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https://www.readbyqxmd.com/read/28503189/eicosapentaenoic-acid-shows-anti-inflammatory-effect-via-gpr120-in-3t3-l1-adipocytes-and-attenuates-adipose-tissue-inflammation-in-diet-induced-obese-mice
#1
Hodaka Yamada, Tomio Umemoto, Masafumi Kakei, Shin-Ichi Momomura, Masanobu Kawakami, San-E Ishikawa, Kazuo Hara
BACKGROUND: Saturated fatty acids have been shown to cause insulin resistance and low-grade chronic inflammation, whereas unsaturated fatty acids suppress inflammation via G-protein coupled receptor 120 (GPR120) in macrophages. However, the anti-inflammatory effects of unsaturated fatty acids in adipocytes have yet to be elucidated. Hence, the aims of the present study were to evaluate the anti-inflammatory effects of eicosapentaenoic acid (EPA) via GPR120 in adipocytes. METHODS: We used 250 μM palmitate as a representative saturated fatty acid...
2017: Nutrition & Metabolism
https://www.readbyqxmd.com/read/28495174/ppar%C3%AE-mediated-g-protein-coupled-receptor-120-signaling-pathway-promotes-transcriptional-activation-of-mir-143-in-adipocytes
#2
In-Seon Bae, Phil June Park, Jeong Hwa Lee, Eun-Gyung Cho, Tae Ryong Lee, Sang Hoon Kim
MicroRNAs (miRNAs), the small noncoding RNAs, regulate various biological processes such as adipogenesis. MicroRNA-143 (miR-143) promotes adipocyte differentiation, and is correlated with obesity in mice fed a high-fat diet. However, the transcriptional regulation of miR-143 is largely unknown. In this study, we identified that miR-143 is a target of peroxisome proliferator-activated receptor γ (PPARγ), a key transcription factor in adipogenesis. Four putative peroxisome proliferator response elements (PPREs) were identified in the miR-143 promoter region...
May 8, 2017: Gene
https://www.readbyqxmd.com/read/28455435/cd40l-dependent-pathway-is-active-at-various-stages-of-rheumatoid-arthritis-disease-progression
#3
Yanxia Guo, Alice M Walsh, Ursula Fearon, Malcolm D Smith, Mihir D Wechalekar, Xuefeng Yin, Suzanne Cole, Carl Orr, Trudy McGarry, Mary Canavan, Stephan Kelly, Tai-An Lin, Xuejun Liu, Susanna M Proudman, Douglas J Veale, Costantino Pitzalis, Sunil Nagpal
The inflammatory CD40-CD40L pathway is implicated in various autoimmune diseases, but the activity status of this pathway in various stages of rheumatoid arthritis (RA) progression is unknown. In this study, we used gene signatures of CD40L stimulation derived from human immature dendritic cells and naive B cells to assess the expression of CD40-downstream genes in synovial tissues from anti-citrullinated protein Ab-positive arthralgia, undifferentiated arthritis (UA), early RA, and established RA cohorts in comparison with healthy donors...
April 28, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28446241/polyunsaturated-fatty-acid-receptors-gpr40-and-gpr120-are-expressed-in-the-hypothalamus-and-control-energy-homeostasis-and-inflammation
#4
Nathalia R V Dragano, Carina Solon, Albina F Ramalho, Rodrigo F de Moura, Daniela S Razolli, Elisabeth Christiansen, Carlos Azevedo, Trond Ulven, Licio A Velloso
BACKGROUND: The consumption of large amounts of dietary fats is one of the most important environmental factors contributing to the development of obesity and metabolic disorders. GPR120 and GPR40 are polyunsaturated fatty acid receptors that exert a number of systemic effects that are beneficial for metabolic and inflammatory diseases. Here, we evaluate the expression and potential role of hypothalamic GPR120 and GPR40 as targets for the treatment of obesity. METHODS: Male Swiss (6-weeks old), were fed with a high fat diet (HFD, 60% of kcal from fat) for 4 weeks...
April 26, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28446062/metabolite-sensing-g-protein-coupled-receptors-facilitators-of-diet-related-immune-regulation
#5
Jian K Tan, Craig McKenzie, Eliana Mariño, Laurence Macia, Charles R Mackay
Nutrition and the gut microbiome regulate many systems, including the immune, metabolic, and nervous systems. We propose that the host responds to deficiency (or sufficiency) of dietary and bacterial metabolites in a dynamic way, to optimize responses and survival. A family of G protein-coupled receptors (GPCRs) termed the metabolite-sensing GPCRs bind to various metabolites and transmit signals that are important for proper immune and metabolic functions. Members of this family include GPR43, GPR41, GPR109A, GPR120, GPR40, GPR84, GPR35, and GPR91...
