Drugs or diet? - Developing novel therapeutic strategies targeting the free fatty acid family of GPCRs

Fatty Acid Receptor Gpr40 Mediates Neuromicrovascular Degeneration Induced by Transarachidonic Acids in Rodents

(2013) Jean-Claude Honoré et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

The Therapeutic Potential of Allosteric Ligands for Free Fatty Acid Sensitive GPCRs

(2013) Brian D. Hudson et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Reevaluation of Fatty Acid Receptor 1 as a Drug Target for the Stimulation of Insulin Secretion in Humans

(2013) R. Wagner et al.   DIABETES

Co-localisation and secretion of glucagon-like peptide 1 and peptide YY from primary cultured human L cells

(2013) A. M. Habib et al.   DIABETOLOGIA

Short-Chain Fatty Acids Activate GPR41 and GPR43 on Intestinal Epithelial Cells to Promote Inflammatory Responses in Mice

(2013) Myung H. Kim et al.   GASTROENTEROLOGY

The Free Fatty Acid Receptor G Protein-coupled Receptor 40 (GPR40) Protects from Bone Loss through Inhibition of Osteoclast Differentiation

(2013) Fabien Wauquier et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2013) Brian D. Hudson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Potent and Selective Free Fatty Acid Receptor 1 Agonist with Low Lipophilicity and High Oral Bioavailability

(2013) Elisabeth Christiansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Minireview: The Effects of Species Ortholog and SNP Variation on Receptors for Free Fatty Acids

(2013) Brian D. Hudson et al.   MOLECULAR ENDOCRINOLOGY

Conserved Shifts in the Gut Microbiota Due to Gastric Bypass Reduce Host Weight and Adiposity

(2013) A. P. Liou et al.   Science Translational Medicine

The gut microbiota suppresses insulin-mediated fat accumulation via the short-chain fatty acid receptor GPR43

(2013) Ikuo Kimura et al.   Nature Communications

Postprandial inhibition of gastric ghrelin secretion by long-chain fatty acid through GPR120 in isolated gastric ghrelin cells and mice

(2012) Xinping Lu et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Effects of a wheat bran extract containing arabinoxylan oligosaccharides on gastrointestinal health parameters in healthy adult human volunteers: a double-blind, randomised, placebo-controlled, cross-over trial

(2012) Isabelle E. J. A. François et al.   BRITISH JOURNAL OF NUTRITION

A Systems Genetics Approach Identifies Genes and Pathways for Type 2 Diabetes in Human Islets

(2012) Jalal Taneera et al.   Cell Metabolism

A Multiple-Ascending-Dose Study to Evaluate Safety, Pharmacokinetics, and Pharmacodynamics of a Novel GPR40 Agonist, TAK-875, in Subjects With Type 2 Diabetes

(2012) E Leifke et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Protective and Therapeutic Effects of Ghrelin in the Gut

(2012) Z. Warzecha et al.   CURRENT MEDICINAL CHEMISTRY

G protein-coupled receptor (GPR)40-dependent potentiation of insulin secretion in mouse islets is mediated by protein kinase D1

(2012) M. Ferdaoussi et al.   DIABETOLOGIA

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

Transfer of Intestinal Microbiota From Lean Donors Increases Insulin Sensitivity in Individuals With Metabolic Syndrome

(2012) Anne Vrieze et al.   GASTROENTEROLOGY

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

Effects of Acute and One-Week Fatty Acid Lowering on Cardiac Function and Insulin Sensitivity in Relation with Myocardial and Muscle Fat and Adiponectin Levels

(2012) Hanna-Riikka Lehto et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

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

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

Functional Selectivity in GPCR Signaling: Understanding the Full Spectrum of Receptor Conformations

(2012) E. Goupil et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human

(2012) Atsuhiko Ichimura et al.   NATURE

Unsaturated Fatty Acids Revert Diet-Induced Hypothalamic Inflammation in Obesity

(2012) Dennys E. Cintra et al.   PLoS One

PPARs are a unique set of fatty acid regulated transcription factors controlling both lipid metabolism and inflammation

