Related references
Note: Only part of the references are listed.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
Rebecca N. Burns et al.
BIOCHEMICAL PHARMACOLOGY (2014)
Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus
Elisabeth Defossa et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2014)
GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans
Virginia M. Stone et al.
DIABETOLOGIA (2014)
Free fatty acids and protein kinase C activation induce GPR120 (free fatty acid receptor 4) phosphorylation
Omar B. Sanchez-Reyes et al.
EUROPEAN JOURNAL OF PHARMACOLOGY (2014)
GPR40 activation leads to CREB and ERK phosphorylation in primary cultures of neurons from the mouse CNS and in human neuroblastoma cells
Marta Zamarbide et al.
HIPPOCAMPUS (2014)
Concomitant Action of Structural Elements and Receptor Phosphorylation Determines Arrestin-3 Interaction with the Free Fatty Acid Receptor FFA4
Adrian J. Butcher et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2014)
Alteration of the Glucagon Axis in GPR120 (FFAR4) Knockout Mice A ROLE FOR GPR120 IN GLUCAGON SECRETION
Arthur T. Suckow et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2014)
The Molecular Basis of Ligand Interaction at Free Fatty Acid Receptor 4 (FFA4/GPR120)
Brian D. Hudson et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2014)
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875
Ankita Srivastava et al.
NATURE (2014)
The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands
Adam J. Pawson et al.
NUCLEIC ACIDS RESEARCH (2014)
Long-Chain Omega-3 Polyunsaturated Fatty Acid Intake and Risk of Colorectal Cancer
Elizabeth D. Kantor et al.
NUTRITION AND CANCER-AN INTERNATIONAL JOURNAL (2014)
Expression of the Fatty Acid Receptor GPR120 in the Gut of Diet-Induced-Obese Rats and Its Role in GLP-1 Secretion
Sarah Juel Paulsen et al.
PLOS ONE (2014)
G Protein-Coupled Receptor Deorphanizations
Olivier Civelli et al.
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 53, 2013 (2013)
The combined effects of genetic variations in the GPR120 gene and dietary fat intake on obesity risk
Toshiharu Waguri et al.
BIOMEDICAL RESEARCH-TOKYO (2013)
Drugs or diet? - Developing novel therapeutic strategies targeting the free fatty acid family of GPCRs
H. J. Dranse et al.
BRITISH JOURNAL OF PHARMACOLOGY (2013)
THE CONCISE GUIDE TO PHARMACOLOGY 2013/14: NUCLEAR HORMONE RECEPTORS
Stephen P. H. Alexander et al.
BRITISH JOURNAL OF PHARMACOLOGY (2013)
THE CONCISE GUIDE TO PHARMACOLOGY 2013/14: ENZYMES
Stephen P. H. Alexander et al.
BRITISH JOURNAL OF PHARMACOLOGY (2013)
THE CONCISE GUIDE TO PHARMACOLOGY 2013/14: G PROTEIN-COUPLED RECEPTORS
Stephen P. H. Alexander et al.
BRITISH JOURNAL OF PHARMACOLOGY (2013)
Randomized, Double-Blind, Dose-Ranging Study of TAK-875, a Novel GPR40 Agonist, in Japanese Patients With Inadequately Controlled Type 2 Diabetes
Kohei Kaku et al.
DIABETES CARE (2013)
FFAR1 Is Involved in Both the Acute and Chronic Effects of Palmitate on Insulin Secretion
Hjalti Kristinsson et al.
ENDOCRINOLOGY (2013)
The therapeutic potential of GPR120: a patent review
Somnath Halder et al.
EXPERT OPINION ON THERAPEUTIC PATENTS (2013)
Cyclooxygenase-2 induction in macrophages is modulated by docosahexaenoic acid via interactions with free fatty acid receptor 4 (FFA4)
Xinzhi Li et al.
FASEB JOURNAL (2013)
The Free Fatty Acid Receptor G Protein-coupled Receptor 40 (GPR40) Protects from Bone Loss through Inhibition of Osteoclast Differentiation
Fabien Wauquier et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2013)
Discovery of a Potent and Selective Free Fatty Acid Receptor 1 Agonist with Low Lipophilicity and High Oral Bioavailability
Elisabeth Christiansen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2013)
Minireview: The Effects of Species Ortholog and SNP Variation on Receptors for Free Fatty Acids
Brian D. Hudson et al.
