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Your search keyword '"van der Stelt, Mario"' showing total 7 results
Start Over Author "van der Stelt, Mario" Journal nature communications
7 results on '"van der Stelt, Mario"'

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

Author

Jiang, Ming, Huizenga, Mirjam C. W., Wirt, Jonah L., Paloczi, Janos, Amedi, Avand, van den Berg, Richard J. B. H. N., Benz, Joerg, Collin, Ludovic, Deng, Hui, Di, Xinyu, Driever, Wouter F., Florea, Bogdan I., Grether, Uwe, Janssen, Antonius P. A., Hankemeier, Thomas, Heitman, Laura H., Lam, Tsang-Wai, Mohr, Florian, Pavlovic, Anto, Ruf, Iris, van den Hurk, Helma, Stevens, Anna F., van der Vliet, Daan, van der Wel, Tom, Wittwer, Matthias B., van Boeckel, Constant A. A., Pacher, Pal, Hohmann, Andrea G., and van der Stelt, Mario

Published
2023
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2. Structural basis of selective cannabinoid CB2 receptor activation

Author

Li, Xiaoting, Chang, Hao, Bouma, Jara, de Paus, Laura V., Mukhopadhyay, Partha, Paloczi, Janos, Mustafa, Mohammed, van der Horst, Cas, Kumar, Sanjay Sunil, Wu, Lijie, Yu, Yanan, van den Berg, Richard J. B. H. N., Janssen, Antonius P. A., Lichtman, Aron, Liu, Zhi-Jie, Pacher, Pal, van der Stelt, Mario, Heitman, Laura H., and Hua, Tian

Published
2023
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5. Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity

Author

Soethoudt, Marjolein, primary, Grether, Uwe, additional, Fingerle, Jürgen, additional, Grim, Travis W., additional, Fezza, Filomena, additional, de Petrocellis, Luciano, additional, Ullmer, Christoph, additional, Rothenhäusler, Benno, additional, Perret, Camille, additional, van Gils, Noortje, additional, Finlay, David, additional, MacDonald, Christa, additional, Chicca, Andrea, additional, Gens, Marianela Dalghi, additional, Stuart, Jordyn, additional, de Vries, Henk, additional, Mastrangelo, Nicolina, additional, Xia, Lizi, additional, Alachouzos, Georgios, additional, Baggelaar, Marc P., additional, Martella, Andrea, additional, Mock, Elliot D., additional, Deng, Hui, additional, Heitman, Laura H., additional, Connor, Mark, additional, Di Marzo, Vincenzo, additional, Gertsch, Jürg, additional, Lichtman, Aron H., additional, Maccarrone, Mauro, additional, Pacher, Pal, additional, Glass, Michelle, additional, and van der Stelt, Mario, additional

Published
2017
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6. Identification of an allosteric binding site for RORγt inhibition

Author

Scheepstra, Marcel, primary, Leysen, Seppe, additional, van Almen, Geert C., additional, Miller, J. Richard, additional, Piesvaux, Jennifer, additional, Kutilek, Victoria, additional, van Eenennaam, Hans, additional, Zhang, Hongjun, additional, Barr, Kenneth, additional, Nagpal, Sunil, additional, Soisson, Stephen M., additional, Kornienko, Maria, additional, Wiley, Kristen, additional, Elsen, Nathaniel, additional, Sharma, Sujata, additional, Correll, Craig C., additional, Trotter, B. Wesley, additional, van der Stelt, Mario, additional, Oubrie, Arthur, additional, Ottmann, Christian, additional, Parthasarathy, Gopal, additional, and Brunsveld, Luc, additional

Published
2015
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7. Cannabinoid CB 2 receptor ligand profiling reveals biased signalling and off-target activity.

Author

Soethoudt M, Grether U, Fingerle J, Grim TW, Fezza F, de Petrocellis L, Ullmer C, Rothenhäusler B, Perret C, van Gils N, Finlay D, MacDonald C, Chicca A, Gens MD, Stuart J, de Vries H, Mastrangelo N, Xia L, Alachouzos G, Baggelaar MP, Martella A, Mock ED, Deng H, Heitman LH, Connor M, Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M, Pacher P, Glass M, and van der Stelt M

Subjects
Animals, Bridged Bicyclo Compounds pharmacology, CHO Cells, Cannabinoids pharmacology, Cell Line, Tumor, Cricetulus, Gene Expression, HEK293 Cells, High-Throughput Screening Assays, Humans, Keratinocytes cytology, Keratinocytes drug effects, Keratinocytes metabolism, Kinetics, Ligands, Macrophages cytology, Macrophages drug effects, Macrophages metabolism, Mice, Neurons cytology, Neurons metabolism, Protein Binding, Receptor, Cannabinoid, CB1 genetics, Receptor, Cannabinoid, CB2 genetics, Cannabinoid Receptor Agonists pharmacology, Neurons drug effects, Receptor, Cannabinoid, CB1 metabolism, Receptor, Cannabinoid, CB2 metabolism, Signal Transduction
Abstract

The cannabinoid CB 2 receptor (CB 2 R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB 2 R, their selectivity, molecular mode of action and pharmacokinetic properties have been poorly characterized. Here we report the most extensive characterization of the molecular pharmacology of the most widely used CB 2 R ligands to date. In a collaborative effort between multiple academic and industry laboratories, we identify marked differences in the ability of certain agonists to activate distinct signalling pathways and to cause off-target effects. We reach a consensus that HU910, HU308 and JWH133 are the recommended selective CB 2 R agonists to study the role of CB 2 R in biological and disease processes. We believe that our unique approach would be highly suitable for the characterization of other therapeutic targets in drug discovery research., Competing Interests: Industry authors U.G., J.F., C.U., B.R. and C.P. are full-time employees of Hoffmann-La Roche and P.P. is full time employee of NIH. All academic authors state that they have no conflict of interest.

Published
2017
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