| Year |
Citation |
Score |
| 2024 |
Dudley MW, Peet NP, Demeter DA, Weintraub HJR, Ijzerman AP, Nordvall G, van Galen PJM, Jacobson KA. Adenosine A Receptor and Ligand Molecular Modeling. Drug Development Research. 28: 237-243. PMID 38239889 DOI: 10.1002/ddr.430280309 |
0.526 |
|
| 2024 |
Jacobson KA, IJzerman AP, Linden J. 1,3-Dialkylxanthine Derivatives Having High Potency as Antagonists at Human A Adenosine Receptors. Drug Development Research. 47: 45-53. PMID 38239816 DOI: 10.1002/(sici)1098-2299(199905)47:1<45::aid-ddr6>3.0.co;2-u |
0.505 |
|
| 2020 |
Burggraaff L, van Veen A, Lam CC, Van Vlijmen H, IJzerman AP, van Westen GJP. Annotation of Allosteric Compounds to Enhance Bioactivity Modeling for Class A GPCRs. Journal of Chemical Information and Modeling. PMID 32931270 DOI: 10.1021/acs.jcim.0c00695 |
0.675 |
|
| 2020 |
Yang X, Dilweg MA, Osemwengie D, Burggraaff L, van der Es D, Heitman LH, IJzerman AP. Design and Pharmacological Profile of a Novel Covalent Partial Agonist for the Adenosine A Receptor. Biochemical Pharmacology. 114144. PMID 32653590 DOI: 10.1016/j.bcp.2020.114144 |
0.411 |
|
| 2020 |
Wang X, Jespers W, Bongers BJ, Habben Jansen MCC, Stangenberger CM, Dilweg MA, Gutiérrez-de-Terán H, IJzerman AP, Heitman LH, van Westen GJP. Characterization of cancer-related somatic mutations in the adenosine A receptor. European Journal of Pharmacology. 173126. PMID 32348778 DOI: 10.1016/j.ejphar.2020.173126 |
0.31 |
|
| 2020 |
Burggraaff L, Lenselink EB, Jespers W, van Engelen J, Bongers BJ, Gorostiola González M, Liu R, Hoos HH, Van Vlijmen H, IJzerman AP, van Westen GJP. Successive Statistical and Structure-Based Modeling to Identify Chemically Novel Kinase Inhibitors. Journal of Chemical Information and Modeling. PMID 32343143 DOI: 10.1021/acs.jcim.9b01204 |
0.62 |
|
| 2019 |
Ortiz Zacarías NV, van Veldhoven JPD, den Hollander LS, Dogan B, Openy J, Hsiao YY, Lenselink EB, Heitman LH, IJzerman AP. Synthesis and pharmacological evaluation of triazolo-pyrimidinone derivatives as noncompetitive, intracellular antagonists for CC chemokine receptors 2 and 5. Journal of Medicinal Chemistry. PMID 31742400 DOI: 10.1021/acs.jmedchem.9b00742 |
0.379 |
|
| 2019 |
Massink A, Amelia T, Karamychev A, IJzerman AP. Allosteric modulation of G protein-coupled receptors by amiloride and its derivatives. Perspectives for drug discovery? Medicinal Research Reviews. 40: 683-708. PMID 31495942 DOI: 10.1002/med.21633 |
0.336 |
|
| 2019 |
Bouzo-Lorenzo M, Stoddart LA, Xia L, IJzerman AP, Heitman LH, Briddon SJ, Hill SJ. A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A receptor. Purinergic Signalling. PMID 30919204 DOI: 10.1007/S11302-019-09650-9 |
0.32 |
|
| 2019 |
Yun Y, Chen J, Liu R, Chen W, Liu C, Wang R, Hou Z, Yu Z, Sun Y, IJzerman AP, Heitman LH, Yin X, Guo D. Long residence time adenosine A receptor agonists produce sustained wash-resistant antilipolytic effect in rat adipocytes. Biochemical Pharmacology. PMID 30905656 DOI: 10.1016/j.bcp.2019.03.032 |
0.326 |
|
| 2019 |
Yang X, van Veldhoven JPD, Offringa J, Kuiper BJ, Lenselink EB, Heitman LH, van der Es D, IJzerman AP. Development of covalent ligands for G protein-coupled receptors: a case for the human adenosine A receptor. Journal of Medicinal Chemistry. PMID 30869893 DOI: 10.1021/acs.jmedchem.8b02026 |
0.419 |
|
| 2019 |
van der Putten C, Veth J, Sukurova L, Zuiderwijk-Sick EA, Simonetti E, Koenen HJPM, Burm SM, van Noort JM, IJzerman AP, van Hijum SAFT, Diavatopoulos D, Bajramovic JJ. TLR-Induced IL-12 and CCL2 Production by Myeloid Cells Is Dependent on Adenosine A Receptor-Mediated Signaling. Journal of Immunology (Baltimore, Md. : 1950). PMID 30804043 DOI: 10.4049/Jimmunol.1800618 |
0.311 |
|
| 2019 |
Fredholm BB, Frenguelli BG, Hills R, IJzerman AP, Jacobson KA, Klotz K, Linden J, Müller CE, Schwabe U, Stiles GL. Adenosine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database Iuphar/Bps Guide to Pharmacology Cite. 2019. DOI: 10.2218/gtopdb/f3/2019.4 |
0.517 |
|
| 2018 |
Ortiz Zacarías NV, van Veldhoven JPD, Portner L, van Spronsen E, Ullo S, Veenhuizen M, van der Velden WJC, Zweemer AJM, Kreekel RM, Oenema K, Lenselink EB, Heitman LH, IJzerman AP. 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: 9146-9161. PMID 30256641 DOI: 10.1021/acs.jmedchem.8b00605 |
0.382 |
|
| 2018 |
Yang X, Michiels TJM, de Jong C, Soethoudt M, Dekker N, Gordon E, van der Stelt M, Heitman LH, van der Es D, IJzerman AP. An Affinity-based Probe for the human Adenosine A Receptor. Journal of Medicinal Chemistry. PMID 30080404 DOI: 10.1021/acs.jmedchem.8b00860 |
0.353 |
|
| 2018 |
Ortiz Zacarías NV, Lenselink EB, IJzerman AP, Handel TM, Heitman LH. Intracellular Receptor Modulation: Novel Approach to Target GPCRs. Trends in Pharmacological Sciences. PMID 29653834 DOI: 10.1016/J.Tips.2018.03.002 |
0.373 |
|
| 2018 |
Doornbos MLJ, Van der Linden I, Vereyken L, Tresadern G, IJzerman AP, Lavreysen H, Heitman LH. Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor. Biochemical Pharmacology. PMID 29605627 DOI: 10.1016/j.bcp.2018.03.026 |
0.354 |
|
| 2018 |
Doornbos MLJ, Wang X, Vermond SC, Peeters L, Pérez-Benito L, Trabanco AA, Lavreysen H, Cid JM, Heitman LH, Tresadern G, IJzerman AP. A covalent allosteric probe for the metabotropic glutamate receptor 2: Design, synthesis and pharmacological characterization. Journal of Medicinal Chemistry. PMID 29494768 DOI: 10.1021/acs.jmedchem.8b00051 |
0.394 |
|
| 2018 |
Soethoudt M, Stolze SC, Westphal MV, van Stralen L, Martella A, van Rooden EJ, Guba W, Varga ZV, Deng H, van Kasteren SI, Grether U, IJzerman AP, Pacher P, Carreira EM, Overkleeft HS, et al. A selective photoaffinity probe enables assessment of cannabinoid CB2 receptor expression and ligand engagement in human cells. Journal of the American Chemical Society. PMID 29420021 DOI: 10.1021/Jacs.7B11281 |
