Ad P. IJzerman - Publications

Affiliations: 
Leiden University, Leiden, Netherlands 
Area:
Pharmacochemistry
Website:
https://hoogleraren.leidenuniv.nl/id/3592

327 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2021 Liu X, IJzerman AP, van Westen GJP. Computational Approaches for De Novo Drug Design: Past, Present, and Future. Methods in Molecular Biology (Clifton, N.J.). 2190: 139-165. PMID 32804364 DOI: 10.1007/978-1-0716-0826-5_6  0.68
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  0.68
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  0.48
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  0.68
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  0.68
2020 Superti-Furga G, Lackner D, Wiedmer T, Ingles-Prieto A, Barbosa B, Girardi E, Goldmann U, Gürtl B, Klavins K, Klimek C, Lindinger S, Liñeiro-Retes E, Müller AC, Onstein S, Redinger G, ... ... IJzerman AP, et al. The RESOLUTE consortium: unlocking SLC transporters for drug discovery. Nature Reviews. Drug Discovery. PMID 32265506 DOI: 10.1038/d41573-020-00056-6  0.68
2020 Qile M, Ji Y, Golden TD, Houtman MJC, Romunde F, Fransen D, van Ham WB, IJzerman AP, January CT, Heitman LH, Stary-Weinzinger A, Delisle BP, van der Heyden MAG. LUF7244 plus dofetilide rescues aberrant Kv11.1 trafficking and produces functional IKv11.1. Molecular Pharmacology. PMID 32241959 DOI: 10.1124/mol.119.118190  0.48
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  0.56
2019 Oranje P, Gouka R, Burggraaff L, Vermeer M, Chalet C, Duchateau G, van der Pijl P, Geldof M, de Roo N, Clauwaert F, Vanpaeschen T, Nicolaï J, de Bruyn T, Annaert P, IJzerman AP, et al. Novel natural and synthetic inhibitors of solute carriers SGLT1 and SGLT2. Pharmacology Research & Perspectives. 7: e00504. PMID 31384471 DOI: 10.1002/prp2.504  0.68
2019 Qile M, Beekman HDM, Sprenkeler DJ, Houtman MJC, van Ham WB, Stary-Weinzinger A, Beyl S, Hering S, van den Berg DJ, de Lange ECM, Heitman LH, IJzerman AP, Vos MA, van der Heyden MAG. LUF7244, an allosteric modulator/activator of K 11.1 channels, counteracts dofetilide-induced TdP arrhythmia in the chronic atrioventricular block dog model. British Journal of Pharmacology. PMID 31339551 DOI: 10.1111/bph.14798  0.48
2019 Liu X, Ye K, van Vlijmen HWT, IJzerman AP, van Westen GJP. An exploration strategy improves the diversity of de novo ligands using deep reinforcement learning: a case for the adenosine A receptor. Journal of Cheminformatics. 11: 35. PMID 31127405 DOI: 10.1186/s13321-019-0355-6  0.68
2019 IJzerman AP, Guo D. Drug-Target Association Kinetics in Drug Discovery. Trends in Biochemical Sciences. PMID 31101454 DOI: 10.1016/j.tibs.2019.04.004  0.32
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  0.48
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  0.48
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  0.56
2019 Sydow D, Burggraaff L, Szengel A, van Vlijmen HWT, IJzerman AP, van Westen GJP, Volkamer A. Advances and Challenges in Computational Target Prediction. Journal of Chemical Information and Modeling. PMID 30817146 DOI: 10.1021/acs.jcim.8b00832  0.68
2019 Burggraaff L, Oranje P, Gouka R, van der Pijl P, Geldof M, van Vlijmen HWT, IJzerman AP, van Westen GJP. Identification of novel small molecule inhibitors for solute carrier SGLT1 using proteochemometric modeling. Journal of Cheminformatics. 11: 15. PMID 30767155 DOI: 10.1186/s13321-019-0337-8  0.68
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  0.48
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  0.56
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  0.48
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  0.48
2018 Guo D, Peletier LA, Bridge L, Keur W, de Vries H, Zweemer A, Heitman LH, IJzerman AP. A two-state model for the kinetics of competitive radioligand binding. British Journal of Pharmacology. PMID 29486053 DOI: 10.1111/bph.14184  0.64
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  0.48
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  0.68
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  0.32
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  0.68
2017 Donkers JM, Zehnder B, van Westen GJP, Kwakkenbos MJ, IJzerman AP, Oude Elferink RPJ, Beuers U, Urban S, van de Graaf SFJ. Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP. Scientific Reports. 7: 15307. PMID 29127322 DOI: 10.1038/s41598-017-15338-0  0.68
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  0.56
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  0.56