MOLECULAR ENDOCRINOLOGY (2013)
In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469
C. Urban et al.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (2013)
Identification of G-protein-coupled receptor 120 as a tumor-promoting receptor that induces angiogenesis and migration in human colorectal carcinoma
Q. Wu et al.
ONCOGENE (2013)
DC260126: A Small-Molecule Antagonist of GPR40 that Protects against Pancreatic β-Cells Dysfunction in db/db Mice
Peng Sun et al.
PLOS ONE (2013)
A Novel Antidiabetic Drug, Fasiglifam/TAK-875, Acts as an Ago-Allosteric Modulator of FFAR1
Chiori Yabuki et al.
PLOS ONE (2013)
Hypothalamic GPR40 Signaling Activated by Free Long Chain Fatty Acids Suppresses CFA-Induced Inflammatory Chronic Pain
Kazuo Nakamoto et al.
PLOS ONE (2013)
The fatty acid receptor FFA1/GPR40 a decade later: how much do we know?
Arturo D. Mancini et al.
TRENDS IN ENDOCRINOLOGY AND METABOLISM (2013)
Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes
Elisabeth Christiansen et al.
ACS MEDICINAL CHEMISTRY LETTERS (2013)
Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells
Maja S. Engelstoft et al.
MOLECULAR METABOLISM (2013)
The Pharmacology of TUG-891, a Potent and Selective Agonist of the Free Fatty Acid Receptor 4 (FFA4/GPR120), Demonstrates Both Potential Opportunity and Possible Challenges to Therapeutic Agonism
Brian D. Hudson et al.
MOLECULAR PHARMACOLOGY (2013)
Chronic Treatment with Novel GPR40 Agonists Improve Whole-Body Glucose Metabolism Based on the Glucose-Dependent Insulin Secretion
Hirotsugu Tanaka et al.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2013)
International Union of Basic and Clinical Pharmacology. LXXXVIII. G Protein-Coupled Receptor List: Recommendations for New Pairings with Cognate Ligands
Anthony P. Davenport et al.
PHARMACOLOGICAL REVIEWS (2013)
A Systems Genetics Approach Identifies Genes and Pathways for Type 2 Diabetes in Human Islets
Jalal Taneera et al.
CELL METABOLISM (2012)
G Protein-Coupled Receptors in Human Fat Taste Perception
Maria Mercedes Galindo et al.
CHEMICAL SENSES (2012)
An update of novel screening methods for GPCR in drug discovery
Linjie Chen et al.
EXPERT OPINION ON DRUG DISCOVERY (2012)
Thiazolidinediones Induce Osteocyte Apoptosis by a G Protein-coupled Receptor 40-dependent Mechanism
Aleksandra Mieczkowska et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2012)
Discovery of a Potent and Selective GPR120 Agonist
Bharat Shimpukade et al.
JOURNAL OF MEDICINAL CHEMISTRY (2012)
Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists: Mesylpropoxy Appendage Lowers Lipophilicity and Improves ADME Properties
Elisabeth Christiansen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2012)
Optimization of (2,3-Dihydro-1-benzofuran-3-yl)acetic Acids: Discovery of a Non-Free Fatty Acid-Like, Highly Bioavailable G Protein-Coupled Receptor 40/Free Fatty Acid Receptor 1 Agonist as a Glucose-Dependent Insulinotropic Agent
Nobuyuki Negoro et al.
JOURNAL OF MEDICINAL CHEMISTRY (2012)
Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human
Atsuhiko Ichimura et al.
NATURE (2012)
A Potent Class of GPR40 Full Agonists Engages the EnteroInsular Axis to Promote Glucose Control in Rodents
Jian Luo et al.
PLOS ONE (2012)
Omega-3 fatty acids in anti-inflammation (pro-resolution) and GPCRs
Dong-Soon Im
PROGRESS IN LIPID RESEARCH (2012)
'PUFA-GPR40-CREB signaling' hypothesis for the adult primate neurogenesis
Tetsumori Yamashima
PROGRESS IN LIPID RESEARCH (2012)
Identification and Pharmacological Characterization of Multiple Allosteric Binding Sites on the Free Fatty Acid 1 Receptor
Daniel C. -H. Lin et al.
MOLECULAR PHARMACOLOGY (2012)
Differential Signaling by Splice Variants of the Human Free Fatty Acid Receptor GPR120
Sarah-Jane Watson et al.
