Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization

Author:

Butini Stefania1ORCID,Grether Uwe2ORCID,Jung Kwang-Mook3ORCID,Ligresti Alessia4ORCID,Allarà Marco4,Postmus Annemarieke G. J.5,Maramai Samuele1ORCID,Brogi Simone6ORCID,Papa Alessandro1,Carullo Gabriele1ORCID,Sykes David78,Veprintsev Dmitry7ORCID,Federico Stefano1ORCID,Grillo Alessandro1,Di Guglielmo Bruno1,Ramunno Anna9ORCID,Stevens Anna Floor5,Heer Dominik2ORCID,Lamponi Stefania1,Gemma Sandra1ORCID,Benz Jörg2,Di Marzo Vincenzo410111213,van der Stelt Mario5,Piomelli Daniele3ORCID,Campiani Giuseppe114

Affiliation:

1. Department of Biotechnology, Chemistry and Pharmacy, University of Siena, via Aldo Moro 2, 53100 Siena, Italy

2. Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd, CH-4070 Basel, Switzerland

3. Department of Anatomy and Neurobiology, University of California Irvine, Irvine, California 92697, United States

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

5. Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University and Oncode Institute, 2300 CC, Leiden, Netherlands

6. Department of Pharmacy, University of Pisa, via Bonanno, 56126 Pisa, Italy

7. Faculty of Medicine & Health Sciences, University of Nottingham, Nottingham NG7 2UH, United Kingdom

8. Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Edgbaston, B15 2TT Birmingham, Midlands, United Kingdom

9. Department of Pharmacy/DIFARMA, University of Salerno, via Giovanni Paolo II 132, Salerno 84084, Fisciano, Italy

10. Centre Nutrition, Santé et Société (NUTRISS), Institut sur La Nutrition Et Les Aliments Fonctionnels (INAF), École de Nutrition, Université Laval, 2440 Boulevard Hochelaga, Québec G1V 0A6, Canada

11. Canada Excellence Research Chair in the Microbiome-Endocannabinoidome Axis in Metabolic Health, PO Box 2325, Quebec G1V 0A6, Canada

12. Centre de Recherche de l’Institut de Cardiologie et de Pneumologie de Québec, Faculté de Médecine, Département de Médecine, Université Laval, PO Box 2725, Québec G1V 4G5, Canada

13. Unité Mixte Internationale en Recherche Chimique et Biomoléculaire sur le Microbiome et Son Impact Sur la Santé Métabolique et la Nutrition (UMI-MicroMeNu), Université Laval, PO Box 2325, Quebec G1V 0A6, Canada

14. Bioinformatics Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan 81746-7346, Iran

Funder

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

U.S. Department of Health and Human Services

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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