Endogenous metabolites as ligands for G protein-coupled receptors modulating risk factors for metabolic and cardiovascular disease

Diabetes Mellitus and the β Cell: The Last Ten Years

(2012) Frances M. Ashcroft et al.   CELL

G-Protein-Coupled Receptors in Intestinal Chemosensation

(2012) Frank Reimann et al.   Cell Metabolism

Omega 3 Fatty Acids and GPR120

(2012) Da Young Oh et al.   Cell Metabolism

GPRC6A Mediates the Effects ofl-Arginine on Insulin Secretion in Mouse Pancreatic Islets

(2012) Min Pi et al.   ENDOCRINOLOGY

Multiligand Specificity and Wide Tissue Expression of GPRC6A Reveals New Endocrine Networks

(2012) Min Pi et al.   ENDOCRINOLOGY

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

(2012) Hiroshi Nagasaki et al.   FEBS LETTERS

Short-chain fatty acid receptor GPR41-mediated activation of sympathetic neurons involves synapsin 2b phosphorylation

(2012) Daisuke Inoue et al.   FEBS LETTERS

Bile acid receptors as targets for the treatment of dyslipidemia and cardiovascular disease

(2012) Geoffrey Porez et al.   JOURNAL OF LIPID RESEARCH

(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic Acid (MK-1903): A Potent GPR109a Agonist that Lowers Free Fatty Acids in Humans

(2012) P. Douglas Boatman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Potent and Selective GPR120 Agonist

(2012) Bharat Shimpukade 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

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

(2012) Atsuhiko Ichimura et al.   NATURE

G protein-coupled receptors for energy metabolites as new therapeutic targets

(2012) Clara C. Blad et al.   NATURE REVIEWS DRUG DISCOVERY

Sweet taste receptor signaling in beta cells mediates fructose-induced potentiation of glucose-stimulated insulin secretion

(2012) G. A. Kyriazis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

It Ain't Over 'Til the Fat Lady Sings

(2012) S. Offermanns   Science Translational Medicine

Niacin Lipid Efficacy Is Independent of Both the Niacin Receptor GPR109A and Free Fatty Acid Suppression

(2012) B. Lauring et al.   Science Translational Medicine

GPR119 as a fat sensor

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

The role of the gut sweet taste receptor in regulating GLP-1, PYY, and CCK release in humans

(2011) A. C. Gerspach et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

The extracellular calcium-sensing receptor is required for cholecystokinin secretion in response to l-phenylalanine in acutely isolated intestinal I cells

(2011) Alice P. Liou et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Discovery of a potent and selective small molecule hGPR91 antagonist

(2011) Debnath Bhuniya et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

AMG 837: A potent, orally bioavailable GPR40 agonist

(2011) Jonathan B. Houze et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion

(2011) HE Parker et al.   BRITISH JOURNAL OF PHARMACOLOGY

Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways

(2011) H Lan et al.   BRITISH JOURNAL OF PHARMACOLOGY

Endocrine Regulation of Male Fertility by the Skeleton

(2011) Franck Oury et al.   CELL

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading

(2011) Thijs W.H. Pols et al.   Cell Metabolism

The role of G-protein-coupled receptors in mediating the effect of fatty acids on inflammation and insulin sensitivity

(2011) Da Young Oh et al.   CURRENT OPINION IN CLINICAL NUTRITION AND METABOLIC CARE

Metabolic diseases and cancer risk

(2011) Malin H. Faulds et al.   CURRENT OPINION IN ONCOLOGY

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

Inflammation inhibits GPR81 expression in adipose tissue

(2011) Kenneth R. Feingold et al.   INFLAMMATION RESEARCH

GPRC6A mediates responses to osteocalcin in β-cells in vitro and pancreas in vivo

(2011) Min Pi et al.   JOURNAL OF BONE AND MINERAL RESEARCH

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

Nicotinic acid inhibits progression of atherosclerosis in mice through its receptor GPR109A expressed by immune cells

(2011) Martina Lukasova et al.   JOURNAL OF CLINICAL INVESTIGATION

Nutrient sensing receptors in gastric endocrine cells

(2011) Désirée Haid et al.   JOURNAL OF MOLECULAR HISTOLOGY

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

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

Type 2 diabetes across generations: from pathophysiology to prevention and management

(2011) Christopher J Nolan et al.   LANCET

Calcium-sensing receptor activating phosphorylation of PKCδ translocation on mitochondria to induce cardiomyocyte apoptosis during ischemia/reperfusion

(2011) Huishuang Zheng et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

The G Protein-Coupled Bile Acid Receptor, TGR5, Stimulates Gallbladder Filling

(2011) Tingting Li et al.   MOLECULAR ENDOCRINOLOGY

Exciting Times beyond the Brain: Metabotropic Glutamate Receptors in Peripheral and Non-Neural Tissues

(2011) M. Julio-Pieper et al.   PHARMACOLOGICAL REVIEWS

International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B)

(2011) S. Offermanns et al.   PHARMACOLOGICAL REVIEWS

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

The sweet taste of true synergy: positive allosteric modulation of the human sweet taste receptor

(2011) Guy Servant et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Nicotinic acid (niacin): new lipid-independent mechanisms of action and therapeutic potentials

(2011) Martina Lukasova 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

Calcium-sensing receptor: a sensor and mediator of ischemic preconditioning in the heart

(2010) Junhui Sun et al.   AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY

Metabotropic Glutamate Receptors: Physiology, Pharmacology, and Disease

(2010) Colleen M. Niswender et al.   Annual Review of Pharmacology and Toxicology

LPA Receptors: Subtypes and Biological Actions

(2010) Ji Woong Choi et al.   Annual Review of Pharmacology and Toxicology

Evidence That Niacin Inhibits Acute Vascular Inflammation and Improves Endothelial Dysfunction Independent of Changes in Plasma Lipids

(2010) Ben J. Wu et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

The membrane-bound bile acid receptor TGR5 (Gpbar-1) is localized in the primary cilium of cholangiocytes

(2010) Verena Keitel et al.   BIOLOGICAL CHEMISTRY

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

(2010) Da Young Oh et al.   CELL

An Autocrine Lactate Loop Mediates Insulin-Dependent Inhibition of Lipolysis through GPR81

(2010) Kashan Ahmed et al.   Cell Metabolism

Molecular mechanisms underlying nutrient-stimulated incretin secretion

(2010) Helen E. Parker et al.   EXPERT REVIEWS IN MOLECULAR MEDICINE

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 bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain

(2010) Verena Keitel et al.   GLIA

GPRC6A Mediates the Non-genomic Effects of Steroids

(2010) Min Pi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Gq/G11-mediated signaling pathway is critical for autocrine potentiation of insulin secretion in mice

(2010) Antonia Sassmann et al.   JOURNAL OF CLINICAL INVESTIGATION

Nicotinic acid– and monomethyl fumarate–induced flushing involves GPR109A expressed by keratinocytes and COX-2–dependent prostanoid formation in mice

(2010) Julien Hanson et al.   JOURNAL OF CLINICAL INVESTIGATION

Gender-dependent effect of Gpbar1 genetic deletion on the metabolic profiles of diet-induced obese mice

(2010) Galya Vassileva et al.   JOURNAL OF ENDOCRINOLOGY

The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation

(2010) Thijs W.H. Pols et al.   JOURNAL OF HEPATOLOGY

Taste Preference for Fatty Acids Is Mediated by GPR40 and GPR120

(2010) C. Cartoni et al.   JOURNAL OF NEUROSCIENCE

High glucose and renin release: the role of succinate and GPR91

(2010) János Peti-Peterdi   KIDNEY INTERNATIONAL

Glucose-mediated spatial interactions of voltage dependent calcium channels and calcium sensing receptor in insulin producing β-cells

(2010) Jai Parkash   LIFE SCIENCES

Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation

(2010) Q. Sun et al.   MOLECULAR PHARMACOLOGY

Expression and function of the bile acid receptor GpBAR1 (TGR5) in the murine enteric nervous system

(2010) D. P. Poole et al.   NEUROGASTROENTEROLOGY AND MOTILITY

Broad-spectrum amino acid-sensing class C G-protein coupled receptors: Molecular mechanisms, physiological significance and options for drug development

(2010) Arthur D. Conigrave et al.   PHARMACOLOGY & THERAPEUTICS

T1r3 and α-Gustducin in Gut Regulate Secretion of Glucagon-like Peptide-1

(2009) Zaza Kokrashvili et al.   Annals of the New York Academy of Sciences

Expression of short-chain fatty acid receptor GPR41 in the human colon

(2009) Hideaki Tazoe et al.   BIOMEDICAL RESEARCH-TOKYO

5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b

(2009) Philip J. Skinner et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

Molecular determinants of non-competitive antagonist binding to the mouse GPRC6A receptor

