (2002), Therapeutic efficacy of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) against organophosphate intoxication, Archives of Toxicology 76: 650-656.
Soudijn W., Wijngaarden I. van & IJzerman A.P. (2001), Allosteric modulation of G-protein-coupled receptors, Expert opinion on therapeutic patents 11(12): 1889-1904.
Fredholm B.B., Ijzerman A.P., Jacobson K.A., Klotz K.N. & Linden J. (2001), International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors, Pharmacological Reviews 53(4): 527-552.
Gao Z.G., Muijlwijk-Koezen J.E. van, Chen A.S., Muller C.E., IJzerman A.P. & Jacobson K.A. (2001), Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives, Molecular Pharmacology 60(5): 1057-1063.
Tilburg E.W. van, Klein P.A.M. van der, Frijtag J. von, Kunzel D., Groote M. de, Stannek C., Lorenzen A. & IJzerman A.P. (2001), 5 '-O-alkyl ethers of N,2-substituted adenosine derivatives: Partial agonists for the adenosine A(1) and A(3) receptors, Journal of Medicinal Chemistry 44(18): 2966-2975.
Tilburg E.W. van, Klein P.A.M. van der, Groote M. de, Beukers M.W. & IJzerman A.P. (2001), Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor, 11(15): 2017-2019.
Muijlwijk-Koezen J.E. van, Timmerman H., Sluis R.P. van der, Stolpe A.C. van de, Menge W.M.P.B., Beukers M.W., Graaf P.H. van der, Groote M. de & IJzerman A.P. (2001), Synthesis and use of FSCPX, an irreversible adenosine A(1) antagonist, as a 'receptor knock-down' tool, Bioorganic and Medicinal Chemistry Letters 11(6): 815-818.
Muijlwijk-Koezen J.E. van, Timmerman H., Vollinga R.C., Kunzel J.F.V., Groote M. de, Visser S. & IJzerman A.P. (2001), Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists, Journal of Medicinal Chemistry 44(5): 749-762.
Schrier S.M., Tilburg E.W. van, Meulen H. van der, IJzerman A.P., Mulder G.J. & Nagelkerke J.F. (2001), Extracellular adenosine-induced apoptosis in mouse neuroblastoma cells - Studies on involvement of adenosine receptors and adenosine uptake, Biochemical Pharmacology 61(4): 417-425.
Kourounakis A., Visser C., Groote M. de & IJzerman A.P. (2001), Differential effects of the allosteric enhancer (2-amino-4,5-dimethyl-trienyl)[3-(trifluoromethyl) phenyl]methanone (PD81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A(1) receptor, Biochemical Pharmacology 61(2): 137-144.
Schrier S.M., Tilburg E.W. van, Meulen J. van der, IJzerman A.P. & Nagelkerke J.F. (2001), extracellular adenosine-induced apoptosis in mouse neuroblastoma cells studies on involvement of adenosine receptors and adenosine uptake, Biochemical Pharmacology 61(4): 417-425.
Kourounakis A.P., Visser C., Groote M. de & IJzerman A.P. (2000), Allosteric modulation of the rat adenosine A(1) receptor: Differential effects on agonist and antagonist binding, Drug Development Research 51(4): 207-215.
Horn F., Wenden E.M. van der, Oliveira L., IJzerman A.P. & Vriend G. (2000), Receptors coupling to G proteins: Is there a signal behind the sequence?, 41(4): 448-459.
Ligt R.A.F. de, Kourounakis A.P. & Ijzerman A.P. (2000), Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery (vol 130, pg 1, 2000), British Journal of Pharmacology 131(1): 160-160.
Wanner M.J., Kunzel J.K.V.D., IJzerman A.P. & Koomen G.J. (2000), 2-nitro analogues of adenosine and 1-deazaadenosine: Synthesis and binding studies at the adenosine A(1), A(2A) and A(3) receptor subtypes, 10(18): 2141-2144.
Gao Z.G. & IJzerman A.P. (2000), Allosteric modulation of A(2A) adenosine receptors by amiloride analogues and sodium ions, Biochemical Pharmacology 60(5): 669-676.
Gao Z.G., Jiang Q.L., Jacobson K.A. & IJzerman A.P. (2000), Site-directed mutagenesis studies of human A(2A) adenosine receptors - Involvement of Glu(13) and His(278) in ligand binding and sodium modulation, Biochemical Pharmacology 60(5): 661-668.
Muijlwijk-Koezen J.E. van, Timmerman H., Goot H. van der, Menge W.M.P.B., Kunzel J.F.V., Groote M. de & IJzerman A.P. (2000), Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor, Journal of Medicinal Chemistry 43(11): 2227-2238.
Ligt R.A.F. de, Kourounakis A.P. & IJzerman A.P. (2000), Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery, British Journal of Pharmacology 130(1): 1-12.
Kourounakis A.P., Klein P.A.M. van der & IJzerman A.P. (2000), Elucidation of structure-activity relationships of 2-amino-3-benzoylthiophenes: Study of their allosteric enhancing vs. antagonistic activity on adenosine A(1) receptors, Drug Development Research 49(4): 227-237.
Ingkaninan K., IJzerman A.P. & Verpoorte R. (2000), Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea, 63(3): 315-317.
Zwart M. de, Groote M. de, Klein P.A.M. van der, Dun S. van, Bronsing R., Kunzel J.K.V.D. & Ijzerman A.P. (2000), Phenyl-substituted N-6-phenyladenosines and N-6-phenyl-5 '-N-ethylcarboxamidoadenosines with high activity at human adenosine A(2B) receptors, Drug Development Research 49(2): 85-93.
Vittori S., Lorenzen A., Stannek C., Costanzi S., Volpini R., IJzerman A.P., Kunzel J.K.V.D. & Cristalli G. (2000), N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor, Journal of Medicinal Chemistry 43(2): 250-260.
Beukers M.W., Dulk H. den, Tilburg E.W. van, Brouwer J. & IJzerman A.P. (2000), Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A2B receptor for 2-(1-hexynyl) adenosine, Molecular Pharmacology 58(6): 1349-1356.
