G protein-coupled receptors as targets for anti-diabetic therapeutics

Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases

(2015) Elisabeth Christiansen et al.   BRITISH JOURNAL OF NUTRITION

GPR40 agonists for the treatment of type 2 diabetes: life after ‘TAKing’ a hit

(2015) A. D. Mancini et al.   DIABETES OBESITY & METABOLISM

Contribution of the low-frequency, loss-of-function p.R270H mutation inFFAR4(GPR120) to increased fasting plasma glucose levels

(2015) Amélie Bonnefond et al.   JOURNAL OF MEDICAL GENETICS

Leptin resistance in diet-induced obesity: the role of hypothalamic inflammation

(2015) K. C. G. de Git et al.   Obesity Reviews

Gαi/o-coupled receptor signaling restricts pancreatic β-cell expansion

(2015) Miles Berger et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mechanisms of homologous and heterologous phosphorylation of FFA receptor 4 (GPR120): GRK6 and PKC mediate phosphorylation of Thr347, Ser350, and Ser357 in the C-terminal tail

(2014) Rebecca N. Burns et al.   BIOCHEMICAL PHARMACOLOGY

Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus

(2014) Elisabeth Defossa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a Class of Endogenous Mammalian Lipids with Anti-Diabetic and Anti-inflammatory Effects

(2014) Mark M. Yore et al.   CELL

The fish oil ingredient, docosahexaenoic acid, activates cytosolic phospholipase A2via GPR120 receptor to produce prostaglandin E2and plays an anti-inflammatory role in macrophages

(2014) Yueqin Liu et al.   IMMUNOLOGY

GLP-1 receptor agonists vs. DPP-4 inhibitors for type 2 diabetes: is one approach more successful or preferable than the other?

(2014) S. Brunton   INTERNATIONAL JOURNAL OF CLINICAL PRACTICE

Alteration of the Glucagon Axis in GPR120 (FFAR4) Knockout Mice

(2014) Arthur T. Suckow et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The arcuate nucleus mediates GLP-1 receptor agonist liraglutide-dependent weight loss

(2014) Anna Secher et al.   JOURNAL OF CLINICAL INVESTIGATION

Neuronal GLP1R mediates liraglutide’s anorectic but not glucose-lowering effect

(2014) Stephanie Sisley et al.   JOURNAL OF CLINICAL INVESTIGATION

Activation of the omega-3 fatty acid receptor GPR120 mediates anti-inflammatory actions in immortalized hypothalamic neurons

(2014) Leigh Wellhauser et al.   Journal of Neuroinflammation

A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice

(2014) Da Young Oh et al.   NATURE MEDICINE

Omega-3 Free Fatty Acids Suppress Macrophage Inflammasome Activation by Inhibiting NF-κB Activation and Enhancing Autophagy

(2014) Yolanda Williams-Bey et al.   PLoS One

Food and Symptom Generation in Functional Gastrointestinal Disorders: Physiological Aspects

(2013) Ricard Farré et al.   AMERICAN JOURNAL OF GASTROENTEROLOGY

Use of Twice-Daily Exenatide in Basal Insulin–Treated Patients With Type 2 Diabetes

(2013) John B. Buse et al.   ANNALS OF INTERNAL MEDICINE

Inflammation, Cytokines and Insulin Resistance: A Clinical Perspective

(2013) Verena Wieser et al.   ARCHIVUM IMMUNOLOGIAE ET THERAPIAE EXPERIMENTALIS

Activation of GPR119 by fatty acid agonists augments insulin release from clonal β-cells and isolated pancreatic islets and improves glucose tolerance in mice

(2013) Brian M. Moran et al.   BIOLOGICAL CHEMISTRY

Randomized clinical trial of perioperative omega-3 fatty acid supplements in elective colorectal cancer surgery

(2013) L. S. Sorensen et al.   BRITISH JOURNAL OF SURGERY

Metabolic inflammation: role of cytokines in the crosstalk between adipose tissue and liver

(2013) Romana R. Gerner et al.   CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY

The Fractalkine/CX3CR1 System Regulates β Cell Function and Insulin Secretion

(2013) Yun Sok Lee et al.   CELL

The Origins and Drivers of Insulin Resistance

(2013) Andrew M.F. Johnson et al.   CELL

Inflammation in Obesity and Diabetes: Islet Dysfunction and Therapeutic Opportunity

