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Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
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, van der Stelt M. Soethoudt M, et al. Among authors: gertsch j. Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958. Nat Commun. 2017. PMID: 28045021 Free PMC article.
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
Granchi C, Lapillo M, Glasmacher S, Bononi G, Licari C, Poli G, El Boustani M, Caligiuri I, Rizzolio F, Gertsch J, Macchia M, Minutolo F, Tuccinardi T, Chicca A. Granchi C, et al. Among authors: gertsch j. J Med Chem. 2019 Feb 28;62(4):1932-1958. doi: 10.1021/acs.jmedchem.8b01483. Epub 2019 Feb 11. J Med Chem. 2019. PMID: 30715876
Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
Granchi C, Bononi G, Ferrisi R, Gori E, Mantini G, Glasmacher S, Poli G, Palazzolo S, Caligiuri I, Rizzolio F, Canzonieri V, Perin T, Gertsch J, Sodi A, Giovannetti E, Macchia M, Minutolo F, Tuccinardi T, Chicca A. Granchi C, et al. Among authors: gertsch j. Eur J Med Chem. 2021 Jan 1;209:112857. doi: 10.1016/j.ejmech.2020.112857. Epub 2020 Oct 7. Eur J Med Chem. 2021. PMID: 33045662
Mitochondrial CB₁ receptors regulate neuronal energy metabolism.
Bénard G, Massa F, Puente N, Lourenço J, Bellocchio L, Soria-Gómez E, Matias I, Delamarre A, Metna-Laurent M, Cannich A, Hebert-Chatelain E, Mulle C, Ortega-Gutiérrez S, Martín-Fontecha M, Klugmann M, Guggenhuber S, Lutz B, Gertsch J, Chaouloff F, López-Rodríguez ML, Grandes P, Rossignol R, Marsicano G. Bénard G, et al. Among authors: gertsch j. Nat Neurosci. 2012 Mar 4;15(4):558-64. doi: 10.1038/nn.3053. Nat Neurosci. 2012. PMID: 22388959
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
Bertini S, Chicca A, Gado F, Arena C, Nieri D, Digiacomo M, Saccomanni G, Zhao P, Abood ME, Macchia M, Gertsch J, Manera C. Bertini S, et al. Among authors: gertsch j. Bioorg Med Chem. 2017 Dec 15;25(24):6427-6434. doi: 10.1016/j.bmc.2017.10.015. Epub 2017 Oct 16. Bioorg Med Chem. 2017. PMID: 29079014 Free PMC article.
216 results