0.307 |
|
| 2018 |
Xia L, Kyrizaki A, Tosh DK, van Duijl TT, Cornelia Roorda J, Jacobson KA, IJzerman AP, Heitman LH. A Binding Kinetics Study of Human Adenosine A3 Receptor Agonists. Biochemical Pharmacology. PMID 29305857 DOI: 10.1016/J.Bcp.2017.12.026 |
0.526 |
|
| 2018 |
Guo D, IJzerman AP. Molecular Basis of Ligand Dissociation from G Protein-Coupled Receptors and Predicting Residence Time. Methods in Molecular Biology (Clifton, N.J.). 1705: 197-206. PMID 29188564 DOI: 10.1007/978-1-4939-7465-8_9 |
0.342 |
|
| 2017 |
Du L, Gao ZG, Paoletta S, Wan TC, Gizewski ET, Barbour S, van Veldhoven JPD, IJzerman AP, Jacobson KA, Auchampach JA. Species differences and mechanism of action of A3 adenosine receptor allosteric modulators. Purinergic Signalling. PMID 29170977 DOI: 10.1007/S11302-017-9592-1 |
0.502 |
|
| 2017 |
Xia L, de Vries H, Lenselink EB, Louvel J, Waring MJ, Cheng L, Pahlén S, Petersson MJ, Schell P, Olsson RI, Heitman LH, Sheppard RJ, IJzerman AP. Structure-affinity Relationships and Structure-kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists. Journal of Medicinal Chemistry. PMID 29111736 DOI: 10.1021/Acs.Jmedchem.7B00861 |
0.407 |
|
| 2017 |
Xia L, de Vries H, Yang X, Lenselink EB, Kyrizaki A, Barth F, Louvel J, Dreyer M, van der Es D, IJzerman AP, Heitman LH. Kinetics of human Cannabinoid 1 (CB1) receptor antagonists: structure-kinetics relationships (SKRs) and implications for insurmountable antagonism. Biochemical Pharmacology. PMID 29102677 DOI: 10.1016/j.bcp.2017.10.014 |
0.369 |
|
| 2017 |
Xia L, Burger WAC, van Veldhoven JPD, Kuiper BJ, van Duijl TT, Lenselink EB, Paasman E, Heitman LH, IJzerman AP. Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists. Journal of Medicinal Chemistry. PMID 28806076 DOI: 10.1021/acs.jmedchem.7b00950 |
0.392 |
|
| 2017 |
Martella A, Sijben H, Rufer AC, Grether U, Fingerle J, Ullmer C, Hartung T, IJzerman AP, van der Stelt M, Heitman LH. A Novel Selective Inverse Agonist of the CB Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies. Molecular Pharmacology. 92: 389-400. PMID 28747489 DOI: 10.1124/mol.117.108605 |
0.323 |
|
| 2017 |
Schuetz DA, de Witte WEA, Wong YC, Knasmueller B, Richter L, Kokh DB, Sadiq SK, Bosma R, Nederpelt I, Segala E, Amaral M, Guo D, Andres D, Georgi V, Stoddart LA, ... ... IJzerman AP, et al. Kinetics for Drug Discovery: an industry-driven effort to target drug residence time. Drug Discovery Today. PMID 28412474 DOI: 10.1016/J.Drudis.2017.02.002 |
0.455 |
|
| 2017 |
Bot I, Ortiz Zacarías NV, de Witte WE, de Vries H, van Santbrink PJ, van der Velden D, Kröner MJ, van der Berg DJ, Stamos D, de Lange EC, Kuiper J, IJzerman AP, Heitman LH. A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy. Scientific Reports. 7: 52. PMID 28246398 DOI: 10.1038/s41598-017-00104-z |
0.316 |
|
| 2016 |
Lenselink EB, Louvel J, Forti AF, van Veldhoven JPD, de Vries H, Mulder-Krieger T, McRobb FM, Negri A, Goose J, Abel R, van Vlijmen HWT, Wang L, Harder E, Sherman W, IJzerman AP, et al. Predicting Binding Affinities for GPCR Ligands Using Free-Energy Perturbation. Acs Omega. 1: 293-304. PMID 30023478 DOI: 10.1021/acsomega.6b00086 |
0.365 |
|
| 2016 |
Zheng Y, Qin L, Zacarías NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, et al. Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists. Nature. PMID 27926736 DOI: 10.1038/Nature20605 |
0.375 |
|
| 2016 |
Yang X, Dong G, Michiels TJ, Lenselink EB, Heitman L, Louvel J, IJzerman AP. A covalent antagonist for the human adenosine A2A receptor. Purinergic Signalling. PMID 27915383 DOI: 10.1007/S11302-016-9549-9 |
0.505 |
|
| 2016 |
Hothersall JD, Guo D, Sarda S, Sheppard RJ, Chen H, Keur W, Waring MJ, IJzerman AP, Hill SJ, Dale IL, Rawlins P. Structure-activity relationships of the sustained effects of adenosine A2A receptor agonists driven by slow dissociation kinetics. Molecular Pharmacology. PMID 27803241 DOI: 10.1124/Mol.116.105551 |
0.37 |
|
| 2016 |
Nederpelt I, Bunnik J, IJzerman AP, Heitman LH. Kinetic Profile of Neuropeptide-Receptor Interactions. Trends in Neurosciences. 39: 830-839. PMID 27793433 DOI: 10.1016/j.tins.2016.09.008 |
0.319 |
|
| 2016 |
Paricharak S, Méndez-Lucio O, Chavan Ravindranath A, Bender A, IJzerman AP, van Westen GJ. Data-driven approaches used for compound library design, hit triage and bioactivity modeling in high-throughput screening. Briefings in Bioinformatics. PMID 27789427 DOI: 10.1093/Bib/Bbw105 |
0.745 |
|
| 2016 |
Alachouzos G, Lenselink EB, Mulder-Krieger T, de Vries H, IJzerman AP, Louvel J. Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A receptor antagonists. European Journal of Medicinal Chemistry. 125: 586-602. PMID 27718474 DOI: 10.1016/j.ejmech.2016.09.081 |
0.323 |
|
| 2016 |
Guo D, Heitman LH, IJzerman AP. The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery. Acs Medicinal Chemistry Letters. 7: 819-21. PMID 27660682 DOI: 10.1021/acsmedchemlett.6b00273 |
0.32 |
|
| 2016 |
Lenselink EB, Beuming T, van Veen C, Massink A, Sherman W, van Vlijmen HW, IJzerman AP. In search of novel ligands using a structure-based approach: a case study on the adenosine A2A receptor. Journal of Computer-Aided Molecular Design. PMID 27629350 DOI: 10.1007/S10822-016-9963-7 |
0.716 |
|
| 2016 |
Lenselink EB, Jespers W, van Vlijmen HW, IJzerman AP, van Westen GJ. Interacting with GPCRs: Using Interaction Fingerprints for Virtual Screening. Journal of Chemical Information and Modeling. 56: 2053-2060. PMID 27626908 DOI: 10.1021/acs.jcim.6b00314 |
0.805 |
|
| 2016 |
Paricharak S, IJzerman AP, Jenkins JL, Bender A, Nigsch F. Data-driven Derivation of an "Informer Compound Set" for Improved Selection of Active Compounds in High-Throughput Screening. Journal of Chemical Information and Modeling. PMID 27487177 DOI: 10.1021/Acs.Jcim.6B00244 |