2017 Lenselink EB, Ten Dijke N, Bongers B, Papadatos G, van Vlijmen HWT, Kowalczyk W, IJzerman AP, van Westen GJP. Beyond the hype: deep neural networks outperform established methods using a ChEMBL bioactivity benchmark set. Journal of Cheminformatics. 9: 45. PMID 29086168 DOI: 10.1186/s13321-017-0232-0  0.68
2017 Nederpelt I, Kuzikov M, de Witte WEA, Schnider P, Tuijt B, Gul S, IJzerman AP, de Lange ECM, Heitman LH. From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action. Scientific Reports. 7: 14169. PMID 29075004 DOI: 10.1038/s41598-017-14257-4  0.48
2017 Lowe PT, Dall'Angelo S, Mulder-Krieger T, IJzerman AP, Zanda M, O'Hagan D. A New Class of Fluorinated A2A Adenosine Receptor Agonist with Application to Last-Step Enzymatic [(18) F]Fluorination for PET Imaging. Chembiochem : a European Journal of Chemical Biology. 18: 2156-2164. PMID 28851015 DOI: 10.1002/cbic.201700382  0.52
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  0.56
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  0.4
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  0.52
2017 Hillger JM, le Roy B, Wang Z, Mulder-Krieger T, Boomsma DI, Slagboom PE, Danen EH, IJzerman AP, Heitman LH. Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype. Biochemical Pharmacology. PMID 28159624 DOI: 10.1016/j.bcp.2017.01.014  0.52
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  0.68
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  0.52
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  0.56
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  0.32
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  0.96
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  0.92
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  0.88
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  0.96
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  0.96
2016 Massink A, Louvel JA, Adlere I, van Veen C, Huisman BJ, Dijksteel GS, Guo D, Lenselink EB, Buckley BJ, Matthews H, Ranson M, Kelso MJ, IJzerman AP. 5'-Substituted amiloride derivatives as allosteric modulators binding in the sodium ion pocket of the adenosine A2A receptor. Journal of Medicinal Chemistry. PMID 27124340 DOI: 10.1021/acs.jmedchem.6b00142  0.56
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  0.48
2016 Yu Z, Liu J, van Veldhoven JP, IJzerman AP, Schalij MJ, Pijnappels DA, Heitman LH, de Vries AA. Allosteric Modulation of Kv11.1 (hERG) Channels Protects Against Drug-Induced Ventricular Arrhythmias. Circulation. Arrhythmia and Electrophysiology. 9. PMID 27071825 DOI: 10.1161/CIRCEP.115.003439  0.92
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  0.92
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  0.96
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  0.92
2016 Peeters MC, Mos I, Lenselink EB, Lucchesi M, IJzerman AP, Schwartz TW. Getting from A to B-exploring the activation motifs of the class B adhesion G protein-coupled receptor subfamily G member 4/GPR112. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. PMID 26823453 DOI: 10.1096/fj.201500110  0.56
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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 & Bioelectronics. 74: 233-42. PMID 26143464 DOI: 10.1016/j.bios.2015.06.031  0.48
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  0.56
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
2015 Massink A, Gutiérrez-de-Terán H, Lenselink EB, Ortiz Zacarías 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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.96
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.96
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
2013 Gutiérrez-de-Terán H, Massink A, Rodríguez 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  0.92
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
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  0.96
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
2010 Vittori S, Lorenzen A, Stannek C, Costanzi S, Volpini R, IJzerman AP, Von Frijtag Drabbe Kunzel JK, Cristalli G. ChemInform Abstract: N-Cycloalkyl Derivatives of Adenosine and 1-Deazaadenosine as Agonists and Partial Agonists of the A1 Adenosine Receptor. Cheminform. 31: no-no. DOI: 10.1002/chin.200016239  0.36
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
2009 Göblyös A, Ijzerman AP. Allosteric modulation of adenosine receptors. Purinergic Signalling. 5: 51-61. PMID 18615273 DOI: 10.1007/s11302-008-9105-3  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.64
