| Year |
Citation |
Score |
| 2016 |
Guo D, Pan AC, Dror RO, Mocking T, Liu R, Heitman L, Shaw DE, IJzerman AP. Molecular basis of ligand dissociation from the adenosine A2A receptor. Molecular Pharmacology. PMID 26873858 DOI: 10.1124/mol.115.102657 |
1 |
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| 2016 |
Nederpelt I, Vergroesen RD, IJzerman AP, Heitman LH. Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology Biosensors and Bioelectronics. 79: 721-727. DOI: 10.1016/j.bios.2015.12.066 |
1 |
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| 2015 |
Liu R, van Veldhoven JP, IJzerman AP. 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. PMID 26656756 DOI: 10.1016/j.ejphar.2015.11.052 |
1 |
|
| 2015 |
Xia L, de Vries H, IJzerman AP, Heitman LH. 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. PMID 26647040 DOI: 10.1007/s11302-015-9485-0 |
1 |
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| 2015 |
Doornbos ML, Pérez-Benito L, Tresadern G, Mulder-Krieger T, Biesmans I, Trabanco AA, Cid JM, Lavreysen H, IJzerman AP, Heitman LH. Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222. British Journal of Pharmacology. PMID 26589404 DOI: 10.1111/bph.13390 |
1 |
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| 2015 |
Yu Z, van Veldhoven JP, 't Hart IM, Kopf AH, Heitman LH, IJzerman AP. Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel. European Journal of Medicinal Chemistry. 106: 50-59. PMID 26519929 DOI: 10.1016/j.ejmech.2015.10.032 |
1 |
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| 2015 |
Guo D, Heitman LH, IJzerman AP. The Role of Target Binding Kinetics in Drug Discovery. Chemmedchem. 10: 1793-6. PMID 26506404 DOI: 10.1002/cmdc.201500310 |
1 |
|
| 2015 |
Massink A, Holzheimer M, Hölscher A, Louvel J, Guo D, Spijksma G, Hankemeier T, IJzerman AP. Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors. Purinergic Signalling. PMID 26482925 DOI: 10.1007/s11302-015-9477-0 |
1 |
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| 2015 |
Nederpelt I, Schuldt V, Schiele F, Nowak-Reppel K, Fernández-Montalván AE, IJzerman AP, Heitman LH. Characterization of 12 GnRH peptide agonists - a kinetic perspective. British Journal of Pharmacology. PMID 26398856 DOI: 10.1111/bph.13342 |
1 |
|
| 2015 |
Peeters MC, Fokkelman M, Boogaard B, Egerod KL, van de Water B, IJzerman AP, Schwartz TW. The adhesion G protein-coupled receptor G2 (ADGRG2/GPR64) constitutively activates SRE and NFκB and is involved in cell adhesion and migration. Cellular Signalling. PMID 26321231 DOI: 10.1016/j.cellsig.2015.08.015 |
1 |
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| 2015 |
Louvel J, Guo D, Soethoudt M, Mocking TA, Lenselink EB, Mulder-Krieger T, Heitman LH, IJzerman AP. Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists. European Journal of Medicinal Chemistry. 101: 681-91. PMID 26210506 DOI: 10.1016/j.ejmech.2015.07.023 |
1 |
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| 2015 |
Yu Z, van Veldhoven JP, Louvel JA, 't Hart IM, Rook MB, van der Heyden MA, Heitman LH, IJzerman AP. Structure-affinity relationships (SARs) and structure-kinetics relationships (SKRs) of Kv11.1 blockers. Journal of Medicinal Chemistry. PMID 26125327 DOI: 10.1021/acs.jmedchem.5b00518 |
1 |
|
| 2015 |
Vilums M, Zweemer AJ, Dilanchian A, van Veldhoven JP, de Vries H, Brussee J, Saunders J, Stamos D, Heitman LH, IJzerman AP. Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor. Chemmedchem. PMID 26033831 DOI: 10.1002/cmdc.201500058 |
1 |
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| 2015 |
Vilums M, Heuberger J, Heitman LH, IJzerman AP. Indanes-Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors. Medicinal Research Reviews. PMID 26018667 DOI: 10.1002/med.21352 |
1 |
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| 2015 |
Paricharak S, Cortés-Ciriano I, IJzerman AP, Malliavin TE, Bender A. 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. PMID 25926892 DOI: 10.1186/s13321-015-0063-9 |
1 |
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| 2015 |
Liu R, Nahon D, le Roy B, Lenselink EB, IJzerman AP. Scanning mutagenesis in a yeast system delineates the role of the NPxxY(x)5,6F motif and helix 8 of the adenosine A2B receptor in G protein coupling. Biochemical Pharmacology. 95: 290-300. PMID 25896847 DOI: 10.1016/j.bcp.2015.04.005 |
1 |
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| 2015 |
van Veldhoven JP, Liu R, Thee SA, Wouters Y, Verhoork SJ, Mooiman C, Louvel J, IJzerman AP. Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists. Bioorganic & Medicinal Chemistry. 23: 4013-25. PMID 25737085 DOI: 10.1016/j.bmc.2015.02.018 |
1 |
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| 2015 |
Vilums M, Zweemer AJ, Barmare F, van der Gracht AM, Bleeker DC, Yu Z, de Vries H, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, IJzerman AP. 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. PMID 25666912 DOI: 10.1016/j.ejmech.2015.01.063 |
1 |
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| 2015 |
Massink A, Gutiérrez-de-Terán H, Lenselink EB, Ortiz ZacarÃas NV, Xia L, Heitman LH, Katritch V, Stevens RC, IJzerman AP. Sodium ion binding pocket mutations and adenosine A2A receptor function. Molecular Pharmacology. 87: 305-13. PMID 25473121 DOI: 10.1124/mol.114.095737 |
1 |
|
| 2015 |
Yu Z, IJzerman AP, Heitman LH. Kv 11.1 (hERG)-induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypical Kv 11.1 (hERG) inhibitors. British Journal of Pharmacology. 172: 940-55. PMID 25296617 DOI: 10.1111/bph.12967 |
1 |
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| 2015 |
Cortés-Ciriano I, Ain QU, Subramanian V, Lenselink EB, Méndez-Lucio O, Ijzerman AP, Wohlfahrt G, Prusis P, Malliavin TE, Van Westen GJP, Bender A. Polypharmacology modelling using proteochemometrics (PCM): Recent methodological developments, applications to target families, and future prospects Medchemcomm. 6: 24-50. DOI: 10.1039/c4md00216d |
1 |
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| 2015 |
Romagnoli R, Baraldi PG, Lopez-Cara C, Cruz-Lopez O, Moorman AR, Massink A, Ijzerman AP, Vincenzi F, Borea PA, Varani K. 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. DOI: 10.1016/j.ejmech.2015.06.041 |
1 |
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| 2015 |
Hillger JM, Schoop J, Boomsma DI, Eline Slagboom P, IJzerman AP, Heitman LH. Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines Biosensors and Bioelectronics. 74: 233-242. DOI: 10.1016/j.bios.2015.06.031 |
1 |
|
| 2014 |
Vilums M, Zweemer AJ, Dekkers S, Askar Y, de Vries H, Saunders J, Stamos D, Brussee J, Heitman LH, IJzerman AP. Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives. Bioorganic & Medicinal Chemistry Letters. 24: 5377-80. PMID 25453791 DOI: 10.1016/j.bmcl.2014.10.060 |
1 |
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| 2014 |
Bansal M, Yang J, Karan C, Menden MP, Costello JC, Tang H, Xiao G, Li Y, Allen J, Zhong R, Chen B, Kim M, Wang T, Heiser LM, Realubit R, et al. A community computational challenge to predict the activity of pairs of compounds. Nature Biotechnology. 32: 1213-22. PMID 25419740 DOI: 10.1038/nbt.3052 |
1 |
|
| 2014 |
Cohen S, Barer F, Bar-Yehuda S, IJzerman AP, Jacobson KA, Fishman P. A₃ adenosine receptor allosteric modulator induces an anti-inflammatory effect: in vivo studies and molecular mechanism of action. Mediators of Inflammation. 2014: 708746. PMID 25374446 DOI: 10.1155/2014/708746 |
1 |
|
| 2014 |
Romagnoli R, Baraldi PG, IJzerman AP, Massink A, Cruz-Lopez O, Lopez-Cara LC, Saponaro G, Preti D, Aghazadeh Tabrizi M, Baraldi S, Moorman AR, Vincenzi F, Borea PA, Varani K. Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. Journal of Medicinal Chemistry. 57: 7673-86. PMID 25181013 DOI: 10.1021/jm5008853 |
1 |
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| 2014 |
