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https://www.readbyqxmd.com/read/28039475/gpr120-a-potential-therapeutic-target-for-experimental-colitis-in-il-10-deficient-mice
#1
Jie Zhao, Honggang Wang, Peiliang Shi, Wenbo Wang, Ye Sun
It has been proved that interleukin-10-knockout (IL-10 KO) mice display the most similar characteristics to that of human Crohn's disease (CD). Docosahexaenoic acid (DHA) has well established beneficial effects on human and animal models health with potent anti-inflammatory effects with poorly understood mechanisms. This study was aimed at figuring out whether DHA could ameliorate the Crohn's colitis by activating GPR120 and whether GPR120 could be a potential therapeutic target for CD.16 week-old mice included in our present study were divided into three groups, WT group, IL-10 KO group and DHA group(IL-10 KO mice with DHA treatment, i...
December 26, 2016: Oncotarget
https://www.readbyqxmd.com/read/28025563/novel-structural-approaches-to-study-gpcr-regulation
#2
REVIEW
Marco A Alfonzo-Méndez, Rocío Alcántara-Hernández, J Adolfo García-Sáinz
BACKGROUND: Upon natural agonist or pharmacological stimulation, G protein-coupled receptors (GPCRs) are subjected to posttranslational modifications, such as phosphorylation and ubiquitination. These posttranslational modifications allow protein-protein interactions that turn off and/or switch receptor signaling as well as trigger receptor internalization, recycling or degradation, among other responses. Characterization of these processes is essential to unravel the function and regulation of GPCR...
December 23, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28017961/ginsenoside-rb2-enhances-the-anti-inflammatory-effect-of-%C3%AF-3-fatty-acid-in-lps-stimulated-raw264-7-macrophages-by-upregulating-gpr120-expression
#3
Qi Huang, Ting Wang, He-Yao Wang
Recent studies confirm that chronic low-grade inflammation is closely associated with metabolic syndromes, and anti-inflammatory therapy is a potential approach for treating cardiovascular diseases and type 2 diabetes. Accumulating evidence suggests that GPR120 activation is a feasible solution to ameliorating chronic inflammation and improving glucose metabolism. In this study we investigated whether ginsenoside Rb2 (Rb2), which exhibited regulatory activities in glucose and lipid metabolism, affected GPR120 expression in lipopolysaccharide (LPS)-activated mouse macrophage RAW264...
December 26, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27999451/ffar4-gpr120-signaling-is-not-required-for-anti-inflammatory-and-insulin-sensitizing-effects-of-omega-3-fatty-acids
#4
Simone Isling Pærregaard, Marianne Agerholm, Annette Karen Serup, Tao Ma, Bente Kiens, Lise Madsen, Karsten Kristiansen, Benjamin Anderschou Holbech Jensen
Free fatty acid receptor-4 (FFAR4), also known as GPR120, has been reported to mediate the beneficial effects of omega-3 polyunsaturated fatty acids (ω3-PUFAs) by inducing an anti-inflammatory immune response. Thus, activation of FFAR4 has been reported to ameliorate chronic low-grade inflammation and insulin resistance accompanying obesity. However, conflicting reports on the role of FFAR4 in mediating the effects of ω3-PUFAs are emerging, suggesting that FFAR4 may not be the sole effector. Hence analyses of the importance of this receptor in relation to other signaling pathways and prominent effects of ω3-PUFAs remain to be elucidated...
2016: Mediators of Inflammation
https://www.readbyqxmd.com/read/27986832/placental-and-cord-blood-methylation-of-genes-involved-in-energy-homeostasis-association-with-fetal-growth-and-neonatal-body-composition
#5
Marta Díaz, Cristina García, Giorgia Sebastiani, Francis de Zegher, Abel López-Bermejo, Lourdes Ibáñez
Low weight at birth associates with subsequent susceptibility to diabetes. Epigenetic modulation is among the mechanisms potentially mediating this association. We performed a genome-wide DNA methylation analysis in placentas from term infants born appropriate-for-gestational-age (AGA) or small-for-gestational-age (SGA), to identify new genes related to fetal growth and neonatal body composition. Candidate genes were validated by bisulfite pyrosequencing (30 AGA, 21 SGA) and also analyzed in cord blood. Gene expression analyses were performed by RT-PCR...