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  0.92
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  0.92
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  0.92
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  0.92
2008 Ye K, Vriend G, IJzerman AP. Tracing evolutionary pressure. Bioinformatics (Oxford, England). 24: 908-15. PMID 18304936 DOI: 10.1093/bioinformatics/btn057  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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+  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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.  0.92
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.  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
2003 Soudijn W, Van Wijngaarden I, IJzerman AP. Stereoselectivity of drug-receptor interactions Idrugs. 6: 43-56. PMID 12789621  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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.  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.88
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  0.88
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  0.92
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  0.92
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  0.92
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  0.92
2000 Horn F, Van Der Wenden EM, Oliveira L, Ijzerman AP, Vriend G. Receptors coupling to G proteins: Is there a signal behind the sequence? Proteins: Structure, Function and Genetics. 41: 448-459. PMID 11056033 DOI: 10.1002/1097-0134(20001201)41:4<448::AID-PROT30>3.0.CO;2-C  0.92
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  0.92
2000 Gao ZG, Ijzerman AP. Allosteric modulation of A(2A) adenosine receptors by amiloride analogues and sodium ions. Biochemical Pharmacology. 60: 669-76. PMID 10927025 DOI: 10.1016/S0006-2952(00)00360-9  0.44
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  0.32
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  1
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  0.56
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  0.92
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  0.56
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
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
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  0.68
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  0.56
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  0.92
1997 Van Schaick EA, De Greef HJMM, Langemeijer MWE, Sheehan MJ, IJzerman AP, Danhof M. Pharmacokinetic-pharmacodynamic modelling of the anti-lipolytic and anti-ketotic effects of the adenosine A1-receptor agonist N6-(p-sulphophenyl)adenosine in rats British Journal of Pharmacology. 122: 525-533. PMID 9351510 DOI: 10.1038/sj.bjp.0701412  0.92
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  0.56
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  0.92
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  0.36
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  0.92
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  0.92
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  0.92
1995 Mathot RAA, Cleton A, Soudijn W, Ijzerman AP, Danhof M. Pharmacokinetic modelling of the haemodynamic effects of the A(2a) adenosine receptor agonist CGS 21680C in conscious normotensive rats British Journal of Pharmacology. 114: 761-768. PMID 7773536 DOI: 10.1111/j.1476-5381.1995.tb13270.x  0.92
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  0.92
1995 Beukers MW, Kerkhof CJM, van Rhee MA, Ardanuy U, Gurgel C, Widjaja H, Nickel P, IJzerman AP, Soudijn W. Suramin analogs, divalent cations and ATPγS as inhibitors of ecto-ATPase Naunyn-Schmiedeberg's Archives of Pharmacology. 351: 523-528. PMID 7643916 DOI: 10.1007/BF00171044  0.92
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  0.92
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  0.92
1994 Beukers MW, Kerkhof CJM, Ijzerman AP, Soudijn W. Nucleoside transport inhibition and platelet aggregation in human blood: R75231 and its enantiomers, draflazine and R88016 European Journal of Pharmacology: Molecular Pharmacology. 266: 57-62. PMID 8137884 DOI: 10.1016/0922-4106(94)90209-7  0.92