Peeters MC, Li Q, Elands R, van Westen GJ, Lenselink EB, Müller CE, IJzerman AP. Domains for activation and inactivation in G protein-coupled receptors--a mutational analysis of constitutive activity of the adenosine A2B receptor. Biochemical Pharmacology. 92: 348-57. PMID 25179146 DOI: 10.1016/j.bcp.2014.08.022 |
1 |
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| 2014 |
Guo D, Venhorst SN, Massink A, van Veldhoven JP, Vauquelin G, IJzerman AP, Heitman LH. Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor. British Journal of Pharmacology. 171: 5295-312. PMID 25040887 DOI: 10.1111/bph.12836 |
1 |
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| 2014 |
Zweemer AJ, Bunnik J, Veenhuizen M, Miraglia F, Lenselink EB, Vilums M, de Vries H, Gibert A, Thiele S, Rosenkilde MM, IJzerman AP, Heitman LH. Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2. Molecular Pharmacology. 86: 358-68. PMID 25024169 DOI: 10.1124/mol.114.093328 |
1 |
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| 2014 |
Costello JC, Heiser LM, Georgii E, Gönen M, Menden MP, Wang NJ, Bansal M, Ammad-ud-din M, Hintsanen P, Khan SA, Mpindi JP, Kallioniemi O, Honkela A, Aittokallio T, Wennerberg K, et al. A community effort to assess and improve drug sensitivity prediction algorithms. Nature Biotechnology. 32: 1202-12. PMID 24880487 DOI: 10.1038/nbt.2877 |
1 |
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| 2014 |
Lenselink EB, Beuming T, Sherman W, van Vlijmen HW, IJzerman AP. Selecting an optimal number of binding site waters to improve virtual screening enrichments against the adenosine A2A receptor. Journal of Chemical Information and Modeling. 54: 1737-46. PMID 24835542 DOI: 10.1021/ci5000455 |
1 |
|
| 2014 |
Zweemer AJ, Toraskar J, Heitman LH, IJzerman AP. Bias in chemokine receptor signalling. Trends in Immunology. 35: 243-52. PMID 24679437 DOI: 10.1016/j.it.2014.02.004 |
1 |
|
| 2014 |
Louvel J, Guo D, Agliardi M, Mocking TA, Kars R, Pham TP, Xia L, de Vries H, Brussee J, Heitman LH, Ijzerman AP. Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines. Journal of Medicinal Chemistry. 57: 3213-22. PMID 24669958 DOI: 10.1021/jm401643m |
1 |
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| 2014 |
Guo D, Xia L, van Veldhoven JP, Hazeu M, Mocking T, Brussee J, Ijzerman AP, Heitman LH. Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor. Chemmedchem. 9: 752-61. PMID 24591302 DOI: 10.1002/cmdc.201300474 |
1 |
|
| 2014 |
Guo D, Hillger JM, IJzerman AP, Heitman LH. Drug-target residence time--a case for G protein-coupled receptors. Medicinal Research Reviews. 34: 856-92. PMID 24549504 DOI: 10.1002/med.21307 |
1 |
|
| 2014 |
Liu R, Groenewoud NJ, Peeters MC, Lenselink EB, IJzerman AP. 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: 441-53. PMID 24464644 DOI: 10.1007/s11302-014-9407-6 |
1 |
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| 2014 |
Koutsoukas A, Paricharak S, Galloway WR, Spring DR, Ijzerman AP, Glen RC, Marcus D, Bender A. How diverse are diversity assessment methods? A comparative analysis and benchmarking of molecular descriptor space. Journal of Chemical Information and Modeling. 54: 230-42. PMID 24289493 DOI: 10.1021/ci400469u |
1 |
|
| 2014 |
Yu Z, Klaasse E, Heitman LH, Ijzerman AP. Allosteric modulators of the hERG K(+) channel: radioligand binding assays reveal allosteric characteristics of dofetilide analogs. Toxicology and Applied Pharmacology. 274: 78-86. PMID 24200993 DOI: 10.1016/j.taap.2013.10.024 |
1 |
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| 2013 |
Louvel J, Carvalho JF, Yu Z, Soethoudt M, Lenselink EB, Klaasse E, Brussee J, Ijzerman AP. Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues. Journal of Medicinal Chemistry. 56: 9427-40. PMID 24224763 DOI: 10.1021/jm4010434 |
1 |
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| 2013 |
Gutiérrez-de-Terán H, Massink A, RodrÃguez D, Liu W, Han GW, Joseph JS, Katritch I, Heitman LH, Xia L, Ijzerman AP, Cherezov V, Katritch V, Stevens RC. The role of a sodium ion binding site in the allosteric modulation of the A(2A) adenosine G protein-coupled receptor. Structure (London, England : 1993). 21: 2175-85. PMID 24210756 DOI: 10.1016/j.str.2013.09.020 |
1 |
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| 2013 |
van Westen GJ, Swier RF, Cortes-Ciriano I, Wegner JK, Overington JP, Ijzerman AP, van Vlijmen HW, Bender A. Benchmarking of protein descriptor sets in proteochemometric modeling (part 2): modeling performance of 13 amino acid descriptor sets. Journal of Cheminformatics. 5: 42. PMID 24059743 DOI: 10.1186/1758-2946-5-42 |
1 |
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| 2013 |
van Westen GJ, Swier RF, Wegner JK, Ijzerman AP, van Vlijmen HW, Bender A. Benchmarking of protein descriptor sets in proteochemometric modeling (part 1): comparative study of 13 amino acid descriptor sets. Journal of Cheminformatics. 5: 41. PMID 24059694 DOI: 10.1186/1758-2946-5-41 |
1 |
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| 2013 |
Lane JR, IJzerman AP. Allosteric approaches to GPCR drug discovery. Drug Discovery Today. Technologies. 10: e219-21. PMID 24050271 DOI: 10.1016/j.ddtec.2013.01.006 |
1 |
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| 2013 |
Vilums M, Zweemer AJ, Yu Z, de Vries H, Hillger JM, Wapenaar H, Bollen IA, Barmare F, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, ... Ijzerman AP, et al. 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: 7706-14. PMID 24028535 DOI: 10.1021/jm4011737 |
1 |
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| 2013 |
Chen D, Ranganathan A, IJzerman AP, Siegal G, Carlsson J. 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: 2701-14. PMID 23971943 DOI: 10.1021/ci4003156 |
1 |
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| 2013 |
Zweemer AJ, Nederpelt I, Vrieling H, Hafith S, Doornbos ML, de Vries H, Abt J, Gross R, Stamos D, Saunders J, Smit MJ, Ijzerman AP, Heitman LH. Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2. Molecular Pharmacology. 84: 551-61. PMID 23877010 DOI: 10.1124/mol.113.086850 |
1 |
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| 2013 |
Bouma HR, Mandl JN, Strijkstra AM, Boerema AS, Kok JW, van Dam A, Ijzerman A, Kroese FG, Henning RH. 5'-AMP impacts lymphocyte recirculation through activation of A2B receptors. Journal of Leukocyte Biology. 94: 89-98. PMID 23682128 DOI: 10.1189/jlb.1212613 |
1 |
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| 2013 |
Varkevisser R, Houtman MJ, Linder T, de Git KC, Beekman HD, Tidwell RR, Ijzerman AP, Stary-Weinzinger A, Vos MA, van der Heyden MA. Structure-activity relationships of pentamidine-affected ion channel trafficking and dofetilide mediated rescue. British Journal of Pharmacology. 169: 1322-34. PMID 23586323 DOI: 10.1111/bph.12208 |
1 |
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| 2013 |
De Bruyn T, van Westen GJ, Ijzerman AP, Stieger B, de Witte P, Augustijns PF, Annaert PP. Structure-based identification of OATP1B1/3 inhibitors. Molecular Pharmacology. 83: 1257-67. PMID 23571415 DOI: 10.1124/mol.112.084152 |
1 |
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| 2013 |
Carvalho JF, Louvel J, Doornbos ML, Klaasse E, Yu Z, Brussee J, IJzerman AP. Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide. Journal of Medicinal Chemistry. 56: 2828-40. PMID 23473309 DOI: 10.1021/jm301564f |
1 |
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| 2013 |
van Westen GJ, Hendriks A, Wegner JK, Ijzerman AP, van Vlijmen HW, Bender A. Significantly improved HIV inhibitor efficacy prediction employing proteochemometric models generated from antivirogram data. Plos Computational Biology. 9: e1002899. PMID 23436985 DOI: 10.1371/journal.pcbi.1002899 |
1 |
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| 2013 |
Guo D, van Dorp EJ, Mulder-Krieger T, van Veldhoven JP, Brussee J, Ijzerman AP, Heitman LH. Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics. Journal of Biomolecular Screening. 18: 309-20. PMID 23093571 DOI: 10.1177/1087057112464776 |
1 |