December 16, 2016: Diabetes
https://www.readbyqxmd.com/read/27980130/insulinotropic-effects-of-gpr120-agonists-are-altered-in-obese-non-diabetic-and-diabetic-states
#6
Dan Zhang, Wing Yan So, Yi Wang, Shang Ying Wu, Qianni Cheng, Po Sing Leung
G protein-coupled receptor 120 (GPR120) is a putative target for obesity and diabetes therapies. However, it remains controversial whether resident GPR120 plays a direct regulatory role in islet β-cell insulin secretion. This study examined this issue in isolated rodent islets and rat β-cell line INS-1E, and assessed the role of GPR120 in islet insulin secretion in obese non-diabetic (OND) and diabetic states. GPR120 expression was detected in rodent islet β cells. Docosahexaenoic acid (DHA) and synthetic GPR120 agonist GSK137647 (GSK) augmented insulin release from rat/mouse islets and INS-1E; DHA effects were partially mediated by GPR40...
December 15, 2016: Clinical Science (1979-)
https://www.readbyqxmd.com/read/27959384/pro-metastatic-intracellular-signaling-of-the-elaidic-trans-fatty-acid
#7
Kiyomu Fujii, Yi Luo, Rina Fujiwara-Tani, Shingo Kishi, Song He, Shuyun Yang, Takamitsu Sasaki, Hitoshi Ohmori, Hiroki Kuniyasu
Trans fatty acids (TFAs) are risk factors of cardiovascular disorders, and a few studies have reported the cancer-promoting effects of TFAs. In the present study, we examined the effects and signaling of elaidic acid (EA), a TFA, in colorectal cancer (CRC) cells. Oral intake of EA increased the metastasis of CT26 mouse CRC cells by inducing the expression of stemness markers nucleostemin (NS) and CD133. Mechanisms underlying EA-induced signaling were confirmed by determining the binding of EA to G-protein coupled receptor 40 (GPR40) and GPR120 by performing surface protein internalization assay...
January 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/27881903/forskolin-inhibits-lipopolysaccharide-induced-modulation-of-mcp-1-and-gpr120-in-3t3-l1-adipocytes-through-an-inhibition-of-nf%C3%AE%C2%BAb
#8
Jeanne Durendale Chiadak, Tatjana Arsenijevic, Kevin Verstrepen, Françoise Gregoire, Nargis Bolaky, Valérie Delforge, Véronique Flamand, Jason Perret, Christine Delporte
In an obese state, Toll-like receptor-4 (TLR-4) upregulates proinflammatory adipokines secretion including monocyte chemotactic protein-1 (MCP-1) in adipose tissue. In contrast, G-protein coupled receptor 120 (GPR120) mediates antiobesity effects. The aim of this study was to determine the signaling pathway by which Forskolin (FK), a cyclic adenosine monophosphate- (cAMP-) promoting agent causing positive changes in body composition in overweight and obese adult men, affects MCP-1 and GPR120 expression during an inflammatory response induced by lipopolysaccharide (LPS) in adipocytes, such as in an obese state...
2016: Mediators of Inflammation
https://www.readbyqxmd.com/read/27873088/anti-inflammatory-and-insulin-sensitizing-effects-of-free-fatty-acid-receptors
#9
Junki Miyamoto, Mayu Kasubuchi, Akira Nakajima, Ikuo Kimura
Chronic low-grade inflammation in macrophages and adipose tissues can promote the development of obesity and type 2 diabetes. Free fatty acids (FFAs) have important roles in various tissues, acting as both essential energy sources and signaling molecules. FFA receptors (FFARs) can modulate inflammation in various types of cells and tissues; however the underlying mechanisms mediating these effects are unclear. FFARs are activated by specific FFAs; for example, GPR40 and GPR120 are activated by medium and long chain FFAs, GPR41 and GPR43 are activated by short chain FFAs, and GPR84 is activated by medium-chain FFAs...