(2013) Marc Y. Donath et al.   Cell Metabolism

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

(2013) R. Wagner et al.   DIABETES

Identification and Characterization of GLP-1 Receptor-Expressing Cells Using a New Transgenic Mouse Model

(2013) P. Richards et al.   DIABETES

Macrophages and islet inflammation in type 2 diabetes

(2013) K. Eguchi et al.   DIABETES OBESITY & METABOLISM

Cyclooxygenase-2 induction in macrophages is modulated by docosahexaenoic acid via interactions with free fatty acid receptor 4 (FFA4)

(2013) Xinzhi Li et al.   FASEB JOURNAL

Omega-3 Fatty Acids Prevent Inflammation and Metabolic Disorder through Inhibition of NLRP3 Inflammasome Activation

(2013) Yiqing Yan et al.   IMMUNITY

GPR120 on Kupffer cells mediates hepatoprotective effects of ω3-fatty acids

(2013) Dimitri Aristotle Raptis et al.   JOURNAL OF HEPATOLOGY

Rapid Incorporation of ω-3 Fatty Acids Into Colonic Tissue After Oral Supplementation in Patients With Colorectal Cancer

(2013) Lone Schmidt Sorensen et al.   JOURNAL OF PARENTERAL AND ENTERAL NUTRITION

Limited Impact of 2 g/day Omega-3 Fatty Acid Ethyl Esters (Omacor®) on Plasma Lipids and Inflammatory Markers in Patients Awaiting Carotid Endarterectomy

(2013) Hayati Yusof et al.   Marine Drugs

Activation of FFA1 mediates GLP-1 secretion in mice. Evidence for allosterism at FFA1

(2013) Yumei Xiong et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Pharmacology and therapeutics of omega-3 polyunsaturated fatty acids in chronic inflammatory disease

(2013) Clara M. Yates et al.   PHARMACOLOGY & THERAPEUTICS

Blocking Macrophage Leukotriene B4 Prevents Endothelial Injury and Reverses Pulmonary Hypertension

(2013) W. Tian et al.   Science Translational Medicine

The fatty acid receptor FFA1/GPR40 a decade later: how much do we know?

(2013) Arturo D. Mancini et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Islet inflammation: a unifying target for diabetes treatment?

(2013) Yumi Imai et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Clinical Efficacy and Safety of Once-Weekly Glucagon-Like Peptide-1 Agonists in Development for Treatment of Type 2 Diabetes Mellitus in Adults

(2012) Maria Tzefos et al.   ANNALS OF PHARMACOTHERAPY

Structure-Function of the G Protein–Coupled Receptor Superfamily

(2012) Vsevolod Katritch et al.   Annual Review of Pharmacology and Toxicology

Mechanisms for Insulin Resistance: Common Threads and Missing Links

(2012) Varman T. Samuel et al.   CELL

Insulin Resistance in the Defense against Obesity

(2012) Alan R. Saltiel   Cell Metabolism

LTB4 Is a Signal-Relay Molecule during Neutrophil Chemotaxis

(2012) Philippe V. Afonso et al.   DEVELOPMENTAL CELL

Randomized, Double-Blind, Dose-Ranging Study of TAK-875, a Novel GPR40 Agonist, in Japanese Patients With Inadequately Controlled Type 2 Diabetes

(2012) K. Kaku et al.   DIABETES CARE

Efficacy and Safety of the Once-Daily GLP-1 Receptor Agonist Lixisenatide in Monotherapy: A randomized, double-blind, placebo-controlled trial in patients with type 2 diabetes (GetGoal-Mono)

(2012) V. A. Fonseca et al.   DIABETES CARE

Monotherapy with the once-weekly GLP-1 analogue dulaglutide for 12 weeks in patients with Type 2 diabetes: dose-dependent effects on glycaemic control in a randomized, double-blind, placebo-controlled study

(2012) G. Grunberger et al.   DIABETIC MEDICINE

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

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

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

(2012) Atsuhiko Ichimura et al.   NATURE

Neutrophils mediate insulin resistance in mice fed a high-fat diet through secreted elastase

