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Chicca, Andrea; Bátora, Daniel; Ullmer, Christoph; Caruso, Antonello; Grüner, Sabine; Fingerle, Jürgen; Hartung, Thomas; Degen, Roland; Müller, Matthias; Grether, Uwe; Pacher, Pal; Gertsch, Jürg (2024). A Highly Potent, Orally Bioavailable Pyrazole-Derived Cannabinoid CB2 Receptor- Selective Full Agonist for In Vivo Studies. ACS pharmacology & translational science, 7(8), pp. 2424-2438. ACS Publications 10.1021/acsptsci.4c00269
Chicca, Andrea; Batora, Daniel; Ullmer, Christoph; Caruso, Antonello; Fingerle, Jürgen; Hartung, Thomas; Degen, Roland; Müller, Matthias; Grether, Uwe; Pacher, Pal; Gertsch, Jürg (29 April 2024). A highly potent, orally bioavailable pyrazole-derived cannabinoid CB2 receptor-selective full agonist for in vivo studies. (bioRxiv). Cold Spring Harbor Laboratory 10.1101/2024.04.26.591311
Di Stefano, Miriana; Masoni, Samuele; Bononi, Giulia; Poli, Giulio; Galati, Salvatore; Gado, Francesca; Manzi, Simone; Vagaggini, Chiara; Brai, Annalaura; Caligiuri, Isabella; Asif, Kanwal; Rizzolio, Flavio; Macchia, Marco; Chicca, Andrea; Sodi, Andrea; Di Bussolo, Valeria; Minutolo, Filippo; Meier, Philip; Gertsch, Jürg; Granchi, Carlotta; ... (2024). Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors. European journal of medicinal chemistry, 263(115916), p. 115916. Elsevier 10.1016/j.ejmech.2023.115916
Reynoso-Moreno, Ines; Rau, Mark; Chicca, Andrea; Nicolussi, Simon; Gertsch, Jürg (2023). Assay of Endocannabinoid Uptake. Methods in molecular biology, 2576, pp. 329-348. Springer 10.1007/978-1-0716-2728-0_28
Bononi, Giulia; Di Stefano, Miriana; Poli, Giulio; Ortore, Gabriella; Meier, Philip; Masetto, Francesca; Caligiuri, Isabella; Rizzolio, Flavio; Macchia, Marco; Chicca, Andrea; Avan, Amir; Giovannetti, Elisa; Vagaggini, Chiara; Brai, Annalaura; Dreassi, Elena; Valoti, Massimo; Minutolo, Filippo; Granchi, Carlotta; Gertsch, Jürg and Tuccinardi, Tiziano (2022). Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives. Journal of medicinal chemistry, 65(10), pp. 7118-7140. American Chemical Society 10.1021/acs.jmedchem.1c01806
Andrieu, Thomas; Chicca, Andrea; Pellegata, Daniele; Bersinger, Nick A.; Imboden, Sara; Nirgianakis, Konstantinos; Gertsch, Jürg; Mueller, Michael D. (2022). Association of endocannabinoids with pain in endometriosis. Pain, 163(1), pp. 193-203. Elsevier 10.1097/j.pain.0000000000002333
Schafroth, Michael A; Mazzoccanti, Giulia; Reynoso-Moreno, Ines; Erni, Reto; Pollastro, Federica; Caprioglio, Diego; Botta, Bruno; Allegrone, Gianna; Grassi, Giulio; Chicca, Andrea; Gasparrini, Francesco; Gertsch, Jürg; Carreira, Erick M; Appendino, Giovanni (2021). Δ9-cis-Tetrahydrocannabinol: Natural Occurrence, Chirality, and Pharmacology. Journal of natural products, 84(9), pp. 2502-2510. American Chemical Society 10.1021/acs.jnatprod.1c00513
Reynoso-Moreno, Ines; Tietz, Silvia; Vallini, Erika; Engelhardt, Britta; Gertsch, Jürg; Chicca, Andrea (2021). Selective Endocannabinoid Reuptake Inhibitor WOBE437 Reduces Disease Progression in a Mouse Model of Multiple Sclerosis. ACS pharmacology & translational science, 4(2), pp. 765-779. ACS Publications 10.1021/acsptsci.0c00214