(2011) Tamas Varga et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

FATTY ACIDS AS BIOCOMPOUNDS: THEIR ROLE IN HUMAN METABOLISM, HEALTH AND DISEASE - A REVIEW. PART 2: FATTY ACID PHYSIOLOGICAL ROLES AND APPLICATIONS IN HUMAN HEALTH AND DISEASE

(2011) Lefkothea-Stella Kremmyda et al.   BIOMEDICAL PAPERS-OLOMOUC

FATTY ACIDS AS BIOCOMPOUNDS: THEIR ROLE IN HUMAN METABOLISM, HEALTH AND DISEASE - A REVIEW. PART 1: CLASSIFICATION, DIETARY SOURCES AND BIOLOGICAL FUNCTIONS

(2011) Eva Tvrzicka et al.   BIOMEDICAL PAPERS-OLOMOUC

Guide to Receptors and Channels (GRAC), 5th edition

(2011) SPH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

(2011) G. Tolhurst et al.   DIABETES

GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes

(2011) T. Araki et al.   DIABETES OBESITY & METABOLISM

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

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

Selective Orthosteric Free Fatty Acid Receptor 2 (FFA2) Agonists

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

Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis

(2011) Jinwei Wu et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Fermentation in the Human Large Intestine

(2011) George T. Macfarlane et al.   JOURNAL OF CLINICAL GASTROENTEROLOGY

Inflammatory links between obesity and metabolic disease

(2011) Carey N. Lumeng et al.   JOURNAL OF CLINICAL INVESTIGATION

Acute stimulation of glucagon secretion by linoleic acid results from GPR40 activation and [Ca2+]i increase in pancreatic islet α-cells

(2011) Li Wang et al.   JOURNAL OF ENDOCRINOLOGY

Free Fatty Acid Receptors FFAR1 and GPR120 as Novel Therapeutic Targets for Metabolic Disorders

(2011) Takafumi Hara et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

National, regional, and global trends in fasting plasma glucose and diabetes prevalence since 1980: systematic analysis of health examination surveys and epidemiological studies with 370 country-years and 2·7 million participants

(2011) Goodarz Danaei et al.   LANCET

Dietary Monounsaturated Fatty Acids Are Protective Against Metabolic Syndrome and Cardiovascular Disease Risk Factors

(2011) Leah G. Gillingham et al.   LIPIDS

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

Variation in the FFAR1 Gene Modifies BMI, Body Composition and Beta-Cell Function in Overweight Subjects: An Exploratory Analysis

(2011) Celia G. Walker et al.   PLoS One

SCFAs Induce Mouse Neutrophil Chemotaxis through the GPR43 Receptor

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

AMG 837: A Novel GPR40/FFA1 Agonist that Enhances Insulin Secretion and Lowers Glucose Levels in Rodents

(2011) Daniel C.-H. Lin et al.   PLoS One

Omega-3 fatty acids and metabolic syndrome: Effects and emerging mechanisms of action

(2011) Hemant Poudyal et al.   PROGRESS IN LIPID RESEARCH

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

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

Improved glucose control and reduced body fat mass in free fatty acid receptor 2-deficient mice fed a high-fat diet

(2010) Mikael Bjursell et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

The relationship between GPR40 and lipotoxicity of the pancreatic β-cells as well as the effect of pioglitazone

(2010) Peiwen Wu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Agonism with the omega-3 fatty acids α-linolenic acid and docosahexaenoic acid mediates phosphorylation of both the short and long isoforms of the human GPR120 receptor

(2010) Rebecca N. Burns et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Effects of Lactobacillus acidophilus NCFM on insulin sensitivity and the systemic inflammatory response in human subjects

(2010) Anne Sofie Andreasen et al.   BRITISH JOURNAL OF NUTRITION

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

(2010) Da Young Oh et al.   CELL

Metabolic and nonmetabolic regulatory functions of peroxisome proliferator-activated receptor β

(2010) Paul A Grimaldi   CURRENT OPINION IN LIPIDOLOGY

Obesity, Diabetes, and Gut Microbiota: The hygiene hypothesis expanded?

