Selective Orthosteric Free Fatty Acid Receptor 2 (FFA2) Agonists

Drugging challenging targets using fragment-based approaches

(2010) Anthony G Coyne et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

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

When simple agonism is not enough: Emerging modalities of GPCR ligands

(2010) Nicola J. Smith et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

A holistic view of GPCR signaling

(2010) Terry Kenakin   NATURE BIOTECHNOLOGY

Deconvolution of complex G protein–coupled receptor signaling in live cells using dynamic mass redistribution measurements

(2010) Ralf Schröder et al.   NATURE BIOTECHNOLOGY

Free fatty acid receptor 2 and nutrient sensing: a proposed role for fibre, fermentable carbohydrates and short-chain fatty acids in appetite regulation

(2010) Michelle L. Sleeth et al.   NUTRITION RESEARCH REVIEWS

The minor binding pocket: a major player in 7TM receptor activation

(2010) Mette M. Rosenkilde et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators

(2009) Yingcai Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

7TM pharmacology measured by label-free: a holistic approach to cell signalling

(2009) Magalie Rocheville et al.   CURRENT OPINION IN PHARMACOLOGY

Transforming fragments into candidates: small becomes big in medicinal chemistry

(2009) Gerdien E. de Kloe et al.   DRUG DISCOVERY TODAY

The Action and Mode of Binding of Thiazolidinedione Ligands at Free Fatty Acid Receptor 1

(2009) Nicola J. Smith et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Deorphanization of GPR109B as a Receptor for the β-Oxidation Intermediate 3-OH-octanoic Acid and Its Role in the Regulation of Lipolysis

(2009) Kashan Ahmed et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Molecular Pharmacology of Promiscuous Seven Transmembrane Receptors Sensing Organic Nutrients

(2009) P. Wellendorph et al.   MOLECULAR PHARMACOLOGY

Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43

(2009) Kendle M. Maslowski et al.   NATURE

Cellular assays as portals to seven-transmembrane receptor-based drug discovery

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptors

(2009) Kashan Ahmed et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Functional Selectivity in GPCR Modulator Screening

(2008) Terry Kenakin   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

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