Calenbergh S. van, Link A., Fujikawa S., Vanheusden V., Keukeleire D. de, IJzerman A.P. & Herdewijn P. (1999), 5 '-deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N-6-cyclopentyladenine: New adenosine A(1) receptor antagonists, Symposium on the chemistry of nucleic acid components (in de serie Nucleic acids symposium series) 2: 273-276.
Ingkaninan K., Ijzerman A.P., Taesotikul T. & Verpoorte R. (1999), Isolation of opioid-active compounds from Tabernaemontana pachysiphon leaves, 51(12): 1441-1446.
Beukers M.W., Kristiansen K., IJzerman A.P. & Edvardsen O. (1999), TinyGRAP database: a bioinformatics tool to mine G-protein-coupled receptor mutant data, Trends in Pharmacological Sciences 20(12): 475-477.
Zwart M. de, Vollinga R.C., Beukers M.W., Sleegers D.F., Kunzel J.K.V.D., Groote M. de & IJzerman A.P. (1999), Potent antagonists for the human adenosine A(2B) receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity, Drug Development Research 48(3): 95-103.
Zuurmond H.M., Hessling J., Bluml K., Lohse M. & IJzerman A.P. (1999), Study of interaction between agonists and Asn293 in helix VI of human beta(2)-adrenergic receptor, Molecular Pharmacology 56(5): 909-916.
Klein P.A.M. van der, Kourounakis A.P. & IJzerman A.P. (1999), Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding, Journal of Medicinal Chemistry 42(18): 3629-3635.
Graaf P.H. van der, Schaick E.A. van, Visser S.A.G., Greef H.J.M.M. van, IJzerman A.P. & Danhof M. (1999), Mechanism-based pharmacokinetic-pharmacodynamic modeling of antilipolytic effects of adenosine A(1) receptor agonists in rats: Prediction of tissue-dependent efficacy in vivo, Journal of Pharmacology and Experimental Therapeutics 290(2): 702-709.
Dalpiaz A., Scatturin A., Pavan B., Varani K., IJzerman A.P. & Borea P.A. (1999), Thermodynamic in vitro studies as a method to investigate the pharmacodynamic behavior of adenosine A(1) receptor ligands, PHARMACEUTICAL RESEARCH 16(7): 1054-1058.
Ingkaninan K., Kunzel J.K.V.D., IJzerman A.P. & Verpoorte R. (1999), Interference of linoleic acid fraction in some receptor binding assays, 62(6): 912-914.
Jacobson K.A., Ijzerman A.P. & Linden J. (1999), 1,3-dialkylxanthine derivatives having high potency as antagonists at human A(2B) adenosine receptors, Drug Development Research 47(1): 45-53.
Zwart M. de, Kourounakis A., Kooijman H., Spek A.L., Link R., Frijtag Drabbe Künzel J.K. von & IJzerman A.P. (1999), 5'-N-Substituted carboxamidoadenosines as agonists for adenosine receptors, Journal of Medicinal Chemistry 42(8): 1384-1392.
Tilburg E.W. van, Frijtag Drabbe Künzel J.K. von, Groote M. de, Vollinga R.C., Lorenzen A. & IJzerman A.P. (1999), N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor, Journal of Medicinal Chemistry 42(8): 1393-1400.
Rivkees S.A., Barbhaiya H. & IJzerman A.P. (1999), Identification of the adenine binding site of the human A(1) adenosine receptor, Journal of Biological Chemistry 274(6): 3617-3621.
Calenbergh S. van, Ijzerman A.P. & Herdewijn P. (1998), 3 '-amidated 3 '-deoxyxylofuranose analogues of N-6-cyclopentyladenosines: A new class of non-xanthine antagonists at the adenosine A(1) receptor, Nucleosides and Nucleotides 17(9-11): 1571-1576.
Zwart M. de, Link R., Kunzel J.K.V., Cristalli G., Jacobson K.A., Townsend-Nicholson A. & IJzerman A.P. (1998), A functional screening of adenosine analogues at the adenosine A(2B) receptor: A search for potent agonists, Nucleosides and Nucleotides 17(6): 969-985.
Tilburg E.W. van, Muijlwijk-Koezen J.E. van & IJzerman A.P. (1998), Medicinal chemistry of the human adenosine A3 receptor, Drug Development Research 45(3-4): 182-189.
Rivkees S. A., IJzerman A.P. & Swanson T. (1998), New insights into the molecular mechanisms of A(1) adenosine receptor action, Drug Development Research 45(3-4): 93-102.
Pavan B. & IJzerman A.P. (1998), Processing of adenosine receptor agonists in rat and human whole blood, Biochemical Pharmacology 56(12): 1625-1632.
Dalpiaz A., Townsend-Nicholson A., Beukers M.W., Schofield P.R. & IJzerman A.P. (1998), Thermodynamics of full agonist, partial agonist and antagonist binding to wild type and mutant adenosine A1 receptors, Biochemical Pharmacology 56(11): 1437-1445.
Schaick E.A. van, Zuideveld K.P., Tukker H.J., Langemeijer M.W.E., IJzerman A.P. & Danhof M. (1998), Metabolic and cardiovascular effects of the adenosine A(1) receptor agonist N-6-(p-sulfophenyl)adenosine in diabetic Zucker rats: Influence of the disease on the selectivity of action, Journal of Pharmacology and Experimental Therapeutics 287(1): 21-30.
Muijlwijk-Koezen J.E. van, Timmerman H., Link R., Goot H. van der & IJzerman A.P. (1998), A novel class of adenosine A3 receptor ligands. I. 3-(2-Pyridinyl)isoquinoline derivatives, Journal of Medicinal Chemistry 41(21): 3987-3993.
Kim Y.C., Zwart M. de, Chang L., Moro S., Frijtag Drabbe Künzel J.K. von, Melman N., IJzerman A.P. & Jacobson K.A. (1998), Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) having high potency at the human A2B and A3 receptor subtypes, Journal of Medicinal Chemistry 41(15): 2835-2845.
Schaick E.A. van, Tukker H.J., Roelen H.C.P.F., IJzerman A.P. & Danhof M. (1998), Selectivity of action of 8-alkylamino analogues of N-6-cyclopentyladenosine in vivo: haemodynamic versus anti-lipolytic responses in rats, British Journal of Pharmacology 124(3): 607-618.