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| 2013 |
Langemeijer EV, Verzijl D, Dekker SJ, Ijzerman AP. Functional selectivity of adenosine A1 receptor ligands? Purinergic Signalling. 9: 91-100. PMID 23054444 DOI: 10.1007/s11302-012-9334-3 |
1 |
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| 2012 |
Chen D, Errey JC, Heitman LH, Marshall FH, Ijzerman AP, Siegal G. Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A(2A) receptor with novel biological activity. Acs Chemical Biology. 7: 2064-73. PMID 23013674 DOI: 10.1021/cb300436c |
1 |
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| 2012 |
van Westen GJ, van den Hoven OO, van der Pijl R, Mulder-Krieger T, de Vries H, Wegner JK, Ijzerman AP, van Vlijmen HW, Bender A. Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data. Journal of Medicinal Chemistry. 55: 7010-20. PMID 22827545 DOI: 10.1021/jm3003069 |
1 |
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| 2012 |
Liu W, Chun E, Thompson AA, Chubukov P, Xu F, Katritch V, Han GW, Roth CB, Heitman LH, IJzerman AP, Cherezov V, Stevens RC. Structural basis for allosteric regulation of GPCRs by sodium ions. Science (New York, N.Y.). 337: 232-6. PMID 22798613 DOI: 10.1126/science.1219218 |
1 |
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| 2012 |
Bot I, de Vries H, Korporaal SJ, Foks AC, Bot M, van Veldhoven J, Ter Borg MN, van Santbrink PJ, van Berkel TJ, Kuiper J, Ijzerman AP. Adenosine A₂B receptor agonism inhibits neointimal lesion development after arterial injury in apolipoprotein E-deficient mice. Arteriosclerosis, Thrombosis, and Vascular Biology. 32: 2197-205. PMID 22743060 DOI: 10.1161/ATVBAHA.112.252924 |
1 |
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| 2012 |
van der Horst E, Marqués-Gallego P, Mulder-Krieger T, van Veldhoven J, Kruisselbrink J, Aleman A, Emmerich MT, Brussee J, Bender A, Ijzerman AP. Multi-objective evolutionary design of adenosine receptor ligands. Journal of Chemical Information and Modeling. 52: 1713-21. PMID 22647079 DOI: 10.1021/ci2005115 |
1 |
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| 2012 |
Li Z, Blad CC, van der Sluis RJ, de Vries H, Van Berkel TJ, Ijzerman AP, Hoekstra M. Effects of pyrazole partial agonists on HCA(2) -mediated flushing and VLDL-triglyceride levels in mice. British Journal of Pharmacology. 167: 818-25. PMID 22616721 DOI: 10.1111/j.1476-5381.2012.02039.x |
1 |
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| 2012 |
Sanders MP, Roumen L, van der Horst E, Lane JR, Vischer HF, van Offenbeek J, de Vries H, Verhoeven S, Chow KY, Verkaar F, Beukers MW, McGuire R, Leurs R, Ijzerman AP, de Vlieg J, et al. A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design. Journal of Medicinal Chemistry. 55: 5311-25. PMID 22563707 DOI: 10.1021/jm300280e |
1 |
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| 2012 |
Peeters MC, Wisse LE, Dinaj A, Vroling B, Vriend G, Ijzerman AP. The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation. Biochemical Pharmacology. 84: 76-87. PMID 22449615 DOI: 10.1016/j.bcp.2012.03.008 |
1 |
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| 2012 |
Blad CC, van Veldhoven JP, Klopman C, Wolfram DR, Brussee J, Lane JR, Ijzerman AP. Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A). Journal of Medicinal Chemistry. 55: 3563-7. PMID 22420767 DOI: 10.1021/jm300164q |
1 |
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| 2012 |
Guo D, Mulder-Krieger T, IJzerman AP, Heitman LH. Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time. British Journal of Pharmacology. 166: 1846-59. PMID 22324512 DOI: 10.1111/j.1476-5381.2012.01897.x |
1 |
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| 2012 |
Heitman LH, Kleinau G, Brussee J, Krause G, Ijzerman AP. 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: 326-36. PMID 22269095 DOI: 10.1016/j.mce.2012.01.010 |
1 |
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| 2012 |
Lane JR, Klein Herenbrink C, van Westen GJ, Spoorendonk JA, Hoffmann C, IJzerman AP. 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: 475-87. PMID 22188926 DOI: 10.1124/mol.111.075937 |
1 |
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| 2012 |
Du L, Gao ZG, Nithipatikom K, Ijzerman AP, Veldhoven JP, Jacobson KA, Gross GJ, Auchampach JA. Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor. The Journal of Pharmacology and Experimental Therapeutics. 340: 210-7. PMID 22011434 DOI: 10.1124/jpet.111.187559 |
1 |
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| 2012 |
Vilums M, Overman J, Klaasse E, Scheel O, Brussee J, IJzerman AP. Understanding of molecular substructures that contribute to hERG K+ channel blockade: synthesis and biological evaluation of E-4031 analogues. Chemmedchem. 7: 107-13. PMID 21919210 DOI: 10.1002/cmdc.201100366 |
1 |
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| 2012 |
Peeters MC, Li Q, van Westen GJ, Ijzerman AP. 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: 23-38. PMID 21818573 DOI: 10.1007/s11302-011-9251-x |
1 |
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| 2011 |
van Westen GJ, Wegner JK, Geluykens P, Kwanten L, Vereycken I, Peeters A, Ijzerman AP, van Vlijmen HW, Bender A. Which compound to select in lead optimization? Prospectively validated proteochemometric models guide preclinical development. Plos One. 6: e27518. PMID 22132107 DOI: 10.1371/journal.pone.0027518 |
1 |
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| 2011 |
van der Horst E, van der Pijl R, Mulder-Krieger T, Bender A, Ijzerman AP. Substructure-based virtual screening for adenosine A2A receptor ligands. Chemmedchem. 6: 2302-11. PMID 22021213 DOI: 10.1002/cmdc.201100369 |
1 |
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| 2011 |
Blad CC, Ahmed K, IJzerman AP, Offermanns S. Biological and pharmacological roles of HCA receptors. Advances in Pharmacology (San Diego, Calif.). 62: 219-50. PMID 21907911 DOI: 10.1016/B978-0-12-385952-5.00005-1 |
1 |
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| 2011 |
Blad CC, von Frijtag Drabbe Künzel JK, de Vries H, Mulder-Krieger T, Bar-Yehuda S, Fishman P, Ijzerman AP. Putative role of the adenosine A(3) receptor in the antiproliferative action of N (6)-(2-isopentenyl)adenosine. Purinergic Signalling. 7: 453-62. PMID 21720785 DOI: 10.1007/s11302-011-9244-9 |
1 |
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| 2011 |
Gao ZG, Verzijl D, Zweemer A, Ye K, Göblyös A, Ijzerman AP, Jacobson KA. Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers. Biochemical Pharmacology. 82: 658-68. PMID 21718691 DOI: 10.1016/j.bcp.2011.06.017 |
1 |
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| 2011 |
Jacobson KA, Gao ZG, Göblyös A, Ijzerman AP. Allosteric modulation of purine and pyrimidine receptors. Advances in Pharmacology (San Diego, Calif.). 61: 187-220. PMID 21586360 DOI: 10.1016/B978-0-12-385526-8.00007-2 |
1 |
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| 2011 |
Lane JR, Jaakola VP, Ijzerman AP. The structure of the adenosine receptors: implications for drug discovery. Advances in Pharmacology (San Diego, Calif.). 61: 1-40. PMID 21586354 DOI: 10.1016/B978-0-12-385526-8.00001-1 |
1 |
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| 2011 |
Verzijl D, Ijzerman AP. Functional selectivity of adenosine receptor ligands. Purinergic Signalling. 7: 171-92. PMID 21544511 DOI: 10.1007/s11302-011-9232-0 |
1 |
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| 2011 |
van der Horst E, Peironcely JE, van Westen GJ, van den Hoven OO, Galloway WR, Spring DR, Wegner JK, van Vlijmen HW, Ijzerman AP, Overington JP, Bender A. Chemogenomics approaches for receptor deorphanization and extensions of the chemogenomics concept to phenotypic space. Current Topics in Medicinal Chemistry. 11: 1964-77. PMID 21470175 DOI: 10.2174/156802611796391230 |
1 |
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| 2011 |
