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GoPubMed Proteins lists recent and important papers and reviews for proteins. Page last changed on 19 Dec 2016.

G-protein coupled receptor 119

GPR119, gpcr2, G protein-coupled receptor 119, glucose-dependent insulinotropic receptor
This gene encodes a member of the rhodopsin subfamily of G-protein-coupled receptors that is expressed in the pancreas and gastrointestinal tract. The encoded protein is activated by lipid amides including lysophosphatidylcholine and oleoylethanolamide and may be involved in glucose homeostasis. This protein is a potential drug target in the treatment of type 2 diabetes.[provided by RefSeq, Jan 2010] (from NCBI)
Top mentioned proteins: Insulin, Glucagon, E4, ACID, CAN
Papers on GPR119
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
GPR119 is activated by fatty acid ethanolamides and binds to Gαs utilising the adenylate cyclase pathway, which is dependent upon protein kinase A. Current research indicates that GPCR therapies may be approved for clinical use in the near future.
GPR119: a promising target for nonalcoholic fatty liver disease.
Kang et al., Seoul, South Korea. In Faseb J, Jan 2016
G-protein-coupled receptor 119 (GPR119) is a promising target for type 2 diabetes.
Ageing is associated with molecular signatures of inflammation and type 2 diabetes in rat pancreatic islets.
Constância et al., Cambridge, United Kingdom. In Diabetologia, Jan 2016
Age-associated transcriptional differences negatively correlated with promoter DNA methylation at several loci related to inflammation, glucose homeostasis, cell proliferation and cell-matrix interactions (Il33, Cxcl9, Gpr119, Fbp2, Col3a1, Dpt, Spp1).
Mutation-Guided Unbiased Modeling of the Fat Sensor GPR119 for High-Yield Agonist Screening.
Frimurer et al., Copenhagen, Denmark. In Structure, Jan 2016
We have developed a data-driven optimization protocol, which integrates mutational data and structural information from multiple X-ray receptor structures in combination with a fully flexible ligand docking protocol to determine the binding conformation of AR231453, a small-molecule agonist, in the GPR119 receptor.
Toxicokinetics and toxicity of atorvastatin in dogs.
Polli et al., United States. In Toxicol Appl Pharmacol, Dec 2015
We recently had a clinical development program evaluating a combination of atorvastatin with a GPR119 agonist as a treatment for dyslipidemia, where toxicological evaluations in dogs were completed.
Discovery of the oxazabicyclo[3.3.1]nonane derivatives as potent and orally active GPR119 agonists.
Greenlee et al., United States. In Bioorg Med Chem Lett, Dec 2015
The design and synthesis of two conformationally restricted oxazabicyclo octane derivatives as GRP119 agonists is described.
G Protein-Coupled Receptor 119 (GPR119) Agonists for the Treatment of Diabetes: Recent Progress and Prevailing Challenges.
Schwink et al., Frankfurt am Main, Germany. In J Med Chem, Dec 2015
UNASSIGNED: In this Perspective, recent advances and challenges in the development of GPR119 agonists as new oral antidiabetic drugs will be discussed.
Constitutive Activity among Orphan Class-A G Protein Coupled Receptors.
Aronstam et al., Rolla, United States. In Plos One, 2014
Five patterns of activity were noted: 1) inhibition under both baseline and forskolin stimulated expression (GPR15, GPR17, GPR18, GPR20, GPR25, GPR27, GPR31, GPR32, GPR45, GPR57, GPR68, GPR83, GPR84, GPR132, GPR150, GPR176); 2) no effect on baseline expression, but inhibition of forskolin stimulated expression (GPR4, GPR26, GPR61, GPR62, GPR78, GPR101, GPR119); 3) elevation of baseline signaling coupled with inhibition of forskolin stimulated expression (GPR6, GPR12); 4) elevation of baseline signaling without inhibition of forskolin stimulated expression (GPR3, GPR21, GPR52, GPR65); and 5) no effect on expression (GPR1, GPR19, GPR22, GPR34, GPR35, GPR39, GPR63, GPR82, GPR85, GPR87).
Simvastatin Impairs Insulin Secretion by Multiple Mechanisms in MIN6 Cells.
Laakso et al., Kuopio, Finland. In Plos One, 2014
Impaired insulin secretion caused by simvastatin treatment were efficiently restored by GPR119 or GLP-1 receptor stimulation and by direct activation of cAMP-dependent signaling pathways with forskolin.
Lysophosphatidylcholine and lysophosphatidylinosiol--novel promissing signaling molecules and their possible therapeutic activity.
Koziołkiewicz et al., In Acta Pol Pharm, 2014
Their recently revealed activities as novel ligands of orphan G protein-coupled receptors (i.e., GPR55 and GPR119) involved in modulation of tumor physiology and insulin secretion seem to be one of the most interesting aspects of these compounds.
Classical endocannabinoid-like compounds and their regulation by nutrients.
Hansen et al., Copenhagen, Denmark. In Biofactors, 2014
A chronic high-fat diet will decrease intestinal levels of these anorectic N-acylethanolamines and this may contribute to the hyperphagic effect of high-fat diet; 2-monoacylglycerols mediate endocrine responses in the small intestine; probably trough activation of GPR119 on enteroendocrine cells, and diet-derived 2-monoacylglycerols, for example, 2-oleoylglycerol and 2-palmitoylglycerol might be important for intestinal fat sensing.
[Current status and issues of clinical development of novel anti-diabetic drugs].
Kaku et al., Kawasaki, Japan. In Nihon Rinsho, 2013
Clinical development of new antidiabetic drugs such as SGLT2 inhibitor, GPR40 agonist, GPR119 agonist, and GKA has been progressing world wide.
Current therapies and emerging drugs in the pipeline for type 2 diabetes.
Plodkowski et al., Reno, United States. In Am Health Drug Benefits, 2011
This article focuses on several new classes, including the sodium-glucose cotransporter-2 inhibitors (which are furthest along in development); 11beta-hydroxysteroid dehydrogenase (some of which are now in phase 2 trials); glycogen phosphorylase inhibitors; glucokinase activators; G protein-coupled receptor 119 agonists; protein tyrosine phosphatase 1B inhibitors; and glucagon-receptor antagonists.
GPR119 regulates murine glucose homeostasis through incretin receptor-dependent and independent mechanisms.
Drucker et al., Toronto, Canada. In Endocrinology, 2011
GPR119 engages multiple complementary pathways for control of glucose homeostasis.
Peptide YY is critical for acylethanolamine receptor Gpr119-induced activation of gastrointestinal mucosal responses.
Herzog et al., London, United Kingdom. In Cell Metab, 2010
Enteroendocrine L cells contain PYY and express the acylethanolamine receptor, Gpr119.
A conserved aromatic lock for the tryptophan rotameric switch in TM-VI of seven-transmembrane receptors.
Schwartz et al., Copenhagen, Denmark. In J Biol Chem, 2010
Data show that Phe-V:13 can serve as an aromatic lock for the proposed active conformation of the Trp-VI:13 rotameric switch, being involved in the global movement of TM-V and TM-VI in 7TM receptor activation.
N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Leonard et al., San Diego, United States. In Mol Endocrinol, 2010
findings show that N-oleoyldopamine (OLDA)& structurally related hydroxybenzyl amides are robust activators of GPR119; studies indicate that multiple, distinct classes of lipid amides, acting via GPR119, may be important modulators of glucose homeostasis
GPR119 is essential for oleoylethanolamide-induced glucagon-like peptide-1 secretion from the intestinal enteroendocrine L-cell.
Brubaker et al., Toronto, Canada. In Diabetes, 2009
oleoylethanolamine increases glucagon-like peptide-1 secretion from intestinal L-cells through activation of the novel GPR119 fatty acid derivate receptor in vitro and in vivo.
GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis.
Kowalski et al., United States. In J Endocrinol, 2009
GPR119 is important for incretin and insulin secretion, but not for appetite suppression.
Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents.
Reynet et al., Oxford, United Kingdom. In Cell Metab, 2006
GPR119 therefore represents a novel and attractive potential target for the therapy of obesity and related metabolic disorders.
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