(2012) Saswata Talukdar et al.   NATURE MEDICINE

GLP-1 receptor agonists for individualized treatment of type 2 diabetes mellitus

(2012) Juris J. Meier   Nature Reviews Endocrinology

Unsaturated Fatty Acids Revert Diet-Induced Hypothalamic Inflammation in Obesity

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

A Potent Class of GPR40 Full Agonists Engages the EnteroInsular Axis to Promote Glucose Control in Rodents

(2012) Jian Luo et al.   PLoS One

Glucose activates free fatty acid receptor 1 gene transcription via phosphatidylinositol-3-kinase-dependent O-GlcNAcylation of pancreas-duodenum homeobox-1

(2012) M. Kebede et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

GPR119 as a fat sensor

(2012) Harald S. Hansen et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

DPP-4 inhibition increases GIP and decreases GLP-1 incretin effects during intravenous glucose tolerance test in Wistar rats

(2011) Ernst-Joachim Freyse et al.   BIOLOGICAL CHEMISTRY

Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system

(2011) Kazuo Nakamoto et al.   BRAIN RESEARCH

Insulin Resistance, Hyperglycemia, and Atherosclerosis

(2011) Karin E. Bornfeldt et al.   Cell Metabolism

A Pilot Study to Assess Whether Glucagon-Like Peptide-1 Protects the Heart From Ischemic Dysfunction and Attenuates Stunning After Coronary Balloon Occlusion in Humans

(2011) Philip A. Read et al.   Circulation-Cardiovascular Interventions

Fractalkine Is a Novel Human Adipochemokine Associated With Type 2 Diabetes

(2011) R. Shah et al.   DIABETES

DPP-4 Inhibitors: Impact on glycemic control and cardiovascular risk factors

(2011) D. Dicker   DIABETES CARE

Glucolipotoxicity and beta cells in type 2 diabetes mellitus: Target for durable therapy?

(2011) Daniel H. van Raalte et al.   DIABETES RESEARCH AND CLINICAL PRACTICE

Incretin effect: GLP-1, GIP, DPP4

(2011) Kyriakos Kazakos   DIABETES RESEARCH AND CLINICAL PRACTICE

Exenatide Once-Weekly Clinical Development: Safety and Efficacy Across a Range of Background Therapies

(2011) Anthony Stonehouse et al.   Diabetes Technology & Therapeutics

2-Oleoyl Glycerol Is a GPR119 Agonist and Signals GLP-1 Release in Humans

(2011) Katrine B. Hansen et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Pancreatic GLP-1 receptor activation is sufficient for incretin control of glucose metabolism in mice

(2011) Benjamin J. Lamont 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

Deficiency of the Leukotriene B4 Receptor, BLT-1, Protects against Systemic Insulin Resistance in Diet-Induced Obesity

(2011) M. Spite et al.   JOURNAL OF IMMUNOLOGY

B cells promote insulin resistance through modulation of T cells and production of pathogenic IgG antibodies

(2011) Daniel A Winer et al.   NATURE MEDICINE

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

Glucagon-like peptide-1 (GLP-1) receptor agonists: Differentiating the new medications

(2011) Jeffrey R. Unger et al.   Diabetes Therapy

Incretin-Based Therapies: Review of Current Clinical Trial Data

(2010) Anne Peters   AMERICAN JOURNAL OF MEDICINE

Macrophages, Inflammation, and Insulin Resistance

(2010) Jerrold M. Olefsky et al.   Annual Review of Physiology

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

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

(2010) Da Young Oh et al.   CELL

Dipeptidyl Peptidase-4 Inhibitors Administered in Combination With Metformin Result in an Additive Increase in the Plasma Concentration of Active GLP-1

(2010) E M Migoya et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Common Genetic Variation Influences the Heterogeneity of Response to Oral Glucose

(2010) Adrian Vella   Current Diabetes Reports

CX3CL1-CX3CR1 interaction prevents carbon tetrachloride-induced liver inflammation and fibrosis in mice

(2010) Tomonori Aoyama et al.   HEPATOLOGY

Blockade of LTB4/BLT1 pathway improves CD8+ T-cell-mediated colitis

(2010) Stephane Nancey et al.   INFLAMMATORY BOWEL DISEASES

Functional Heterogeneity of CD11c-positive Adipose Tissue Macrophages in Diet-induced Obese Mice

(2010) Pingping Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Addition of metformin to exogenous glucagon-like peptide–1 results in increased serum glucagon-like peptide–1 concentrations and greater glucose lowering in type 2 diabetes mellitus