Offermanns S, Colletti SL, Lovenberg TW, Semple G, Wise A, IJzerman AP. International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B). Pharmacological Reviews. 63: 269-90. PMID 21454438 DOI: 10.1124/pr.110.003301 |
1 |
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| 2011 |
Gomes I, Ijzerman AP, Ye K, Maillet EL, Devi LA. G protein-coupled receptor heteromerization: a role in allosteric modulation of ligand binding. Molecular Pharmacology. 79: 1044-52. PMID 21415307 DOI: 10.1124/mol.110.070847 |
1 |
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| 2011 |
Fredholm BB, IJzerman AP, Jacobson KA, Linden J, Müller CE. International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacological Reviews. 63: 1-34. PMID 21303899 DOI: 10.1124/pr.110.003285 |
1 |
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| 2011 |
van Veldhoven JP, Blad CC, Artsen CM, Klopman C, Wolfram DR, Abdelkadir MJ, Lane JR, Brussee J, Ijzerman AP. Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A). Bioorganic & Medicinal Chemistry Letters. 21: 2736-9. PMID 21167710 DOI: 10.1016/j.bmcl.2010.11.091 |
1 |
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| 2011 |
Peeters MC, van Westen GJ, Li Q, IJzerman AP. Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation. Trends in Pharmacological Sciences. 32: 35-42. PMID 21075459 DOI: 10.1016/j.tips.2010.10.001 |
1 |
|
| 2011 |
Peeters MC, van Westen GJ, Guo D, Wisse LE, Müller CE, Beukers MW, Ijzerman AP. GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 25: 632-43. PMID 21030693 DOI: 10.1096/fj.10-164319 |
1 |
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| 2011 |
Früh V, IJzerman AP, Siegal G. How to catch a membrane protein in action: a review of functional membrane protein immobilization strategies and their applications. Chemical Reviews. 111: 640-56. PMID 20831158 DOI: 10.1021/cr900088s |
1 |
|
| 2011 |
Göblyös A, Ijzerman AP. Allosteric modulation of adenosine receptors. Biochimica Et Biophysica Acta. 1808: 1309-18. PMID 20599682 DOI: 10.1016/j.bbamem.2010.06.013 |
1 |
|
| 2011 |
Van Westen GJP, Wegner JK, Ijzerman AP, Van Vlijmen HWT, Bender A. Proteochemometric modeling as a tool to design selective compounds and for extrapolating to novel targets Medchemcomm. 2: 16-30. DOI: 10.1039/c0md00165a |
1 |
|
| 2010 |
Lane JR, Klaasse E, Lin J, van Bruchem J, Beukers MW, Ijzerman AP. Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor. Biochemical Pharmacology. 80: 1180-9. PMID 20599769 DOI: 10.1016/j.bcp.2010.06.041 |
1 |
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| 2010 |
Jaakola VP, Ijzerman AP. 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: 401-14. PMID 20538452 DOI: 10.1016/j.sbi.2010.05.002 |
1 |
|
| 2010 |
van der Horst E, Peironcely JE, Ijzerman AP, Beukers MW, Lane JR, van Vlijmen HW, Emmerich MT, Okuno Y, Bender A. A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization. Bmc Bioinformatics. 11: 316. PMID 20537162 DOI: 10.1186/1471-2105-11-316 |
1 |
|
| 2010 |
Doddareddy MR, Klaasse EC, Shagufta, Ijzerman AP, Bender A. Prospective validation of a comprehensive in silico hERG model and its applications to commercial compound and drug databases. Chemmedchem. 5: 716-29. PMID 20349498 DOI: 10.1002/cmdc.201000024 |
1 |
|
| 2010 |
Narlawar R, Lane JR, Doddareddy M, Lin J, Brussee J, Ijzerman AP. Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. Journal of Medicinal Chemistry. 53: 3028-37. PMID 20345101 DOI: 10.1021/jm901252a |
1 |
|
| 2010 |
Jaakola VP, Lane JR, Lin JY, Katritch V, Ijzerman AP, Stevens RC. Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues. The Journal of Biological Chemistry. 285: 13032-44. PMID 20147292 DOI: 10.1074/jbc.M109.096974 |
1 |
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| 2010 |
van Westen GJ, Wegner JK, Bender A, Ijzerman AP, van Vlijmen HW. Mining protein dynamics from sets of crystal structures using "consensus structures". Protein Science : a Publication of the Protein Society. 19: 742-52. PMID 20120021 DOI: 10.1002/pro.350 |
1 |
|
| 2010 |
Katritch V, Jaakola VP, Lane JR, Lin J, Ijzerman AP, Yeager M, Kufareva I, Stevens RC, Abagyan R. Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists. Journal of Medicinal Chemistry. 53: 1799-809. PMID 20095623 DOI: 10.1021/jm901647p |
1 |
|
| 2010 |
Willems LI, Ijzerman AP. Small molecule antagonists for chemokine CCR3 receptors. Medicinal Research Reviews. 30: 778-817. PMID 19967721 DOI: 10.1002/med.20181 |
1 |
|
| 2010 |
Lane JR, Beukers MW, Mulder-Krieger T, Ijzerman AP. The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor. Biochemical Pharmacology. 79: 48-56. PMID 19665453 DOI: 10.1016/j.bcp.2009.07.024 |
1 |
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| 2010 |
Heitman LH, Narlawar R, De Vries H, Willemsen MN, Wolfram D, Brussee J, Ijzerman AP. Corrections to substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor (Journal of Medicinal Chemistry (2009) 52, (2036) DOI: 10.1021/jm801561h) Journal of Medicinal Chemistry. 53: 520. DOI: 10.1021/jm901700k |
1 |
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| 2010 |
Merighi S, Simioni C, Lane R, Ijzerman AP. Regulation of second messenger systems and intracellular pathways A3 Adenosine Receptors From Cell Biology to Pharmacology and Therapeutics. 61-73. DOI: 10.1007/978-90-481-3144-0_4 |
1 |
|
| 2010 |
Kruisselbrink JW, Emmerich MTM, Bäck T, Bender A, IJzerman AP, Van Der Horst E. Combining aggregation with Pareto optimization: A case study in evolutionary molecular design Lecture Notes in Computer Science (Including Subseries Lecture Notes in Artificial Intelligence and Lecture Notes in Bioinformatics). 5467: 453-467. DOI: 10.1007/978-3-642-01020-0_36 |
1 |
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| 2009 |
Guo D, Klaasse E, de Vries H, Brussee J, Nalos L, Rook MB, Vos MA, van der Heyden MA, Ijzerman AP. Exploring chemical substructures essential for HERG k(+) channel blockade by synthesis and biological evaluation of dofetilide analogues. Chemmedchem. 4: 1722-32. PMID 19725081 DOI: 10.1002/cmdc.200900203 |
1 |
|
| 2009 |
van der Putten C, Zuiderwijk-Sick EA, van Straalen L, de Geus ED, Boven LA, Kondova I, IJzerman AP, Bajramovic JJ. Differential expression of adenosine A3 receptors controls adenosine A2A receptor-mediated inhibition of TLR responses in microglia. Journal of Immunology (Baltimore, Md. : 1950). 182: 7603-12. PMID 19494284 DOI: 10.4049/jimmunol.0803383 |
1 |
|
| 2009 |
van der Horst E, Okuno Y, Bender A, IJzerman AP. Substructure mining of GPCR ligands reveals activity-class specific functional groups in an unbiased manner. Journal of Chemical Information and Modeling. 49: 348-60. PMID 19434836 DOI: 10.1021/ci8003896 |
1 |
|
| 2009 |
Heitman LH, Narlawar R, de Vries H, Willemsen MN, Wolfram D, Brussee J, Ijzerman AP. Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor. Journal of Medicinal Chemistry. 52: 2036-42. PMID 19296599 DOI: 10.1021/jm801561h |
1 |
|
| 2009 |
Kim Y, de Castro S, Gao ZG, Ijzerman AP, Jacobson KA. 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: 2098-108. PMID 19284749 DOI: 10.1021/jm801659w |
1 |
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| 2009 |
Heitman LH, Göblyös A, Zweemer AM, Bakker R, Mulder-Krieger T, van Veldhoven JP, de Vries H, Brussee J, Ijzerman AP. A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. Journal of Medicinal Chemistry. 52: 926-31. PMID 19161279 DOI: 10.1021/jm8014052 |
1 |
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| 2009 |
Yuliana ND, Khatib A, Link-Struensee AM, Ijzerman AP, Rungkat-Zakaria F, Choi YH, Verpoorte R. Adenosine A1 receptor binding activity of methoxy flavonoids from Orthosiphon stamineus. Planta Medica. 75: 132-6. PMID 19137497 DOI: 10.1055/s-0028-1088379 |
1 |
|
| 2009 |
Göblyös A, Ijzerman AP. Allosteric modulation of adenosine receptors. Purinergic Signalling. 5: 51-61. PMID 18615273 DOI: 10.1007/s11302-008-9105-3 |
1 |
|
| 2009 |
Horst EVD, Bender A, Ijzerman AP. Frequent substructure mining of GPCR ligands Chemistry Central Journal. 3. DOI: 10.1186/1752-153X-3-S1-P69 |