Wenden E.M. van der, Carnielli M., Roelen H.C.P.F., Lorenzen A., Frijtag Drabbe Künzel J.K. von & IJzerman A.P. (1998), 5'-Substituted adenosine analogs as new high affinity partial agonists for the adenosine A1 receptor, Journal of Medicinal Chemistry 41(1): 102-108.
IJzerman A.P. (1998), Adenosine receptor antagonists and asthma. National Institute of Health, NIDDK. Bethesda, USA. [lecture].
Muijlwijk-Koezen J.E. van, Timmerman H., Link R., Goot H. van der & IJzerman A.P. (1998), A novel class of adenosine A3 receptor ligands. II. Structure affinity profile of a series of isoquinoline and quinazoline compounds, Journal of Medicinal Chemistry 41: 3994-4000.
Zwart M. de, Link R., Frijtag Drabbe Künzel J.K. von, Cristalli G., Jacobson K.A., Townsend-Nicholson A. & IJzerman A.P. (1998), A screening of adenosine analogues at the human adenosine A2B receptor: a search for potent agonists, Nucleosides and Nucleotides 17: 969-986.
IJzerman A.P. (1998), Bioinformatics in drug design. Lezing. London, UK. [lecture].
IJzerman A.P., Wenden E.M. van der & Kuipers W. (1998), Computational chemistry in receptor-based drug design. In: Leff P. (Ed.), Receptor-based drug design. New York, USA: Marcel Dekker. 323-344.
Pavan B. & IJzerman A.P. (1998), In vitro pharmacokinetic and metabolic study of adenosine receptor agonists in rat and human whole blood, Biochemical Pharmacology 56: 1625-1632.
Graaf P.H. van der, Schaick E.A. van, Visser S.A.G., Greef H.J.M.M. de, IJzerman A.P. & Danhof M. (1998), Mechanism-based pharmacokinetic-pharmacodynamic modeling of anti-lipolytic effects of adenosine A1 receptor agonists in rats: prediction of tissue-dependent efficay in vivo, Journal of Pharmacology and Experimental Therapeutics : .
IJzerman A.P. (1998), Medicinal chemistry of adenosine receptor antagonists. Lezing. Horsham, UK. [lecture].
IJzerman A.P. (1998), Medicinal chemistry of adenosine receptor antagonists. Biogen Inc.. Cambridge, USA. [lecture].
IJzerman A.P. (1998), Medicinal chemistry of the human adenosine A3 receptor. Lezing. Ferrara, Italy. [lecture].
IJzerman A.P. (1998), Molecular modelling of G protein-coupled receptors. Lezing. München, Duitsland. [lecture].
IJzerman A.P. (1998), Molecular modelling of G protein-coupled receptors. Lezing. Utrecht, NL. [lecture].
Rivkees S., IJzerman A.P. & Swanson T. (1998), New insight into the molecular mechanisms of A1 adenosine receptor action, Drug Development Research 45: 182-189.
IJzerman A.P. (1998), Partial agonists for adenosine receptors. EMBL. Heidelberg, Germany. [lecture].
Schaick E.A. van, Greef H.J.M.M. de, IJzerman A.P. & Danhof M. (1998), Physiological indirect effect modeling of the antilipolytic effects of adenosine A1-receptor agonists, Journal of Pharmacokinetics and Biopharmaceutics 25(6): 673-694.
Schwartz T. & IJzerman A.P. (1998), Principles of agonism: undressing efficacy, Trends in Pharmacological Sciences 19: 433-436.
Bouwstra J.A., Gooris G.S., Dubbelaar F.E.R., Weerheim A.M., IJzerman A.P. & Ponec M. (1998), Role of Ceramide 1 in the molecular organization of the stratum corneum lipids, 39: 186-196.
IJzerman A.P. (1998), The adenosine A2A receptor in the CNS: an attractive drug target. Lezing. Weesp, NL. [lecture].
Bouwstra J.A., Gooris G.S., Dubbelaar F.E.R., Weerheim A.M., IJzerman A.P. & Ponec-Waelsch M.H. (1998), The role of ceramide 1 in the molecular organisation of the stratum corneum lipids, 39: 186-196.
Kuipers W., Oliveira L., Vriend G. & Ijzerman A.P. (1997), Identification of class-determining residues in G protein-coupled receptors by sequence analysis, Receptors and Channels 5(3-4): 159-174.
Schaick E.A. van, Greef H.J.M.M. de, IJzerman A.P. & Danhof M. (1997), Physiological indirect effect modeling of the antilipolytic effects of adenosine A(1)-receptor agonists, Journal of Pharmacokinetics and Biopharmaceutics 25(6): 673-694.
Lorenzen A., Vogt H., vanderWenden E.M., Roelen H.C.P.F., Carnielli M., Ijzerman A.P. & Schwabe U. (1997), Potency and efficacy of partial agonists of the adenosine A(1) receptor in G protein activation and inhibition of adenylate cyclase, Naunyn-Schmiedeberg's Archives of Pharmacology 355(4): 110-110.
Schaick E.A. van, Kulkarni C., Kunzel J.K.V.D., Mathot R.A.A., Cristalli G., Ijzerman A.P. & Danhof M. (1997), Time course of action of three adenosine A(1) receptor agonists with differing lipophilicity in rats: comparison of pharmacokinetic, haemodynamic and EEG effects, Naunyn-Schmiedeberg's Archives of Pharmacology 356(6): 827-837.
VanSchaick E.A., Mathot R.A.A., GubbensStibbe J.M., Langemeijer M.W.E., Roelen H.C.P.F., IJzerman A.P. & Danhof M. (1997), 8-Alkylamino-substituted analogs of N-6-cyclopentyladenosine are partial agonists for the cardiovascular adenosine A(1) receptors in vivo, Journal of Pharmacology and Experimental Therapeutics 283(2): 800-808.
Graaf P.H. van der, Schaick E.A. van, Mathot R.A.A., IJzerman A.P. & Danhof M. (1997), Mechanism-based pharmacokinetic-pharmacodynamic modeling of the effects of N-6-cyclopentyladenosine analogs on heart rate in rat: Estimation of in vivo operational affinity and efficacy at adenosine A(1) receptors, Journal of Pharmacology and Experimental Therapeutics 283(2): 809-816.