(2009) Helene Faure et al.   CELL CALCIUM

TGR5-Mediated Bile Acid Sensing Controls Glucose Homeostasis

(2009) Charles Thomas et al.   Cell Metabolism

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

The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders

(2009) Verena Keitel et al.   HEPATOLOGY

Unique Ligand Selectivity of the GPR92/LPA5Lysophosphatidate Receptor Indicates Role in Human Platelet Activation

(2009) Jesica R. Williams et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Peroxisome Proliferator-activated Receptor γ Regulates Expression of the Anti-lipolytic G-protein-coupled Receptor 81 (GPR81/Gpr81)

(2009) Ellen H. Jeninga 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

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

Colonic Gene Expression in Conventional and Germ-Free Mice with a Focus on the Butyrate Receptor GPR109A and the Butyrate Transporter SLC5A8

(2009) Gail A. Cresci et al.   JOURNAL OF GASTROINTESTINAL SURGERY

Activation of the Succinate Receptor GPR91 in Macula Densa Cells Causes Renin Release

(2009) S. L. Vargas et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Localization of the succinate receptor in the distal nephron and its signaling in polarized MDCK cells

(2009) Joris H. Robben et al.   KIDNEY INTERNATIONAL

N-Oleoyldopamine Enhances Glucose Homeostasis through the Activation of GPR119

(2009) Zhi-Liang Chu et al.   MOLECULAR ENDOCRINOLOGY

Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B

(2009) Y. Irukayama-Tomobe et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lipolysis and lipid mobilization in human adipose tissue

(2009) Max Lafontan et al.   PROGRESS IN LIPID RESEARCH

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

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

The psoriasis drug monomethylfumarate is a potent nicotinic acid receptor agonist

(2008) Hua Tang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Role of GPR81 in lactate-mediated reduction of adipose lipolysis

(2008) Tian-Quan Cai et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Expression and function of the bile acid receptor TGR5 in Kupffer cells

(2008) Verena Keitel et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Free Fatty Acid Receptors and Drug Discovery

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

Anatomical Profiling of G Protein-Coupled Receptor Expression

(2008) Jean B. Regard et al.   CELL

Glucose Sensing in L Cells: A Primary Cell Study

(2008) Frank Reimann et al.   Cell Metabolism

Niacin: An old drug rejuvenated

(2008) Vaijinath S. Kamanna et al.   Current Atherosclerosis Reports

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

(2008) M. Kebede 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

Lactate Inhibits Lipolysis in Fat Cells through Activation of an Orphan G-protein-coupled Receptor, GPR81

(2008) Changlu Liu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans

(2008) Eseng Lai et al.   Journal of Clinical Lipidology

No evidence for a bone phenotype in GPRC6A knockout mice under normal physiological conditions

(2008) Petrine Wellendorph et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

An energy supply network of nutrient absorption coordinated by calcium and T1R taste receptors in rat small intestine

(2008) Oliver J. Mace et al.   JOURNAL OF PHYSIOLOGY-LONDON

Antilipolytic effect of calcium-sensing receptor in human adipocytes

(2008) Mariana Cifuentes et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

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

(2008) T. Lee et al.   MOLECULAR PHARMACOLOGY

Triggering the succinate receptor GPR91 on dendritic cells enhances immunity

(2008) Tina Rubic et al.   NATURE IMMUNOLOGY

The succinate receptor GPR91 in neurons has a major role in retinal angiogenesis

(2008) Przemyslaw Sapieha et al.   NATURE MEDICINE

Colocalization of GPR120 with phospholipase-Cβ2 and α-gustducin in the taste bud cells in mice

(2008) Shigenobu Matsumura et al.   NEUROSCIENCE LETTERS

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

GPRC6A Null Mice Exhibit Osteopenia, Feminization and Metabolic Syndrome

(2008) Min Pi et al.   PLoS One

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

Nicotinic Acid: Pharmacological Effects and Mechanisms of Action

(2007) Andreas Gille et al.   Annual Review of Pharmacology and Toxicology

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

Nicotinic acid: an old drug with a promising future

(2007) E T Bodor et al.   BRITISH JOURNAL OF PHARMACOLOGY