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

Get full text

Label-free detection of prostaglandin transporter (SLCO2A1) function and inhibition: insights by wound healing and TRACT assays by Tamara A. M. Mocking, Wieke M. van Oostveen, Jacobus P. D. van Veldhoven, Hugo Minnee, Cynthia M. Fehres, Charles E. Whitehurst, Adriaan P. IJzerman, Laura H. Heitman, Laura H. Heitman

Get full text

A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery by Hubert J. Sijben, Julie J. E. van den Berg, Jeremy D. Broekhuis, Adriaan P. IJzerman, Laura H. Heitman

Get full text

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

Get full text

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

Get full text

Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors by Hubert J. Sijben, Wieke M. van Oostveen, Peter B. R. Hartog, Laura Stucchi, Andrea Rossignoli, Giovanna Maresca, Lia Scarabottolo, Adriaan P. IJzerman, Laura H. Heitman

Get full text

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

Get full text

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

Get full text

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

Get full text

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

Get full text

Advancing drug discovery through assay development: a survey of tool compounds within the human solute carrier superfamily by Daniela Digles, Alvaro Ingles-Prieto, Vojtech Dvorak, Tamara A. M. Mocking, Ulrich Goldmann, Andrea Garofoli, Evert J. Homan, Alberto Di Silvio, Lucia Azzollini, Francesca Sassone, Mario Fogazza, Felix Bärenz, Antje Pommereau, Yasmin Zuschlag, Jasper F. Ooms, Jeppe Tranberg-Jensen, Jesper S. Hansen, Josefina Stanka, Hubert J. Sijben, Helena Batoulis, Eckhard Bender, Riccardo Martini, Adriaan P. IJzerman, David B. Sauer, Laura H. Heitman, Vania Manolova, Juergen Reinhardt, Alexander Ehrmann, Philipp Leippe, Gerhard F. Ecker, Kilian V. M. Huber, Thomas Licher, Lia Scarabottolo, Tabea Wiedmer, Giulio Superti-Furga, Giulio Superti-Furga

Get full text