Calenbergh S. van, Frijtag J.K. von, Kunzel D., Blaton N.M., Peeters O.M., Rozenski J., VanAerschot A., DeBruyn A., DeKeukeleire D., Ijzerman A.P. & Herdewijn P. (1997), N-6-cyclopentyl-3'-substituted-xylofuranosyladenosines: A new class of non-xanthine adenosine A(1) receptor antagonists, Journal of Medicinal Chemistry 40(23): 3765-3772.
Schaick E.A. van, Greef H.J.M.M. de, Langemeijer M.W.E., Sheehan M.J., IJzerman A.P. & Danhof M. (1997), Pharmacokinetic-pharmacodynamic modelling of the anti-lipolytic and anti-ketotic effects of the adenosine A(1)-receptor agonist N-6-(p-sulphophenyl)adenosine in rats, British Journal of Pharmacology 122(3): 525-533.
Lorenzen A., Sebastiao A.M., Sellink A., Vogt H., Schwabe U., Ribeiro J.A. & IJzerman A.P. (1997), Biological activities of N-6,C8-disubstituted adenosine derivatives as partial agonists at rat brain adenosine A(1) receptors, European Journal of Pharmacology 334(2-3): 299-307.
Bol C.J.JG., Ijzerman A.P., Danhof M. & Mandema J.W. (1997), Determination of dexmedetomidine in rat plasma by a sensitive [H-3]clonidine radioreceptor assay, JOURNAL OF PHARMACEUTICAL SCIENCES 86(7): 822-826.
Kuipers W., Link R., Standaar P.J., Stoit A.R., VanWijngaarden I., Leurs R. & IJzerman A.P. (1997), Study of the interaction between aryloxypropanolamines and Asn386 in helix VII of the human 5-hydroxytryptamine(1A) receptor, Molecular Pharmacology 51(5): 889-896.
Smeets R.L.L., IJzerman A.P., Hermsen H.P.H., Ophorst O.J.A.E., Vries S.E.V., DePont J.J.H.H.M. & Willems P.H.G.M. (1997), Mutational analysis of the putative devazepide binding site of the CCKA receptor, European Journal of Pharmacology 325(1): 93-99.
Kuipers W., Kruse C.G., Wijngaarden I. van, Standaar P.J., Tulp M.T.M., Veldman N., Spek A.L. & IJzerman A.P. (1997), 5-HT1A-versus D-2-receptor selectivity of flesinoxan and analogous N-4-substituted N-1-arylpiperazines, Journal of Medicinal Chemistry 40(3): 300-312.
Jacobson K.A., IJzerman A.P., Starke K., Barnard E.A. & North R.A. (1996), General discussion .1. Molecular modelling of P2Y purinoceptors, Ciba Foundation Symposium 198: 189-192.
Mathot R.A.A., Wenden E.M. van der, Soudijn W., Breimer D.D., Ijzerman A.P. & Danhof M. (1996), Partial agonism of the nonselective adenosine receptor agonist 8-butylaminoadenosine at the A(1) receptor in vivo, Journal of Pharmacology and Experimental Therapeutics 279(3): 1439-1446.
Beindl W., Mitterauer T., Hohenegger M., IJzerman A.P., Nanoff C. & Freissmuth M. (1996), Inhibition of receptor/G protein coupling by suramin analogues, Molecular Pharmacology 50(2): 415-423.
Ijzerman A.P., Kunzel J.K.V.D., Kim J., Jiang Q.L. & Jacobson K.A. (1996), Site-directed mutagenesis of the human adenosine A(2A) receptor. Critical involvement of Glu(13) in agonist recognition, European Journal of Pharmacology 310(2-3): 269-272.
Wieland K., Zuurmond H.M., Krasel C., IJzerman A.P. & Lohse M.J. (1996), Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta(2)-adrenergic receptor, Proceedings of the National Academy of Sciences 93(17): 9276-9281.
Schaick E.A. van, Jacobson K.A., Kim H.O., IJzerman A.P. & Danhof M. (1996), Hemodynamic effects and histamine release elicited by the selective adenosine A(3) receptor agonist 2-Cl-IB-MECA in conscious rats, European Journal of Pharmacology 308(3): 311-314.
Mathot R.A.A., Soudijn W., Breimer D.D., IJzerman A.P. & Danhof M. (1996), Pharmacokinetic-haemodynamic relationships of 2-chloroadenosine at adenosine A(1) and A(2a) receptors in vivo, British Journal of Pharmacology 118(2): 369-377.
Freissmuth M., Boehm S., Beindl W., Nickel P., Ijzerman A.P., Hohenegger M. & Nanoff C. (1996), Suramin analogues as subtype-selective G protein inhibitors, Molecular Pharmacology 49(4): 602-611.
Roelen H., Veldman N., Spek A.L., Kunzel J.V.D., Mathot R.A.A. & IJzerman A.P. (1996), N-6,C8-disubstituted adenosine derivatives as partial agonists for adenosine A(1) receptors?, Journal of Medicinal Chemistry 39(7): 1463-1471.
Frijtag J.K. von, Kunzel D., Zee J. van der & IJzerman A.P. (1996), Radical scavenging properties of adenosine and derivatives in vitro, Drug Development Research 37(1): 48-54.
IJzerman A.P., Wenden N.M. van der, Galen P.J.M. van & Jacobson K.A. (1995), Molecular modeling of adenosine A(1) and A(2a) receptors. In: , Adenosine and Adenine Nucleotides: From Molecular Biology to integrative physiology: Springer. 27-37.
Anonymous (1995), Molecular modelling of the adenosine A(1) receptor [New perspectives in drugs design] (translation: Ijzerman A.P., Galen P.J.M. van & Wenden E.M. van der). Rhone-Poulenc Rorer Round Table Conference Series: Academic Press Inc.