1 |
|
| 2009 |
Kruisselbrink JW, Aleman A, Emmerich MTM, IJzerman AP, Bender A, Bäck T, Van Der Horst E. Enhancing search space diversity in multi-objective evolutionary drug molecule design using niching Proceedings of the 11th Annual Genetic and Evolutionary Computation Conference, Gecco-2009. 217-224. DOI: 10.1145/1569901.1569932 |
1 |
|
| 2009 |
Doddareddy MR, van Westen GJP, van der Horst E, Peironcely JE, Corthals F, Ijzerman AP, Emmerich M, Jenkins JL, Bender A. Chemogenomics: Looking at biology through the lens of chemistry Statistical Analysis and Data Mining. 2: 149-160. DOI: 10.1002/sam.10046 |
1 |
|
| 2008 |
Gao ZG, Ye K, Göblyös A, Ijzerman AP, Jacobson KA. Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000. Bmc Pharmacology. 8: 20. PMID 19077268 DOI: 10.1186/1471-2210-8-20 |
1 |
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| 2008 |
Jaakola VP, Griffith MT, Hanson MA, Cherezov V, Chien EY, Lane JR, Ijzerman AP, Stevens RC. The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science (New York, N.Y.). 322: 1211-7. PMID 18832607 DOI: 10.1126/science.1164772 |
1 |
|
| 2008 |
Heitman LH, van Veldhoven JP, Zweemer AM, Ye K, Brussee J, IJzerman AP. False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase. Journal of Medicinal Chemistry. 51: 4724-9. PMID 18646744 DOI: 10.1021/jm8004509 |
0.44 |
|
| 2008 |
Mantri M, de Graaf O, van Veldhoven J, Göblyös A, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Link R, de Vries H, Beukers MW, Brussee J, Ijzerman AP. 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. Journal of Medicinal Chemistry. 51: 4449-55. PMID 18637670 DOI: 10.1021/jm701594y |
1 |
|
| 2008 |
Heitman LH, Ijzerman AP. G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: a case for Gnrh, LH, FSH, and GPR54 receptor ligands. Medicinal Research Reviews. 28: 975-1011. PMID 18561294 DOI: 10.1002/med.20129 |
1 |
|
| 2008 |
Klaasse EC, Ijzerman AP, de Grip WJ, Beukers MW. Internalization and desensitization of adenosine receptors. Purinergic Signalling. 4: 21-37. PMID 18368531 DOI: 10.1007/s11302-007-9086-7 |
1 |
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| 2008 |
Heitman LH, Ye K, Oosterom J, Ijzerman AP. Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor. Molecular Pharmacology. 73: 1808-15. PMID 18344315 DOI: 10.1124/mol.107.043521 |
1 |
|
| 2008 |
Ye K, Vriend G, IJzerman AP. Tracing evolutionary pressure. Bioinformatics (Oxford, England). 24: 908-15. PMID 18304936 DOI: 10.1093/bioinformatics/btn057 |
1 |
|
| 2008 |
Bonger KM, van den Berg RJ, Knijnenburg AD, Heitman LH, Ijzerman AP, Oosterom J, Timmers CM, Overkleeft HS, van der Marel GA. Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core. Bioorganic & Medicinal Chemistry. 16: 3744-58. PMID 18282756 DOI: 10.1016/j.bmc.2008.01.054 |
1 |
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| 2008 |
van Veldhoven JP, Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Struensee-Link R, Beukers MW, Brussee J, IJzerman AP. A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorganic & Medicinal Chemistry. 16: 2741-52. PMID 18258439 DOI: 10.1016/j.bmc.2008.01.013 |
1 |
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| 2008 |
Ye K, Feenstra KA, Heringa J, Ijzerman AP, Marchiori E. Multi-RELIEF: a method to recognize specificity determining residues from multiple sequence alignments using a Machine-Learning approach for feature weighting. Bioinformatics (Oxford, England). 24: 18-25. PMID 18024975 DOI: 10.1093/bioinformatics/btm537 |
1 |
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| 2008 |
Priego EM, Pérez-Pérez MJ, von Frijtag Drabbe Kuenzel JK, de Vries H, Ijzerman AP, Camarasa MJ, Martín-Santamaría S. Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding. Chemmedchem. 3: 111-9. PMID 18000937 DOI: 10.1002/cmdc.200700173 |
1 |
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| 2008 |
Heitman LH, Oosterom J, Bonger KM, Timmers CM, Wiegerinck PH, Ijzerman AP. [3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor. Molecular Pharmacology. 73: 518-24. PMID 17989351 DOI: 10.1124/mol.107.039875 |
1 |
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| 2008 |
Biber K, Pinto-Duarte A, Wittendorp MC, Dolga AM, Fernandes CC, Von Frijtag Drabbe Künzel J, Keijser JN, de Vries R, Ijzerman AP, Ribeiro JA, Eisel U, Sebastião AM, Boddeke HW. Interleukin-6 upregulates neuronal adenosine A1 receptors: implications for neuromodulation and neuroprotection. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 33: 2237-50. PMID 17987062 DOI: 10.1038/sj.npp.1301612 |
1 |
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| 2008 |
Kazius J, Wurdinger K, van Iterson M, Kok J, Bäck T, Ijzerman AP. GPCR NaVa database: natural variants in human G protein-coupled receptors. Human Mutation. 29: 39-44. PMID 17924574 DOI: 10.1002/humu.20638 |
1 |
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| 2008 |
Biber K, Pinto-Duarte A, Wittendorp MC, Dolga AM, Fernandes CC, Von Frijtag Drabbe Künzel J, Keijser JN, De Vries R, Ijzerman AP, Ribeiro JA, Eisel U, Sebastião AM, Boddeke HWGM. Interleukin-6 upregulates neuronal adenosine A1 receptors: Implications for neuromodulation and neuroprotection (Neuropsychopharmacology (2008) 33, (2237-2250) DOI: 10.1038/sj.npp.1301612) Neuropsychopharmacology. 33: 2789. DOI: 10.1038/npp.2008.92 |
1 |
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| 2007 |
Bonger KM, van den Berg RJ, Heitman LH, IJzerman AP, Oosterom J, Timmers CM, Overkleeft HS, van der Marel GA. Synthesis and evaluation of homo-bivalent GnRHR ligands. Bioorganic & Medicinal Chemistry. 15: 4841-56. PMID 17517510 DOI: 10.1016/j.bmc.2007.04.065 |
1 |
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| 2007 |
Lameijer EW, Tromp RA, Spanjersberg RF, Brussee J, IJzerman AP. Designing active template molecules by combining computational de novo design and human chemist's expertise Journal of Medicinal Chemistry. 50: 1925-1932. PMID 17367122 DOI: 10.1021/jm061356+ |
1 |
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| 2007 |
Chang LCW, Von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Westerhout J, Spangenberg T, Brussee J, Ijzerman AP. 2,6,8-Trisubstituted 1-deazapurines as adenosine receptor antagonists Journal of Medicinal Chemistry. 50: 828-834. PMID 17300165 DOI: 10.1021/jm0607956 |
1 |
|
| 2007 |
Samsonova EV, Krause P, Bäck T, IJzerman AP. Characteristic amino acid combinations in olfactory G protein-coupled receptors. Proteins. 67: 154-66. PMID 17243181 DOI: 10.1002/prot.21112 |
1 |
|
| 2007 |
Soudijn W, Van Wijngaarden I, Ijzerman AP. Nicotinic acid receptor subtypes and their ligands Medicinal Research Reviews. 27: 417-433. PMID 17238156 DOI: 10.1002/med.20102 |
1 |
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| 2007 |
Ye K, Kosters WA, IJzerman AP. An efficient, versatile and scalable pattern growth approach to mine frequent patterns in unaligned protein sequences Bioinformatics. 23: 687-693. PMID 17237070 DOI: 10.1093/bioinformatics/btl665 |
1 |
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| 2007 |
Li Q, Ye K, Blad CC, den Dulk H, Brouwer J, Ijzerman AP, Beukers MW. ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor. The Journal of Pharmacology and Experimental Therapeutics. 320: 637-45. PMID 17077318 DOI: 10.1124/jpet.106.111203 |
1 |
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| 2006 |
Beukers MW, Meurs I, Ijzerman AP. Structure-affinity relationships of adenosine A2B receptor ligands Medicinal Research Reviews. 26: 667-698. PMID 16847822 DOI: 10.1002/med.20069 |
1 |
|
| 2006 |
Samsonova EV, Kok JN, Ijzerman AP. TreeSOM: Cluster analysis in the self-organizing map. Neural Networks : the Official Journal of the International Neural Network Society. 19: 935-49. PMID 16781116 DOI: 10.1016/j.neunet.2006.05.003 |
1 |
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| 2006 |