1994 Irth H, Cleton A, Mathôt RAA, Danhof M, IJzerman AP, Tjaden UR, van der Greef J. Liquid chromatographic determination of the adenosine receptor agonist CGS 21680 in blood using on-line solid-phase extraction on a phenylboronic acid support and fluorescence detection Journal of Chromatography B: Biomedical Sciences and Applications. 658: 207-212. PMID 7952127 DOI: 10.1016/0378-4347(94)00216-9  0.92
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  0.6
1994 van Rhee AM, van der Heijden MP, Beukers MW, IJzerman AP, Soudijn W, Nickel P. Novel competitive antagonists for P2 purinoceptors. European Journal of Pharmacology. 268: 1-7. PMID 7925607 DOI: 10.1016/0922-4106(94)90114-7  0.92
1994 Van Der Bent A, Van Den Brink I, IJzerman AP, Van Wijngaarden I, Soudijn W. Synthesis and biological evaluation of lorglumide-like hybrid cholecystokinin-A receptor antagonists Drug Development Research. 31: 197-205. DOI: 10.1002/ddr.430310307  0.92
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  0.92
1993 Beukers MW, Pirovano IM, van Weert A, Kerkhof CJM, Ijzerman AP, Soudijn W. Characterization of ECTO-ATPase on human blood cells. A physiological role in platelet aggregation? Biochemical Pharmacology. 46: 1959-1966. PMID 8267645 DOI: 10.1016/0006-2952(93)90637-C  0.92
1993 Mathôt RAA, Appel S, van Schaick EA, Soudijn W, Ijzerman AP, Danhof M. High-performance liquid chromatography of the adenosine A1 agonist N6-cyclopentyladenosine and the A1 antagonist 8-cyclopentyltheophylline and its application in a pharmacokinetic study in rats Journal of Chromatography B: Biomedical Sciences and Applications. 620: 113-120. PMID 8106577 DOI: 10.1016/0378-4347(93)80058-C  0.92
1992 Van der Bent A, Blommaert AGS, Melman CTM, IJzerman AP, Van Wijngaarden I, Soudijn W. Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718 Journal of Medicinal Chemistry. 35: 1042-1049. PMID 1552499 DOI: 10.1021/jm00084a009  0.92
1992 Van Der Wenden EM, IJzerman AP, Soudijn W. A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor Journal of Medicinal Chemistry. 35: 629-635. PMID 1542091 DOI: 10.1021/jm00082a003  0.92
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  0.92
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  0.92
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  0.92
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  0.92
1991 Van Rhee AM, Ijzerman AP, Soudijn W. P2-purinoceptor mediated inhibition of adenylate cyclase activity Nucleosides and Nucleotides. 10: 1239-1240. DOI: 10.1080/07328319108047291  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
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  0.92
1990 Van Rhee AM, Ijzerman AP, Soudijn W. Purinoceptor mediated inhibition of adenylate cyclase activity European Journal of Pharmacology. 183: 2168. DOI: 10.1016/0014-2999(90)93694-L  0.92
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  0.92
1989 Van Galen PJM, Leusen FJJ, Ijzerman AP, Soudijn W. Mapping the N6-region of the adenosine A1 receptor with computer graphics European Journal of Pharmacology: Molecular Pharmacology. 172: 19-27. PMID 2714369 DOI: 10.1016/0922-4106(89)90041-2  0.92
1989 Ijzerman AP, Soudijn W. The antiarrhythmic properties of β-adrenoceptor antagonists Trends in Pharmacological Sciences. 10: 31-36. PMID 2574509 DOI: 10.1016/0165-6147(89)90104-1  0.92
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  0.88
1989 Garritsen A, Ijzerman AP, Soudijn W. Adenosine-A1 receptors are not coupled to Ca2+ uptake in rat brain synaptosomes Biochemical Pharmacology. 38: 693-695. PMID 2537086 DOI: 10.1016/0006-2952(89)90218-9  0.92
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  0.88
1988 Garritsen A, Ijzerman AP, Soudijn W. [3H]batrachotoxinin-A 20-α-benzoate binding to sodium channels in rat brain: sensitivity to tetrodotoxin and divalent cations European Journal of Pharmacology. 145: 261-266. PMID 2450762 DOI: 10.1016/0014-2999(88)90428-1  0.92
1987 van Galen PJM, Ijzerman AP, Soudijn W. Adenosine derivatives with N6-alkyl, -alkylamine or -alkyladenosine substituents as probes for the A1-receptor Febs Letters. 223: 197-201. PMID 2959564 DOI: 10.1016/0014-5793(87)80535-5  0.92
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  1
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
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  1
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  1
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  1
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  1
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  1
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  1
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