Mathot R.A., Wenden E.M. van den, Soudijn W., IJzerman A.P. & Danhof M. (1995), DEOXYRIBOSE ANALOGS OF N-6-CYCLOPENTYLADENOSINE (CPA) - PARTIAL AGONISTS AT THE ADENOSINE A(1) RECEPTOR IN-VIVO, British Journal of Pharmacology 116(3): 1957-1964.
Mathot R.A.A., Gubbensstibbe J.M., Soudijn W., Jacobson K.A., IJzerman A.P. & Danhof M. (1995), Quantification of the in vivo potency of the adenosine A2 receptor antagonist 8-(3-chlorostyryl)caffeine, Journal of Pharmacology and Experimental Therapeutics 275(1): 245-253.
Wenden E.M. van der, Kunzel J.K.V.D., Mathot R.A.A., Danhof M., Ijzerman A.P. & Soudijn W. (1995), Ribose-modified adenosine-analogs as potential partial agonists for the adenosine receptor, Journal of Medicinal Chemistry 38(20): 4000-4006.
Appel S., Mathot R.A.A., Langemijer M.W.E., IJzerman A.P. & Danhof M. (1995), MODELING OF THE PHARMACODYNAMIC INTERACTION OF AN A(1) ADENOSINE RECEPTOR AGONIST AND ANTAGONIST IN-VIVO - N-6-CYCLOPENTYLADENOSINE AND 8-CYCLOPENTYLTHEOPHYLLINE, British Journal of Pharmacology 115(7): 1253-1259.
Wenden E.M. van der, Hartogwitte H.R., Roelen H.C.P.F., Kunzel J.K.V., Pirovano I.M., Mathot R.A.A., Danhof M., Aerschot A. van, Lidaks M.J., IJzerman A.P. & Soudijn W. (1995), 8-SUBSTITUTED ADENOSINE AND THEOPHYLLINE-7-RIBOSIDE ANALOGS AS POTENTIAL PARTIAL AGONISTS FOR THE ADENOSINE A(1) RECEPTOR, European Journal of Pharmacology : Molecular Pharmacology Section 290(3): 189-199.
Beukers M.W., Kerkhof C.J.M., Rhee M.A. van, Ardanuy U., Gurgel C., Widjaja H., Nickel P., IJzerman A.P. & Soudijn W. (1995), Suramin analogs, divalent-cations and ATP-gamma-S as inhibitors of ecto-ATPase, Naunyn-Schmiedeberg's Archives of Pharmacology 351(5): 523-528.
Kuipers W., Wijngaarden I. van, Kruse C.G., Horst van Amstel M. ter, Tulp M.T.M. & IJzerman A.P. (1995), N-4-UNSUBSTITUTED N-1-ARYLPIPERAZINES AS HIGH-AFFINITY 5-HT1A RECEPTOR LIGANDS, Journal of Medicinal Chemistry 38(11): 1942-1954.
Mathot R.A.A., Aarsen B.C.F.M van den, Soudijn W., Breimer D.D., Ijzerman A.P. & Danhof M. (1995), PHARMACOKINETIC-PHARMACODYNAMIC MODELING OF THE CARDIOVASCULAR EFFECTS OF R-N-6-PHENYLISOPROPYLADENOSINE AND S-N-6-PHENYLISOPROPYLADENOSINE IN CONSCIOUS NORMOTENSIVE RATS, Journal of Pharmacology and Experimental Therapeutics 273(1): 405-414.
Siddiqi SM., Jacobson K.A., Esker J.L., Olah M.E., Ji X.D., Melman N., Tiwari K.N., Secrist J.A., Schneller S.W., Cristalli G., Stiles G.L., Johnson C.R. & IJzerman A.P. (1995), SEARCH FOR NEW PURINE-MODIFIED AND RIBOSE-MODIFIED ADENOSINE-ANALOGS AS SELECTIVE AGONISTS AND ANTAGONISTS AT ADENOSINE RECEPTORS, Journal of Medicinal Chemistry 38(7): 1174-1188.
Mathot R.A.A., Cleton A., Soudijn W., IJzerman A.P. & Danhof M. (1995), PHARMACOKINETIC MODELING OF THE HEMODYNAMIC-EFFECTS OF THE A(2A) ADENOSINE RECEPTOR AGONIST CGS 21680C IN CONSCIOUS NORMOTENSIVE RATS, British Journal of Pharmacology 114(4): 761-768.
Wenden E.M., Price S.L., Apaya R.P., Ijzerman A.P. & Soudijn W. (1995), Relative binding orientations of adenosine-A(1) receptor ligands - a test-case for Distributed Multipole Analysis in medicinal chemistry, Journal of Computer-Aided Molecular Design 9(1): 44-54.
IJzerman A.P., Wenden E.M. van der, Kunzel J.K. V.D., Mathot R.A.A., Danhof M., Borea P.A. & Varani K. (1994), PARTIAL AGONISM OF THEOPHYLLINE-7-RIBOSIDE ON ADENOSINE RECEPTORS, Naunyn-Schmiedeberg's Archives of Pharmacology 350(6): 638-645.
Crack B.E., Beukers M.W., McKechnie K.C.W., IJzerman A.P. & leff P. (1994), Pharmacological analysis of ecto‐ATPase inhibition: evidence for combined enzyme inhibition and receptor antagonism in P2X‐purinoceptor ligands, British Journal of Pharmacology 113(4): 1432-1438.
IJzerman A.P., Kunzel J.K.V.D., Vittori S. & Cristalli G. (1994), Purine-substituted adenosine derivatives with small N-6-substituents as adenosine receptor agonists, Nucleosides and Nucleotides 13(10): 2267-2281.
Irth H., Cleton A., Mathot R.A.A., Danhof M., Ijzerman A.P., Tjaden U.R. & Greef J. van der (1994), LIQUID-CHROMATOGRAPHIC DETERMINATION OF THE ADENOSINE RECEPTOR AGONIST CGS-21680 IN BLOOD USING ONLINE SOLID-PHASE EXTRACTION ON A PHENYLBORONIC ACID SUPPORT AND FLUORESCENCE DETECTION, Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences 658(1): 207-212.
