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

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

TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial

(2012) Charles F Burant et al.   LANCET

The role of G-protein-coupled receptors in mediating the effect of fatty acids on inflammation and insulin sensitivity

(2011) Da Young Oh et al.   CURRENT OPINION IN CLINICAL NUTRITION AND METABOLIC CARE

Selective Orthosteric Free Fatty Acid Receptor 2 (FFA2) Agonists

(2011) Johannes Schmidt et al.   JOURNAL OF BIOLOGICAL 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

Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases

(2011) Saswata Talukdar et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Identification of novel species-selective agonists of the G-protein-coupled receptor GPR35 that promote recruitment of β-arrestin-2 and activate Gα13

(2010) Laura Jenkins et al.   BIOCHEMICAL JOURNAL

Pathway-Specific, Species, and Sub-Type Counterscreening for Better GPCR Hits in High Throughput Screening

(2010) Robert Swanson et al.   CURRENT PHARMACEUTICAL BIOTECHNOLOGY

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

X-ray structure breakthroughs in the GPCR transmembrane region

(2009) Sid Topiol et al.   BIOCHEMICAL PHARMACOLOGY

Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3

(2009) Graeme Milligan et al.   BRITISH JOURNAL OF PHARMACOLOGY

GPR40: Good Cop, Bad Cop?

(2009) T. Alquier et al.   DIABETES

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum 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

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

(2008) T. Lee et al.   MOLECULAR PHARMACOLOGY

International Union of Pharmacology. LXXI. Free Fatty Acid Receptors FFA1, -2, and -3: Pharmacology and Pathophysiological Functions

(2008) L. A. Stoddart et al.   PHARMACOLOGICAL REVIEWS