November 22, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27853148/the-lipid-sensor-gpr120-promotes-brown-fat-activation-and-fgf21-release-from-adipocytes
#10
Tania Quesada-López, Rubén Cereijo, Jean-Valery Turatsinze, Anna Planavila, Montserrat Cairó, Aleix Gavaldà-Navarro, Marion Peyrou, Ricardo Moure, Roser Iglesias, Marta Giralt, Decio L Eizirik, Francesc Villarroya
The thermogenic activity of brown adipose tissue (BAT) and browning of white adipose tissue are important components of energy expenditure. Here we show that GPR120, a receptor for polyunsaturated fatty acids, promotes brown fat activation. Using RNA-seq to analyse mouse BAT transcriptome, we find that the gene encoding GPR120 is induced by thermogenic activation. We further show that GPR120 activation induces BAT activity and promotes the browning of white fat in mice, whereas GRP120-null mice show impaired cold-induced browning...
November 17, 2016: Nature Communications
https://www.readbyqxmd.com/read/27815121/discovery-of-benzofuran-propanoic-acid-gpr120-agonists-from-uhts-hit-to-mechanism-based-pharmacodynamic-effects
#11
Matthew Lombardo, Kate Bender, Clare London, Melissa Kirkland, Joel Mane, Michele Pachanski, Wayne Geissler, John Cummings, Bahanu Habulihaz, Taro E Akiyama, Jerry Di Salvo, Maria Madeira, Joanna Pols, Mary Ann Powles, Michael F Finley, Eric Johnson, Thomas Roussel, Victor N Uebele, Alejandro Crespo, Dennis Leung, Candice Alleyne, Dorina Trusca, Ying Lei, Andrew D Howard, Feroze Ujjainwalla, James R Tata, Christopher J Sinz
The transformation of an aryloxybutanoic acid ultra high-throughput screening (uHTS) hit into a potent and selective series of G-protein coupled receptor 120 (GPR120) agonists is reported. uHTS hit 1 demonstrated an excellent rodent pharmacokinetic profile and selectivity over the related fatty acid receptor GPR40, but only modest GPR120 potency. Optimization of the "left-hand" aryl group led to compound 6, which demonstrated a GPR120 mechanism-based pharmacodynamic effect in a mouse oral glucose tolerance test (oGTT)...
October 24, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27811230/in-vivo-activation-of-leukocyte-gpr120-ffar4-by-pufas-has-minimal-impact-on-atherosclerosis-in-ldl-receptor-knockout-mice
#12
Swapnil V Shewale, Amanda L Brown, Xin Bi, Elena Boudyguina, Janet K Sawyer, Martha A Alexander-Miller, John S Parks
G protein-coupled receptor (GPR)120/FFA receptor (FFAR)4 (GPR120/FFAR4) activation by n-3 PUFAs attenuates inflammation, but its impact on atherosclerosis is unknown. We determined whether in vivo activation of leukocyte GPR120/FFAR4 by n-3 versus n-6 PUFAs is atheroprotective. Leukocyte GPR120/FFAR4 WT or KO mice in the LDL receptor KO background were generated by bone marrow transplantation. Mice were fed one of the four atherogenic diets containing 0.2% cholesterol and 10% calories as palm oil (PO) + 10% calories as: 1) PO, 2) fish oil (FO; 20:5 n-3 and 22:6 n-3 enriched), 3) echium oil (EO; 18:4 n-3 enriched), or 4) borage oil (BO; 18:3 n-6 enriched) for 16 weeks...
January 2017: Journal of Lipid Research
https://www.readbyqxmd.com/read/27807695/pharmacological-tool-compounds-for-the-free-fatty-acid-receptor-4-ffa4-gpr120
#13
Steffen V F Hansen, Trond Ulven
The free fatty acid receptor 4 (FFA4), also known as GPR120, is a G protein-coupled receptor that is activated by long-chain fatty acids and that has been associated with regulation of appetite, release of insulin controlling hormones, insulin sensitization, anti-inflammatory and potentially anti-obesity activity, and is progressively appearing as an attractive potential target for the treatment of metabolic dysfunctions such as obesity, type 2 diabetes and inflammatory disorders. Ongoing investigations of the pharmacological functions of FFA4 and validation of its potential as a therapeutic target depend critically on the appropriateness and quality of the available pharmacological probes or tool compounds...