Mathot RA.A., Aarsen BC.F.M. van den, Kunzel J.K. vd, Danhof M. & IJzerman A.P. (1994), ASSESSMENT OF THE ENANTIOMERIC PURITY OF R AND S-N-6-PHENYLISOPROPYLADENOSINE (PIA) - IMPLICATIONS FOR ADENOSINE RECEPTOR SUBCLASSIFICATION, Naunyn-Schmiedeberg's Archives of Pharmacology 350(1): 109-112.
Galen P.J.M. van, Bergen A.H. van, Gallorodriquez C., Melman N., Olah M.E., IJzerman A.P., Stiles G.L. & Jacobson K.A. (1994), A BINDING-SITE MODEL AND STRUCTURE-ACTIVITY-RELATIONSHIPS FOR THE RAT A(3)-ADENOSINE RECEPTOR, Molecular Pharmacology 45(6): 1101-1111.
Ijzerman A.P., Wenden E.M. van der, Galen P.J.M. van & Jacobson K.A. (1994), MOLECULAR MODELING OF ADENOSINE RECEPTORS - THE LIGAND-BINDING SITE ON THE RAT ADENOSINE A(2A) RECEPTOR, European Journal of Pharmacology : Molecular Pharmacology Section 268(1): 95-104.
Rhee A.M. van, Heijden M.P.A. van der, Beukers M.W., IJzerman A.P., Soudijn W. & Nickel P. (1994), NOVEL COMPETITIVE ANTAGONISTS FOR P-2 PURINOCEPTORS, European Journal of Pharmacology : Molecular Pharmacology Section 268(1): 1-7.
Bent A. van der, Brink I. van den, IJzerman A.P., Wijngaarden I. van & soudijn W. (1994), SYNTHESIS AND BIOLOGICAL EVALUATION OF LORGLUMIDE-LIKE HYBRID CHOLECYSTOKININ-A RECEPTOR ANTAGONISTS, Drug Development Research 31(3): 197-205.
Borea P.A., Varani K., Dalpiaz A., Capuzzo A., Fabbri E. & Ijzerman A.P. (1994), FULL AND PARTIAL AGONISTIC BEHAVIOR AND THERMODYNAMIC BINDING PARAMETERS OF ADENOSINE-A1-RECEPTOR LIGANDS, European Journal of Pharmacology : Molecular Pharmacology Section 267(1): 55-61.
Mathot R.A.A., Schaick E.A. van, Langemeijer M.W.E., Soudijn W., Breimer D.D., IJzerman A.P. & Danhof M. (1994), PHARMACOKINETIC-PHARMACODYNAMIC RELATIONSHIP OF THE CARDIOVASCULAR EFFECTS OF ADENOSINE A(1) RECEPTOR AGONIST N-6-CYCLOPENTYLADENOSINE IN THE RAT, Journal of Pharmacology and Experimental Therapeutics 268(2): 616-624.
Beukers M.W., Kerkhof C.J.M., IJzerman A.P. & Soudijn W. (1994), Nucleoside transport inhibition and platelet aggregation in human blood: R75231 and its enantiomers, draflazine and R88016, European Journal of Pharmacology : Molecular Pharmacology Section 266(1): 57-62.
Beukers M.W., Pirovano I.M., Vanweert A., Kerkhof C.J.M., IJzerman A.P. & Soudijn W. (1993), CHARACTERIZATION OF ECTO-ATPASE ON HUMAN BLOOD-CELLS - A PHYSIOLOGICAL-ROLE IN PLATELET-AGGREGATION, Biochemical Pharmacology 46(11): 1959-1966.
Mathot R.A.A., Appel S., Vanschaick E.A., Soudijn W., IJzerman A.P. & Danhof M. (1993), HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY OF THE ADENOSINE A(1) AGONIST N-6-CYCLOPENTYLADENOSINE AND THE A(1) ANTAGONIST 8-CYCLOPENTYLTHEOPHYLLINE AND ITS APPLICATION IN A PHARMACOKINETIC STUDY IN RATS, Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences 620(1): 113-120.
Dudley M.W., Peet N.P., Demeter D.A., Weintraub H.J.R., IJzerman A.P., Nordvall G., Galen P.J.M. van & Jacobson K.A. (1993), Adenosine A1 receptor and ligand molecular modeling, Drug Development Research 28(3): 237-243.
IJzerman A.P. (1993), STRUCTURAL-ANALYSIS OF KAPPA-OPIOID RECEPTOR AGONISTS, Recueil des Travaux Chimiques des Pays-Bas = Journal of the Royal Netherlands Chemical Society 112(2): 169-173.
Rhee A.M. van, Winden E.C.A. van, Nagelkerke J.F., Bont H.J.G.M. de, Ijzerman A.P. & Soudijn W. (1993), BINDING OF THE RADIOLIGAND [S-35] ADENOSINE 5'-O-(2-THIODIPHOSPHATE) AND INTRACELLULAR CALCIUM RESPONSE IN RAT-LIVER PARENCHYMAL-CELLS, Biochemical Pharmacology 45(4): 801-807.
Bent A. van der, Laak A.M. ter, IJzerman A.P. & Soudijn W. (1992), MOLECULAR MODELING OF ASPERLICIN DERIVED CHOLECYSTOKININ-A RECEPTOR ANTAGONISTS, European Journal of Pharmacology : Molecular Pharmacology Section 226(4): 327-334.
Ijzerman A.P., Kruidering M., Vanweert A., Vanbelle H. & Janssen C. (1992), [H-3] R75231 - A NEW RADIOLIGAND FOR THE NITROBENZYLTHIOINOSINE SENSITIVE NUCLEOSIDE TRANSPORT PROTEINS - CHARACTERIZATION OF (+/-)-[H-3]R75231 BINDING TO CALF LUNG MEMBRANES, STEREOSPECIFICITY OF ITS 2 STEREOISOMERS, AND COMPARISON WITH [H-3] NITROBENZYLTHIOINOSINE BINDING, Naunyn-Schmiedeberg's Archives of Pharmacology 345(5): 558-563.
Bent A. van der, Blommaert A.G.S., Melman C.T.M., IJzerman A.P., Wijngaarden I. van & Soudijn W. (1992), HYBRID CHOLECYSTOKININ-A ANTAGONISTS BASED ON MOLECULAR MODELING OF LORGLUMIDE AND L-364,718, Journal of Medicinal Chemistry 35(6): 1042-1049.