Mäder, Patrick; Bartholomäus, Ruben; Nicolussi, Simon; Baumann, Alice; Weis, Melanie; Chicca, Andrea; Rau, Mark; Simão, Ana Catarina; Gertsch, Jürg; Altmann, Karl-Heinz (2021). Synthesis and Biological Evaluation of Endocannabinoid Uptake Inhibitors Derived from WOBE437. ChemMedChem, 16(1), pp. 145-154. Wiley-VCH 10.1002/cmdc.202000153
Granchi, Carlotta; Bononi, Giulia; Ferrisi, Rebecca; Gori, Eleonora; Mantini, Giulia; Glasmacher, Sandra; Poli, Giulio; Palazzolo, Stefano; Caligiuri, Isabella; Rizzolio, Flavio; Canzonieri, Vincenzo; Perin, Tiziana; Gertsch, Jürg; Sodi, Andrea; Giovannetti, Elisa; Macchia, Marco; Minutolo, Filippo; Tuccinardi, Tiziano; Chicca, Andrea (2021). Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. European journal of medicinal chemistry, 209, p. 112857. Elsevier 10.1016/j.ejmech.2020.112857
Arena, Chiara; Gado, Francesca; Di Cesare Mannelli, Lorenzo; Cervetto, Chiara; Carpi, Sara; Reynoso-Moreno, Ines; Polini, Beatrice; Vallini, Erika; Chicca, Stefano; Lucarini, Elena; Bertini, Simone; D'Andrea, Felicia; Digiacomo, Maria; Poli, Giulio; Tuccinardi, Tiziano; Macchia, Marco; Gertsch, Jürg; Marcoli, Manuela; Nieri, Paola; Ghelardini, Carla; ... (2020). The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis. European journal of medicinal chemistry, 208, p. 112858. Elsevier 10.1016/j.ejmech.2020.112858
Petrelli, Francesco; Dallérac, Glenn; Pucci, Luca; Calì, Corrado; Zehnder, Tamara; Sultan, Sébastien; Lecca, Salvatore; Chicca, Andrea; Ivanov, Andrei; Asensio, Cédric S; Gundersen, Vidar; Toni, Nicolas; Knott, Graham William; Magara, Fulvio; Gertsch, Jürg; Kirchhoff, Frank; Déglon, Nicole; Giros, Bruno; Edwards, Robert H; Mothet, Jean-Pierre; ... (2020). Dysfunction of homeostatic control of dopamine by astrocytes in the developing prefrontal cortex leads to cognitive impairments. Molecular psychiatry, 25(4), pp. 732-749. Nature Publishing Group 10.1038/s41380-018-0226-y
Gado, Francesca; Arena, Chiara; Fauci, Cristiana La; Reynoso-Moreno, Ines; Bertini, Simone; Digiacomo, Maria; Meini, Serena; Poli, Giulio; Macchia, Marco; Tuccinardi, Tiziano; Gertsch, Jürg; Chicca, Andrea; Manera, Clementina (2020). Modification on the 1,2-dihydro-2-oxo-pyridine-3-carboxamide core to obtain multi-target modulators of endocannabinoid system. Bioorganic chemistry, 94, p. 103353. Elsevier 10.1016/j.bioorg.2019.103353
Gaugaz, Fabienne Zdenka; Chicca, Andrea; Redondo-Horcajo, Mariano; Barasoain, Isabel; Díaz, J Fernando; Altmann, Karl-Heinz (2019). Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate. International journal of molecular sciences, 20(5) MDPI 10.3390/ijms20051113
Granchi, Carlotta; Lapillo, Margherita; Glasmacher, Sandra; Bononi, Giulia; Licari, Cristina; Poli, Giulio; El Boustani, Maguie; Caligiuri, Isabella; Rizzolio, Flavio; Gertsch, Jürg; Macchia, Marco; Minutolo, Filippo; Tuccinardi, Tiziano; Chicca, Andrea (2019). Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor. Journal of medicinal chemistry, 62(4), pp. 1932-1958. American Chemical Society 10.1021/acs.jmedchem.8b01483
Chicca, Andrea; Schafroth, M A; Reynoso, Ines del Carmen; Erni, R; Petrucci, Vanessa; Carreira, E M; Gertsch, Jürg (2018). Uncovering the psychoactivity of a cannabinoid from liverworts associated with a legal high. Science Advances, 4(10), eaat2166. American Association for the Advancement of Science 10.1126/sciadv.aat2166
Bononi, Giulia; Granchi, Carlotta; Lapillo, Margherita; Giannotti, Massimiliano; Nieri, Daniela; Fortunato, Serena; Boustani, Maguie El; Caligiuri, Isabella; Poli, Giulio; Carlson, Kathryn E; Kim, Sung Hoon; Macchia, Marco; Martinelli, Adriano; Rizzolio, Flavio; Chicca, Andrea; Katzenellenbogen, John A; Minutolo, Filippo; Tuccinardi, Tiziano (2018). Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors. European journal of medicinal chemistry, 157, pp. 817-836. Elsevier Masson SAS 10.1016/j.ejmech.2018.08.038
Chicca, Andrea; Arena, Chiara; Bertini, Simone; Gado, Francesca; Ciaglia, Elena; Abate, Mario; Digiacomo, Maria; Lapillo, Margherita; Poli, Giulio; Bifulco, Maurizio; Macchia, Marco; Tuccinardi, Tiziano; Gertsch, Jürg; Manera, Clementina (2018). Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system. European journal of medicinal chemistry, 154, pp. 155-171. Elsevier 10.1016/j.ejmech.2018.05.019
Aghazadeh Tabrizi, Mojgan; Baraldi, Pier Giovanni; Baraldi, Stefania; Ruggiero, Emanuela; De Stefano, Lucia; Rizzolio, Flavio; Di Cesare Mannelli, Lorenzo; Ghelardini, Carla; Chicca, Andrea; Lapillo, Margherita; Gertsch, Jürg; Manera, Clementina; Macchia, Marco; Martinelli, Adriano; Granchi, Carlotta; Minutolo, Filippo; Tuccinardi, Tiziano (2018). Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors. Journal of medicinal chemistry, 61(3), pp. 1340-1354. American Chemical Society 10.1021/acs.jmedchem.7b01845
Varga, Zoltan V; Matyas, Csaba; Erdelyi, Katalin; Cinar, Resat; Nieri, Daniela; Chicca, Andrea; Nemeth, Balazs Tamas; Paloczi, Janos; Lajtos, Tamas; Corey, Lukas; Hasko, Gyorgy; Gao, Bin; Kunos, George; Gertsch, Jürg; Pacher, Pal (2018). Beta-caryophyllene protects against alcoholic steatohepatitis by attenuating inflammation and metabolic dysregulation in mice. British journal of pharmacology, 175(2), pp. 320-334. Wiley-Blackwell 10.1111/bph.13722
Reynoso, Ines del Carmen; Chicca, Andrea; Flores-Soto, Mario E; Viveros-Paredes, Juan M; Gertsch, Jürg (2018). The Endocannabinoid Reuptake Inhibitor WOBE437 Is Orally Bioavailable and Exerts Indirect Polypharmacological Effects via Different Endocannabinoid Receptors. Frontiers in molecular neuroscience, 11, p. 180. Frontiers Research Foundation 10.3389/fnmol.2018.00180
Bertini, Simone; Chicca, Andrea; Gado, Francesca; Arena, Chiara; Nieri, Daniela; Digiacomo, Maria; Saccomanni, Giuseppe; Zhao, Pingwei; Abood, Mary E; Macchia, Marco; Gertsch, Jürg; Manera, Clementina (2017). Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. Bioorganic & medicinal chemistry, 25(24), pp. 6427-6434. Elsevier 10.1016/j.bmc.2017.10.015
Chicca, Andrea; Berg, Regina; Jessen, Henning J; Marck, Nicolas; Schmid, Fabian; Burch, Patrick; Gertsch, Jürg; Gademann, Karl (2017). Biological evaluation of pyridone alkaloids on the endocannabinoid system. Bioorganic & medicinal chemistry, 25(22), pp. 6102-6114. Elsevier 10.1016/j.bmc.2017.02.031
Patsenker, Eleonora; Chicca, Andrea; Petrucci, Vanessa; Moghadamrad, Sheida; De Gottardi, Andrea; Hampe, Jochen; Gertsch, Jürg; Semmo, Nasser; Stickel, Felix (2017). 4-O'-methylhonokiol protects from alcohol/carbon tetrachloride-induced liver injury in mice. Journal of molecular medicine JMM, 95(10), pp. 1077-1089. Springer 10.1007/s00109-017-1556-y
Petrucci, Vanessa; Chicca, Andrea; Glasmacher, Sandra Patricia; Paloczi, Janos; Cao, Zongxian; Pacher, Pal; Gertsch, Jürg (2017). Pepcan-12 (RVD-hemopressin) is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage. Scientific Reports, 7(1), p. 9560. Nature Publishing Group 10.1038/s41598-017-09808-8
Chicca, Andrea; Nicolussi, Simon; Bartholomäus, Ruben; Blunder, Martina; Aparisi Rey, Alejandro; Petrucci, Vanessa; Reynoso, Ines del Carmen; Viveros-Paredes, Juan Manuel; Dalghi Gens, Marianela Gisela; Lutz, Beat; Schiöth, Helgi B; Soeberdt, Michael; Abels, Christoph; Charles, Roch-Philippe; Altmann, Karl-Heinz; Gertsch, Jürg (2017). Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake. Proceedings of the National Academy of Sciences of the United States of America - PNAS, 114(25), E5006-E5015. National Academy of Sciences NAS 10.1073/pnas.1704065114
Soethoudt, Marjolein; Grether, Uwe; Fingerle, Jürgen; Grim, Travis W; Fezza, Filomena; de Petrocellis, Luciano; Ullmer, Christoph; Rothenhäusler, Benno; Perret, Camille; van Gils, Noortje; Finlay, David; MacDonald, Christa; Chicca, Andrea; Gens, Marianela Dalghi; Stuart, Jordyn; de Vries, Henk; Mastrangelo, Nicolina; Xia, Lizi; Alachouzos, Georgios; Baggelaar, Marc P; ... (2017). Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. Nature communications, 8(13958), p. 13958. Nature Publishing Group 10.1038/ncomms13958
Bertini, Simone; Chicca, Andrea; Arena, Chiara; Chicca, Stefano; Saccomanni, Giuseppe; Gertsch, Jürg; Manera, Clementina; Macchia, Marco (2016). Synthesis and pharmacological evaluation of new biphenylic derivatives as CB2 receptor ligands. European journal of medicinal chemistry, 116, pp. 252-266. Elsevier Masson SAS 10.1016/j.ejmech.2016.03.072
Rau, Mark; Nicolussi, Simon; Chicca, Andrea; Gertsch, Jürg (2016). Assay of Endocannabinoid Uptake. In: Maccarrone, Mauro (ed.) Endocannabinoid Signaling. Methods and Protocols. Methods in Molecular Biology: Vol. 1412 (pp. 191-203). New York: Springer 10.1007/978-1-4939-3539-0_20
Iakovenko, Roman O; Kazakova, Anna N; Muzalevskiy, Vasiliy M; Ivanov, Alexander Yu; Boyarskaya, Irina A; Chicca, Andrea; Petrucci, Vanessa; Gertsch, Jürg; Krasavin, Mikhail; Starova, Galina L; Zolotarev, Andrey A; Avdontceva, Margarita S; Nenajdenko, Valentine G; Vasilyev, Aleksander V (2015). Reactions of CF3-enones with arenes under superelectrophilic activation: a pathway to trans-1,3-diaryl-1-CF3-indanes, new cannabinoid receptor ligands. Organic & biomolecular chemistry, 13(33), pp. 8827-8842. Royal Society of Chemistry 10.1039/c5ob01072a
