Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probeElectronic supplementary information (ESI) available: Supplementary figures and tables; general synthetic methods; compound synthesis and characterization; molecular docking; in vitro pharmacology; fluorescence spectroscopy; TR-FRET kinetic CB2R binding assay; FACS analysis; time-lapse confocal imaging; in vivo zebrafish imaging; NMR spectra; and N-terminal SNAP-hCB2R sequence. CCDC 1923120. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/d1sc06659e

Authors: 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, Rufer, Arne C., Kusznir, Eric A., Huber, Sylwia, Raposo, Catarina, Zirwes, Elisabeth A., Osterwald, Anja, Pavlovic, Anto, Moes, Svenja, Beck, Jennifer, Nettekoven, Matthias, Benito-Cuesta, Irene, Grande, Teresa, Drawnel, Faye, Widmer, Gabriella, Holzer, Daniela, van der Wel, Tom, Mandhair, Harpreet, Honer, Michael, Fingerle, Jürgen, Scheffel, Jörg, Broichhagen, Johannes, Gawrisch, Klaus, Romero, Julián, Hillard, Cecilia J., Varga, Zoltan V., van der Stelt, Mario, Pacher, Pal, Gertsch, Jürg, Ullmer, Christoph, McCormick, Peter J., Oddi, Sergio, Spaink, Herman P., Maccarrone, Mauro, Veprintsev, Dmitry B., Carreira, Erick M., Grether, Uwe, Nazaré, Marc

Source: Chemical science. 13(19):5539-5545

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Cannabinoid receptor type 2 ligands: an analysis of granted patents since 2010

Authors: Brennecke, Benjamin, Gazzi, Thais, Atz, Kenneth, Fingerle, Jürgen, Kuner, Pascal, Schindler, Torsten, Weck, Guy de, Nazaré, Marc, Grether, Uwe

Source: Pharmaceutical patent analyst. 10(3):111-163

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100187979435.0x000001&indx=1&recIds=ETOCvdc_100187979435.0x000001

Infusions of Large Synthetic HDL Containing Trimeric apoA-I Stabilize Atherosclerotic Plaques in Hypercholesterolemic Rabbits

Authors: Parolini, Cinzia, Adorni, Maria Pia, Busnelli, Marco, Manzini, Stefano, Cipollari, Eleonora, Favari, Elda, Lorenzon, Paolo, Ganzetti, Giulia S., Fingerle, Juergen, Bernini, Franco, Chiesa, Giulia

Source: In Canadian Journal of Cardiology October 2019 35(10):1400-1408

RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models.

Authors: Grether, Uwe, Foxton, Richard H., Gruener, Sabine, Korn, Claudia, Kimbara, Atsushi, Osterwald, Anja, Zirwes, Elisabeth, Uhles, Sabine, Thoele, Janina, Colé, Nadine, Rogers-Evans, Mark, Röver, Stephan, Nettekoven, Matthias, Martin, Rainer E., Adam, Jean-Michel, Fingerle, Jürgen, Bissantz, Caterina, Guba, Wolfgang, Alker, André, Szczesniak, Anna M.

Source: Frontiers in Pharmacology; 2024, p1-20, 20p

Subject Terms: ANIMAL models of inflammation, CANNABINOID receptors, EYE inflammation, RETINAL diseases, DIABETIC retinopathy, THERAPEUTICS, CHO cell, RETROLENTAL fibroplasia

Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.

Authors: Aebia, Johannes, Atza, Kenneth, Ametamey, Simon M., Benza, Jörg, Blaising, Julie, Butini, Stefania, Campiani, Giuseppe, Carreira, Erick M., Collin, Ludovic, de Lago, Eva, Gazzi, Thais, Gertsch, Jürg, Gobbi, Luca, Guba, Wolfgang, Fernández-Ruize, Javier, Fingerle, Jürgen, Haider, Ahmed, Yingfang He, Heitman, Laura H., Honer, Michael

Source: Chimia; 2024, Vol. 78 Issue 7/8, p499-512, 14p

Regulated efflux of photoreceptor outer segment-derived cholesterol by human RPE cells

Authors: Storti, Federica, Raphael, Gabriele, Griesser, Vera, Klee, Katrin, Drawnel, Faye, Willburger, Carolin, Scholz, Rebecca, Langmann, Thomas, von Eckardstein, Arnold, Fingerle, Jürgen, Grimm, Christian, Maugeais, Cyrille

Source: In Experimental Eye Research December 2017 165:65-77

A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies

Authors: Martella, Andrea, Sijben, Huub, Rufer, Arne C., Grether, Uwe, Fingerle, Juergen, Ullmer, Christoph, Hartung, Thomas, IJzerman, Adriaan P., van der Stelt, Mario, Heitman, Laura H. ^*

Source: In Molecular Pharmacology October 2017 92(4):389-400

Selective Cathepsin S Inhibition Attenuates Atherosclerosis in Apolipoprotein E–Deficient Mice with Chronic Renal Disease

