Pharmacology of Free Fatty Acid Receptors and Their Allosteric Modulators

Controversial Roles of Gut Microbiota-Derived Short-Chain Fatty Acids (SCFAs) on Pancreatic β-Cell Growth and Insulin Secretion

(2020) Jun-Li Liu et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Maternal gut microbiota in pregnancy influences offspring metabolic phenotype in mice

(2020) Ikuo Kimura et al.   SCIENCE

Bifidobacterium animalis subsp. lactis GCL2505 modulates host energy metabolism via the short-chain fatty acid receptor GPR43

(2020) Hiroko Horiuchi et al.   Scientific Reports

Gut Dysbiosis during Influenza Contributes to Pulmonary Pneumococcal Superinfection through Altered Short-Chain Fatty Acid Production

(2020) Valentin Sencio et al.   Cell Reports

Deficiency of Prebiotic Fiber and Insufficient Signaling Through Gut Metabolite-Sensing Receptors Leads to Cardiovascular Disease

(2020) David M. Kaye et al.   CIRCULATION

Dietary Fiber Protects against Diabetic Nephropathy through Short-Chain Fatty Acid–Mediated Activation of G Protein–Coupled Receptors GPR43 and GPR109A

(2020) Yan Jun Li et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Chronic activation of GPR40 does not negatively impact upon BRIN-BD11 pancreatic β-cell physiology and function

(2020) Eloisa Aparecida Vilas-Boas et al.   Pharmacological Reports

The Medium-Chain Fatty Acid Receptor GPR84 Mediates Myeloid Cell Infiltration Promoting Steatohepatitis and Fibrosis

(2020) Tobias Puengel et al.   Journal of Clinical Medicine

Interdependent allosteric free fatty acid receptor 2 modulators synergistically induce functional selective activation and desensitization in neutrophils

(2020) Simon Lind et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Gut Microbial Metabolites Induce Donor-Specific Tolerance of Kidney Allografts through Induction of T Regulatory Cells by Short-Chain Fatty Acids

(2020) Huiling Wu et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Short-Chain Fatty Acids Ameliorate Diabetic Nephropathy via GPR43-Mediated Inhibition of Oxidative Stress and NF-κB Signaling

(2020) Wei Huang et al.   Oxidative Medicine and Cellular Longevity

Internalization-dependent free fatty acid receptor 2 signaling is essential for propionate-induced anorectic gut hormone release

(2020) Natarin Caengprasath et al.   iScience

GPR120 agonists for the treatment of diabetes: a patent review (2014 present)

(2020) Xuqing Zhang et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Allosteric targeting of the FFA2 receptor (GPR43) restores responsiveness of desensitized human neutrophils

(2020) Robert Frei et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety

(2020) Hideki Furukawa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial

(2020) Frédéric Labéguère et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Convergence of Extracellular Vesicle and GPCR Biology

(2020) Maarten P. Bebelman et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The operational model of allosteric modulation of pharmacological agonism

(2020) Jan Jakubík et al.   Scientific Reports

Heterotrimeric G Protein Subunit Gαq Is a Master Switch for Gβγ-Mediated Calcium Mobilization by Gi-Coupled GPCRs

(2020) Eva Marie Pfeil et al.   MOLECULAR CELL

Biased Receptor Signaling in Drug Discovery

(2019) Terry Kenakin   PHARMACOLOGICAL REVIEWS

Functional selective ATP receptor signaling controlled by the free fatty acid receptor 2 through a novel allosteric modulation mechanism

(2019) Simon Lind et al.   FASEB JOURNAL

Microbiota Metabolite Short-Chain Fatty Acids Facilitate Mucosal Adjuvant Activity of Cholera Toxin through GPR43

(2019) Wenjing Yang et al.   JOURNAL OF IMMUNOLOGY

Activation of GPR40 produces mechanical antiallodynia via the spinal glial interleukin-10/β-endorphin pathway

(2019) Xiao-Fang Mao et al.   Journal of Neuroinflammation

Chemogenetics defines receptor-mediated functions of short chain free fatty acids

