OpenURL Connection Search

Select item for more details and to access through your institution.

Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters.
Published in:
Frontiers in Pharmacology, 2022, v. 13, p. 1, doi. 10.3389/fphar.2022.872335
By:
- Sijben, Hubert J.;
- Dall' Acqua, Laura;
- Liu, Rongfang;
- Jarret, Abigail;
- Christodoulaki, Eirini;
- Onstein, Svenja;
- Wolf, Gernot;
- Verburgt, Simone J.;
- Le Dévédec, Sylvia E.;
- Wiedmer, Tabea;
- Superti-Furga, Giulio;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
MPP + -Induced Changes in Cellular Impedance as a Measure for Organic Cation Transporter (SLC22A1-3) Activity and Inhibition.
Published in:
International Journal of Molecular Sciences, 2022, v. 23, n. 3, p. 1203, doi. 10.3390/ijms23031203
By:
- Mocking, Tamara A. M.;
- Sijben, Hubert J.;
- Vermeulen, Yimé W.;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
The 17th EFMC Short Course on Medicinal Chemistry on Small Molecule Protein Degraders.
Published in:
ChemMedChem, 2023, v. 18, n. 20, p. 1, doi. 10.1002/cmdc.202300464
By:
- Ciulli, Alessio;
- O'Connor, Suzanne;
- Chung, Chun‐Wa;
- Hartung, Ingo V.;
- Testa, Andrea;
- Daniels, Danette L.;
- Heitman, Laura H.
Publication type:
Article
Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors.
Published in:
ChemMedChem, 2021, v. 16, n. 4, p. 640, doi. 10.1002/cmdc.202000728
By:
- Wagner, Stefan;
- Moura Gatti, Fernando;
- Silva, Daniel G.;
- Ortiz Zacarias, Natalia V.;
- Zweemer, Annelien J. M.;
- Hermann, Sven;
- De Maria, Monica;
- Koch, Michael;
- Weiss, Christina;
- Schepmann, Dirk;
- Heitman, Laura H.;
- Tschammer, Nuska;
- Kopka, Klaus;
- Junker, Anna
Publication type:
Article
An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters.
Published in:
Frontiers in Pharmacology, 2021, v. 12, p. 1, doi. 10.3389/fphar.2021.722889
By:
- Dvorak, Vojtech;
- Wiedmer, Tabea;
- Ingles-Prieto, Alvaro;
- Altermatt, Patrick;
- Batoulis, Helena;
- Bärenz, Felix;
- Bender, Eckhard;
- Digles, Daniela;
- Dürrenberger, Franz;
- Heitman, Laura H.;
- IJzerman, Adriaan P.;
- Kell, Douglas B.;
- Kickinger, Stefanie;
- Körzö, Daniel;
- Leippe, Philipp;
- Licher, Thomas;
- Manolova, Vania;
- Rizzetto, Riccardo;
- Sassone, Francesca;
- Scarabottolo, Lia
Publication type:
Article
A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence.
Published in:
Nature Communications, 2023, v. 14, n. 1, p. 1, doi. 10.1038/s41467-023-43606-3
By:
- Jiang, Ming;
- Huizenga, Mirjam C. W.;
- Wirt, Jonah L.;
- Paloczi, Janos;
- Amedi, Avand;
- van den Berg, Richard J. B. H. N.;
- Benz, Joerg;
- Collin, Ludovic;
- Deng, Hui;
- Di, Xinyu;
- Driever, Wouter F.;
- Florea, Bogdan I.;
- Grether, Uwe;
- Janssen, Antonius P. A.;
- Hankemeier, Thomas;
- Heitman, Laura H.;
- Lam, Tsang-Wai;
- Mohr, Florian;
- Pavlovic, Anto;
- Ruf, Iris
Publication type:
Article
Targeting the CCL2–CCR2 axis for atheroprotection.