0.475 |
|
| 2016 |
Guo D, Heitman LH, IJzerman AP. Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors. Chemical Reviews. PMID 27088232 DOI: 10.1021/acs.chemrev.6b00025 |
0.414 |
|
| 2016 |
Liu R, Wong W, IJzerman AP. Human G protein-coupled receptor studies in Saccharomyces cerevisiae. Biochemical Pharmacology. PMID 26920251 DOI: 10.1016/j.bcp.2016.02.010 |
0.326 |
|
| 2016 |
Paricharak S, IJzerman AP, Bender A, Nigsch F. Analysis of Iterative Screening with Stepwise Compound Selection Based on Novartis In-house HTS Data. Acs Chemical Biology. 11: 1255-64. PMID 26878899 DOI: 10.1021/Acschembio.6B00029 |
0.462 |
|
| 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 |
0.392 |
|
| 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 |
0.333 |
|
| 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 |
0.45 |
|
| 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 |
0.313 |
|
| 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 |
0.324 |
|
| 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 |
0.392 |
|
| 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. PMID 26141910 DOI: 10.1016/j.ejmech.2015.06.041 |
0.316 |
|
| 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 |
0.33 |
|
| 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 |
0.491 |
|
| 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 |
0.315 |
|
| 2015 |
Li P, Rial D, Canas PM, Yoo JH, Li W, Zhou X, Wang Y, van Westen GJ, Payen MP, Augusto E, Gonçalves N, Tomé AR, Li Z, Wu Z, Hou X, et al. Optogenetic activation of intracellular adenosine A2A receptor signaling in the hippocampus is sufficient to trigger CREB phosphorylation and impair memory. Molecular Psychiatry. PMID 25687775 DOI: 10.1038/mp.2014.182 |
0.695 |
|
| 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 |
0.376 |
|
| 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 |
0.306 |
|
| 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 |
0.472 |
|
| 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 |
0.306 |
|
| 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 |
0.302 |
|
| 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 |
0.398 |
|
| 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 |
0.35 |
|
| 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 |
0.759 |
|
| 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 |
0.369 |
|
| 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 |
0.324 |
|
| 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 |
0.628 |
|
| 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 |
0.396 |
|
| 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 |
0.412 |
|
| 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 |
0.4 |
|
| 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 |
0.482 |
|
| 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 |
0.321 |
|
| 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 |
0.767 |
|
| 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 |
0.76 |
|
| 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 |
0.347 |
|
| 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 |
0.318 |
|
| 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 |
0.6 |
|
| 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 |
0.703 |
|
| 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 |
0.766 |
|
| 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 |
0.354 |
|
| 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 |
0.363 |
|
| 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 |
0.371 |
|
| 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 |
0.817 |
|
| 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 |
0.594 |
|
| 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 |
0.691 |
|
| 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 |
0.476 |
|
| 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 |
0.314 |
|
| 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 |
0.38 |
|
| 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 |
0.352 |
|
| 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 |
0.774 |
|
| 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 |
0.379 |
|
| 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 |
0.771 |
|
| 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 |
0.778 |
|
| 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 |
0.552 |
|
| 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 |
0.459 |
|
| 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 |
0.439 |
|
| 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 |
0.513 |
|
| 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 |
0.415 |
|
| 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 |
0.46 |
|
| 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 |
0.781 |
|
| 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 |
0.367 |
|
| 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 |
0.397 |
|
| 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 |
0.524 |
|
| 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 |
0.31 |
|
| 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 |
0.454 |
|
| 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 |
0.758 |
|
| 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 |
0.498 |
|
| 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 |
0.507 |
|
| 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 |
0.348 |
|
| 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 |
0.327 |
|
| 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 |
0.75 |
|
| 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 |
0.491 |
|
| 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 |
0.391 |
|
| 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 |
0.39 |
|
| 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 |
0.775 |
|
