Selective Orthosteric Free Fatty Acid Receptor 2 (ffa2) Agonists: Identification of the Structural and Chemical Requirements for Selective Activation of Ffa2 versus Ffa3
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چکیده
SELECTIVE ORTHOSTERIC FREE FATTY ACID RECEPTOR 2 (FFA2) AGONISTS: IDENTIFICATION OF THE STRUCTURAL AND CHEMICAL REQUIREMENTS FOR SELECTIVE ACTIVATION OF FFA2 VERSUS FFA3 Johannes Schmidt, Nicola J. Smith, Elisabeth Christiansen, Irina G. Tikhonova, Manuel Grundmann, Brian D. Hudson, Richard J. Ward, Christel Drewke, Graeme Milligan, Evi Kostenis and Trond Ulven Molecular, Cellular, and Pharmacobiology Section, Institute of Pharmaceutical Biology, University of Bonn, Nußallee 6, 53115 Bonn, Germany, Molecular Pharmacology Group, Institute of Neuroscience and Psychology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, U.K., Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark, School of Pharmacy, Medical Biology Centre, Queen’s University Belfast BT9 7BL, Northern Ireland, United Kingdom. #both authors contributed equally *Address correspondence to: T. Ulven, Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark. Tel +45 655
منابع مشابه
Selective Orthosteric Free Fatty Acid Receptor 2 (FFA2) Agonists
Free fatty acid receptor 2 (FFA2; GPR43) is a G protein-coupled seven-transmembrane receptor for short-chain fatty acids (SCFAs) that is implicated in inflammatory and metabolic disorders. The SCFA propionate has close to optimal ligand efficiency for FFA2 and can hence be considered as highly potent given its size. Propionate, however, does not discriminate between FFA2 and the closely related...
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