Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4
Published 2015 View Full Article
- Home
- Publications
- Publication Search
- Publication Details
Title
Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4
Authors
Keywords
-
Journal
BRITISH JOURNAL OF PHARMACOLOGY
Volume 172, Issue 13, Pages 3254-3265
Publisher
Wiley
Online
2014-08-18
DOI
10.1111/bph.12879
References
Ask authors/readers for more resources
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
- (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
- 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
- GPR40 activation leads to CREB and ERK phosphorylation in primary cultures of neurons from the mouse CNS and in human neuroblastoma cells
- (2014) Marta Zamarbide et al. HIPPOCAMPUS
- Concomitant Action of Structural Elements and Receptor Phosphorylation Determines Arrestin-3 Interaction with the Free Fatty Acid Receptor FFA4
- (2014) Adrian J. Butcher et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Alteration of the Glucagon Axis in GPR120 (FFAR4) Knockout Mice
- (2014) Arthur T. Suckow et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- The Molecular Basis of Ligand Interaction at Free Fatty Acid Receptor 4 (FFA4/GPR120)
- (2014) Brian D. Hudson et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875
- (2014) Ankita Srivastava et al. NATURE
- 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
- The combined effects of genetic variations in the GPR120 gene and dietary fat intake on obesity risk
- (2013) Toshiharu WAGURI et al. BIOMEDICAL RESEARCH-TOKYO
- Drugs or diet? - Developing novel therapeutic strategies targeting the free fatty acid family of GPCRs
- (2013) H J Dranse et al. BRITISH JOURNAL OF PHARMACOLOGY
- The Concise Guide to PHARMACOLOGY 2013/14: Nuclear Hormone Receptors
- (2013) Stephen P.H. Alexander et al. BRITISH JOURNAL OF PHARMACOLOGY
- The Concise Guide to PHARMACOLOGY 2013/14: Enzymes
- (2013) Stephen P.H. Alexander et al. BRITISH JOURNAL OF PHARMACOLOGY
- The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors
- (2013) Stephen P.H. Alexander et al. BRITISH JOURNAL OF PHARMACOLOGY
- FFAR1 Is Involved in Both the Acute and Chronic Effects of Palmitate on Insulin Secretion
- (2013) Hjalti Kristinsson et al. ENDOCRINOLOGY
- Free fatty acids and protein kinase C activation induce GPR120 (free fatty acid receptor 4) phosphorylation
- (2013) Omar B. Sánchez-Reyes et al. EUROPEAN JOURNAL OF PHARMACOLOGY
- The therapeutic potential of GPR120: a patent review
- (2013) Somnath Halder et al. EXPERT OPINION ON THERAPEUTIC PATENTS
- 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
- 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
- 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
- In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469
- (2013) C. Urban et al. NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
- The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands
- (2013) Adam J. Pawson et al. NUCLEIC ACIDS RESEARCH
- Long-Chain Omega-3 Polyunsaturated Fatty Acid Intake and Risk of Colorectal Cancer
- (2013) Elizabeth D. Kantor et al. NUTRITION AND CANCER-AN INTERNATIONAL JOURNAL
- Identification of G-protein-coupled receptor 120 as a tumor-promoting receptor that induces angiogenesis and migration in human colorectal carcinoma
- (2013) Q Wu et al. ONCOGENE
- 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
- Hypothalamic GPR40 Signaling Activated by Free Long Chain Fatty Acids Suppresses CFA-Induced Inflammatory Chronic Pain
- (2013) Kazuo Nakamoto et al. PLoS One
- 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
- Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes
- (2013) Elisabeth Christiansen et al. ACS Medicinal Chemistry Letters
- Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells
- (2013) Maja S. Engelstoft et al. Molecular Metabolism
- A Systems Genetics Approach Identifies Genes and Pathways for Type 2 Diabetes in Human Islets
- (2012) Jalal Taneera et al. Cell Metabolism
- 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
- An update of novel screening methods for GPCR in drug discovery
- (2012) Linjie Chen et al. Expert Opinion on Drug Discovery
- 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
- 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
- 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
- (2012) Nobuyuki Negoro 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
- A Potent Class of GPR40 Full Agonists Engages the EnteroInsular Axis to Promote Glucose Control in Rodents
- (2012) Jian Luo et al. PLoS One
- Omega-3 fatty acids in anti-inflammation (pro-resolution) and GPCRs
- (2012) Dong-Soon Im PROGRESS IN LIPID RESEARCH
- ‘PUFA–GPR40–CREB signaling’ hypothesis for the adult primate neurogenesis
- (2012) Tetsumori Yamashima PROGRESS IN LIPID RESEARCH
- G Protein–Coupled Receptor Deorphanizations
- (2011) Olivier Civelli et al. Annual Review of Pharmacology and Toxicology
- G Protein-Coupled Receptors in Human Fat Taste Perception
- (2011) M. M. Galindo et al. CHEMICAL SENSES
- Conjugated Linoleic Acids Mediate Insulin Release through Islet G Protein-coupled Receptor FFA1/GPR40
- (2011) Johannes Schmidt et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Identification of a Potent and Selective Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist with Favorable Physicochemical and in Vitro ADME Properties
- (2011) Elisabeth Christiansen et al. JOURNAL OF MEDICINAL CHEMISTRY
- Applying label-free dynamic mass redistribution technology to frame signaling of G protein–coupled receptors noninvasively in living cells
- (2011) Ralf Schröder et al. Nature Protocols
- Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases
- (2011) Saswata Talukdar et al. TRENDS IN PHARMACOLOGICAL SCIENCES
- 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
- Fishing Out a Sensor for Anti-inflammatory Oils
- (2010) Alan R. Saltiel CELL
- 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
- Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation
- (2010) Q. Sun et al. MOLECULAR PHARMACOLOGY
- Structure−Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469
- (2010) Elisabeth Christiansen et al. ACS Medicinal Chemistry Letters
- A novel class of antagonists for the FFAs receptor GPR40
- (2009) Hui Hu et al. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
- Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists
- (2009) Paul S. Humphries et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists
- (2009) Changyou Zhou et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3
- (2009) Graeme Milligan et al. BRITISH JOURNAL OF PHARMACOLOGY
- 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
- The Action and Mode of Binding of Thiazolidinedione Ligands at Free Fatty Acid Receptor 1
- (2009) Nicola J. Smith et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Gpr40 Is Expressed in Enteroendocrine Cells and Mediates Free Fatty Acid Stimulation of Incretin Secretion
- (2008) S. Edfalk et al. DIABETES
- Modulation of Osteoclastogenesis by Fatty Acids
- (2008) Jillian Cornish et al. ENDOCRINOLOGY
- 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
- (2008) Elisabeth Christiansen et al. JOURNAL OF MEDICINAL CHEMISTRY
- Identification of G protein-coupled receptor 120-selective agonists derived from PPARγ agonists
- (2008) Takayoshi Suzuki et al. JOURNAL OF MEDICINAL CHEMISTRY
- Discovery of Novel Agonists and Antagonists of the Free Fatty Acid Receptor 1 (FFAR1) Using Virtual Screening
- (2008) Irina G. Tikhonova et al. JOURNAL OF MEDICINAL CHEMISTRY
- 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
Discover Peeref hubs
Discuss science. Find collaborators. Network.
Join a conversationBecome a Peeref-certified reviewer
The Peeref Institute provides free reviewer training that teaches the core competencies of the academic peer review process.
Get Started