Garritsen A., Beukers M.W., Ijzerman A.P., Cragoe E.J. & Soudijn W. (1992), THE MODE OF INTERACTION OF AMILORIDE AND SOME OF ITS ANALOGS WITH THE ADENOSINE-A1-RECEPTOR, 20(2): 207-213.
Wenden E.M. van der, IJzerman A.P. & Soudijn W. (1992), A STERIC AND ELECTROSTATIC COMPARISON OF 3 MODELS FOR THE AGONIST ANTAGONIST BINDING-SITE ON THE ADENOSINE-A1-RECEPTOR, Journal of Medicinal Chemistry 35(4): 629-635.
Ijzerman A.P. & Melman C.T.M. (1992), CHEMICAL MODIFICATION OF CHOLECYSTOKININ-A RECEPTORS IN RAT PANCREATIC MEMBRANES, European Journal of Biochemistry 203(3): 521-526.
Garritsen A., Ijzerman A.P., Tulp M.T.M., Cragoe E.J. & Soudijn W. (1991), RECEPTOR-BINDING PROFILES OF AMILORIDE ANALOGS PROVIDE NO EVIDENCE FOR A LINK BETWEEN RECEPTORS AND THE NA+/H+ EXCHANGER, BUT INDICATE A COMMON STRUCTURE ON RECEPTOR PROTEINS, Journal of Receptor Research 11(6): 891-907.
Garritsen A., Beukers M.W., IJzerman A.P. & Soudijn W. (1991), Recognition of adenosine receptors by amiloride and its analogues, Nucleosides and Nucleotides 10(5): 1107-1111.
Hoogstraate A.J., Verhoef J., Brussee J., IJzerman A.P., Spies F. & Bodde H.E. (1991), KINETICS, ULTRASTRUCTURAL ASPECTS AND MOLECULAR MODELING OF TRANSDERMAL PEPTIDE FLUX ENHANCEMENT BY N-ALKYLAZACYCLOHEPTANONES, 76(1-2): 37-47.
Wenden E.M. van der, Galen P.J.M. van, Ijzerman A.P. & Soudijn W. (1991), A MODEL FOR THE HYDROGEN-BONDING INTERACTIONS BETWEEN ADENOSINE RECEPTOR LIGANDS AND HISTIDYL RESIDUES IN THE ADENOSINE-A1-RECEPTOR BINDING-SITE, BASED ON AM1 CALCULATIONS, Journal of Molecular Structure: Theochem 77: 175-184.
Wenden E.M van der, Galen P.J.M. van, IJzerman A.P. & Soudijn W. (1991), MAPPING THE XANTHINE C8-REGION OF THE ADENOSINE-A1-RECEPTOR WITH COMPUTER-GRAPHICS, European Journal of Pharmacology : Molecular Pharmacology Section 206(4): 315-323.
Galen P.J.M. van, Nissen P., Wijngaarden I. van, IJzerman A.P. & Soudijn W. (1991), 1H-Imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists, Journal of Medicinal Chemistry 34(3): 1202-1206.
Galen P.J.M. van, Ijzerman A.P. & Soudijn W. (1990), XANTHINE-7-RIBOSIDES AS ADENOSINE-A1 RECEPTOR ANTAGONISTS - FURTHER EVIDENCE FOR ADENOSINES ANTI MODE OF BINDING, Nucleosides and Nucleotides 9(2): 275-291.
Pirovano I.M., Vanbelle H. & IJzerman A.P. (1990), INHIBITION OF NUCLEOSIDE UPTAKE IN HUMAN ERYTHROCYTES BY A NEW SERIES OF COMPOUNDS RELATED TO LIDOFLAZINE AND MIOFLAZINE, European Journal of Pharmacology : Molecular Pharmacology Section 189(6): 419-422.
Ijzerman A.P. & Voorschuur A.H. (1990), The relationship between ionization and affinity of nucleoside transport inhibitors, Naunyn-Schmiedeberg's Archives of Pharmacology 342(3): 336-341.
Garritsen A., IJzerman A.P., Beukers M.W. & Soudijn W. (1990), CHEMICAL MODIFICATION OF ADENOSINE-A1 RECEPTORS - IMPLICATIONS FOR THE INTERACTION WITH R-PIA, DPCPX AND AMILORIDE, Biochemical Pharmacology 40(4): 835-842.
Garritsen A., IJzerman A.P., Beukers M.W., Cragoe E.J. & Soudijn W. (1990), INTERACTION OF AMILORIDE AND ITS ANALOGS WITH ADENOSINE-A1 RECEPTORS IN CALF BRAIN, Biochemical Pharmacology 40(4): 827-834.
Galen P.J.M. van, Vlijmen H.W.T. van, IJzerman A.P. & Soudijn W. (1990), A MODEL FOR THE ANTAGONIST BINDING-SITE ON THE ADENOSINE-A1 RECEPTOR, BASED ON STERIC, ELECTROSTATIC, AND HYDROPHOBIC PROPERTIES, Journal of Medicinal Chemistry 33(6): 1708-1713.
IJzerman A.P., Thedinga K.H., Custers A.F.C.M., Hoos B. & Belle H. van (1989), INHIBITION OF NUCLEOSIDE TRANSPORT BY A NEW SERIES OF COMPOUNDS RELATED TO LIDOFLAZINE AND MIOFLAZINE, European Journal of Pharmacology : Molecular Pharmacology Section 172(3): 273-281.
Vlijmen H.W.T. van & Ijzerman A.P. (1989), MOLECULAR MODELING OF A PUTATIVE ANTAGONIST BINDING-SITE ON HELIX-III OF THE BETA-ADRENOCEPTOR, 3(2): 165-174.
Pirovano I.M., Ijzerman A.P., Galen P.J.M. van & Soudijn W. (1989), INFLUENCE OF THE MOLECULAR-STRUCTURE OF N-6-(OMEGA-AMINOALKYL)ADENOSINES ON ADENOSINE RECEPTOR AFFINITY AND INTRINSIC ACTIVITY, European Journal of Pharmacology : Molecular Pharmacology Section 172(2): 185-193.