Göblyös A, Gao ZG, Brussee J, Connestari R, Santiago SN, Ye K, Ijzerman AP, Jacobson KA. 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: 3354-61. PMID 16722654 DOI: 10.1021/jm060086s |
1 |
|
| 2006 |
Chang LCW, Spanjersberg RF, Von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Brussee J, Ijzerman AP. 2,6-Disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists Journal of Medicinal Chemistry. 49: 2861-2867. PMID 16686529 DOI: 10.1021/jm050640i |
1 |
|
| 2006 |
Kazius J, Nijssen S, Kok J, Bäck T, IJzerman AP. Substructure mining using elaborate chemical representation Journal of Chemical Information and Modeling. 46: 597-605. PMID 16562988 DOI: 10.1021/ci0503715 |
1 |
|
| 2006 |
Lameijer EW, Kok JN, Bäck T, Ijzerman AP. Mining a chemical database for fragment co-occurrence: discovery of "chemical clichés". Journal of Chemical Information and Modeling. 46: 553-62. PMID 16562983 DOI: 10.1021/ci050370c |
1 |
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| 2006 |
Lameijer EW, Kok JN, Bäck T, Ijzerman AP. The molecule evoluator. An interactive evolutionary algorithm for the design of drug-like molecules. Journal of Chemical Information and Modeling. 46: 545-52. PMID 16562982 DOI: 10.1021/ci050369d |
1 |
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| 2006 |
Ye K, Lameijer EWM, Beukers MW, Ijzerman AP. A two-entropies analysis to identify functional positions in the transmembrane region of class A G protein-coupled receptors Proteins: Structure, Function and Genetics. 63: 1018-1030. PMID 16532452 DOI: 10.1002/prot.20899 |
1 |
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| 2006 |
Heitman LH, Mulder-Krieger T, Spanjersberg RF, Von Frijtag Drabbe Künzel JK, Dalpiaz A, Ijzerman AP. Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A 1 receptors of LUF5831, a novel nonadenosine-like agonist British Journal of Pharmacology. 147: 533-541. PMID 16444290 DOI: 10.1038/sj.bjp.0706655 |
1 |
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| 2006 |
Bond RA, Ijzerman AP. Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery. Trends in Pharmacological Sciences. 27: 92-6. PMID 16406086 DOI: 10.1016/j.tips.2005.12.007 |
1 |
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| 2006 |
Rozenfeld R, Décaillot FM, IJzerman AP, Devi LA. Heterodimers of G protein-coupled receptors as novel and distinct drug targets Drug Discovery Today: Therapeutic Strategies. 3: 437-443. DOI: 10.1016/j.ddstr.2006.11.001 |
1 |
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| 2005 |
Klaasse EC, van den Hout G, Roerink SF, de Grip WJ, Ijzerman AP, Beukers MW. Allosteric modulators affect the internalization of human adenosine A1 receptors. European Journal of Pharmacology. 522: 1-8. PMID 16214128 DOI: 10.1016/j.ejphar.2005.08.052 |
1 |
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| 2005 |
Beukers MW, Ijzerman AP. Techniques: How to boost GPCR mutagenesis studies using yeast Trends in Pharmacological Sciences. 26: 533-539. PMID 16126284 DOI: 10.1016/j.tips.2005.08.005 |
1 |
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| 2005 |
Gao ZG, Kim SK, Ijzerman AP, Jacobson KA. Allosteric modulation of the adenosine family of receptors. Mini Reviews in Medicinal Chemistry. 5: 545-53. PMID 15974932 DOI: 10.2174/1389557054023242 |
1 |
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| 2005 |
Schaddelee MP, Collins SD, DeJongh J, de Boer AG, Ijzerman AP, Danhof M. Pharmacokinetic/pharmacodynamic modelling of the anti-hyperalgesic and anti-nociceptive effect of adenosine A1 receptor partial agonists in neuropathic pain. European Journal of Pharmacology. 514: 131-40. PMID 15910799 DOI: 10.1016/j.ejphar.2005.03.026 |
1 |
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| 2005 |
Soudijn W, Van Wijngaarden I, Ijzerman AP. Structure-activity relationships of inverse agonists for G-protein-coupled receptors Medicinal Research Reviews. 25: 398-426. PMID 15816047 DOI: 10.1002/med.20031 |
1 |
|
| 2005 |
Chang LCW, Von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Spanjersberg RF, Roerink SF, Van Den Hout G, Beukers MW, Brussee J, Ijzerman AP. A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor Journal of Medicinal Chemistry. 48: 2045-2053. PMID 15771447 DOI: 10.1021/jm049597+ |
1 |
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| 2005 |
de Ligt RA, Rivkees SA, Lorenzen A, Leurs R, IJzerman AP. A "locked-on," constitutively active mutant of the adenosine A1 receptor. European Journal of Pharmacology. 510: 1-8. PMID 15740718 DOI: 10.1016/j.ejphar.2005.01.007 |
1 |
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| 2005 |
Göblyös A, Santiago SN, Pietra D, Mulder-Krieger T, von Frijtag Drabbe Künzel J, Brussee J, Ijzerman AP. 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: 2079-87. PMID 15727861 DOI: 10.1016/j.bmc.2005.01.006 |
1 |
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| 2005 |
Göblyös A, De Vries H, Brussee J, Ijzerman AP. 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. PMID 15715480 DOI: 10.1021/jm049337s |
1 |
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| 2005 |
Tromp RA, Spanjersberg RF, Von Frijtag Drabbe Künzel JK, IJzerman AP. Inhibition of nucleoside transport proteins by C8-alkylamine- substituted purines Journal of Medicinal Chemistry. 48: 321-329. PMID 15634027 DOI: 10.1021/jm049303k |
1 |
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| 2005 |
Schaddelee MP, Read KD, Cleypool CGJ, Ijzerman AP, Danhof M, De Boer AG. Brain penetration of synthetic adenosine A 1 receptor agonists in situ: Role of the rENT1 nucleoside transporter and binding to blood constituents European Journal of Pharmaceutical Sciences. 24: 59-66. PMID 15626578 DOI: 10.1016/j.ejps.2004.09.010 |
1 |
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| 2005 |
Lameijer EW, Bäck T, Kok JN, Ijzerman AP. Evolutionary algorithms in drug design Natural Computing. 4: 177-243. DOI: 10.1007/s11047-004-5237-8 |
1 |
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| 2005 |
Samsonova EV, Bäck T, Kok JN, IJzerman AP. Reliable hierarchical clustering with the self-organizing map Lecture Notes in Computer Science (Including Subseries Lecture Notes in Artificial Intelligence and Lecture Notes in Bioinformatics). 3646: 385-396. |
1 |
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| 2005 |
Lameijer EW, Ijzerman AP, Kok JN. Using data mining to improve mutation in a tool for molecular evolution 2005 Ieee Congress On Evolutionary Computation, Ieee Cec 2005. Proceedings. 1: 314-321. |
1 |
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| 2004 |
Chang LCW, Brussee J, IJzerman AP. Non-xanthine antagonists for the adenosine A1 receptor Chemistry and Biodiversity. 1: 1591-1626. PMID 17191804 DOI: 10.1002/cbdv.200490122 |
1 |
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| 2004 |
Chang LCW, Spanjersberg RF, Von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Van Den Hout G, Beukers MW, Brussee J, IJzerman AP. 2,4,6-Trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists Journal of Medicinal Chemistry. 47: 6529-6540. PMID 15588088 DOI: 10.1021/jm049448r |
1 |
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| 2004 |
Schaddelee MP, Dejongh J, Collins SD, de Boer AG, Ijzerman AP, Danhof M. 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. PMID 15507215 DOI: 10.1016/j.ejphar.2004.09.029 |
1 |
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| 2004 |
Tromp RA, Van Ameijde S, Pütz C, Sundermann C, Sundermann B, Von Frijtag Drabbe Künzel JK, Ijzerman AP. Inhibition of nucleoside transport by new analogues of 4- nitrobenzylthioinosine: Replacement of the ribose moiety by substituted benzyl groups Journal of Medicinal Chemistry. 47: 5441-5450. PMID 15481982 DOI: 10.1021/jm049735v |
1 |
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| 2004 |
Soudijn W, Van Wijngaarden I, Ijzerman AP. Allosteric modulation of G protein-coupled receptors: Perspectives and recent developments Drug Discovery Today. 9: 752-758. PMID 15450241 DOI: 10.1016/S1359-6446(04)03220-9 |