| 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 |
0.392 |
|
| 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 |
0.442 |
|
| 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 |
0.424 |
|
| 2010 |
van der Eelke H, Kruisselbrink J, Aleman A, Emmerich M, Bender A, IJzerman A. Evolutionary design of selective adenosine receptor ligands Journal of Cheminformatics. 2. DOI: 10.1186/1758-2946-2-S1-P48 |
0.577 |
|
| 2010 |
Van Westen GJ, Wegner J, IJzerman A, Van Vlijmen H, Bender A. Molecular bioactivity extrapolation to novel targets by support vector machines Journal of Cheminformatics. 2. DOI: 10.1186/1758-2946-2-S1-O3 |
0.504 |
|
| 2010 |
van Muijlwijk-Koezen JE, Timmerman H, van der Sluis RP, van de Stolpe AC, Menge WMPB, Beukers MW, van der Graaf PH, de Groote M, IJzerman AP. ChemInform Abstract: Synthesis and Use of FSCPX, an Irreversible Adenosine A1 Antagonist, as a “Receptor Knock-Down” Tool. Cheminform. 32: no-no. DOI: 10.1002/chin.200128214 |
0.43 |
|
| 2010 |
van Muijilwijk-Koezen JE, Timmerman H, Vollinga RC, Frijtag von Drabbe Kuenzel J, de Groote M, Visser S, IJzerman AP. ChemInform Abstract: Thiazole and Thiadiazole Analogues as a Novel Class of Adenosine Receptor Antagonists. Cheminform. 32: no-no. DOI: 10.1002/chin.200124137 |
0.334 |
|
| 2010 |
VAN MUIJLWIJK-KOEZEN JE, TIMMERMAN H, LINK R, VAN DER GOOT H, IJZERMAN AP. ChemInform Abstract: A Novel Class of Adenosine A3 Receptor Ligands. Part 2. Structure Affinity Profile of a Series of Isoquinoline and Quinazoline Compounds. Cheminform. 30: no-no. DOI: 10.1002/chin.199911156 |
0.365 |
|
| 2010 |
VAN MUIJLWIJK-KOEZEN JE, TIMMERMAN H, LINK R, VAN DER GOOT H, IJZERMAN AP. ChemInform Abstract: A Novel Class of Adenosine A3 Receptor Ligands. Part 1. 3-(2-Pyridinyl)isoquinoline Derivatives. Cheminform. 30: no-no. DOI: 10.1002/chin.199911155 |
0.328 |
|
| 2010 |
DE ZWART M, LINK R, VON FRIJTAG DRABBE KUENZEL JK, CRISTALLI G, JACOBSON KA, TOWNSEND-NICHOLSON A, IJZERMAN AP. ChemInform Abstract: A Functional Screening of Adenosine Analogues at the Adenosine A2B Receptor: A Search for Potent Agonists. Cheminform. 29: no-no. DOI: 10.1002/chin.199837252 |
0.49 |
|
| 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 |
0.369 |
|
| 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 |
0.572 |
|
| 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 |
0.384 |
|
| 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 |
0.485 |
|
| 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 |
0.418 |
|
| 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 |
0.305 |
|
| 2009 |
Göblyös A, Ijzerman AP. Allosteric modulation of adenosine receptors. Purinergic Signalling. 5: 51-61. PMID 18615273 DOI: 10.1007/S11302-008-9105-3 |
0.491 |
|
| 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 |
0.533 |
|
| 2009 |
Emmerich M, Lee B, Bender A, Faddiev E, Kruisselbrink J, Deutz A, Horst Evd, IJzerman A, Bäck T. Analyzing molecular landscapes using random walks and information theory Chemistry Central Journal. 3. DOI: 10.1186/1752-153X-3-S1-P20 |
0.429 |
|
| 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.V2:3 |
0.41 |
|
| 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 |
0.48 |
|
| 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 |
0.39 |
|
| 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 |
0.374 |
|
| 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 |
0.365 |
|
| 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 |
0.384 |
|
| 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 |
0.461 |
|
| 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 |
0.384 |
|
| 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 |
0.317 |
|
| 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 |
0.357 |
|
| 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 |
0.375 |
|
| 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 |
0.349 |
|
| 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 |
0.492 |
|
| 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 |
0.348 |
|
| 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 |
0.402 |
|
| 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 |
0.459 |
|
| 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/chin.200647254 |
0.38 |
|
| 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 |
0.519 |
|
| 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 |
0.364 |
|
| 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 |
0.381 |
|
| 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 |
0.474 |
|
| 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 |
0.338 |
|
| 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 |
0.434 |
|
| 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 |
0.358 |
|
| 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 |
0.47 |
|
| 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 |
0.314 |
|
| 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+ |
0.406 |
|
| 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 |
0.607 |
|
| 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 |
0.374 |
|
| 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 |
0.338 |
|
| 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 |
0.432 |
|
| 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 |
0.589 |
|
| 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 |
0.326 |
|
| 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 |
0.464 |
|
| 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 |
0.362 |
|
| 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 |
0.325 |
|
| 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 |
0.365 |
|
| 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 |
0.467 |
|
| 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 |
0.377 |
|
| 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 |
0.313 |
|
| 2003 |
