作者
Roman C Sarott, Matthias V Westphal, Patrick Pfaff, Claudia Korn, David A Sykes, Thais Gazzi, Benjamin Brennecke, Kenneth Atz, Marie Weise, Yelena Mostinski, Pattarin Hompluem, Eline Koers, Tamara Miljus, Nicolas J Roth, Hermon Asmelash, Man C Vong, Jacopo Piovesan, Wolfgang Guba, Arne C Rufer, Eric A Kusznir, Sylwia Huber, Catarina Raposo, Elisabeth A Zirwes, Anja Osterwald, Anto Pavlovic, Svenja Moes, Jennifer Beck, Irene Benito-Cuesta, Teresa Grande, Samuel Ruiz de Martı́n Esteban, Alexei Yeliseev, Faye Drawnel, Gabriella Widmer, Daniela Holzer, Tom van der Wel, Harpreet Mandhair, Cheng-Yin Yuan, William R Drobyski, Yurii Saroz, Natasha Grimsey, Michael Honer, Jürgen Fingerle, Klaus Gawrisch, Julian Romero, Cecilia J Hillard, Zoltan V Varga, Mario van der Stelt, Pal Pacher, Jürg Gertsch, Peter J McCormick, Christoph Ullmer, Sergio Oddi, Mauro Maccarrone, Dmitry B Veprintsev, Marc Nazare, Uwe Grether, Erick M Carreira
发表日期
2020/9/9
期刊
Journal of the American Chemical Society
卷号
142
期号
40
页码范围
16953-16964
出版商
American Chemical Society
简介
Pharmacological modulation of cannabinoid type 2 receptor (CB2R) holds promise for the treatment of numerous conditions, including inflammatory diseases, autoimmune disorders, pain, and cancer. Despite the significance of this receptor, researchers lack reliable tools to address questions concerning the expression and complex mechanism of CB2R signaling, especially in cell-type and tissue-dependent contexts. Herein, we report for the first time a versatile ligand platform for the modular design of a collection of highly specific CB2R fluorescent probes, used successfully across applications, species, and cell types. These include flow cytometry of endogenously expressing cells, real-time confocal microscopy of mouse splenocytes and human macrophages, as well as FRET-based kinetic and equilibrium binding assays. High CB2R specificity was demonstrated by competition experiments in living cells …
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