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Free fatty acid receptor 1

GPR40, FFAR1, free fatty acid receptor 1, free fatty acid receptor
This gene encodes a member of the GP40 family of G protein-coupled receptors that are clustered together on chromosome 19. The encoded protein is a receptor for medium and long chain free fatty acids and may be involved in the metabolic regulation of insulin secretion. Polymorphisms in this gene may be associated with type 2 diabetes. [provided by RefSeq, Apr 2009] (from NCBI)
Top mentioned proteins: ACID, Insulin, GPR120, V1a, Glucagon
Papers on GPR40
G protein-coupled receptors: signalling and regulation by lipid agonists for improved glucose homoeostasis.
McKillop et al., Coleraine, United Kingdom. In Acta Diabetol, Feb 2016
GPR40 and GPR120 are activated by long-chain fatty acids (>C12) with both receptors coupling to the Gαq subunit that activates the Ca(2+)-dependent pathway.
Discovery of the imidazole-derived GPR40 agonist AM-3189.
Houze et al., San Francisco, United States. In Bioorg Med Chem Lett, Feb 2016
As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k).
New Insights into the High-Density Lipoprotein Dilemma.
Gotto et al., Houston, United States. In Trends Endocrinol Metab, Jan 2016
We propose here that the cardioprotective effects of alcohol are mediated by the interaction of its terminal metabolite, acetate, with the adipocyte free fatty acid receptor 2 (FFAR2), which elicits a profound antilipolytic effect that may increase insulin sensitivity without necessarily raising plasma HDL-C concentration.
Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists.
Helal et al., Ismailia, Egypt. In Eur J Med Chem, Jan 2016
Another emerging target for the design of antidiabetic agents is the free fatty acid receptor 1 (FFAR1), previously known as GPR40.
GPR40, a free fatty acid receptor, differentially impacts osteoblast behavior depending on differentiation stage and environment.
Wittrant et al., Clermont-Ferrand, France. In Mol Cell Biochem, Jan 2016
GPR40 is a free fatty acid receptor that has been recently shown to impact bone remodeling.
Alpha-cell dysfunctions and molecular alterations in male insulinopenic diabetic mice are not completely corrected by insulin.
Gosmain et al., Genève, Switzerland. In Endocrinology, Jan 2016
Pten, insulin receptor, NeuroD1, GPR40 and Sumo1 genes, which were abnormally regulated in diabetic mice.
L-Rhamnose as a source of colonic propionate inhibits insulin secretion but does not influence measures of appetite or food intake.
Robertson et al., Guildford, United Kingdom. In Appetite, Jan 2016
UNASSIGNED: Activation of free fatty acid receptor (FFAR)2 and FFAR3 via colonic short-chain fatty acids, particularly propionate, are postulated to explain observed inverse associations between dietary fiber intake and body weight.
GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus: Benefits and Challenges.
Mohammad, Riyadh, Saudi Arabia. In Curr Drug Targets, Jan 2016
GPR40 (also known as FFA receptor 1) is primarily expressed in pancreatic β-cells and is activated by medium-chain and long-chain FFAs.
Dietary Lipids Inform the Gut and Brain about Meal Arrival via CD36-Mediated Signal Transduction.
Abumrad et al., Saint Louis, United States. In J Nutr, Oct 2015
Components of dietary fat that are recognized by these receptors are the long-chain fatty acids that act as ligands for 2 G protein-coupled receptors, GPR40 and GPR120, and the fatty acid (FA) translocase/CD36.
Dietary Fatty Acids and Their Potential for Controlling Metabolic Diseases Through Activation of FFA4/GPR120.
Christiansen et al., Odense, Denmark. In Annu Rev Nutr, 2014
The free fatty acid receptor 4 (FFA4, previously GPR120) is linked to the regulation of body weight, inflammation, and insulin resistance and represents a potential target for the treatment of metabolic disorders, including type 2 diabetes and obesity.
High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.
Okada et al., San Diego, United States. In Nature, 2014
Human GPR40 receptor (hGPR40), also known as free fatty-acid receptor 1 (FFAR1), is a G-protein-coupled receptor that binds long-chain free fatty acids to enhance glucose-dependent insulin secretion.
A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice.
Olefsky et al., San Diego, United States. In Nat Med, 2014
Gpr40 is another lipid-sensing G protein-coupled receptor, and it has been difficult to identify compounds with a high degree of selectivity for Gpr120 over Gpr40 (ref.
Gut microbiota metabolism of dietary fiber influences allergic airway disease and hematopoiesis.
Marsland et al., Lausanne, Switzerland. In Nat Med, 2014
The effects of propionate on allergic inflammation were dependent on G protein-coupled receptor 41 (GPR41, also called free fatty acid receptor 3 or FFAR3), but not GPR43 (also called free fatty acid receptor 2 or FFAR2).
Pax6 is a key component of regulated glucagon secretion.
Philippe et al., Genève, Switzerland. In Endocrinology, 2012
Results indicate that Pax6 acts on the regulation of glucagon secretion at least through the transcriptional control of GCK, GPR40, and GIPR.
Thiazolidinediones induce osteocyte apoptosis by a G protein-coupled receptor 40-dependent mechanism.
Mabilleau et al., Oxford, United Kingdom. In J Biol Chem, 2012
Data indicate that thiazolidinediones (TZDs) rapidly activated Erk1/2 and p38 through G protein-coupled receptor 40 (GPR40), a receptor expressed on the surface of osteocytes.
GPR41 gene expression is mediated by internal ribosome entry site (IRES)-dependent translation of bicistronic mRNA encoding GPR40 and GPR41 proteins.
Walker et al., Israel. In J Biol Chem, 2012
GPR41 gene expression is mediated by internal ribosome entry site (IRES)-dependent translation of bicistronic mRNA encoding GPR40 and GPR41 proteins
TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial.
Leifke et al., Ann Arbor, United States. In Lancet, 2012
BACKGROUND: Activation of free fatty acid receptor 1 (FFAR1; also known as G-protein-coupled receptor 40) by fatty acids stimulated glucose-dependent β-cell insulin secretion in preclinical models.
The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets.
Rorsman et al., Ōsaka, Japan. In J Pharmacol Exp Ther, 2012
GPR40/FFA1 influences both insulin and glucagon secretion in rat islets, but only insulin secretion in human islets.
Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system.
Tokuyama et al., Kōbe, Japan. In Brain Res, 2012
Antinociception via beta-endorphin release is mediated through GPR40 signaling in the supraspinal area and provides valuable information on a novel therapeutic approach for pain control.
The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse.
Edlund et al., Umeå, Sweden. In Cell Metab, 2005
GPR40 plays an important role in the chain of events linking obesity and type 2 diabetes.
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