Molecular insights into disease-associated glutamate transporter (EAAT1 / SLC1A3) variants using in silico and in vitro approaches by Marina Gorostiola González, Marina Gorostiola González, Hubert J. Sijben, Laura Dall’ Acqua, Rongfang Liu, Adriaan P. IJzerman, Laura H. Heitman, Laura H. Heitman, Gerard J. P. van Westen

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MPP⁺-Induced Changes in Cellular Impedance as a Measure for Organic Cation Transporter (SLC22A1-3) Activity and Inhibition by Tamara A. M. Mocking, Hubert J. Sijben, Yimé W. Vermeulen, Adriaan P. IJzerman, Laura H. Heitman

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Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters by Hubert J. Sijben, Laura Dall’ Acqua, Rongfang Liu, Abigail Jarret, Eirini Christodoulaki, Svenja Onstein, Gernot Wolf, Simone J. Verburgt, Sylvia E. Le Dévédec, Tabea Wiedmer, Giulio Superti-Furga, Adriaan P. IJzerman, Laura H. Heitman, Laura H. Heitman

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Computational Characterization of Membrane Proteins as Anticancer Targets: Current Challenges and Opportunities by Marina Gorostiola González, Pepijn R. J. Rakers, Willem Jespers, Adriaan P. IJzerman, Laura H. Heitman, Gerard J. P. van Westen

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Development of Bicyclo[3.1.0]hexane-Based A₃ Receptor Ligands: Closing the Gaps in the Structure–Affinity Relationships by Jan Phillip Lemmerhirt, Andreas Isaak, Rongfang Liu, Max Kock, Constantin G. Daniliuc, Kenneth A. Jacobson, Laura H. Heitman, Anna Junker

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Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology by Xuesong Wang, Willem Jespers, Kim A. N. Wolff, Jill Buytelaar, Adriaan P. IJzerman, Gerard J. P. van Westen, Laura H. Heitman

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Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations. by Willem Jespers, Laura H Heitman, Adriaan P IJzerman, Eddy Sotelo, Gerard J P van Westen, Johan Åqvist, Hugo Gutiérrez-de-Terán

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3DDPDs: describing protein dynamics for proteochemometric bioactivity prediction. A case for (mutant) G protein-coupled receptors by Marina Gorostiola González, Remco L. van den Broek, Thomas G. M. Braun, Magdalini Chatzopoulou, Willem Jespers, Adriaan P. IJzerman, Laura H. Heitman, Gerard J. P. van Westen

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Cancer-Associated Mutations of the Adenosine A_2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions by Chenlin Feng, Xuesong Wang, Willem Jespers, Rongfang Liu, Sofía Denise Zamarbide Losada, Marina Gorostiola González, Gerard J. P. van Westen, Erik H. J. Danen, Laura H. Heitman

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A multiple classifier system identifies novel cannabinoid CB2 receptor ligands by David Ruano-Ordás, Lindsey Burggraaff, Rongfang Liu, Cas van der Horst, Laura H. Heitman, Michael T. M. Emmerich, Jose R. Mendez, Iryna Yevseyeva, Gerard J. P. van Westen

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A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy by Ilze Bot, Natalia V. Ortiz Zacarías, Wilhelmus E. A. de Witte, Henk de Vries, Peter J. van Santbrink, Daniël van der Velden, Mara J. Kröner, Dirk-Jan van der Berg, Dean Stamos, Elizabeth C. M. de Lange, Johan Kuiper, Adriaan P. IJzerman, Laura H. Heitman

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Structural basis of selective cannabinoid CB2 receptor activation by Xiaoting Li, Hao Chang, Jara Bouma, Laura V. de Paus, Partha Mukhopadhyay, Janos Paloczi, Mohammed Mustafa, Cas van der Horst, Sanjay Sunil Kumar, Lijie Wu, Yanan Yu, Richard J. B. H. N. van den Berg, Antonius P. A. Janssen, Aron Lichtman, Zhi-Jie Liu, Pal Pacher, Mario van der Stelt, Laura H. Heitman, Tian Hua

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An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters by Vojtech Dvorak, Tabea Wiedmer, Alvaro Ingles-Prieto, Patrick Altermatt, Helena Batoulis, Felix Bärenz, Eckhard Bender, Daniela Digles, Franz Dürrenberger, Laura H. Heitman, Adriaan P. IJzerman, Douglas B. Kell, Douglas B. Kell, Stefanie Kickinger, Daniel Körzö, Philipp Leippe, Thomas Licher, Vania Manolova, Riccardo Rizzetto, Francesca Sassone, Lia Scarabottolo, Avner Schlessinger, Vanessa Schneider, Hubert J. Sijben, Anna-Lena Steck, Hanna Sundström, Sara Tremolada, Maria Wilhelm, Marina Wright Muelas, Diana Zindel, Claire M. Steppan, Giulio Superti-Furga, Giulio Superti-Furga

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Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity by Marjolein Soethoudt, Uwe Grether, Jürgen Fingerle, Travis W. Grim, Filomena Fezza, Luciano de Petrocellis, Christoph Ullmer, Benno Rothenhäusler, Camille Perret, Noortje van Gils, David Finlay, Christa MacDonald, Andrea Chicca, Marianela Dalghi Gens, Jordyn Stuart, Henk de Vries, Nicolina Mastrangelo, Lizi Xia, Georgios Alachouzos, Marc P. Baggelaar, Andrea Martella, Elliot D. Mock, Hui Deng, Laura H. Heitman, Mark Connor, Vincenzo Di Marzo, Jürg Gertsch, Aron H. Lichtman, Mauro Maccarrone, Pal Pacher, Michelle Glass, Mario van der Stelt

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A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence by Ming Jiang, Mirjam C. W. Huizenga, Jonah L. Wirt, Janos Paloczi, Avand Amedi, Richard J. B. H. N. van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F. Driever, Bogdan I. Florea, Uwe Grether, Antonius P. A. Janssen, Thomas Hankemeier, Laura H. Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F. Stevens, Daan van der Vliet, Tom van der Wel, Matthias B. Wittwer, Constant A. A. van Boeckel, Pal Pacher, Andrea G. Hohmann, Mario van der Stelt

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