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

Miroslav Kosar; Roman C. Sarott; David A. Sykes; Alexander E. G. Viray; Rosa Maria Vitale; Nataša Tomašević; Xiaoting Li; Rudolf L. Z. Ganzoni; Bilal Kicin; Lisa Reichert; Kacper J. Patej; Uxía Gómez-Bouzó; Wolfgang Guba; Peter J. McCormick; Tian Hua; Christian W. Gruber; Dmitry B. Veprintsev; James A. Frank; Uwe Grether; Erick M. Carreira

doi:10.1021/acscentsci.3c01461

ACS Central Science (Mar 2024)

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

Miroslav Kosar,
Roman C. Sarott,
David A. Sykes,
Alexander E. G. Viray,
Rosa Maria Vitale,
Nataša Tomašević,
Xiaoting Li,
Rudolf L. Z. Ganzoni,
Bilal Kicin,
Lisa Reichert,
Kacper J. Patej,
Uxía Gómez-Bouzó,
Wolfgang Guba,
Peter J. McCormick,
Tian Hua,
Christian W. Gruber,
Dmitry B. Veprintsev,
James A. Frank,
Uwe Grether,
Erick M. Carreira

Affiliations

Miroslav Kosar: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland
Roman C. Sarott: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland
David A. Sykes: Faculty of Medicine & Health Sciences, University of Nottingham, Nottingham, U.K.
Alexander E. G. Viray: Department of Chemical Physiology & Biochemistry, Oregon Health & Science University, Portland, Oregon, United States
Rosa Maria Vitale: Institute of Biomolecular Chemistry, National Research Council, Pozzuoli, Italy
Nataša Tomašević: Center for Physiology and Pharmacology, Medical University of Vienna, Vienna, Austria
Xiaoting Li: iHuman Institute, ShanghaiTech University, Shanghai, China
Rudolf L. Z. Ganzoni: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland
Bilal Kicin: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland
Lisa Reichert: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland
Kacper J. Patej: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland
Uxía Gómez-Bouzó: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland
Wolfgang Guba: Roche Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland
Peter J. McCormick: Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool, U.K.
Tian Hua: iHuman Institute, ShanghaiTech University, Shanghai, China
Christian W. Gruber: Center for Physiology and Pharmacology, Medical University of Vienna, Vienna, Austria
Dmitry B. Veprintsev: Faculty of Medicine & Health Sciences, University of Nottingham, Nottingham, U.K.
James A. Frank: Department of Chemical Physiology & Biochemistry, Oregon Health & Science University, Portland, Oregon, United States
Uwe Grether: Roche Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland
Erick M. Carreira: Laboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland

DOI: https://doi.org/10.1021/acscentsci.3c01461
Journal volume & issue: Vol. 10, no. 5
pp. 956 – 968

Abstract

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Published in ACS Central Science

ISSN: 2374-7951 (Online)
Publisher: American Chemical Society
Country of publisher: United States
LCC subjects: Science: Chemistry
Website: https://pubs.acs.org/journal/acscii

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