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Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)
Affiliation:1. Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States;2. Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States;3. Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States;1. Centre for Chronic Disease Prevention and Management, College of Health and Biomedicine, Victoria University, Melbourne 8001, Australia;2. Department of Physiology, The University of Melbourne, Melbourne 3010, Australia;1. Department of Animal Nutrition and Feed Science, College of Animal Science and Technology, Huazhong Agricultural University, Wuhan, 430070, China;2. The Cooperative Innovation Center for Sustainable Pig Production, Wuhan, 430070, China;3. Department of Anatomy, Physiology and Pharmacology, College of Veterinary Medicine, Auburn University, AL, 36849, USA;1. Instituto de Fisiología Celular, Universidad Nacional Autónoma de México. Ap., Postal 70-248, Ciudad de México 04510, Mexico;2. Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan;3. Medical Research Council Toxicology Unit, University of Leicester, Hodgkin building, Lancaster Road, Leicester LE1 9HN, United Kingdom;4. Molecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom;5. Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark
Abstract:The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
Keywords:Free fatty acid receptor 4  Free fatty acid receptor 4 agonist  Free fatty acid receptor 4 antagonist  FFA4  GPR120
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