(2019) Daniele Bolognini et al.   Nature Chemical Biology

PBI-4050 via GPR40 activation improves adenine-induced kidney injury in mice

(2019) Jean-François Thibodeau et al.   CLINICAL SCIENCE

Regulation of mitochondrial metabolism in murine skeletal muscle by the medium-chain fatty acid receptor Gpr84

(2019) Magdalene K. Montgomery et al.   FASEB JOURNAL

Free Fatty Acid Receptors in Health and Disease

(2019) Ikuo Kimura et al.   PHYSIOLOGICAL REVIEWS

GPR40 full agonism exerts feeding suppression and weight loss through afferent vagal nerve

(2019) Hikaru Ueno et al.   PLoS One

Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold

(2019) Zheng Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Metabolite-Sensing Receptor Ffar2 Regulates Colonic Group 3 Innate Lymphoid Cells and Gut Immunity

(2019) Eunyoung Chun et al.   IMMUNITY

An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights

(2019) Meryem Köse et al.   JOURNAL OF MEDICINAL CHEMISTRY

The G protein-coupled receptor FFAR2 promotes internalization during influenza A virus entry

(2019) Guangwen Wang et al.   JOURNAL OF VIROLOGY

Ketone body receptor GPR43 regulates lipid metabolism under ketogenic conditions

(2019) Junki Miyamoto et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Current status of GPR40/FFAR1 modulators in medicinal chemistry (2016–2019): a patent review

(2019) Zheng Li et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Acetate coordinates neutrophil and ILC3 responses against C. difficile through FFAR2

(2019) José Luís Fachi et al.   JOURNAL OF EXPERIMENTAL MEDICINE

A Newly Discovered Antifibrotic Pathway Regulated by Two Fatty Acid Receptors

(2018) Lyne Gagnon et al.   AMERICAN JOURNAL OF PATHOLOGY

Discovery of N -arylpyrroles as agonists of GPR120 for the treatment of type II diabetes

(2018) Michael P. Winters et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fiber-Mediated Nourishment of Gut Microbiota Protects against Diet-Induced Obesity by Restoring IL-22-Mediated Colonic Health

(2018) Jun Zou et al.   Cell Host & Microbe

FFAR2-FFAR3 receptor heteromerization modulates short-chain fatty acid sensing

(2018) Zhiwei Ang et al.   FASEB JOURNAL

GPR40-Mediated Gα12 Activation by Allosteric Full Agonists Highly Efficacious at Potentiating Glucose-Stimulated Insulin Secretion in Human Islets

(2018) Marie-Laure Rives et al.   MOLECULAR PHARMACOLOGY

Embelin and its derivatives unravel the signaling, proinflammatory and antiatherogenic properties of GPR84 receptor

(2018) Ibragim Gaidarov et al.   PHARMACOLOGICAL RESEARCH

PAM-Antagonists: A Better Way to Block Pathological Receptor Signaling?

(2018) Terry Kenakin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Structural basis for GPR40 allosteric agonism and incretin stimulation

(2018) Joseph D. Ho et al.   Nature Communications

20-HETE promotes glucose-stimulated insulin secretion in an autocrine manner through FFAR1

(2018) Sorin Tunaru et al.   Nature Communications

Lack of beta-arrestin signaling in the absence of active G proteins

(2018) Manuel Grundmann et al.   Nature Communications

The Metabolic Sensor GPR43 Receptor Plays a Role in the Control of Klebsiella pneumoniae Infection in the Lung

(2018) Izabela Galvão et al.   Frontiers in Immunology

Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages

(2018) Carlota Recio et al.   Frontiers in Immunology

Fatty Acid-Induced Lipotoxicity in Pancreatic Beta-Cells During Development of Type 2 Diabetes

(2018) Yoon S. Oh et al.   Frontiers in Endocrinology

Neutrophil priming that turns natural FFA2R agonists into potent activators of the superoxide generating NADPH-oxidase

(2018) Jonas Mårtensson et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts

(2018) Eric A. Wold et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of FDA-approved drugs as novel allosteric inhibitors of human executioner caspases

(2018) R. N. V. Krishna Deepak et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis

(2018) Nasreen Khalil et al.   EUROPEAN RESPIRATORY JOURNAL

When trafficking and signaling mix: how subcellular location shapes GPCR activation of heterotrimeric G proteins

