Conjugated Linoleic Acids Mediate Insulin Release through Islet G Protein-coupled Receptor FFA1/GPR40

DC260126, a small-molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats

(2010) Xiaodong Zhang et al.   BIOMEDICINE & PHARMACOTHERAPY

Childhood obesity

(2010) Joan C Han et al.   LANCET

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

Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists

(2009) Paul S. Humphries et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Deletion of GPR40 Impairs Glucose-Induced Insulin Secretion In Vivo in Mice Without Affecting Intracellular Fuel Metabolism in Islets

(2009) T. Alquier et al.   DIABETES

GPR40: Good Cop, Bad Cop?

(2009) T. Alquier et al.   DIABETES

Overexpression of GPR40 in Pancreatic  -Cells Augments Glucose-Stimulated Insulin Secretion and Improves Glucose Tolerance in Normal and Diabetic Mice

(2009) K. Nagasumi et al.   DIABETES

Lipid receptors and islet function: therapeutic implications?

(2009) M. A. Kebede et al.   DIABETES OBESITY & METABOLISM

Antiobesity mechanisms of action of conjugated linoleic acid

(2009) Arion Kennedy et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

Metabolism and actions of conjugated linoleic acids on atherosclerosis-related events in vascular endothelial cells and smooth muscle cells

(2009) Klaus Eder et al.   MOLECULAR NUTRITION & FOOD RESEARCH

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

(2009) Terry P. Kenakin   NATURE REVIEWS DRUG DISCOVERY

Effects of conjugated linoleic acid plus n-3 polyunsaturated fatty acids on insulin secretion and estimated insulin sensitivity in men

(2008) B Ahrén et al.   EUROPEAN JOURNAL OF CLINICAL NUTRITION

Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity

(2008) Johannes Antony et al.   FASEB JOURNAL

The C-terminal Tail of CRTH2 Is a Key Molecular Determinant That Constrains Gαiand Downstream Signaling Cascade Activation

(2008) Ralf Schröder 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

Antiobesity effect of PEGylated conjugated linoleic acid on high-fat diet-induced obese C57BL/6J (ob/ob) mice: attenuation of insulin resistance and enhancement of antioxidant defenses

(2008) Hyun-Seuk Moon et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

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

The development of tolerance to drugs that suppress food intake

(2007) John D. Fernstrom et al.   PHARMACOLOGY & THERAPEUTICS