Published in:
European Heart Journal, 2022, v. 43, n. 19, p. 1799, doi. 10.1093/eurheartj/ehac094
By:
- Georgakis, Marios K;
- Bernhagen, Jürgen;
- Heitman, Laura H;
- Weber, Christian;
- Dichgans, Martin
Publication type:
Article
Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations.
Published in:
PLoS Computational Biology, 2021, v. 17, n. 11, p. 1, doi. 10.1371/journal.pcbi.1009152
By:
- Jespers, Willem;
- Heitman, Laura H.;
- IJzerman, Adriaan P.;
- Sotelo, Eddy;
- van Westen, Gerard J. P.;
- Åqvist, Johan;
- Gutiérrez-de-Terán, Hugo
Publication type:
Article
Discovery of a Photoaffinity Probe that Captures the Active Conformation of the Cannabinoid CB2 Receptor.
Published in:
ChemBioChem, 2024, v. 25, n. 7, p. 1, doi. 10.1002/cbic.202300785
By:
- De Paus, Laura V.;
- An, Yu;
- Janssen, Antonius P. A.;
- van den Berg, Richard J. B. H. N.;
- Heitman, Laura H.;
- van der Stelt, Mario
Publication type:
Article
Cancer-Associated Mutations of the Adenosine A 2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions.
Published in:
Molecules, 2022, v. 27, n. 15, p. 4676, doi. 10.3390/molecules27154676
By:
- Feng, Chenlin;
- Wang, Xuesong;
- Jespers, Willem;
- Liu, Rongfang;
- Zamarbide Losada, Sofía Denise;
- Gorostiola González, Marina;
- van Westen, Gerard J. P.;
- Danen, Erik H. J.;
- Heitman, Laura H.
Publication type:
Article
Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology.
Published in:
Molecules, 2022, v. 27, n. 12, p. 3742, doi. 10.3390/molecules27123742
By:
- Wang, Xuesong;
- Jespers, Willem;
- Wolff, Kim A. N.;
- Buytelaar, Jill;
- IJzerman, Adriaan P.;
- van Westen, Gerard J. P.;
- Heitman, Laura H.
Publication type:
Article
Development of Bicyclo[3.1.0]hexane-Based A 3 Receptor Ligands: Closing the Gaps in the Structure–Affinity Relationships.
Published in:
Molecules, 2022, v. 27, n. 7, p. 2283, doi. 10.3390/molecules27072283
By:
- Lemmerhirt, Jan Phillip;
- Isaak, Andreas;
- Liu, Rongfang;
- Kock, Max;
- Daniliuc, Constantin G.;
- Jacobson, Kenneth A.;
- Heitman, Laura H.;
- Junker, Anna
Publication type:
Article
Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1.
Published in:
Scientific Reports, 2019, v. 9, n. 1, p. N.PAG, doi. 10.1038/s41598-019-48829-3
By:
- Vlachodimou, Anna;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
A multiple classifier system identifies novel cannabinoid CB2 receptor ligands.
Published in:
Journal of Cheminformatics, 2019, v. 11, n. 1, p. N.PAG, doi. 10.1186/s13321-019-0389-9
By:
- Ruano-Ordás, David;
- Burggraaff, Lindsey;
- Liu, Rongfang;
- van der Horst, Cas;
- Heitman, Laura H.;
- Emmerich, Michael T. M.;
- Mendez, Jose R.;
- Yevseyeva, Iryna;
- van Westen, Gerard J. P.
Publication type:
Article
Cancer‐related somatic mutations alter adenosine A1 receptor pharmacology—A focus on mutations in the loops and C‐terminus.
Published in:
FASEB Journal, 2022, v. 36, n. 6, p. 1, doi. 10.1096/fj.202200203RR
By:
- Wang, Xuesong;
- Jespers, Willem;
- de Waal, Just J.;
- Wolff, Kim A. N.;
- van Uden, Liedeke;
- IJzerman, Adriaan P.;
- van Westen, Gerard J. P.;
- Heitman, Laura H.