MOLECULAR PHARMACOLOGY (2012)
The G-Protein-Coupled Receptor GPR40 Directly Mediates Long-Chain Fatty Acid-Induced Secretion of Cholecystokinin
Alice P. Liou et al.
GASTROENTEROLOGY (2011)
Conjugated Linoleic Acids Mediate Insulin Release through Islet G Protein-coupled Receptor FFA1/GPR40
Johannes Schmidt et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2011)
Identification of a Potent and Selective Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist with Favorable Physicochemical and in Vitro ADME Properties
Elisabeth Christiansen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2011)
Applying label-free dynamic mass redistribution technology to frame signaling of G protein-coupled receptors noninvasively in living cells
Ralf Schroeder et al.
NATURE PROTOCOLS (2011)
Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases
Saswata Talukdar et al.
TRENDS IN PHARMACOLOGICAL SCIENCES (2011)
The relationship between GPR40 and lipotoxicity of the pancreatic β-cells as well as the effect of pioglitazone
Peiwen Wu et al.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2010)
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists
Changyou Zhou et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2010)
Fishing Out a Sensor for Anti-inflammatory Oils
Alan R. Saltiel
CELL (2010)
GPR120 Is an Omega-3 Fatty Acid Receptor Mediating Potent Anti-inflammatory and Insulin-Sensitizing Effects
Da Young Oh et al.
CELL (2010)
Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation
Qi Sun et al.
MOLECULAR PHARMACOLOGY (2010)
Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469
Elisabeth Christiansen et al.
ACS MEDICINAL CHEMISTRY LETTERS (2010)
A novel class of antagonists for the FFAs receptor GPR40
Hui Hu et al.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2009)
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists
Paul S. Humphries et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3
Graeme Milligan et al.
BRITISH JOURNAL OF PHARMACOLOGY (2009)
Cloning, expression, and pharmacological characterization of the GPR120 free fatty acid receptor from cynomolgus monkey: Comparison with human GPR120 splice variants
Kristina Moore et al.
COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY B-BIOCHEMISTRY & MOLECULAR BIOLOGY (2009)
The Action and Mode of Binding of Thiazolidinedione Ligands at Free Fatty Acid Receptor 1
Nicola J. Smith et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2009)
Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion
Sara Edfalk et al.
DIABETES (2008)
Modulation of Osteoclastogenesis by Fatty Acids
Jillian Cornish et al.
ENDOCRINOLOGY (2008)
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
Elisabeth Christiansen et al.
JOURNAL OF MEDICINAL CHEMISTRY (2008)
Identification of G protein-coupled receptor 120-selective agonists derived from PPARγ agonists
Takayoshi Suzuki et al.
JOURNAL OF MEDICINAL CHEMISTRY (2008)
Discovery of novel Agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening
Irina G. Tikhonova et al.
JOURNAL OF MEDICINAL CHEMISTRY (2008)
International Union of Pharmacology. LXXI. Free Fatty Acid Receptors FFA1,-2, and-3: Pharmacology and Pathophysiological Functions
Leigh A. Stoddart et al.
PHARMACOLOGICAL REVIEWS (2008)
Identification of residues important for agonist recognition and activation in GPR40
Chi Shing Sum et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2007)
Bidirectional, iterative approach to the structural delineation of the functional Chemoprint in GPR40 for agonist recognition
Irina G. Tikhonova et al.
JOURNAL OF MEDICINAL CHEMISTRY (2007)
Uncovering the pharmacology of the G protein-coupled receptor GPR40: High apparent constitutive activity in guanosine 5'-O-(3-[S-35] thio) triphosphate binding studies reflects binding of an endogenous agonist
Leigh A. Stoddart et al.
MOLECULAR PHARMACOLOGY (2007)
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules
Celia P. Briscoe et al.
BRITISH JOURNAL OF PHARMACOLOGY (2006)
Free fatty acid receptor 1 (FFA1R/GPR40) and its involvement in fatty-acid-stimulated insulin secretion
A Salehi et al.
CELL AND TISSUE RESEARCH (2005)
Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120
A Hirasawa et al.
NATURE MEDICINE (2005)
The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
CP Briscoe et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2003)
Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40
Y Itoh et al.
NATURE (2003)
Improved reporter gene assays used to identify ligands acting on orphan seven-transmembrane receptors
K Kotarsky et al.
PHARMACOLOGY & TOXICOLOGY (2003)
Share Paper