November 3, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27779915/gpr119-a-major-enteroendocrine-sensor-of-dietary-triglyceride-metabolites-coacting-in-synergy-with-ffa1-gpr40
#14
Jeppe H Ekberg, Maria Hauge, Line V Kristensen, Andreas N Madsen, Maja S Engelstoft, Anna-Sofie Husted, Rasmus Sichlau, Kristoffer L Egerod, Pascal Timshel, Timothy J Kowalski, Fiona M Gribble, Frank Reiman, Harald S Hansen, Andrew D Howard, Birgitte Holst, Thue W Schwartz
Triglycerides (TGs) are among the most efficacious stimulators of incretin secretion; however, the relative importance of FFA1 (G Protein-coupled Receptor [GPR] 40), FFA4 (GPR120), and GPR119, which all recognize TG metabolites, ie, long-chain fatty acid and 2-monoacylglycerol, respectively, is still unclear. Here, we find all 3 receptors to be highly expressed and highly enriched in fluorescence-activated cell sorting-purified GLP-1 and GIP cells isolated from transgenic reporter mice. In vivo, the TG-induced increase in plasma GIP was significantly reduced in FFA1-deficient mice (to 34%, mean of 4 experiments each with 8-10 animals), in GPR119-deficient mice (to 24%) and in FFA1/FFA4 double deficient mice (to 15%) but not in FFA4-deficient mice...
December 2016: Endocrinology
https://www.readbyqxmd.com/read/27757764/application-of-gpcr-structures-for-modelling-of-free-fatty-acid-receptors
#15
Irina G Tikhonova
Five G protein-coupled receptors (GPCRs) have been identified to be activated by free fatty acids (FFA). Among them, FFA1 (GPR40) and FFA4 (GPR120) bind long-chain fatty acids, FFA2 (GPR43) and FFA3 (GPR41) bind short-chain fatty acids and GPR84 binds medium-chain fatty acids. Free fatty acid receptors have now emerged as potential targets for the treatment of diabetes, obesity and immune diseases. The recent progress in crystallography of GPCRs has now enabled the elucidation of the structure of FFA1 and provided reliable templates for homology modelling of other FFA receptors...
October 19, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27607913/development-of-novel-ligands-for-peptide-gpcrs
#16
REVIEW
Brian M Moran, Aine M McKillop, Finbarr Pm O'Harte
Incretin based glucagon-like peptide-1 receptor (GLP-1R) agonists which target a G-protein coupled receptor (GPCR) are currently used in the treatment of type 2 diabetes. This review focuses on GPCRs from pancreatic β-cells, including GLP-1, glucose-dependent insulinotropic polypeptide (GIP), glucagon, somatostatin, pancreatic polypeptide (PP), cholecystokinin (CCK), peptide YY (PYY), oxyntomodulin (OXM) and ghrelin receptors. In addition, fatty acids GPCRs are thought to have an increasing role in regulating peptide secretions namely short fatty acids GPCR (GPR41, GPR43), medium chain fatty acid GPCR (GPR84), long chain fatty acid GPCR (GPR40, GPR120) and cannabinoid-like GPCR (GPR55, GPR119)...