(2010) Joy Cuthbertson et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

New genetic loci implicated in fasting glucose homeostasis and their impact on type 2 diabetes risk

(2010) Josée Dupuis et al.   NATURE GENETICS

Serotonin regulates pancreatic beta cell mass during pregnancy

(2010) Hail Kim et al.   NATURE MEDICINE

Association of Common Polymorphisms in the Fractalkine Receptor (CX3CR1) With Obesity

(2010) Dave Sirois-Gagnon et al.   Obesity

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

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

Review: The evolving world of GLP-1 agonist therapies for type 2 diabetes

(2010) Kevin C. R. Baynes   Therapeutic Advances in Endocrinology and Metabolism

Exenatide and liraglutide: different approaches to develop GLP-1 receptor agonists (incretin mimetics) – preclinical and clinical results

(2009) Sten Madsbad   BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & 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

GPR119 agonists for the treatment of type 2 diabetes

(2009) Robert M Jones et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Obesity-induced insulin resistance and hepatic steatosis are alleviated by ω-3 fatty acids: a role for resolvins and protectins

(2009) Ana González-Périz et al.   FASEB JOURNAL

GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis

(2009) Hong Lan et al.   JOURNAL OF ENDOCRINOLOGY

Saturated Fatty Acids Produce an Inflammatory Response Predominantly through the Activation of TLR4 Signaling in Hypothalamus: Implications for the Pathogenesis of Obesity

(2009) M. Milanski et al.   JOURNAL OF NEUROSCIENCE

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

Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes

(2009) Bo Ahrén   NATURE REVIEWS DRUG DISCOVERY

Regulation of TNFα and IL1β in rheumatoid arthritis synovial fibroblasts by leukotriene B4

(2009) Shaohua Xu et al.   RHEUMATOLOGY INTERNATIONAL

β-Cell deterioration during diabetes: what's in the gun?

(2009) R. Paul Robertson   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Pancreatic islet inflammation in type 2 diabetes: From α and β cell compensation to dysfunction

(2009) Jan A. Ehses et al.   ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY

Chemokines in Atherosclerosis

(2008) Alma Zernecke et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Fatty acids and glucolipotoxicity in the pathogenesis of Type 2 diabetes

(2008) Miriam Cnop   BIOCHEMICAL SOCIETY TRANSACTIONS

Glucose Sensing in L Cells: A Primary Cell Study

(2008) Frank Reimann et al.   Cell Metabolism

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

Nutrient-dependent secretion of glucose-dependent insulinotropic polypeptide from primary murine K cells

(2008) H. E. Parker et al.   DIABETOLOGIA

Glucolipotoxicity: Fuel Excess and β-Cell Dysfunction

(2008) Vincent Poitout et al.   ENDOCRINE REVIEWS

GPR119: “Double-Dipping” for Better Glycemic Control

(2008) L. Lauffer et al.   ENDOCRINOLOGY

A Role for Intestinal Endocrine Cell-Expressed G Protein-Coupled Receptor 119 in Glycemic Control by Enhancing Glucagon-Like Peptide-1 and Glucose-Dependent Insulinotropic Peptide Release

(2008) Zhi-Liang Chu et al.   ENDOCRINOLOGY

Loss-of-Function Mutation of theGPR40Gene Associates with Abnormal Stimulated Insulin Secretion by Acting on Intracellular Calcium Mobilization

(2008) Roberto Vettor et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

5-Lipoxygenase: mechanisms of regulation

(2008) Olof Rådmark et al.   JOURNAL OF LIPID RESEARCH

 -Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic   cells

(2008) N. Sonoda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dietary Omega-3 Fats for Treatment of Inflammatory Joint Disease: Efficacy and Utility

(2008) Susanna M. Proudman et al.   RHEUMATIC DISEASE CLINICS OF NORTH AMERICA

The islet β-cell: fuel responsive and vulnerable

(2008) Christopher J. Nolan et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Production and characterization of a monoclonal antibody against GPR40 (FFAR1; free fatty acid receptor 1)

(2007) Akira Hirasawa et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Effect of the oral leukotriene B4 receptor antagonist LTB019 on inflammatory sputum markers in patients with chronic obstructive pulmonary disease

(2007) L. Grönke et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS