Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists

Author:

Kosar Miroslav1ORCID,Sarott Roman C.1ORCID,Sykes David A.23,Viray Alexander E. G.4,Vitale Rosa Maria5ORCID,Tomašević Nataša6,Li Xiaoting7,Ganzoni Rudolf L. Z.1,Kicin Bilal1ORCID,Reichert Lisa1,Patej Kacper J.1,Gómez-Bouzó Uxía1,Guba Wolfgang8ORCID,McCormick Peter J.9,Hua Tian7,Gruber Christian W.6ORCID,Veprintsev Dmitry B.23ORCID,Frank James A.410ORCID,Grether Uwe8ORCID,Carreira Erick M.1ORCID

Affiliation:

1. Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Vladimir-Prelog-Weg 3, 8093 Zürich, Switzerland

2. Faculty of Medicine & Health Sciences, University of Nottingham, Nottingham NG7 2UH, U.K.

3. Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham,

4. Department of Chemical Physiology & Biochemistry, Oregon Health & Science University, Portland, Oregon 97239-3098, United States

5. Institute of Biomolecular Chemistry, National Research Council, Via Campi Flegrei 34, 80078 Pozzuoli, Italy

6. Center for Physiology and Pharmacology, Medical University of Vienna, Schwarzspanierstrasse 17, 1090 Vienna, Austria

7. iHuman Institute, ShanghaiTech University, Shanghai 201210, China

8. Roche Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., 4070 Basel, Switzerland

9. Department of Pharmacology and Therapeutics, University of Liverpool, Ashton Street, Liverpool L69 3GE, U.K.

10. Vollum Institute, Oregon Health & Science University, Portland, Oregon 97239-3098, United States

Funder

Roche

Schweizerischer Nationalfonds zur F?rderung der Wissenschaftlichen Forschung

National Key Research and Development Program of China

Ministero dell?Istruzione, dell?Universit? e della Ricerca

European Cooperation in Science and Technology

Publisher

American Chemical Society (ACS)

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