Soudijn W, Van Wijngaarden I, IJzerman AP. Stereoselectivity of drug-receptor interactions Idrugs. 6: 43-56. PMID 12789621 |
0.37 |
|
| 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 |
0.467 |
|
| 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 |
0.364 |
|
| 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 DOI: 10.2174/1568026033392165 |
0.48 |
|
| 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 |
0.521 |
|
| 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 |
0.375 |
|
| 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 |
0.339 |
|
| 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 |
0.322 |
|
| 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 |
0.484 |
|
| 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 |
0.335 |
|
| 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 |
0.302 |
|
| 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 |
0.424 |
|
| 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 |
0.514 |
|
| 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 |
0.357 |
|
| 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 |
0.316 |
|
| 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 |
0.326 |
|
| 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 |
0.46 |
|
| 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 |
0.567 |
|
| 2001 |
van Tilburg EW, van der Klein PA, von Frijtag Drabbe Künzel J, de Groote M, Stannek C, Lorenzen A, IJzerman AP. 5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors. Journal of Medicinal Chemistry. 44: 2966-75. PMID 11520205 DOI: 10.1021/Jm001114O |
0.422 |
|
| 2001 |
van Tilburg EW, van der Klein PA, de Groote M, Beukers MW, IJzerman AP. Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor. Bioorganic & Medicinal Chemistry Letters. 11: 2017-9. PMID 11454470 DOI: 10.1016/S0960-894X(01)00356-0 |
0.368 |
|
| 2001 |
Ijzerman A, Kourounakis A, van der Klein P. Allosteric modulation of G protein-coupled receptors. Farmaco (Societa Chimica Italiana : 1989). 56: 67-70. PMID 11347969 DOI: 10.1016/S0014-827X(01)01015-1 |
0.443 |
|
| 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 |
0.513 |
|
| 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 |
0.584 |
|
| 2001 |
Schrier SM, van Tilburg EW, van der Meulen H, Ijzerman AP, Mulder GJ, Nagelkerke JF. Extracellular adenosine-induced apoptosis in mouse neuroblastoma cells: studies on involvement of adenosine receptors and adenosine uptake. Biochemical Pharmacology. 61: 417-25. PMID 11226375 DOI: 10.1016/S0006-2952(00)00573-6 |
0.356 |
|
| 2001 |
Kourounakis A, Visser C, de Groote M, IJzerman AP. 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 A1 receptor. Biochemical Pharmacology. 61: 137-44. PMID 11163328 DOI: 10.1016/S0006-2952(00)00536-0 |
0.385 |
|
| 2001 |
Soudijn W, Van Wijhngaarden I, Ijzerman AP. Allosteric modulation of G-protein-coupled receptors Expert Opinion On Therapeutic Patents. 11: 1889-1904. DOI: 10.1517/13543776.11.12.1889 |
0.458 |
|
| 2001 |
Gao Z, Van Muijlwijk-Koezen JE, Chen A, Müller CE, Ijzerman AP, Jacobson KA. Allosteric Modulation of A3 Adenosine Receptors by a Series of 3-(2-Pyridinyl)isoquinoline Derivatives Molecular Pharmacology. 60: 1057-1063. DOI: 10.1124/Mol.60.5.1057 |
0.543 |
|
| 2000 |
Schier SM, Ijzerman AP, Mulder GJ, Nagelkerke JF. Adenosine-induced caspase activity in N1E-115 cells. Advances in Experimental Medicine and Biology. 486: 223-6. PMID 11783488 DOI: 10.1007/0-306-46843-3_44 |
0.317 |
|
| 2000 |
Beukers MW, Den Dulk H, Van Tilburg EW, Brouwer J, Ijzerman AP. Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-hexynyl)adenosine Molecular Pharmacology. 58: 1349-1356. PMID 11093773 DOI: 10.1124/Mol.58.6.1349 |
0.378 |
|
| 2000 |
Wanner MJ, Von Frijtag Drabbe Künzel JK, Ijzerman AP, Koomen GJ. 2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes. Bioorganic & Medicinal Chemistry Letters. 10: 2141-4. PMID 10999489 DOI: 10.1016/S0960-894X(00)00415-7 |
0.407 |
|
| 2000 |
Garrido M, Gubbens-Stibbe J, Tukker E, Cox E, von Frijtag J, Künzel D, IJzerman A, Danhof M, van der Graaf PH. Pharmacokinetic-pharmacodynamic analysis of the EEG effect of alfentanil in rats following beta-funaltrexamine-induced mu-opioid receptor "knockdown" in vivo. Pharmaceutical Research. 17: 653-9. PMID 10955836 DOI: 10.1023/A:1007513812018 |
0.317 |
|
| 2000 |
Gao ZG, Jiang Q, Jacobson KA, Ijzerman AP. 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: 661-8. PMID 10927024 DOI: 10.1016/S0006-2952(00)00357-9 |
0.517 |
|
| 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 DOI: 10.1021/Jm000002U |
0.561 |
|
| 2000 |
de Ligt RA, Kourounakis AP, IJzerman AP. Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery. British Journal of Pharmacology. 130: 1-12. PMID 10780991 DOI: 10.1038/Sj.Bjp.0703311 |
0.496 |
|
| 2000 |
Vittori S, Lorenzen A, Stannek C, Costanzi S, Volpini R, IJzerman AP, Kunzel JK, Cristalli G. N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor. Journal of Medicinal Chemistry. 43: 250-60. PMID 10649980 DOI: 10.1021/Jm9911231 |
0.402 |
|
| 2000 |
Kourounakis AP, Visser C, de Groote M, IJzerman AP. Allosteric modulation of the rat adenosine A1 receptor: Differential effects on agonist and antagonist binding Drug Development Research. 51: 207-215. DOI: 10.1002/Ddr.1 |
0.44 |
|
| 2000 |
van Muijlwijk-Koezen JE, Timmerman H, van der Goot H, Menge WMPB, Frijtag von Drabbe Kuenzel J, de Groote M, Ijzerman AP. ChemInform Abstract: Isoquinoline and Quinazoline Urea Analogues as Antagonists for the Human Adenosine A3 Receptor. Cheminform. 31: no-no. DOI: 10.1002/chin.200037161 |
0.515 |
|
| 2000 |
Kourounakis AP, Van der Klein PA, Ijzerman AP. Elucidation of structure-activity relationships of 2-amino-3-benzoylthiophenes: Study of their allosteric enhancing vs. antagonistic activity on adenosine A1 receptors Drug Development Research. 49: 227-237. DOI: 10.1002/1098-2299(200004)49:4<227::Aid-Ddr1>3.0.Co;2-1 |
