Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions von Liu, Wei, Chun, Eugene, Thompson, Aaron A., Chubukov, Pavel, Xu, Fei, Katritch, Vsevolod, Han, Gye Won, Roth, Christopher B., Heitman, Laura H., IJzerman, Adriaan P., Cherezov, Vadim, Stevens, Raymond C.

Volltext

Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors von Guo, Dong, Heitman, Laura H, IJzerman, Adriaan P

Volltext

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

Volltext

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength von Segala, Elena, Guo, Dong, Cheng, Robert K. Y, Bortolato, Andrea, Deflorian, Francesca, Doré, Andrew S, Errey, James C, Heitman, Laura H, IJzerman, Adriaan P, Marshall, Fiona H, Cooke, Robert M

Volltext

Cancer‐related somatic mutations alter adenosine A1 receptor pharmacology—A focus on mutations in the loops and C‐terminus von Wang, Xuesong, Jespers, Willem, Waal, Just J., Wolff, Kim A. N., Uden, Liedeke, IJzerman, Adriaan P., Westen, Gerard J. P., Heitman, Laura H.

Volltext

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

Volltext

Kinetics for Drug Discovery: an industry-driven effort to target drug residence time von Schuetz, Doris A., de Witte, Wilhelmus Egbertus Arnout, Wong, Yin Cheong, Knasmueller, Bernhard, Richter, Lars, Kokh, Daria B., Sadiq, S. Kashif, Bosma, Reggie, Nederpelt, Indira, Heitman, Laura H., Segala, Elena, Amaral, Marta, Guo, Dong, Andres, Dorothee, Georgi, Victoria, Stoddart, Leigh A., Hill, Steve, Cooke, Robert M., De Graaf, Chris, Leurs, Rob, Frech, Matthias, Wade, Rebecca C., de Lange, Elizabeth Cunera Maria, IJzerman, Adriaan P., Müller-Fahrnow, Anke, Ecker, Gerhard F.

Volltext

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

Volltext

Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor von Guo, Dong, Pan, Albert C, Dror, Ron O, Mocking, Tamara, Liu, Rongfang, Heitman, Laura H, Shaw, David E, IJzerman, Adriaan P

Volltext

Indanes-Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors von Vilums, Maris, Heuberger, Jules, Heitman, Laura H., IJzerman, Adriaan P.

Volltext

The Role of a Sodium Ion Binding Site in the Allosteric Modulation of the A2A Adenosine G Protein-Coupled Receptor von Gutiérrez-de-Terán, Hugo, Massink, Arnault, Rodríguez, David, Liu, Wei, Han, Gye Won, Joseph, Jeremiah S., Katritch, Ilia, Heitman, Laura H., Xia, Lizi, IJzerman, Adriaan P., Cherezov, Vadim, Katritch, Vsevolod, Stevens, Raymond C.

Volltext

Inducing Receptor Degradation as a Novel Approach to Target CC Chemokine Receptor 2 (CCR2) von Ortiz Zacarías, Natalia V, Röth, Sascha, Broekhuis, Jeremy D, van der Es, Daan, Moreau, Kevin, Heitman, Laura H

Volltext

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

Volltext

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

Volltext

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

Volltext

Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition von 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

Volltext

Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors von 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.

Volltext

Targeting the CCL2–CCR2 axis for atheroprotection von Georgakis, Marios K, Bernhagen, Jürgen, Heitman, Laura H, Weber, Christian, Dichgans, Martin

Volltext

Cancer-Associated Mutations of the Adenosine A2A Receptor Have Diverse Influences on Ligand Binding and Receptor Functions von 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.

Volltext

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

Volltext