Authors: Figueiredo, Jose-Luiz, Aikawa, Masanori, Zheng, Chunyu, Aaron, Jacob, Lax, Lilian, Libby, Peter, de Lima Filho, Jose Luiz, Gruener, Sabine, Fingerle, Jürgen, Haap, Wolfgang, Hartmann, Guido, Aikawa, Elena

Source: In The American Journal of Pathology April 2015 185(4):1156-1166

Adenosine Attenuates Human Coronary Artery Smooth Muscle Cell Proliferation by Inhibiting Multiple Signaling Pathways That Converge on Cyclin D

Authors: Dubey, Raghvendra K., Fingerle, Jürgen, Gillespie, Delbert G., Mi, Zaichuan, Rosselli, Marinella, Imthurn, Bruno, Jackson, Edwin K.

Source: Hypertension. 66(6):1207-1219

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Trimerized apolipoprotein A-I (TripA) forms lipoproteins, activates lecithin:cholesterol acyltransferase, elicits lipid efflux, and is transported through aortic endothelial cells

Authors: Ohnsorg, Pascale M., Mary, Jean-Luc, Rohrer, Lucia, Pech, Michael, Fingerle, Jürgen, von Eckardstein, Arnold

Source: In BBA - Molecular and Cell Biology of Lipids December 2011 1811(12):1115-1123

Guinea Pig Chymase Is Leucine-specific: A NOVEL EXAMPLE OF FUNCTIONAL PLASTICITY IN THE CHYMASE/GRANZYME FAMILY OF SERINE PEPTIDASES

Authors: Caughey, George H., Beauchamp, Jeremy, Schlatter, Daniel, Raymond, Wilfred W., Trivedi, Neil N., Banner, David, Mauser, Harald, Fingerle, Jürgen

Source: In Journal of Biological Chemistry 16 May 2008 283(20):13943-13951

Methoxyestradiols Mediate the Antimitogenic Effects of Estradiol on Vascular Smooth Muscle Cells via Estrogen Receptor-Independent Mechanisms

Authors: Dubey, Raghvendra K., Gillespie, Delbert G., Zacharia, Lefteris C., Rosselli, Marinella, Korzekwa, Kenneth R., Fingerle, Juergen, Jackson, Edwin K.

Source: In Biochemical and Biophysical Research Communications 11 November 2000 278(1):27-33

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

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

Source: Journal of the American Chemical Society; October 2020, Vol. 142 Issue: 40 p16953-16964, 12p

Highly potent and selective cannabinoid receptor 2 agonists: Initial hit optimization of an adamantyl hit series identified from high-through-put screening

Authors: Nettekoven, Matthias, Fingerle, Jürgen, Grether, Uwe, Grüner, Sabine, Kimbara, Atsushi, Püllmann, Bernd, Rogers-Evans, Mark, Röver, Stephan, Schuler, Franz, Schulz-Gasch, Tanja, Ullmer, Christoph

Source: In Bioorganic & Medicinal Chemistry Letters 1 March 2013 23(5):1177-1181

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NF‐κB activation in astrocytes drives a stage‐specific beneficial neuroimmunological response in ALS.

Authors: Ouali Alami, Najwa, Schurr, Christine, Olde Heuvel, Florian, Tang, Linyun, Li, Qian, Tasdogan, Alpaslan, Kimbara, Atsushi, Nettekoven, Matthias, Ottaviani, Giorgio, Raposo, Catarina, Röver, Stephan, Rogers‐Evans, Mark, Rothenhäusler, Benno, Ullmer, Christoph, Fingerle, Jürgen, Grether, Uwe, Knuesel, Irene, Boeckers, Tobias M., Ludolph, Albert, Wirth, Thomas

Source: EMBO Journal; Aug2018, Vol. 37 Issue 16, p1-1, 23p, 12 Color Photographs, 1 Diagram, 2 Charts, 7 Graphs

Subject Terms: ASTROCYTES, AMYOTROPHIC lateral sclerosis, CELL proliferation, LEUKOCYTES, NEUROPROTECTIVE agents

Structure–Activity Relationship Studies of Pyridine-Based Ligands and Identification of a Fluorinated Derivative for Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors

Authors: Haider, Achi, Kretz, Julian, Gobbi, Luca, Ahmed, Hazem, Atz, Kenneth, Bürkler, Markus, Bartelmus, Christian, Fingerle, Jürgen, Guba, Wolfgang, Ullmer, Christoph, Honer, Michael, Knuesel, Irene, Weber, Markus, Brink, Andreas, Herde, Adrienne Müller, Keller, Claudia, Schibli, Roger, Mu, Linjing, Grether, Uwe, Ametamey, Simon M.

Source: Journal of Medicinal Chemistry; December 2019, Vol. 62 Issue: 24 p11165-11181, 17p

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