Defining the Molecular Basis for the First Potent and Selective Orthosteric Agonists of the FFA2 Free Fatty Acid Receptor

Lifting the lid on GPCRs: the role of extracellular loops

(2012) M Wheatley et al.   BRITISH JOURNAL OF PHARMACOLOGY

Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs

(2012) Brian D. Hudson et al.   FASEB JOURNAL

Extracellular Ionic Locks Determine Variation in Constitutive Activity and Ligand Potency between Species Orthologs of the Free Fatty Acid Receptors FFA2 and FFA3

(2012) Brian D. Hudson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Potent and Selective GPR120 Agonist

(2012) Bharat Shimpukade et al.   JOURNAL OF MEDICINAL CHEMISTRY

Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists: Mesylpropoxy Appendage Lowers Lipophilicity and Improves ADME Properties

(2012) Elisabeth Christiansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets

(2012) Trond Ulven   Frontiers in Endocrinology

AMG 837: A potent, orally bioavailable GPR40 agonist

(2011) Jonathan B. Houze et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Short-Chain Fatty Acids Stimulate Glucagon-Like Peptide-1 Secretion via the G-Protein-Coupled Receptor FFAR2

(2011) G. Tolhurst et al.   DIABETES

Selective Orthosteric Free Fatty Acid Receptor 2 (FFA2) Agonists

(2011) Johannes Schmidt et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of a Potent and Selective Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist with Favorable Physicochemical and in Vitro ADME Properties

(2011) Elisabeth Christiansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Extracellular Loop 2 of the Free Fatty Acid Receptor 2 Mediates Allosterism of a Phenylacetamide Ago-Allosteric Modulator

(2011) N. J. Smith et al.   MOLECULAR PHARMACOLOGY

SCFAs Induce Mouse Neutrophil Chemotaxis through the GPR43 Receptor

(2011) Marco A. R. Vinolo et al.   PLoS One

GPR120 Is an Omega-3 Fatty Acid Receptor Mediating Potent Anti-inflammatory and Insulin-Sensitizing Effects

(2010) Da Young Oh et al.   CELL

Roles of GPR41 and GPR43 in leptin secretory responses of murine adipocytes to short chain fatty acids

(2010) Mohamed S. Zaibi et al.   FEBS LETTERS

Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation

(2010) M.C. Peeters et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Structure−Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469

(2010) Elisabeth Christiansen et al.   ACS Medicinal Chemistry Letters

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist

(2010) Nobuyuki Negoro et al.   ACS Medicinal Chemistry Letters

G Protein-Coupled Receptor 43 Is Essential for Neutrophil Recruitment during Intestinal Inflammation

(2009) C. Sina et al.   JOURNAL OF IMMUNOLOGY

Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43

(2009) Kendle M. Maslowski et al.   NATURE

Activation of G Protein-Coupled Receptor 43 in Adipocytes Leads to Inhibition of Lipolysis and Suppression of Plasma Free Fatty Acids

(2008) Hongfei Ge et al.   ENDOCRINOLOGY

Two Arginine-Glutamate Ionic Locks Near the Extracellular Surface of FFAR1 Gate Receptor Activation

(2008) Chi Shing Sum et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Conserved Polar Residues in Transmembrane Domains V, VI, and VII of Free Fatty Acid Receptor 2 and Free Fatty Acid Receptor 3 Are Required for the Binding and Function of Short Chain Fatty Acids

(2008) Leigh A. Stoddart et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes

(2008) Elisabeth Christiansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of histone-deacetylase activity by short-chain fatty acids and some polyphenol metabolites formed in the colon

(2008) Markus Waldecker et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

Identification and Functional Characterization of Allosteric Agonists for the G Protein-Coupled Receptor FFA2

(2008) T. Lee et al.   MOLECULAR PHARMACOLOGY