(2018) Braden T. Lobingier et al.   TRAFFIC

Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination

(2018) Hui Huang et al.   ACS Medicinal Chemistry Letters

Effect of GPR84 deletion on obesity and diabetes development in mice fed long chain or medium chain fatty acid rich diets

(2017) Eugene Du Toit et al.   EUROPEAN JOURNAL OF NUTRITION

Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance

(2017) Julia M. Houthuijzen et al.   FASEB JOURNAL

Conformational biosensors reveal allosteric interactions between heterodimeric AT1 angiotensin and prostaglandin F2α receptors

(2017) Rory Sleno et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Unbound free fatty acid profiles in human plasma and the unexpected absence of unbound palmitoleate

(2017) Andrew H. Huber et al.   JOURNAL OF LIPID RESEARCH

Free Fatty Acid Receptor 1 (FFAR1) as an Emerging Therapeutic Target for Type 2 Diabetes Mellitus: Recent Progress and Prevailing Challenges

(2017) Zheng Li et al.   MEDICINAL RESEARCH REVIEWS

Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4

(2017) Kenneth R. Watterson et al.   MOLECULAR PHARMACOLOGY

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

(2017) Jun Lu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Free fatty acid receptor 3 activation suppresses neurogenic motility in rat proximal colon

(2017) I. Kaji et al.   NEUROGASTROENTEROLOGY AND MOTILITY

GPR40 partial agonists and AgoPAMs: Differentiating effects on glucose and hormonal secretions in the rodent

(2017) Michele J. Pachanski et al.   PLoS One

Dysfunctional GPR40/FFAR1 signaling exacerbates pain behavior in mice

(2017) Kazuo Nakamoto et al.   PLoS One

Temporal Bias: Time-Encoded Dynamic GPCR Signaling

(2017) Manuel Grundmann et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

(2017) Jun Lu et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84

(2017) Zobaer Al Mahmud et al.   Scientific Reports

Fermentable carbohydrate stimulates FFAR2-dependent colonic PYY cell expansion to increase satiety

(2017) Lucy Brooks et al.   Molecular Metabolism

The short chain fatty acid receptor GPR43 regulates inflammatory signals in adipose tissue M2-type macrophages

(2017) Akira Nakajima et al.   PLoS One

Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects

(2016) Matthew Lombardo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects

(2016) Florence Namour et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Complex Pharmacology of Free Fatty Acid Receptors

(2016) Graeme Milligan et al.   CHEMICAL REVIEWS

Selective novel inverse agonists for human GPR43 augment GLP-1 secretion

(2016) Bi-Oh Park et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development

(2016) Zheng Li et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

GPR41 modulates insulin secretion and gene expression in pancreatic β-cells and modifies metabolic homeostasis in fed and fasting states

(2016) Anna Veprik et al.   FASEB JOURNAL

Targeted Elimination of G Proteins and Arrestins Defines Their Specific Contributions to Both Intensity and Duration of G Protein-coupled Receptor Signaling

(2016) Elisa Alvarez-Curto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias

(2016) Daniele Bolognini et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity

(2016) Carlos M. G. Azevedo et al.   JOURNAL OF MEDICINAL CHEMISTRY

GPR40/FFAR1 deficient mice increase noradrenaline levels in the brain and exhibit abnormal behavior

(2016) Fuka Aizawa et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

The Neutrophil Response Induced by an Agonist for Free Fatty Acid Receptor 2 (GPR43) Is Primed by Tumor Necrosis Factor Alpha and by Receptor Uncoupling from the Cytoskeleton but Attenuated by Tissue Recruitment

(2016) Lena Björkman et al.   MOLECULAR AND CELLULAR BIOLOGY

Microbiota metabolite short-chain fatty acid acetate promotes intestinal IgA response to microbiota which is mediated by GPR43

(2016) W Wu et al.   Mucosal Immunology

Synthesis of the GPR40 Partial Agonist MK-8666 through a Kinetically Controlled Dynamic Enzymatic Ketone Reduction

(2016) Alan M. Hyde et al.   ORGANIC LETTERS

Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents

(2016) Gregory L. Adams et al.   ACS Medicinal Chemistry Letters

GPR41 and GPR43 in Obesity and Inflammation – Protective or Causative?