December 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/27573241/branched-fatty-acid-esters-of-hydroxy-fatty-acids-fahfas-protect-against-colitis-by-regulating-gut-innate-and-adaptive-immune-responses
#17
Jennifer Lee, Pedro M Moraes-Vieira, Angela Castoldi, Pratik Aryal, Eric U Yee, Christopher Vickers, Oren Parnas, Cynthia J Donaldson, Alan Saghatelian, Barbara B Kahn
We recently discovered a structurally novel class of endogenous lipids, branched palmitic acid esters of hydroxy stearic acids (PAHSAs), with beneficial metabolic and anti-inflammatory effects. We tested whether PAHSAs protect against colitis, which is a chronic inflammatory disease driven predominantly by defects in the innate mucosal barrier and adaptive immune system. There is an unmet clinical need for safe and well tolerated oral therapeutics with direct anti-inflammatory effects. Wild-type mice were pretreated orally with vehicle or 5-PAHSA (10 mg/kg) and 9-PAHSA (5 mg/kg) once daily for 3 days, followed by 10 days of either 0% or 2% dextran sulfate sodium water with continued vehicle or PAHSA treatment...
October 14, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27570890/non-acidic-free-fatty-acid-receptor-4-agonists-with-antidiabetic-activity
#18
Carlos M G Azevedo, Kenneth R Watterson, Ed T Wargent, Steffen V F Hansen, Brian D Hudson, Małgorzata A Kępczyńska, Julia Dunlop, Bharat Shimpukade, Elisabeth Christiansen, Graeme Milligan, Claire J Stocker, Trond Ulven
The free fatty acid receptor 4 (FFA4 or GPR120) has appeared as an interesting potential target for the treatment of metabolic disorders. At present, most FFA4 ligands are carboxylic acids that are assumed to mimic the endogenous long-chain fatty acid agonists. Here, we report preliminary structure-activity relationship studies of a previously disclosed nonacidic sulfonamide FFA4 agonist. Mutagenesis studies indicate that the compounds are orthosteric agonists despite the absence of a carboxylate function. The preferred compounds showed full agonist activity on FFA4 and complete selectivity over FFA1, although a significant fraction of these noncarboxylic acids also showed partial antagonistic activity on FFA1...
October 13, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27506947/g-protein-coupled-receptors-mediate-%C3%AF-3-pufas-inhibited-colorectal-cancer-by-activating-the-hippo-pathway
#19
Kun Zhang, Zhimei Hu, Haixia Qi, Zhemin Shi, Yanan Chang, Qingbin Yao, Hongmei Cui, Lina Zheng, Yawei Han, Xiaohui Han, Zhen Zhang, Ting Chen, Wei Hong
Colorectal cancer (CRC) is one of the most common cancers leading to high mortality. However, long-term administration of anti-tumor therapy for CRC is not feasible due to the side effects. Omega-3 polyunsaturated fatty acids (ω-3 PUFAs), particularly DHA and EPA, exert protection against CRC, but the mechanisms are unclear. Here, we show that ω-3 PUFAs inhibit proliferation and induce apoptosis of CRC cells in vitro and alleviate AOM/DSS-induced mice colorectal cancer in vivo. Moreover, ω-3 PUFAs promote phosphorylation and cytoplasmic retention of YAP and this effect was mediated by MST1/2 and LATS1, suggesting that the canonical Hippo Pathway is involved in ω-3 PUFAs function...
September 6, 2016: Oncotarget
https://www.readbyqxmd.com/read/27358389/erk1-2-activation-in-human-taste-bud-cells-regulates-fatty-acid-signaling-and-gustatory-perception-of-fat-in-mice-and-humans
#20
Selvakumar Subramaniam, Mehmet Hakan Ozdener, Souleymane Abdoul-Azize, Katsuyoshi Saito, Bilal Malik, Guillaume Maquart, Toshihiro Hashimoto, Philippe Marambaud, Mourad Aribi, Michael G Tordoff, Philippe Besnard, Naim Akhtar Khan
Obesity is a major public health problem. An in-depth knowledge of the molecular mechanisms of oro-sensory detection of dietary lipids may help fight it. Humans and rodents can detect fatty acids via lipido-receptors, such as CD36 and GPR120. We studied the implication of the MAPK pathways, in particular, ERK1/2, in the gustatory detection of fatty acids. Linoleic acid, a dietary fatty acid, induced via CD36 the phosphorylation of MEK1/2-ERK1/2-ETS-like transcription factor-1 cascade, which requires Fyn-Src kinase and lipid rafts in human taste bud cells (TBCs)...
October 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
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