Galen P.J.M. van, Leusen F.J.J., Ijzerman A.P. & Soudijn W. (1989), MAPPING THE N-6-REGION OF THE ADENOSINE-A1 RECEPTOR WITH COMPUTER-GRAPHICS, European Journal of Pharmacology : Molecular Pharmacology Section 172(1): 19-27.
IJzerman A.P., Menkveld G.J. & Thedinga K.H. (1989), A REFINED METHOD FOR THE PHOTOAFFINITY-LABELING OF THE NITROBENZYLTHIOINOSINE-SENSITIVE NUCLEOSIDE TRANSPORT PROTEIN - APPLICATION TO CELL-MEMBRANES OF CALF LUNG-TISSUE, Biochimica et Biophysica Acta 979(2): 153-156.
Garritsen A., Ijzerman A.P. & Soudijn W. (1989), Adenosine-A1 receptors are not coupled to Ca2+ uptake in rat brain synaptosomes, Biochemical Pharmacology 38(4): 693-695.
Ijzerman A.P. & Soudijn W. (1989), THE ANTIARRHYTHMIC PROPERTIES OF BETA-ADRENOCEPTOR ANTAGONISTS, Trends in Pharmacological Sciences 10(1): 31-36.
IJzerman A.P. (1988), IONIZATION-CONSTANTS OF SPARINGLY SOLUBLE SUBSTANCES FROM AQUEOUS TITRATION DATA, 46(1-2): 173-175.
Ijzerman A.P. & Vlijmen H.W.T. van (1988), A MOLECULAR GRAPHICS STUDY EXPLORING A PUTATIVE LIGAND-BINDING SITE OF THE BETA-ADRENOCEPTOR, 2(1): 43-53.
Bing I. de, Ijzerman A.P. & Vauquelin G. (1988), MELANOSOME BINDING AND OXIDATION-REDUCTION PROPERTIES OF SYNTHETIC L-DOPA-MELANIN AS INVITRO TESTS FOR DRUG TOXICITY, Molecular Pharmacology 33(4): 470-476.
Garritsen A., IJzerman A.P. & Soudijn W. (1988), [H-3]BATRACHOTOXININ-A 20-ALPHA-BENZOATE BINDING TO SODIUM-CHANNELS IN RAT-BRAIN - SENSITIVITY TO TETRODOTOXIN AND DIVALENT-CATIONS, European Journal of Pharmacology 145(3): 261-266.
IJzerman A.P., Nagesser A. & Garritsen A. (1987), THE MEMBRANE STABILIZING ACTIVITY OF BETA-ADRENOCEPTOR LIGANDS - QUANTITATIVE-EVALUATION OF THE INTERACTION OF PHENOXYPROPANOLAMINES WITH THE [H-3]BATRACHOTOXININ-A 20-ALPHA-BENZOATE BINDING-SITE ON VOLTAGE-SENSITIVE SODIUM-CHANNELS IN RAT-BRAIN, Biochemical Pharmacology 36(24): 4239-4244.
Galen P.J.M. van, Ijzerman A.P. & Soudijn W. (1987), ADENOSINE DERIVATIVES WITH N-6-ALKYL, N-6-ALKYLAMINE OR N-6-ALKYLADENOSINE SUBSTITUENTS AS PROBES FOR THE A1-RECEPTOR, FEBS Letters 223(1): 197-201.
Ijzerman A.P., Bultsma T. & Timmerman H. (1986), BINDING CHARACTERISTICS OF THE REGULATORY GUANINE-NUCLEOTIDE BINDING-PROTEIN, AND THE ACTIVATION OF THE ENZYME ADENYLATE-CYCLASE, PRESENT IN A BOVINE SKELETAL-MUSCLE MEMBRANE PREPARATION, Research communications in chemical pathology and pharmacology 52(1): 93-105.
IJzerman A.P., Bultsma T. & Timmerman H. (1986), QUANTITATIVE-EVALUATION OF THE BETA-2-ADRENOCEPTOR INTRINSIC ACTIVITY OF N-TERT-BUTYLPHENYLETHANOLAMINES, Journal of Medicinal Chemistry 29(4): 549-554.
Linschoten M.R., Bultsma T., IJzerman A.P. & Timmerman H. (1986), MAPPING THE TURKEY ERYTHROCYTE-BETA-RECEPTOR - A DISTANCE GEOMETRY APPROACH, Journal of Medicinal Chemistry 29(2): 278-286.
IJzerman A.P., Dorlas R., Aue G.H.J., Bultsma T. & Timmerman H. (1985), FACTORS CONTROLLING BETA-1-ADRENOCEPTOR AFFINITY AND SELECTIVITY, Biochemical Pharmacology 34(16): 2883-2890.
Ijzerman A.P., Aue G.H.J., Bultsma T., Linschoten M.R. & Timmerman H. (1985), QUANTITATIVE-EVALUATION OF THE BETA-2-ADRENOCEPTOR AFFINITY OF PHENOXYPROPANOLAMINES AND PHENYLETHANOLAMINES, Journal of Medicinal Chemistry 28(9): 1328-1334.
IJzerman A.P., Bultsma T., Timmerman H. & Zaagsma J. (1984), THE IONIZATION OF BETA-ADRENOCEPTOR AGONISTS - A METHOD FOR UNRAVELLING IONIZATION SCHEMES, 36(1): 11-15.
Ijzerman A.P., Bultsma T., Timmerman H. & Zaagsma J. (1984), THE RELATION BETWEEN IONIZATION AND AFFINITY OF BETA-ADRENOCEPTOR LIGANDS, Naunyn-Schmiedeberg's Archives of Pharmacology 327(4): 293-298.
Wilting J., Kremer J.M.H., Ijzerman A.P. & Schulman S.G. (1982), THE KINETICS OF THE BINDING OF WARFARIN TO HUMAN-SERUM ALBUMIN AS STUDIED BY STOPPED-FLOW SPECTROPHOTOMETRY, Biochimica et Biophysica Acta 706(1): 96-104.

Koninklijke Hollandsche Maatschappij der Wetenschappen secretaris natuurwetenschappen
Leiden Center for Science and Consult Geven van wetenschappelijke cursussen en adviezen