(2016) Zhiwei Ang et al.   Frontiers in Immunology

Discovery of Small-Molecule Modulators of the Human Y4 Receptor

(2016) Gregory Sliwoski et al.   PLoS One

G Protein-Coupled Receptor 43 Modulates Neutrophil Recruitment during Acute Inflammation

(2016) Marjon E. Kamp et al.   PLoS One

Dietary Fatty Acids and Their Potential for Controlling Metabolic Diseases Through Activation of FFA4/GPR120

(2015) Trond Ulven et al.   Annual Review of Nutrition

Activation of Extracellular Signal-Regulated Protein Kinases 1 and 2 (ERK1/2) by Free Fatty Acid Receptor 1 (FFAR1/GPR40) Protects from Palmitate-Induced Beta Cell Death, but Plays no Role in Insulin Secretion

(2015) Madhura Panse et al.   CELLULAR PHYSIOLOGY AND BIOCHEMISTRY

Structures of mGluRs shed light on the challenges of drug development of allosteric modulators

(2015) Kirstie A Bennett et al.   CURRENT OPINION IN PHARMACOLOGY

GPR43 Potentiates β-Cell Function in Obesity

(2015) Joanne C. McNelis et al.   DIABETES

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

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

Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial

(2015) K. Kaku et al.   DIABETES OBESITY & METABOLISM

Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of AgonistVersusAntagonist Ligands

(2015) Eugenia Sergeev et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1

(2015) Arturo D. Mancini et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

DOP030. GLPG0974, an FFA2 antagonist, in ulcerative colitis: efficacy and safety in a multicenter proof-of-concept study

(2015)   Journal of Crohns & Colitis

An Acetate-Specific GPCR, FFAR2, Regulates Insulin Secretion

(2015) Medha Priyadarshini et al.   MOLECULAR ENDOCRINOLOGY

Loss of FFA2 and FFA3 increases insulin secretion and improves glucose tolerance in type 2 diabetes

(2015) Cong Tang et al.   NATURE MEDICINE

FDA-approved small-molecule kinase inhibitors

(2015) Peng Wu et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

FFAR3 modulates insulin secretion and global gene expression in mouse islets

(2015) Medha Priyadarshini et al.   Islets

GPR120: A bi-potential mediator to modulate the osteogenic and adipogenic differentiation of BMMSCs

(2015) Bo Gao et al.   Scientific Reports

A Role for Gut Microbiota and the Metabolite-Sensing Receptor GPR43 in a Murine Model of Gout

(2015) Angélica T. Vieira et al.   Arthritis & Rheumatology

New perspectives in signaling mediated by receptors coupled to stimulatory G protein: the emerging significance of cAMP efflux and extracellular cAMP-adenosine pathway

(2015) Rosely O. Godinho et al.   Frontiers in Pharmacology

GPR40 (FFAR1) – Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo

(2015) Maria Hauge et al.   Molecular Metabolism

Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)

(2014) Steven M. Sparks et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans

(2014) Virginia M. Stone et al.   DIABETOLOGIA

The Molecular Basis of Ligand Interaction at Free Fatty Acid Receptor 4 (FFA4/GPR120)

(2014) Brian D. Hudson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery and Optimization of an Azetidine Chemical Series As a Free Fatty Acid Receptor 2 (FFA2) Antagonist: From Hit to Clinic

(2014) Mathieu Pizzonero et al.   JOURNAL OF MEDICINAL CHEMISTRY

High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875

(2014) Ankita Srivastava et al.   NATURE

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

(2014) Da Young Oh et al.   NATURE MEDICINE

Effect of Marine-Derived n-3 Polyunsaturated Fatty Acids on C-Reactive Protein, Interleukin 6 and Tumor Necrosis Factor α: A Meta-Analysis

(2014) Kelei Li et al.   PLoS One

Expression of the Fatty Acid Receptor GPR120 in the Gut of Diet-Induced-Obese Rats and Its Role in GLP-1 Secretion

(2014) Sarah Juel Paulsen et al.   PLoS One

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

(2013) R. Wagner et al.   DIABETES

GPR41/FFAR3 and GPR43/FFAR2 as Cosensors for Short-Chain Fatty Acids in Enteroendocrine Cells vs FFAR3 in Enteric Neurons and FFAR2 in Enteric Leukocytes