(2010) G. Musso et al.   DIABETES CARE

Role of metabolically generated reactive oxygen species for lipotoxicity in pancreatic β-cells

(2010) W. Gehrmann et al.   DIABETES OBESITY & METABOLISM

Regulation of abdominal adiposity by probiotics (Lactobacillus gasseri SBT2055) in adults with obese tendencies in a randomized controlled trial

(2010) Y Kadooka et al.   EUROPEAN JOURNAL OF CLINICAL NUTRITION

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

The G-Protein−Coupled Receptor GPR40 Directly Mediates Long-Chain Fatty Acid−Induced Secretion of Cholecystokinin

(2010) Alice P. Liou et al.   GASTROENTEROLOGY

Chronic Inflammation in Obesity and the Metabolic Syndrome

(2010) Rosário Monteiro et al.   MEDIATORS OF INFLAMMATION

Long-term supplementation of isomalto-oligosaccharides improved colonic microflora profile, bowel function, and blood cholesterol levels in constipated elderly people—A placebo-controlled, diet-controlled trial

(2010) Chi-Hua Yen et al.   NUTRITION

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

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

Weight loss during oligofructose supplementation is associated with decreased ghrelin and increased peptide YY in overweight and obese adults

(2009) Jill A Parnell et al.   AMERICAN JOURNAL OF CLINICAL NUTRITION

Thiazolidinediones induce proliferation of human bronchial epithelial cells through the GPR40 receptor

(2009) Delphine Gras et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Fat and Fatty Acid Terminology, Methods of Analysis and Fat Digestion and Metabolism: A Background Review Paper

(2009) W.M. Nimal Ratnayake et al.   ANNALS OF NUTRITION AND METABOLISM

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

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

n-3 Fatty acids and rosiglitazone improve insulin sensitivity through additive stimulatory effects on muscle glycogen synthesis in mice fed a high-fat diet

(2009) O. Kuda et al.   DIABETOLOGIA

Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1): an emerging target for type 2 diabetes

(2009) Sandip B Bharate et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Application of liquid chromatography–mass spectrometry to measure short chain fatty acids in blood

(2009) Hans M.H. van Eijk et al.   JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES

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

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

Acute administration of GPR40 receptor agonist potentiates glucose-stimulated insulin secretion in vivo in the rat

(2009) Lalit S. Doshi et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43

(2009) Kendle M. Maslowski et al.   NATURE

Distribution and regulation of protein expression of the free fatty acid receptor GPR120

(2009) Satoshi Miyauchi et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

G-protein-coupled receptor 40 (GPR40) expression and its regulation in human pancreatic islets: The role of type 2 diabetes and fatty acids

(2009) S. Del Guerra et al.   NUTRITION METABOLISM AND CARDIOVASCULAR DISEASES

Free Fatty Acid Receptors and Drug Discovery

(2008) Akira Hirasawa et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Selective Small-Molecule Agonists of G Protein-Coupled Receptor 40 Promote Glucose-Dependent Insulin Secretion and Reduce Blood Glucose in Mice

(2008) C. P. Tan et al.   DIABETES

The Fatty Acid Receptor GPR40 Plays a Role in Insulin Secretion In Vivo After High-Fat Feeding

(2008) M. Kebede et al.   DIABETES

Lack of FFAR1/GPR40 Does Not Protect Mice From High-Fat Diet-Induced Metabolic Disease

(2008) H. Lan et al.   DIABETES

Gpr40 Is Expressed in Enteroendocrine Cells and Mediates Free Fatty Acid Stimulation of Incretin Secretion

(2008) S. Edfalk et al.   DIABETES

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

Identification of G protein-coupled receptor 120-selective agonists derived from PPARγ agonists

(2008) Takayoshi Suzuki 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

Plasma Omega-3 Fatty Acid Response to a Fish Oil Supplement in the Healthy Elderly

(2008) Milène Vandal et al.   LIPIDS

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

(2008) T. Lee et al.   MOLECULAR PHARMACOLOGY

Cloning and characterization of the rat free fatty acid receptor GPR120: in vivo effect of the natural ligand on GLP-1 secretion and proliferation of pancreatic β cells

(2008) Toshiki Tanaka et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Could the Quality of Dietary Fat, and Not Just Its Quantity, Be Related to Risk of Obesity?

(2008) Nadiah Moussavi et al.   Obesity

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

Effects of the gut microbiota on host adiposity are modulated by the short-chain fatty-acid binding G protein-coupled receptor, Gpr41

(2008) B. S. Samuel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA