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

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Title: Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.
Authors: Soethoudt M; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.; Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Grether U; Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland., Fingerle J; Department of Biochemistry, NMI, University Tübingen, Markwiesenstrasse 55, Reutlingen 72770, Germany., Grim TW; Department of Pharmacology and Toxicology, 1220 East Broad Street, PO Box 980613, Richmond, Virginia 23298-0613, USA., Fezza F; Department of Experimental Medicine and Surgery, Tor Vergata University of Rome, Via Montpellier 1, Rome 00133, Italy.; European Center for Brain Research/IRCCS Santa Lucia Foundation, via del Fosso del Fiorano 65, Rome 00143, Italy., de Petrocellis L; Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R., Via Campi Flegrei 34, Comprensorio Olivetti, Pozzuoli 80078, Italy., Ullmer C; Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland., Rothenhäusler B; Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland., Perret C; Roche Innovation Center Basel, F. Hoffman-La Roche Ltd., Grenzachterstrasse 124, Basel 4070, Switzerland., van Gils N; Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Finlay D; Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland, 85 Park road, Grafton, Auckland 1023, New Zealand., MacDonald C; Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland, 85 Park road, Grafton, Auckland 1023, New Zealand., Chicca A; Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse 28, Bern CH-3012, Switzerland., Gens MD; Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse 28, Bern CH-3012, Switzerland., Stuart J; Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University, North Ryde, New South Wales 2109, Australia., de Vries H; Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Mastrangelo N; Department of Medicine, Campus Bio-Medico University of Rome, Via Alvaro del Portillo 21, Rome 00128, Italy., Xia L; Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Alachouzos G; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Baggelaar MP; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Martella A; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.; Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Mock ED; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Deng H; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Heitman LH; Department of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands., Connor M; Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Macquarie University, North Ryde, New South Wales 2109, Australia., Di Marzo V; Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R., Via Campi Flegrei 34, Comprensorio Olivetti, Pozzuoli 80078, Italy., Gertsch J; Institute of Biochemistry and Molecular Medicine, University of Bern, Bühlstrasse 28, Bern CH-3012, Switzerland., Lichtman AH; Department of Pharmacology and Toxicology, 1220 East Broad Street, PO Box 980613, Richmond, Virginia 23298-0613, USA., Maccarrone M; European Center for Brain Research/IRCCS Santa Lucia Foundation, via del Fosso del Fiorano 65, Rome 00143, Italy.; Department of Medicine, Campus Bio-Medico University of Rome, Via Alvaro del Portillo 21, Rome 00128, Italy., Pacher P; Laboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/NIAAA, 5625 Fishers Lane, Rockville, Maryland 20852, USA., Glass M; Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland, 85 Park road, Grafton, Auckland 1023, New Zealand., van der Stelt M; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
Source: Nature communications [Nat Commun] 2017 Jan 03; Vol. 8, pp. 13958. Date of Electronic Publication: 2017 Jan 03.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: Nature Pub. Group Country of Publication: England NLM ID: 101528555 Publication Model: Electronic Cited Medium: Internet ISSN: 2041-1723 (Electronic) Linking ISSN: 20411723 NLM ISO Abbreviation: Nat Commun Subsets: MEDLINE
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  Data: Cannabinoid CB<subscript>2</subscript> receptor ligand profiling reveals biased signalling and off-target activity.
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Department of Pharmacology and Toxicology, 1220 East Broad Street, PO Box 980613, Richmond, Virginia 23298-0613, USA.<br /><searchLink fieldCode="AU" term="%22Maccarrone+M%22">Maccarrone M</searchLink>; European Center for Brain Research/IRCCS Santa Lucia Foundation, via del Fosso del Fiorano 65, Rome 00143, Italy.; Department of Medicine, Campus Bio-Medico University of Rome, Via Alvaro del Portillo 21, Rome 00128, Italy.<br /><searchLink fieldCode="AU" term="%22Pacher+P%22">Pacher P</searchLink>; Laboratory of Cardiovascular Physiology and Tissue Injury, National Institute of Health/NIAAA, 5625 Fishers Lane, Rockville, Maryland 20852, USA.<br /><searchLink fieldCode="AU" term="%22Glass+M%22">Glass M</searchLink>; Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, University of Auckland, 85 Park road, Grafton, Auckland 1023, New Zealand.<br /><searchLink fieldCode="AU" term="%22van+der+Stelt+M%22">van der Stelt M</searchLink>; Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, Leiden 2333 CC, The Netherlands.
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