Publication type:
Article
Pharmacological characterization of allosteric modulators: A case for chemokine receptors.
Published in:
Medicinal Research Reviews, 2024, v. 44, n. 5, p. 2291, doi. 10.1002/med.22043
By:
- den Hollander, Lisa S.;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
Drug-Target Residence Time-A Case for G Protein-Coupled Receptors.
Published in:
Medicinal Research Reviews, 2014, v. 34, n. 4, p. 856, doi. 10.1002/med.21307
By:
- Guo, Dong;
- Hillger, Julia M.;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
Indanes-Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors.
Published in:
Medicinal Research Reviews, 2015, v. 35, n. 6, p. 1097, doi. 10.1002/med.21352
By:
- Vilums, Maris;
- Heuberger, Jules;
- Heitman, Laura H.;
- IJzerman, Adriaan P.
Publication type:
Article
G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: A case for gnrh, LH, FSH, and GPR54 receptor ligands.
Published in:
Medicinal Research Reviews, 2008, v. 28, n. 6, p. 975, doi. 10.1002/med.20129
By:
- Heitman, Laura H.;
- IJzerman, Adriaan P.
Publication type:
Article
Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition.
Published in:
Scientific Reports, 2021, v. 11, n. 1, p. 1, doi. 10.1038/s41598-021-93419-x
By:
- Wang, Xuesong;
- Jespers, Willem;
- Prieto-Díaz, Rubén;
- Majellaro, Maria;
- IJzerman, Adriaan P.;
- van Westen, Gerard J. P.;
- Sotelo, Eddy;
- Heitman, Laura H.;
- Gutiérrez-de-Terán, Hugo
Publication type:
Article
Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors.
Published in:
Scientific Reports, 2021, v. 11, n. 1, p. 1, doi. 10.1038/s41598-021-91700-7
By:
- Sijben, Hubert J.;
- van Oostveen, Wieke M.;
- Hartog, Peter B. R.;
- Stucchi, Laura;
- Rossignoli, Andrea;
- Maresca, Giovanna;
- Scarabottolo, Lia;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery.
Published in:
Scientific Reports, 2021, v. 10, n. 1, p. 1, doi. 10.1038/s41598-020-79218-w
By:
- Sijben, Hubert J.;
- van den Berg, Julie J. E.;
- Broekhuis, Jeremy D.;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
LUF7244, an allosteric modulator/activator of Kv 11.1 channels, counteracts dofetilide-induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model.
Published in:
2019
By:
- Qile, Muge;
- Beekman, Henriette D.M.;
- Sprenkeler, David J.;
- Houtman, Marien J.C.;
- Ham, Willem B.;
- Stary‐Weinzinger, Anna;
- Beyl, Stanislav;
- Hering, Steffen;
- Berg, Dirk‐Jan;
- Lange, Elizabeth C.M.;
- Heitman, Laura H.;
- IJzerman, Ad P.;
- Vos, Marc A.;
- Heyden, Marcel A.G.;
- van Ham, Willem B;
- Stary-Weinzinger, Anna;
- van den Berg, Dirk-Jan;
- de Lange, Elizabeth C M;
- van der Heyden, Marcel A G
Publication type:
journal article
A two-state model for the kinetics of competitive radioligand binding.
Published in:
2018
By:
- Guo, Dong;
- Peletier, Lambertus A.;
- Bridge, Lloyd;
- Keur, Wesley;
- de Vries, Henk;
- Zweemer, Annelien;
- Heitman, Laura H.;
- IJzerman, Adriaan P.
Publication type:
journal article
Label-free detection of prostaglandin transporter (SLCO2A1) function and inhibition: insights by wound healing and TRACT assays.
