Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists

Autor: Miroslav Kosar, Roman C. Sarott, David A. Sykes, Alexander E. G. Viray, Rosa Maria Vitale, Nataša Tomašević, Xiaoting Li, Rudolf L. Z. Ganzoni, Bilal Kicin, Lisa Reichert, Kacper J. Patej, Uxía Gómez-Bouzó, Wolfgang Guba, Peter J. McCormick, Tian Hua, Christian W. Gruber, Dmitry B. Veprintsev, James A. Frank, Uwe Grether, Erick M. Carreira

Publikováno v: ACS Central Science, Vol 10, Iss 5, Pp 956-968 (2024)

Externí odkaz: https://doaj.org/article/a9641dd9dece4c6580e5b5242c4407b7

Cannabinoid CB2 Receptors Modulate Microglia Function and Amyloid Dynamics in a Mouse Model of Alzheimer’s Disease

Autor: Samuel Ruiz de Martín Esteban, Irene Benito-Cuesta, Itziar Terradillos, Ana M. Martínez-Relimpio, M. Andrea Arnanz, Gonzalo Ruiz-Pérez, Claudia Korn, Catarina Raposo, Roman C. Sarott, Matthias V. Westphal, Izaskun Elezgarai, Erick M. Carreira, Cecilia J. Hillard, Uwe Grether, Pedro Grandes, M. Teresa Grande, Julián Romero

Publikováno v: Frontiers in Pharmacology, Vol 13 (2022)

The distribution and roles of the cannabinoid CB2 receptor in the CNS are still a matter of debate. Recent data suggest that, in addition to its presence in microglial cells, the CB2 receptor may be also expressed at low levels, yet biologically rele

Externí odkaz: https://doaj.org/article/971c3ccb7b28416a96223192611a4cd6

Optical Control of Cannabinoid Receptor 2-Mediated Ca2+ Release Enabled by Synthesis of Photoswitchable Probes

Autor: Patrick Pfaff, Anastasiia Sadybekov, James A. Frank, Erick M. Carreira, Roman C. Sarott, Gabriela Rajic, Alexander E. G. Viray, Vsevolod Katritch

Publikováno v: Journal of the American Chemical Society. 143:736-743

Cannabinoid receptor 2 (CB2) is a promising target for the treatment of neuroinflammation and other diseases. However, a lack of understanding of its complex signaling in cells and tissues complicates the therapeutic exploitation of CB2 as a drug tar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::af8a05b7ad7e2f4608f36f1ce2375b07
https://doi.org/10.1021/jacs.0c08926

Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe

Autor: Thais Gazzi, Benjamin Brennecke, Kenneth Atz, Claudia Korn, David Sykes, Gabriel Forn-Cuni, Patrick Pfaff, Roman C. Sarott, Matthias V. Westphal, Yelena Mostinski, Leonard Mach, Malgorzata Wasinska-Kalwa, Marie Weise, Bradley L. Hoare, Tamara Miljuš, Maira Mexi, Nicolas Roth, Eline J. Koers, Wolfgang Guba, André Alker, Arne C. Rufer, Eric A. Kusznir, Sylwia Huber, Catarina Raposo, Elisabeth A. Zirwes, Anja Osterwald, Anto Pavlovic, Svenja Moes, Jennifer Beck, Matthias Nettekoven, Irene Benito-Cuesta, Teresa Grande, Faye Drawnel, Gabriella Widmer, Daniela Holzer, Tom van der Wel, Harpreet Mandhair, Michael Honer, Jürgen Fingerle, Jörg Scheffel, Johannes Broichhagen, Klaus Gawrisch, Julián Romero, Cecilia J. Hillard, Zoltan V. Varga, Mario van der Stelt, Pal Pacher, Jürg Gertsch, Christoph Ullmer, Peter J. McCormick, Sergio Oddi, Herman P. Spaink, Mauro Maccarrone, Dmitry B. Veprintsev, Erick M. Carreira, Uwe Grether, Marc Nazaré

Publikováno v: Gazzi, Thais; Brennecke, Benjamin; Atz, Kenneth; Korn, Claudia; Sykes, David; Forn-Cuni, Gabriel; Pfaff, Patrick; Sarott, Roman C; Westphal, Matthias V; Mostinski, Yelena; Mach, Leonard; Wasinska-Kalwa, Malgorzata; Weise, Marie; Hoare, Bradley L; Miljuš, Tamara; Mexi, Maira; Roth, Nicolas; Koers, Eline J; Guba, Wolfgang; Alker, André; ... (2022). Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe. Chemical Science, 13(19), pp. 5539-5545. The Royal Society of Chemistry 10.1039/d1sc06659e
Chemical Science, 13(19), 5539-5545
Chemical Science

Despite its essential role in the (patho)physiology of several diseases, CB2R tissue expression profiles and signaling mechanisms are not yet fully understood. We report the development of a highly potent, fluorescent CB2R agonist probe employing str

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69e61ac61b6e5b29da1ceeb545f2c056
http://hdl.handle.net/11697/192023

Light-mediated discovery of surfaceome nanoscale organization and intercellular receptor interaction networks

Autor: Milon Mondal, Fabian Wendt, Alexey I. Nesvizhskii, Bernd Wollscheid, Roman C. Sarott, Marc van Oostrum, Jeffrey W. Bode, Yannik Severin, Annette Oxenius, Maik Müller, Fabienne Gräbnitz, Sebastian N. Steiner, Martin J. Loessner, Niculò Barandun, John A. Robinson, Yang Shen, Stefan U. Vetterli, Berend Snijder, James R. Prudent, Erick M. Carreira, Raphael Hofmann

Publikováno v: Nature Communications, 12 (1)
Nature Communications
Nature Communications, Vol 12, Iss 1, Pp 1-17 (2021)

The molecular nanoscale organization of the surfaceome is a fundamental regulator of cellular signaling in health and disease. Technologies for mapping the spatial relationships of cell surface receptors and their extracellular signaling synapses wou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd97768bdf2a10cdbed425e23f40433c
https://hdl.handle.net/20.500.11850/518702