Del Carlo, S; Manera, C; Chicca, Andrea; Arena, C; Bertini, S; Burgalassi, S; Tampucci, S; Gertsch, Jürg; Macchia, M; Saccomanni, G (2015). Development of an HPLC/UV assay for the evaluation of inhibitors of human recombinant monoacylglycerol lipase. Journal of pharmaceutical and biomedical analysis, 108, pp. 113-121. Pergamon Press 10.1016/j.jpba.2015.02.007
Patsenker, Eleanora; Sachse, Philip; Chicca, Andrea; Gachet Otanez, Maria Salomé; Schneider, Vreni; Mattsson, Johan; Lanz, Christian; Worni, Mathias; De Gottardi, Andrea; Semmo, Mariam; Hampe, Jochen; Schafmayer, Clemens; Brenneisen, Rudolf Max; Gertsch, Jürg; Stickel, Felix; Semmo, Nasser (2015). Elevated levels of endocannabinoids in chronic hepatitis C may modulate cellular immune response and hepatic stellate cell activation. International journal of molecular sciences, 16(4), pp. 7057-7076. MDPI 10.3390/ijms16047057
Chicca, Andrea; Gachet Otanez, Maria Salomé; Petrucci, Vanessa; Schuehly, Wolfgang; Charles, Roch-Philippe; Gertsch, Jürg (2015). 4'-O-methylhonokiol increases levels of 2-arachidonoyl glycerol in mouse brain via selective inhibition of its COX-2-mediated oxygenation. Journal of neuroinflammation, 12, p. 89. BioMed Central 10.1186/s12974-015-0307-7
Nicolussi, Simon; Chicca, Andrea; Rau, Mark; Rihs, Sabine; Soeberdt, Michael; Abels, Christoph; Gertsch, Jürg (2014). Correlating FAAH and anandamide cellular uptake inhibition using N-alkylcarbamate inhibitors: from ultrapotent to hyperpotent. Biochemical pharmacology, 92(4), pp. 669-689. Elsevier 10.1016/j.bcp.2014.09.020
Rosati, Ornelio; Messina, Federica; Pelosi, Azzurra; Curini, Massimo; Petrucci, Vanessa; Gertsch, Jürg; Chicca, Andrea (2014). One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors. European journal of medicinal chemistry, 85, pp. 77-86. Elsevier Masson SAS 10.1016/j.ejmech.2014.07.062
Chicca, Andrea; Caprioglio, Diego; Minassi, Alberto; Petrucci, Vanessa; Appendino, Giovanni; Taglialatela-Scafati, Orazio; Gertsch, Jürg (2014). Functionalization of β-caryophyllene generates novel polypharmacology in the endocannabinoid system. ACS Chemical Biology, 9(7), pp. 1499-1507. American Chemical Society 10.1021/cb500177c
Burch, Patrick; Chicca, Andrea; Gertsch, Jürg; Gademann, Karl (2014). Functionally Optimized Neuritogenic Farinosone C Analogs: SAR-Study and Investigations on Their Mode of Action. ACS medicinal chemistry letters, 5(2), pp. 172-177. American Chemical Society 10.1021/ml400435h
Adinolfi, Barbara; Romanini, Antonella; Vanni, Alessia; Martinotti, Enrica; Chicca, Andrea; Fogli, Stefano; Nieri, Paola (2013). Anticancer activity of anandamide in human cutaneous melanoma cells. European journal of pharmacology, 718(1-3), pp. 154-159. Elsevier 10.1016/j.ejphar.2013.08.039
Simonin, Jonathan; Jack, Thomas; Ruepp, Marc-David; Hothersall, Daniel; Connolly, Christopher; Chicca, Andrea; Gertsch, Jürg; Thompson, Andrew James; Lummis, Sarah C. R.; Lochner, Martin (August 2013). Synthesis of fluorescent probes for the study of the 5-HT3 receptor: applications in imaging and fluorescence polarization. CHIMIA, 67(7/8), p. 524. Schweizerische Chemische Gesellschaft