Published in:
Frontiers in Pharmacology, 2024, p. 1, doi. 10.3389/fphar.2024.1372109
By:
- Mocking, Tamara A. M.;
- van Oostveen, Wieke M.;
- van Veldhoven, Jacobus P. D.;
- Minnee, Hugo;
- Fehres, Cynthia M.;
- Whitehurst, Charles E.;
- Jzerman, Adriaan P. I.;
- Heitman, Laura H.
Publication type:
Article
Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.
Published in:
2016
By:
- Doornbos, Maarten L J;
- Pérez ‐ Benito, Laura;
- Tresadern, Gary;
- Mulder ‐ Krieger, Thea;
- Biesmans, Ilse;
- Trabanco, Andrés A;
- Cid, Jose María;
- Lavreysen, Hilde;
- IJzerman, Adriaan P;
- Heitman, Laura H;
- Pérez-Benito, Laura;
- Mulder-Krieger, Thea;
- Trabanco, Andrés A;
- Cid, Jose María
Publication type:
journal article
Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Published in:
2016
By:
- Nederpelt, Indira;
- Georgi, Victoria;
- Schiele, Felix;
- Nowak ‐ Reppel, Katrin;
- Fernández ‐ Montalván, Amaury E.;
- IJzerman, Adriaan P.;
- Heitman, Laura H.;
- Nowak-Reppel, Katrin;
- Fernández-Montalván, Amaury E
Publication type:
journal article
Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor.
Published in:
2014
By:
- Guo, Dong;
- Venhorst, Suzanne N;
- Massink, Arnault;
- van Veldhoven, Jacobus P D;
- Vauquelin, Georges;
- IJzerman, Adriaan P;
- Heitman, Laura H
Publication type:
journal article
Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor.
Published in:
British Journal of Pharmacology, 2014, v. 171, n. 23, p. 5295, doi. 10.1111/bph.12836
By:
- Guo, Dong;
- Venhorst, Suzanne N;
- Massink, Arnault;
- Veldhoven, Jacobus P D;
- Vauquelin, Georges;
- IJzerman, Adriaan P;
- Heitman, Laura H
Publication type:
Article
Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time.
Published in:
2012
By:
- Guo D;
- Mulder-Krieger T;
- IJzerman AP;
- Heitman LH;
- Guo, Dong;
- Mulder-Krieger, Thea;
- IJzerman, Adriaan P;
- Heitman, Laura H
Publication type:
journal article
Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time.
Published in:
British Journal of Pharmacology, 2012, v. 166, n. 6, p. 1846, doi. 10.1111/j.1476-5381.2012.01897.x
By:
- Guo, Dong;
- Mulder-Krieger, Thea;
- IJzerman, Adriaan P;
- Heitman, Laura H
Publication type:
Article
Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist.
Published in:
2006
By:
- Heitman, Laura H.;
- Mulder-Krieger, Thea;
- Spanjersberg, Ronald F.;
- von Frijtag Drabbe Künzel, Jacobien K.;
- Dalpiaz, Alessandro;
- IJzerman, Adriaan P.;
- von Frijtag Drabbe Künzel, Jacobien K
Publication type:
journal article
3DDPDs: describing protein dynamics for proteochemometric bioactivity prediction. A case for (mutant) G protein-coupled receptors.
Published in:
Journal of Cheminformatics, 2023, v. 15, n. 1, p. 1, doi. 10.1186/s13321-023-00745-5
By:
- Gorostiola González, Marina;
- van den Broek, Remco L.;
- Braun, Thomas G. M.;
- Chatzopoulou, Magdalini;
- Jespers, Willem;
- IJzerman, Adriaan P.;
- Heitman, Laura H.;
- van Westen, Gerard J. P.
Publication type:
Article
Molecular insights into disease-associated glutamate transporter (EAAT1 / SLC1A3) variants using in silico and in vitro approaches.
Published in:
Frontiers in Molecular Biosciences, 2023, p. 1, doi. 10.3389/fmolb.2023.1286673
By:
- González, Marina Gorostiola;
- Sijben, Hubert J.;
- Acqua, Laura Dall';
- Rongfang Liu;
- IJzerman, Adriaan P.;
- Heitman, Laura H.;
- van Westen, Gerard J. P.