1 |
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| 2004 |
Klaasse E, de Ligt RA, Roerink SF, Lorenzen A, Milligan G, Leurs R, IJzerman AP. Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits. European Journal of Pharmacology. 499: 91-8. PMID 15363955 DOI: 10.1016/j.ejphar.2004.07.108 |
1 |
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| 2004 |
Cordeaux Y, Ijzerman AP, Hill SJ. Coupling of the human A1 adenosine receptor to different heterotrimeric G proteins: evidence for agonist-specific G protein activation. British Journal of Pharmacology. 143: 705-14. PMID 15302686 DOI: 10.1038/sj.bjp.0705925 |
1 |
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| 2004 |
Schaddelee MP, Groenendaal D, DeJongh J, Cleypool CGJ, Ijzerman AP, De Boer AG, Danhof M. Population pharmacokinetic modeling of blood-brain barrier transport of synthetic adenosine A1 receptor agonists Journal of Pharmacology and Experimental Therapeutics. 311: 1138-1146. PMID 15292459 DOI: 10.1124/jpet.104.071308 |
1 |
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| 2004 |
Beukers MW, Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Spanjersberg RF, Brussee J, IJzerman AP. 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: 3707-9. PMID 15239649 DOI: 10.1021/jm049947s |
1 |
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| 2004 |
Wittendorp MC, von Frijtag Drabbe Künzel J, Ijzerman AP, Boddeke HW, Biber K. The mouse brain adenosine A1 receptor: functional expression and pharmacology. European Journal of Pharmacology. 487: 73-9. PMID 15033378 DOI: 10.1016/j.ejphar.2004.01.034 |
1 |
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| 2004 |
Beukers MW, van Oppenraaij J, van der Hoorn PP, Blad CC, den Dulk H, Brouwer J, IJzerman AP. 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: 702-10. PMID 14978249 DOI: 10.1124/mol.65.3.702 |
1 |
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| 2004 |
Van Den Nieuwendijk AMCH, Pietra D, Heitman L, Göblyös A, IJzerman AP. Synthesis and Biological Evaluation of 2,3,5-Substituted [1,2,4]Thiadiazoles as Allosteric Modulators of Adenosine Receptors Journal of Medicinal Chemistry. 47: 663-672. PMID 14736246 DOI: 10.1021/jm030863d |
1 |
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| 2004 |
de Ligt RA, van der Klein PA, von Frijtag Drabbe Künzel JK, Lorenzen A, Ait El Maate F, Fujikawa S, van Westhoven R, van den Hoven T, Brussee J, IJzerman AP. 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: 139-49. PMID 14697779 DOI: 10.1016/j.bmc.2003.10.023 |
1 |
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| 2004 |
Mathôt RAA, Van Den Aarsen BCFM, Von Frijtag Drabbe Künzel JK, Danhof M, IJzerman AP. Assessment of the enantiomeric purity of R- and S-N6-phenylisopropyladenosine (PIA): Implications for adenosine receptor subclassification Naunyn-Schmiedeberg's Archives of Pharmacology. 350: 109-112. PMID 7935848 DOI: 10.1007/BF00180020 |
1 |
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| 2004 |
IJzerman AP, Kruidering M, van Weert A, van Belle H, Janssen C. [3H]R75231 - a new radioligand for the nitrobenzylthioinosine sensitive nucleoside transport proteins Characterization of (±)-[3H]R75231 binding to calf lung membranes, stereospecificity of its two stereoisomers, and comparison with [3H]nitrobenzylthioinosine binding Naunyn-Schmiedeberg's Archives of Pharmacology. 345: 558-563. PMID 1528273 DOI: 10.1007/BF00168949 |
1 |
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| 2003 |
Bueters TJ, van Duivenvoorde LM, Danhof M, IJzerman AP, van Helden HP. Cyclopentyladenosine and some of its low-efficacy derivatives inhibit striatal synaptosomal release of acetylcholine to a similar degree. European Journal of Pharmacology. 481: 141-6. PMID 14642778 DOI: 10.1016/j.ejphar.2003.09.027 |
1 |
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| 2003 |
Schaddelee MP, Voorwinden HL, Groenendaal D, Hersey A, Ijzerman AP, Danhof M, De Boer AG. Blood-brain barrier transport of synthetic adenosine A1 receptor agonists in vitro: Structure transport relationships European Journal of Pharmaceutical Sciences. 20: 347-356. PMID 14592701 DOI: 10.1016/j.ejps.2003.08.003 |
1 |
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| 2003 |
Bueters TJ, IJzerman AP, van Helden HP, Danhof M. 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. PMID 14554106 DOI: 10.1016/S0041-008X(03)00252-7 |
1 |
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| 2003 |
van Herk T, Brussee J, van den Nieuwendijk AM, van der Klein PA, IJzerman AP, Stannek C, Burmeister A, Lorenzen A. Pyrazole derivatives as partial agonists for the nicotinic acid receptor. Journal of Medicinal Chemistry. 46: 3945-51. PMID 12930155 DOI: 10.1021/jm030888c |
1 |
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| 2003 |
Harrison PK, Bueters TJH, Ijzerman AP, Van Helden HPM, Tattersall JEH. Partial adenosine A1 receptor agonists inhibit sarin-induced epileptiform activity in the hippocampal slice European Journal of Pharmacology. 471: 97-104. PMID 12818696 DOI: 10.1016/S0014-2999(03)01783-7 |
1 |
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| 2003 |
Soudijn W, Van Wijngaarden I, IJzerman AP. Stereoselectivity of drug-receptor interactions Idrugs. 6: 43-56. PMID 12789621 |
1 |
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| 2003 |
Bueters TJH, Van Helden HPM, IJzerman AP, Danhof M. Low efficacy adenosine A1 agonists inhibit striatal acetylcholine release in rats improving central selectivity of action Neuroscience Letters. 343: 57-61. PMID 12749997 DOI: 10.1016/S0304-3940(03)00311-2 |
1 |
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| 2003 |
Schaddelee MP, Voorwinden HL, Van Tilburg EW, Pateman TJ, Ijzerman AP, Danhof M, De Boer AG. 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. PMID 12729857 DOI: 10.1016/S0928-0987(03)00034-4 |
1 |
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| 2003 |
van Tilburg EW, Gremmen M, von Frijtag Drabbe Künzel J, de Groote M, IJzerman AP. 2,8-Disubstituted adenosine derivatives as partial agonists for the adenosine A2A receptor. Bioorganic & Medicinal Chemistry. 11: 2183-92. PMID 12713828 DOI: 10.1016/S0968-0896(03)00123-8 |
1 |
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| 2003 |
Beukers MW, Wanner MJ, Von Frijtag Drabbe Künzel JK, Klaasse EC, IJzerman AP, Koomen GJ. 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: 1492-503. PMID 12672250 DOI: 10.1021/jm021074j |
1 |
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| 2003 |
Deghati PYF, Borghini A, Van Den Nieuwendijk AMCH, Dissen-de Groote M, IJzerman AP. Inhibition of nucleoside transport by new analogues of nitrobenzylthioinosine Bioorganic and Medicinal Chemistry. 11: 899-908. PMID 12614875 DOI: 10.1016/S0968-0896(02)00544-8 |
1 |
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| 2003 |
Bueters TJ, Joosen MJ, van Helden HP, Ijzerman AP, Danhof M. Adenosine A1 receptor agonist N6-cyclopentyladenosine affects the inactivation of acetylcholinesterase in blood and brain by sarin. The Journal of Pharmacology and Experimental Therapeutics. 304: 1307-13. PMID 12604711 DOI: 10.1124/jpet.102.044644 |
1 |
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| 2003 |
Soudijn W, van Wijngaarden I, IJzerman AP. Medicinal chemistry of adenosine A1 receptor ligands. Current Topics in Medicinal Chemistry. 3: 355-367. PMID 12570755 |
1 |
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| 2003 |
Gao ZG, Melman N, Erdmann A, Kim SG, Müller CE, IJzerman AP, Jacobson KA. Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors. Biochemical Pharmacology. 65: 525-34. PMID 12566079 DOI: 10.1016/S0006-2952(02)01556-3 |
1 |
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| 2003 |
Samsonova EV, Bäck T, Beukers MW, Ijzerman AP, Kok JN. Combining and comparing cluster methods in a receptor database Lecture Notes in Computer Science (Including Subseries Lecture Notes in Artificial Intelligence and Lecture Notes in Bioinformatics). 2810: 341-351. |
