A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence

Autor: 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

Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-19 (2023)

Abstract Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG) and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical potential is limited by central nervous system (CNS)-mediated s

Externí odkaz: https://doaj.org/article/fdb22352db0b4e3798c8149c29653a5f

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

Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells

Autor: Natasha L. Grimsey, Dmitry B. Veprintsev, Roman C. Sarott, Teresa Grande, Patrick Pfaff, Jürg Gertsch, Pal Pacher, Erick M. Carreira, Christoph Ullmer, Hermon Asmelash, Pattarin Hompluem, Svenja Moes, Daniela Holzer, Catarina Raposo, William R. Drobyski, Sylwia Huber, Jennifer Beck, Uwe Grether, Marc Nazaré, Claudia Korn, Zoltán Varga, Eline J. Koers, Jacopo Piovesan, Irene Benito-Cuesta, Klaus Gawrisch, Matthias Westphal, Benjamin Brennecke, Gabriella Widmer, Yurii Saroz, Eric Kusznir, Tom van der Wel, Anto Pavlovic, Kenneth Atz, Man C Vong, Tamara Miljuš, Peter J. McCormick, Mauro Maccarrone, Harpreet Mandhair, Samuel Ruiz de Martín Esteban, Sergio Oddi, Yelena Mostinski, Julián Romero, Elisabeth A. Zirwes, Anja Osterwald, Jürgen Fingerle, Cecilia J. Hillard, David A. Sykes, Alexei Yeliseev, Faye M. Drawnel, Mario van der Stelt, Marie Weise, Arne C. Rufer, Cheng-Yin Yuan, Thais Gazzi, Nicolas J. Roth, Michael Honer, Wolfgang Guba

Publikováno v: Journal of the American Chemical Society
Journal of the American Chemical Society, 142(40), 16953-16964

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 l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1774cb215365081fabff5fd4b151b22f
http://hdl.handle.net/11697/158602

Highly Specific, Fluorescent Cannabinoid Type 2 Receptor Probes Enable Applications in Microscopy, Flow Cytometry and FRET-based Binding Assays

Autor: Faye M. Drawnel, Mauro Maccarrone, Catarina Raposo, Peter J. McCormick, Jürgen Fingerle, Cecilia J. Hillard, Svenja Moes, Marc Nazaré, Sergio Oddi, Natasha L. Grimsey, David A. Sykes, Marie Weise, Sylwia Huber, Matthias Westphal, Yurii Saroz, William R. Drobyski, Anto Pavlovic, Gabriella Widmer, Patrick Pfaff, Dmitry B. Veprintsev, Benjamin Brennecke, Kenneth Atz, Anja Osterwald, Erick M. Carreira, Grether U, Julián Romero, Yelena Mostinski, Yuan C, Christoph Ullmer, Hermon Asmelash, Pattarin Hompluem, Gazzi, Thais, Tamara Miljuš, Daniela Holzer, Alexei Yeliseev, Roman C. Sarott, Stelt Mvd, Wel Tvd, Arne C. Rufer, Harpreet Mandhair, Claudia Korn, Elisabeth A. Zirwes, Zoltán Varga, Irene Benito-Cuesta, Jennifer Beck, Klaus Gawrisch, Teresa Grande, Nicolas J. Roth, Michael Honer, Wolfgang Guba, Vong M, Jürg Gertsch, Pal Pacher

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 its significance, researchers lack reliable tools

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2488c25f21762f3f55fbde432fa91266
https://doi.org/10.26434/chemrxiv.10288547