Publication type:
Article
Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.
Published in:
Chimia, 2024, v. 78, n. 7/8, p. 499, doi. 10.2533/chimia.2024.499
By:
- Aebia, Johannes;
- Atza, Kenneth;
- Ametamey, Simon M.;
- Benza, Jörg;
- Blaising, Julie;
- Butini, Stefania;
- Campiani, Giuseppe;
- Carreira, Erick M.;
- Collin, Ludovic;
- de Lago, Eva;
- Gazzi, Thais;
- Gertsch, Jürg;
- Gobbi, Luca;
- Guba, Wolfgang;
- Fernández-Ruize, Javier;
- Fingerle, Jürgen;
- Haider, Ahmed;
- Yingfang He;
- Heitman, Laura H.;
- Honer, Michael
Publication type:
Article
The Role of Target Binding Kinetics in Drug Discovery.
Published in:
ChemMedChem, 2015, v. 10, n. 11, p. 1793, doi. 10.1002/cmdc.201500310
By:
- Guo, Dong;
- Heitman, Laura H.;
- IJzerman, Adriaan P.
Publication type:
Article
Evaluation of (4-Arylpiperidin-1-yl)cyclopentanecarboxamides As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor.
Published in:
ChemMedChem, 2015, v. 10, n. 7, p. 1249, doi. 10.1002/cmdc.201500058
By:
- Vilums, Maris;
- Zweemer, Annelien J. M.;
- Dilanchian, Arian;
- van Veldhoven, Jacobus P. D.;
- de Vries, Henk;
- Brussee, Johannes;
- Saunders, John;
- Stamos, Dean;
- Heitman, Laura H.;
- IJzerman, Adriaan P.
Publication type:
Article
Binding Kinetics of ZM241385 Derivatives at the Human Adenosine A2A Receptor.
Published in:
ChemMedChem, 2014, v. 9, n. 4, p. 752, doi. 10.1002/cmdc.201300474
By:
- Guo, Dong;
- Xia, Lizi;
- van Veldhoven, Jacobus P. D.;
- Hazeu, Marc;
- Mocking, Tamara;
- Brussee, Johannes;
- IJzerman, Adriaan P.;
- Heitman, Laura H.
Publication type:
Article
Discovery of Selective Luteinizing Hormone Receptor Agonists Using the Bivalent Ligand Method.
Published in:
ChemMedChem, 2009, v. 4, n. 7, p. 1189, doi. 10.1002/cmdc.200900058
By:
- Bonger, Kimberly M.;
- van den Berg, Richard J. B. H. N.;
- Knijnenburg, Annemiek D.;
- Heitman, Laura H.;
- van Koppen, Chris J.;
- Timmers, Cornelis M.;
- Overkleeft, Herman S.;
- van der Marel, Gijsbert A.
Publication type:
Article
Inducing Receptor Degradation as a Novel Approach to Target CC Chemokine Receptor 2 (CCR2).
Published in:
International Journal of Molecular Sciences, 2024, v. 25, n. 16, p. 8984, doi. 10.3390/ijms25168984
By:
- Ortiz Zacarías, Natalia V.;
- Röth, Sascha;
- Broekhuis, Jeremy D.;
- van der Es, Daan;
- Moreau, Kevin;
- Heitman, Laura H.
Publication type:
Article
Computational Characterization of Membrane Proteins as Anticancer Targets: Current Challenges and Opportunities.
Published in:
International Journal of Molecular Sciences, 2024, v. 25, n. 7, p. 3698, doi. 10.3390/ijms25073698
By:
- Gorostiola González, Marina;
- Rakers, Pepijn R. J.;
- Jespers, Willem;
- IJzerman, Adriaan P.;
- Heitman, Laura H.;
- van Westen, Gerard J. P.
Publication type:
Article

Found: 41