(2013) Mark K. Nøhr et al.   ENDOCRINOLOGY

FFAR1 Is Involved in Both the Acute and Chronic Effects of Palmitate on Insulin Secretion

(2013) Hjalti Kristinsson et al.   ENDOCRINOLOGY

The therapeutic potential of GPR120: a patent review

(2013) Somnath Halder et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Medium-chain Fatty Acid-sensing Receptor, GPR84, Is a Proinflammatory Receptor

(2013) Masakatsu Suzuki et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Novel GPR40 agonist AS2575959 exhibits glucose metabolism improvement and synergistic effect with sitagliptin on insulin and incretin secretion

(2013) Hirotsugu Tanaka et al.   LIFE SCIENCES

N-3 Polyunsaturated Fatty Acids: Relationship to Inflammation in Healthy Adults and Adults Exhibiting Features of Metabolic Syndrome

(2013) Lindsay E. Robinson et al.   LIPIDS

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

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

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

DC260126: A Small-Molecule Antagonist of GPR40 that Protects against Pancreatic β-Cells Dysfunction in db/db Mice

(2013) Peng Sun et al.   PLoS One

A Novel Antidiabetic Drug, Fasiglifam/TAK-875, Acts as an Ago-Allosteric Modulator of FFAR1

(2013) Chiori Yabuki et al.   PLoS One

Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex

(2013) Q. Tan et al.   SCIENCE

The Microbial Metabolites, Short-Chain Fatty Acids, Regulate Colonic Treg Cell Homeostasis

(2013) P. M. Smith et al.   SCIENCE

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

(2013) Ikuo Kimura et al.   Nature Communications

Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells

(2013) Maja S. Engelstoft et al.   Molecular Metabolism

Inflammatory changes in adipose tissue enhance expression of GPR84, a medium-chain fatty acid receptor

(2012) Hiroshi Nagasaki et al.   FEBS LETTERS

Thiazolidinediones Induce Osteocyte Apoptosis by a G Protein-coupled Receptor 40-dependent Mechanism

(2012) Aleksandra Mieczkowska et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Potent and Selective GPR120 Agonist

(2012) Bharat Shimpukade et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2012) Atsuhiko Ichimura et al.   NATURE

Allosteric modulators of rhodopsin-like G protein-coupled receptors: Opportunities in drug development

(2012) Christa E. Müller et al.   PHARMACOLOGY & THERAPEUTICS

Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist

(2012) Sean P. Brown et al.   ACS Medicinal Chemistry Letters

Mutational analysis of G-protein coupled receptor – FFA2

(2011) Gayathri Swaminath et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

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

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

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

Short-chain fatty acids and ketones directly regulate sympathetic nervous system via G protein-coupled receptor 41 (GPR41)

(2011) I. Kimura et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

(2010) Da Young Oh et al.   CELL

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

(2010) Alice P. Liou et al.   GASTROENTEROLOGY

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

(2010) Ralf Schröder et al.   NATURE BIOTECHNOLOGY

Cyclooxygenase-2 generates anti-inflammatory mediators from omega-3 fatty acids

(2010) Alison L Groeger et al.   Nature Chemical Biology

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

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

Cloning, expression, and pharmacological characterization of the GPR120 free fatty acid receptor from cynomolgus monkey: Comparison with human GPR120 splice variants

(2009) Kristina Moore et al.   COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY B-BIOCHEMISTRY & MOLECULAR BIOLOGY

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

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

Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43

(2009) Kendle M. Maslowski et al.   NATURE

Allosteric communication between protomers of dopamine class A GPCR dimers modulates activation

(2009) Yang Han et al.   Nature Chemical Biology

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

Two Arginine-Glutamate Ionic Locks Near the Extracellular Surface of FFAR1 Gate Receptor Activation

(2008) Chi Shing Sum et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of Dopamine D1–D3Receptor Heteromers

(2008) Daniel Marcellino et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2008) Takayoshi Suzuki et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2008) T. Lee et al.   MOLECULAR PHARMACOLOGY

Identification of a serotonin/glutamate receptor complex implicated in psychosis

(2008) Javier González-Maeso et al.   NATURE