0.462 |
|
| 2000 |
de Zwart M, de Groote M, van der Klein PA, van Dun S, Bronsing R, von Frijtag Drabbe K�nzel JK, Ijzerman AP. Phenyl-substituted N6-phenyladenosines and N6-phenyl-5?-N-ethylcarboxamidoadenosines with high activity at human adenosine A2B receptors Drug Development Research. 49: 85-93. DOI: 10.1002/(Sici)1098-2299(200002)49:2<85::Aid-Ddr2>3.0.Co;2-W |
0.387 |
|
| 1999 |
Zuurmond HM, Hessling J, Blüml K, Lohse M, Ijzerman AP. Study of interaction between agonists and Asn293 in helix VI of human β2-adrenergic receptor Molecular Pharmacology. 56: 909-916. PMID 10531394 DOI: 10.1124/Mol.56.5.909 |
0.349 |
|
| 1999 |
van der Klein PA, Kourounakis AP, IJzerman AP. 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: 3629-35. PMID 10479294 DOI: 10.1021/Jm991051D |
0.491 |
|
| 1999 |
Dalpiaz A, Scatturin A, Pavan B, Varani K, IJzerman AP, Andrea Borea P. Thermodynamic in vitro studies as a method to investigate the pharmacodynamic behavior of adenosine A1 receptor ligands. Pharmaceutical Research. 16: 1054-8. PMID 10450930 DOI: 10.1023/A:1018987816891 |
0.327 |
|
| 1999 |
Ingkaninan K, von Frijtag Drabbe Künzel JK, IJzerman AP, Verpoorte R. Interference of linoleic acid fraction in some receptor binding assays. Journal of Natural Products. 62: 912-4. PMID 10395519 DOI: 10.1021/Np9805490 |
0.301 |
|
| 1999 |
van Tilburg EW, von Frijtag Drabbe Künzel J, de Groote M, Vollinga RC, Lorenzen A, IJzerman AP. N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor. Journal of Medicinal Chemistry. 42: 1393-400. PMID 10212125 DOI: 10.1021/jm981090+ |
0.324 |
|
| 1999 |
de Zwart M, Kourounakis A, Kooijman H, Spek AL, Link R, von Frijtag Drabbe Künzel JK, IJzerman AP. 5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. Journal of Medicinal Chemistry. 42: 1384-92. PMID 10212124 DOI: 10.1021/jm9804984 |
0.368 |
|
| 1999 |
Rivkees SA, Barbhaiya H, IJzerman AP. Identification of the adenine binding site of the human A1 adenosine receptor. The Journal of Biological Chemistry. 274: 3617-21. PMID 9920910 DOI: 10.1074/jbc.274.6.3617 |
0.342 |
|
| 1999 |
Schwartz TW, IJzerman AP. Principles of agonism: undressing efficacy. Trends in Pharmacological Sciences. 19: 433-6. PMID 9850604 DOI: 10.1016/S0165-6147(98)01262-0 |
0.416 |
|
| 1999 |
de Zwart M, Vollinga RC, Beukers MW, Sleegers DF, von Frijtag Drabbe K�nzel JK, de Groote M, Ijzerman AP. Potent antagonists for the human adenosine A2B receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity Drug Development Research. 48: 95-103. DOI: 10.1002/(Sici)1098-2299(199911)48:3<95::Aid-Ddr1>3.0.Co;2-B |
0.484 |
|
| 1999 |
Jacobson KA, Ijzerman AP, Linden J. 1,3-dialkylxanthine derivatives having high potency as antagonists at human A2B adenosine receptors Drug Development Research. 47: 45-53. DOI: 10.1002/(Sici)1098-2299(199905)47:1<45::Aid-Ddr6>3.0.Co;2-U |
0.567 |
|
| 1998 |
Dalpiaz A, Townsend-Nicholson A, Beukers MW, Schofield PR, IJzerman AP. Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors. Biochemical Pharmacology. 56: 1437-45. PMID 9827575 DOI: 10.1016/S0006-2952(98)00202-0 |
0.363 |
|
| 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 |
0.566 |
|
| 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 |
0.549 |
|
| 1998 |
de Zwart M, Link R, von Frijtag Drabbe Künzel JK, Cristalli G, Jacobson KA, Townsend-Nicholson A, IJzerman AP. A functional screening of adenosine analogues at the adenosine A2B receptor: a search for potent agonists. Nucleosides & Nucleotides. 17: 969-85. PMID 9708319 DOI: 10.1080/07328319808004215 |
0.471 |
|
| 1998 |
Kim YC, de Zwart M, Chang L, Moro S, von Frijtag Drabbe Künzel JK, Melman N, IJzerman AP, Jacobson KA. Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. Journal of Medicinal Chemistry. 41: 2835-45. PMID 9667972 DOI: 10.1021/Jm980094B |
0.5 |
|
| 1998 |
van der Wenden EM, Carnielli M, Roelen HC, Lorenzen A, von Frijtag Drabbe Künzel JK, IJzerman AP. 5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor. Journal of Medicinal Chemistry. 41: 102-8. PMID 9438026 DOI: 10.1021/jm970508l |
0.362 |
|
| 1998 |
Van Calenbergh S, IJzerman AP, Herdewijn P. 3′-Amidated 3′-Deoxyxylofuranose Analogues of N 6-−Cyclopentyladenosines: a New Class of Non-Xanthine Antagonists at the Adenosine A1 Receptor. Nucleosides and Nucleotides. 17: 1571-1576. DOI: 10.1080/07328319808004688 |
0.317 |
|
| 1997 |
Van Calenbergh S, von Frijtag Drabbe Künzel JK, Blaton NM, Peeters OM, Rozenski J, Van Aerschot A, De Bruyn A, De Keukeleire D, IJzerman AP, Herdewijn P. N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists. Journal of Medicinal Chemistry. 40: 3765-72. PMID 9371242 DOI: 10.1021/Jm970176K |
0.328 |
|
| 1997 |
Lorenzen A, Sebastião AM, Sellink A, Vogt H, Schwabe U, Ribeiro JA, IJzerman AP. Biological activities of N6,C8-disubstituted adenosine derivatives as partial agonists at rat brain adenosine A1 receptors. European Journal of Pharmacology. 334: 299-307. PMID 9369361 DOI: 10.1016/S0014-2999(97)01193-X |
0.303 |
|
| 1997 |
Smeets RL, IJzerman AP, Hermsen HP, Ophorst OJ, Van Emst-de Vries SE, De Pont JJ, Willems PH. Mutational analysis of the putative devazepide binding site of the CCK(A) receptor. European Journal of Pharmacology. 325: 93-9. PMID 9151944 DOI: 10.1016/S0014-2999(97)00106-4 |
0.339 |
|
| 1997 |
Kuipers W, Link R, Standaar PJ, Stoit AR, Van Wijngaarden I, Leurs R, Ijzerman AP. Study of the interaction between aryloxypropanolamines and Asn386 in helix VII of the human 5-hydroxytryptamine1A receptor. Molecular Pharmacology. 51: 889-96. PMID 9145928 DOI: 10.1124/mol.51.5.889 |
0.548 |
|
| 1997 |
Kuipers W, Kruse CG, van Wijngaarden I, Standaar PJ, Tulp MT, Veldman N, Spek AL, IJzerman AP. 5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines. Journal of Medicinal Chemistry. 40: 300-12. PMID 9022796 DOI: 10.1021/Jm960496O |
0.329 |
|
| 1997 |
IJzerman AP, Von Frijtag Drabbe Künzel JK, Kim J, Jiang Q, Jacobson KA. Site-directed mutagenesis of the human adenosine A2A receptor. Critical involvement of Glu13 in agonist recognition. European Journal of Pharmacology. 310: 269-72. PMID 8884226 DOI: 10.1016/0014-2999(96)00495-5 |
0.571 |
|
| 1997 |
Van Schaick EA, Jacobson KA, Kim HO, IJzerman AP, Danhof M. Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats. European Journal of Pharmacology. 308: 311-4. PMID 8858305 DOI: 10.1016/S0928-0987(97)86249-5 |
0.433 |
|
| 1996 |
Wieland K, Zuurmond HM, Krasel C, Ijzerman AP, Lohse MJ. Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor. Proceedings of the National Academy of Sciences of the United States of America. 93: 9276-81. PMID 8799191 DOI: 10.1073/Pnas.93.17.9276 |
0.389 |
|
| 1996 |
Mathoôt RA, Soudijn W, Breimer DD, Ijzerman AP, Danhof M. Pharmacokinetic-haemodynamic relationships of 2-chloroadenosine at adenosine A1 and A2a receptors in vivo. British Journal of Pharmacology. 118: 369-77. PMID 8735640 DOI: 10.1111/J.1476-5381.1996.Tb15412.X |
0.301 |
|
| 1996 |
Roelen H, Veldman N, Spek AL, von Frijtag Drabbe Künzel J, Mathôt RA, IJzerman AP. N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors. Journal of Medicinal Chemistry. 39: 1463-71. PMID 8691477 DOI: 10.1021/jm950267m |
0.304 |
|
| 1995 |
Mathot RAA, Van der Wenden EM, Soudijn W, IJzerman AP, Danhof M. Deoxyribose analogues of N6-cyclopentyladenosine (CPA): Partial agonists at the adenosine A1 receptor in vivo British Journal of Pharmacology. 116: 1957-1964. PMID 8640332 DOI: 10.1111/J.1476-5381.1995.Tb16398.X |
0.313 |
|
| 1995 |
Crack BE, Beukers MW, McKechnie KC, Ijzerman AP, Leff P. Pharmacological analysis of ecto-ATPase inhibition: evidence for combined enzyme inhibition and receptor antagonism in P2X-purinoceptor ligands. British Journal of Pharmacology. 113: 1432-8. PMID 7889301 DOI: 10.1111/j.1476-5381.1994.tb17157.x |
0.303 |
|
| 1995 |
Kuipers W, van Wijngaarden I, Kruse CG, ter Horst-van Amstel M, Tulp MT, IJzerman AP. N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands. Journal of Medicinal Chemistry. 38: 1942-54. PMID 7783126 DOI: 10.1021/jm00011a014 |
0.361 |
|
| 1995 |
van der Wenden EM, Price SL, Apaya RP, IJzerman AP, Soudijn W. Relative binding orientations of adenosine A1 receptor ligands--a test case for Distributed Multipole Analysis in medicinal chemistry. Journal of Computer-Aided Molecular Design. 9: 44-54. PMID 7751869 DOI: 10.1007/Bf00117277 |
0.327 |
|
| 1995 |
IJzerman AP, van der Wenden EM, von Frijtag Drabbe Künzel JK, Mathôt RA, Danhof M, Borea PA, Varani K. Partial agonism of theophylline-7-riboside on adenosine receptors. Naunyn-Schmiedeberg's Archives of Pharmacology. 350: 638-45. PMID 7708121 DOI: 10.1007/BF00169369 |
0.343 |
|
| 1995 |
Van der Werten EM, Hartog-Witte HR, Roelen HCPF, von Frijtag Drabbe Künzel JK, Pirovano IM, Mathôt RAA, Danhof M, Van Aerschot A, Lidaks MJ, Ijzerman AP, Soudijn W. 8-substituted adenosine and theophylline-7-riboside analogues as potential partial agonists for the adenosine A1 receptor European Journal of Pharmacology: Molecular Pharmacology. 290: 189-199. PMID 7589213 DOI: 10.1016/0922-4106(95)00064-X |
0.343 |
|
| 1995 |
Appel S, Mathôt RA, Langemeijer MW, IJzerman AP, Danhof M. Modelling of the pharmacodynamic interaction of an A1 adenosine receptor agonist and antagonist in vivo: N6-cyclopentyladenosine and 8-cyclopentyltheophylline. British Journal of Pharmacology. 115: 1253-9. PMID 7582553 DOI: 10.1111/j.1476-5381.1995.tb15033.x |
0.308 |
|
| 1995 |
Van der Wenden EM, Von Frijtag Drabbe Kunzel JK, Mathot RAA, Danhof M, Ijzerman AP, Soudijn W. Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor Journal of Medicinal Chemistry. 38: 4000-4006. PMID 7562934 DOI: 10.1021/jm00020a014 |
0.311 |
|
| 1995 |
Verheggen I, Van Aerschot A, Pillet N, van der Wenden EM, Ijzerman A, Herdewijn P. Synthesis of 1,5-Anhydro-2-(N6-Cyclopentyladenin-9-Yl)-2-Deoxy-D-Altrohexitol Nucleosides, Nucleotides and Nucleic Acids. 14: 321-324. DOI: 10.1080/15257779508012372 |
0.38 |
|
| 1994 |
Borea PA, Varani K, Dalpiaz A, Capuzzo A, Fabbri E, IJzerman AP. Full and partial agonistic behaviour and thermodynamic binding parameters of adenosine A1 receptor ligands. European Journal of Pharmacology. 267: 55-61. PMID 8206130 DOI: 10.1016/0922-4106(94)90224-0 |
0.365 |
|
| 1994 |
IJzerman AP, van der Wenden EM, van Galen PJ, Jacobson KA. Molecular modeling of adenosine receptors. The ligand binding site on the rat adenosine A2A receptor. European Journal of Pharmacology. 268: 95-104. PMID 7925617 DOI: 10.1016/0922-4106(94)90124-4 |
0.613 |
|
| 1994 |
Ijzerman AP, von Frijtag Drabbe Künzel JK, Vittori S, Cristalli G. Purine-Substituted Adenosine Derivatives with Small N6-Substituents as Adenosine Receptor Agonists Nucleosides and Nucleotides. 13: 2267-2281. DOI: 10.1080/15257779408013220 |
0.312 |
|
| 1993 |
van Rhee AM, van Winden ECA, Nagelkerke JF, de Bont HJGM, Ijzerman AP, Soudijn W. Binding of the radioligand [3Sadenosine 5'-O-(2-thiodiphosphate) and intracellular calcium response in rat liver parenchymal cells Biochemical Pharmacology. 45: 801-807. PMID 8452554 DOI: 10.1016/0006-2952(93)90162-P |
0.329 |
|
| 1993 |
Dudley MW, Peet NP, Demeter DA, Weintraub HJR, Ijzerman AP, Nordvall G, van Galen PJM, Jacobson KA. Adenosine A1 receptor and ligand molecular modeling Drug Development Research. 28: 237-243. DOI: 10.1002/Ddr.430280309 |
0.59 |
|
| 1992 |
Ijzerman AP, Melman CT. Chemical modification of cholecystokinin-A receptors in rat pancreatic membranes. European Journal of Biochemistry. 203: 521-6. PMID 1735435 DOI: 10.1111/j.1432-1033.1992.tb16578.x |