1 |
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| 2002 |
Soudijn W, van Wijngaarden I, IJzerman AP. Allosteric modulation of G protein-coupled receptors. Current Opinion in Drug Discovery & Development. 5: 749-55. PMID 12630295 |
1 |
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| 2002 |
Bueters TJ, van Helden HP, Danhof M, IJzerman AP. Effects of the adenosine A1 receptor allosteric modulators PD 81,723 and LUF 5484 on the striatal acetylcholine release. European Journal of Pharmacology. 454: 177-82. PMID 12421644 DOI: 10.1016/S0014-2999(02)02494-9 |
1 |
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| 2002 |
Bueters TJ, Groen B, Danhof M, IJzerman AP, Van Helden HP. Therapeutic efficacy of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) against organophosphate intoxication. Archives of Toxicology. 76: 650-6. PMID 12415428 DOI: 10.1007/s00204-002-0395-x |
1 |
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| 2002 |
de Ligt RA, IJzerman AP. Intrinsic activity at adenosine A1 receptors: partial and inverse agonism. Current Pharmaceutical Design. 8: 2333-44. PMID 12369948 DOI: 10.2174/1381612023392874 |
1 |
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| 2002 |
Lorenzen A, Beukers MW, van der Graaf PH, Lang H, van Muijlwijk-Koezen J, de Groote M, Menge W, Schwabe U, IJzerman AP. Modulation of agonist responses at the A(1) adenosine receptor by an irreversible antagonist, receptor-G protein uncoupling and by the G protein activation state. Biochemical Pharmacology. 64: 1251-65. PMID 12234606 DOI: 10.1016/S0006-2952(02)01293-5 |
1 |
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| 2002 |
Dalpiaz A, Pavan B, Ngos FN, Franchetti P, IJzerman AP. Temperature dependence of the affinity enhancement of selective adenosine A1 receptor agonism: A thermodynamic analysis European Journal of Pharmacology. 448: 123-131. PMID 12144931 DOI: 10.1016/S0014-2999(02)01982-9 |
1 |
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| 2002 |
Priego EM, von Frijtag Drabbe Kuenzel J, IJzerman AP, Camarasa MJ, Pérez-Pérez MJ. Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists. Journal of Medicinal Chemistry. 45: 3337-44. PMID 12139445 DOI: 10.1021/jm0208469 |
1 |
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| 2002 |
Gao ZG, Kim SG, Soltysiak KA, Melman N, IJzerman AP, Jacobson KA. Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives. Molecular Pharmacology. 62: 81-9. PMID 12065758 DOI: 10.1124/mol.62.1.81 |
1 |
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| 2002 |
Van Calenbergh S, Link A, Fujikawa S, De Ligt RAF, Vanheusden V, Golisade A, Blaton NM, Rozenski J, IJzerman AP, Herdewijn P. 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. PMID 11960496 DOI: 10.1021/jm0110439 |
1 |
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| 2002 |
Del Carmine R, Ambrosio C, Sbraccia M, Cotecchia S, Ijzerman AP, Costa T. Mutations inducing divergent shifts of constitutive activity reveal different modes of binding among catecholamine analogues to the β 2-adrenergic receptor British Journal of Pharmacology. 135: 1715-1722. PMID 11934812 DOI: 10.1038/sj.bjp.0704622 |
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| 2002 |
Schrier SM, Florea BI, Mulder GJ, Nagelkerke JF, IJzerman AP. Apoptosis induced by extracellular ATP in the mouse neuroblastoma cell line N1E-115: studies on involvement of P2 receptors and adenosine. Biochemical Pharmacology. 63: 1119-26. PMID 11931844 DOI: 10.1016/S0006-2952(01)00939-X |
1 |
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| 2002 |
den Haan JM, Mutis T, Blokland E, IJzerman AP, Goulmy E. General T-cell receptor antagonists to immunomodulate HLA-A2-restricted minor histocompatibility antigen HA-1-specific T-cell responses. Blood. 99: 985-92. PMID 11807003 DOI: 10.1182/blood.V99.3.985 |
1 |
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| 2002 |
van Tilburg EW, von Frijtag Drabbe Kunzel J, de Groote M, IJzerman AP. 2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor. Journal of Medicinal Chemistry. 45: 420-9. PMID 11784146 DOI: 10.1021/jm010952v |
1 |
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| 2001 |
van Muijlwijk-Koezen JE, Timmerman H, Ijzerman AP. The adenosine A3 receptor and its ligands. Progress in Medicinal Chemistry. 38: 61-113. PMID 11774799 DOI: 10.1016/S0079-6468(08)70092-4 |
1 |
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| 2001 |
van Muijlwijk-Koezen JE, Timmerman H, van der Sluis RP, van de Stolpe AC, Menge WM, Beukers MW, van der Graaf PH, de Groote M, IJzerman AP. Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool. Bioorganic & Medicinal Chemistry Letters. 11: 815-8. PMID 11277527 DOI: 10.1016/S0960-894X(01)00069-5 |
1 |
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| 2001 |
van Muijlwijk-Koezen JE, Timmerman H, Vollinga RC, Frijtag von Drabbe Künzel J, de Groote M, Visser S, IJzerman AP. Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists. Journal of Medicinal Chemistry. 44: 749-62. PMID 11262085 DOI: 10.1021/jm0003945 |
1 |
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| 2000 |
van Muijlwijk-Koezen JE, Timmerman H, van der Goot H, Menge WM, Frijtag Von Drabbe Künzel J, de Groote M, IJzerman AP. Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. Journal of Medicinal Chemistry. 43: 2227-38. PMID 10841801 |
1 |
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| 1998 |
van Muijlwijk-Koezen JE, Timmerman H, Link R, van der Goot H, Ijzerman AP. A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds. Journal of Medicinal Chemistry. 41: 3994-4000. PMID 9767637 DOI: 10.1021/jm980037i |
1 |
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| 1998 |
van Muijlwijk-Koezen JE, Timmerman H, Link R, van der Goot H, IJzerman AP. A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. Journal of Medicinal Chemistry. 41: 3987-93. PMID 9767636 DOI: 10.1021/jm980036q |
1 |
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| 1986 |
Ijzerman AP, Timmerman H. The beta-adrenoceptor-adenylate cyclase complex. From model to biochemical reality. Pharmaceutisch Weekblad. Scientific Edition. 8: 209-22. PMID 3020497 |
1 |
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| 1986 |
Ijzerman AP, Bultsma T, Timmerman H. 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: 93-105. PMID 3012726 |
1 |
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| 1986 |
Linschoten MR, Bultsma T, IJzerman AP, Timmerman H. Mapping the turkey erythrocyte beta receptor: a distance geometry approach. Journal of Medicinal Chemistry. 29: 278-86. PMID 3005570 |
1 |
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| 1986 |
IJzerman AP, Bultsma T, Timmerman H. Quantitative evaluation of the beta 2-adrenoceptor intrinsic activity of N-tert-butylphenylethanolamines. Journal of Medicinal Chemistry. 29: 549-54. PMID 2870189 |
1 |
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| 1985 |
IJzerman AP, Aué GH, Bultsma T, Linschoten MR, Timmerman H. Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines. Journal of Medicinal Chemistry. 28: 1328-34. PMID 2993621 |
1 |
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| 1985 |
Ijzerman AP, Dorlas R, Aué GH, Bultsma T, Timmerman H. Factors controlling beta 1-adrenoceptor affinity and selectivity. Biochemical Pharmacology. 34: 2883-90. PMID 2992521 |
1 |
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| 1984 |
Ijzerman AP, Bultsma T, Timmerman H, Zaagsma J. The ionization of beta-adrenoceptor agonists: a method for unravelling ionization schemes. The Journal of Pharmacy and Pharmacology. 36: 11-5. PMID 6141256 |
1 |
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| 1984 |
IJzerman AP, Bultsma T, Timmerman H, Zaagsma J. The relation between ionization and affinity of beta-adrenoceptor ligands. Naunyn-Schmiedeberg's Archives of Pharmacology. 327: 293-8. PMID 6096722 |
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