0.346 |
|
| 1992 |
Van der Bent A, Ter Laak AM, IJzerman AP, Soudijn W. Molecular modelling of asperlicin derived cholecystokinin A receptor antagonists European Journal of Pharmacology: Molecular Pharmacology. 226: 327-334. PMID 1397061 DOI: 10.1016/0922-4106(92)90050-6 |
0.343 |
|
| 1992 |
Garritsen A, Beukers MW, Ijzerman AP, Cragoe EJ, Soudijn W. The mode of interaction of amiloride and some of its analogues with the adenosine A1 receptor Neurochemistry International. 20: 207-213. PMID 1304860 DOI: 10.1016/0197-0186(92)90169-R |
0.444 |
|
| 1992 |
van der Bent A, ter Laak A, van Vlijmen B, Ijzerman A, Soudijn W. Molecular modelling of asperlicine derived cholecystokinin-A receptor antagonists Journal of Controlled Release. 21: 204. DOI: 10.1016/0168-3659(92)90032-M |
0.322 |
|
| 1991 |
Van Galen PJM, Nissen P, Van Wijngaarden I, Ijzerman AP, Soudijn W. 1H-imidazo[4,5-c]quinolin-4-amines: Novel non-xanthine adenosine antagonists Journal of Medicinal Chemistry. 34: 1202-1206. PMID 2002461 DOI: 10.1021/jm00107a046 |
0.344 |
|
| 1991 |
Garritsen A, Ijzerman AP, Martin MM, Cragoe EJ, Soudijn W. Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the na+/h+ exchange, but indicate a common structure on receptor proteins Journal of Receptors and Signal Transduction. 11: 891-907. PMID 1661335 DOI: 10.3109/10799899109064686 |
0.391 |
|
| 1991 |
Van der Wenden EM, Van Galen PJM, Ijzerman AP, Soudijn W. Mapping the xanthine C8-region of the adenosine A1 receptor with computer graphics Nucleosides and Nucleotides. 10: 1199-1200. DOI: 10.1080/07328319108047274 |
0.376 |
|
| 1991 |
Garritsen A, Beukers MW, Ijzerman AP, Soudijn W. Recognition of adenosine receptors by amiloride and its analogues Nucleosides and Nucleotides. 10: 1107-1111. DOI: 10.1080/07328319108047248 |
0.46 |
|
| 1991 |
Van Der Wenden EM, Van Galen PJM, Ijzerman AP, Soudijn W. A model for the hydrogen-bonding interactions between adenosine receptor ligands and histidyl residues in the adenosine A1 receptor binding site, based on AMI calculations Journal of Molecular Structure: Theochem. 231: 175-184. DOI: 10.1016/0166-1280(91)85215-S |
0.383 |
|
| 1990 |
Van Galen PJM, Van Vlijmen HWT, IJzerman AP, Soudijn W. A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties Journal of Medicinal Chemistry. 33: 1708-1713. PMID 2342066 DOI: 10.1021/jm00168a027 |
0.336 |
|
| 1990 |
Garritsen A, IJzerman AP, Beukers MW, Soudijn W. Chemical modification of adenosine A1 receptors. Implications for the interaction with R-PIA, DPCPX and amiloride Biochemical Pharmacology. 40: 835-842. PMID 2143656 DOI: 10.1016/0006-2952(90)90324-E |
0.435 |
|
| 1990 |
Garritsen A, IJzerman AP, Beukers MW, Cragoe EJ, Soudijn W. Interaction of amiloride and its analogues with adenosine A1 receptors in calf brain Biochemical Pharmacology. 40: 827-834. PMID 2143655 DOI: 10.1016/0006-2952(90)90323-D |
0.423 |
|
| 1990 |
Van Galen PJM, IJzerman AP, Soudijn W. Xanthine-7-ribosides as adenosine A1 receptor antagonists: Further evidence for adenosine's anti mode of binding Nucleosides and Nucleotides. 9: 275-291. DOI: 10.1080/07328319008045138 |
0.458 |
|
| 1990 |
Ijzerman A, van Galen P. Pharmacology of purinergic receptors: implications for drug design Trends in Pharmacological Sciences. 11: 342-343. DOI: 10.1016/0165-6147(90)90157-4 |
0.368 |
|
| 1989 |
Pirovano IM, Ijzerman AP, Van Galen PJM, Soudijn W. Influence of the molecular structure of N6-(ω-aminoalkyl)adenosines on adenosine receptor affinity and intrinsic activity European Journal of Pharmacology: Molecular Pharmacology. 172: 185-193. PMID 2767141 DOI: 10.1016/0922-4106(89)90009-6 |
0.338 |
|
| 1989 |
van Vlijmen HW, IJzerman AP. Molecular modeling of a putative antagonist binding site on helix III of the beta-adrenoceptor. Journal of Computer-Aided Molecular Design. 3: 165-74. PMID 2570825 DOI: 10.1007/Bf01557726 |
0.673 |
|
| 1988 |
IJzerman AP, van Vlijmen HW. A molecular graphics study exploring a putative ligand binding site of the beta-adrenoceptor. Journal of Computer-Aided Molecular Design. 2: 43-53. PMID 2848931 DOI: 10.1007/BF01532052 |
0.677 |
|
| 1987 |
Damsma G, Westerink BHC, de Vries JB, Horn AS, Rettenmayr N, de Miranda JFR, Lambrecht G, Mutschler E, Russel FGM, van Galen PJM, van Viijmen HWT, Ijzerman AP, Soudijn W, Vromans RM, van de Straat R, et al. Abstracts of papers medicinal chemical meeting Pharmaceutisch Weekblad. 9: 338-345. DOI: 10.1007/Bf01956517 |
0.357 |
|
| 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 DOI: 10.1007/Bf01957781 |
0.488 |
|
| 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 |
0.449 |
|
| 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 DOI: 10.1021/Jm00152A017 |
0.591 |
|
| 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 DOI: 10.1021/jm00154a020 |
0.433 |
|
| 1986 |
LINSCHOTEN MR, BULTSMA T, IJZERMAN AP, TIMMERMAN H. ChemInform Abstract: Mapping the Turkey Erythrocyte β Receptor: A Distance Geometry Approach. Chemischer Informationsdienst. 17. DOI: 10.1002/Chin.198623075 |
0.513 |
|
| 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 DOI: 10.1021/jm00147a037 |
0.462 |
|
| 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 DOI: 10.1016/0006-2952(85)90011-5 |
0.414 |
|
| 1985 |
IJZERMAN AP, AUE GHJ, BULTSMA T, LINSCHOTEN MR, TIMMERMAN H. ChemInform Abstract: QUANTITATIVE EVALUATION OF THE β2-ADRENOCEPTOR AFFINITY OF PHENOXYPROPANOLAMINES AND PHENYLETHANOLAMINES Chemischer Informationsdienst. 16. DOI: 10.1002/Chin.198552328 |
0.447 |
|
| 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 DOI: 10.1111/J.2042-7158.1984.Tb02978.X |
0.396 |
|
| 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 DOI: 10.1007/BF00506239 |
0.464 |
|
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