April 26, 2017: Annual Review of Immunology
https://www.readbyqxmd.com/read/28435531/discovery-of-the-first-environment-sensitive-fluorescent-probe-for-gpr120-ffa4-imaging
#6
Jiaxiang Liu, Chengsen Tian, Tianyu Jiang, Yuqi Gao, Yubin Zhou, Minyong Li, Lupei Du
GPR120, which is activated by long-chain free fatty acids (FFAs), has been recognized as a new attractive target for the treatment of type 2 diabetes and metabolic disease. The visualization and location of GPR120 in native cells can provide powerful information for guiding the physiological and pathological studies of GPR120. We report herein the first potent fluorescent probes that sensitively detect GPR120. We designed and synthesized a series of novel environment-sensitive probes with suitable fluorescence property, high biological activity on the GPR120, and acceptable cytotoxicity...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28374589/indazole-6-phenylcyclopropylcarboxylic-acids-as-selective-gpr120-agonists-with-in-vivo-efficacy
#7
William McCoull, Andrew Bailey, Peter Barton, Alan M Birch, Alastair J H Brown, Hayley S Butler, Scott Boyd, Roger J Butlin, Ben Chappell, Paul Clarkson, Shelley Collins, Robert M D Davies, Anne Ertan, Clare D Hammond, Jane L Holmes, Carol Lenaghan, Anita Midha, Pablo Morentin-Gutierrez, Jane E Moore, Piotr Raubo, Graeme Robb
GPR120 agonists have therapeutic potential for the treatment of diabetes, but few selective agonists have been reported. We identified an indazole-6-phenylcyclopropylcarboxylic acid series of GPR120 agonists and conducted SAR studies to optimize GPR120 potency. Furthermore, we identified a (S,S)-cyclopropylcarboxylic acid structural motif which gave selectivity against GPR40. Good oral exposure was obtained with some compounds displaying unexpected high CNS penetration. Increased MDCK efflux was utilized to identify compounds such as 33 with lower CNS penetration, and activity in oral glucose tolerance studies was demonstrated...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28364190/pu-erh-tea-extract-mediated-protection-against-hepatosteatosis-and-insulin-resistance-in-mice-with-diet-induced-obesity-is-associated-with-the-induction-of-de-novo-lipogenesis-in-visceral-adipose-tissue
#8
Xianbin Cai, Shuhei Hayashi, Chongye Fang, Shumei Hao, Xuanjun Wang, Shuhei Nishiguchi, Hiroko Tsutsui, Jun Sheng
BACKGROUND: White adipose tissue (WAT) is important for the maintenance of metabolic homeostasis, and metabolic syndrome is sometimes associated with WAT dysfunction in humans and animals. WAT reportedly plays a key, beneficial role in the maintenance of glucose and lipid homeostasis during de novo lipogenesis (DNL). Pu'erh tea extract (PTE) can inhibit harmful, ectopic DNL in the liver, thus protecting against hepatosteatosis, in mice with diet-induced obesity. We examined whether PTE could induce DNL in WAT and consequently protect against hepatosteatosis...
March 31, 2017: Journal of Gastroenterology
https://www.readbyqxmd.com/read/28324023/long-chain-free-fatty-acid-receptor-gpr120-mediates-oil-induced-gip-secretion-through-cck-in-male-mice
#9
Akiko Sankoda, Norio Harada, Kanako Iwasaki, Shunsuke Yamane, Yuki Murata, Kimitaka Shibue, Yotsapon Thewjitcharoen, Kazuyo Suzuki, Takanari Harada, Yoshinori Kanemaru, Satoko Shimazu-Kuwahara, Akira Hirasawa, Nobuya Inagaki
Free fatty acid receptors GPR120 and GPR40 are involved in the secretion of gut hormones. GPR120 and GPR40 are expressed in enteroendocrine K-cells and their activation induces the secretion of the incretin glucose-dependent insulinotropic polypeptide (GIP). However, the role of these receptors in fat-induced GIP secretion in vivo and the associated mechanisms are unclear. In this study, we investigated corn oil-induced GIP secretion in GPR120-knockout (GPR120-/-) and GPR40-knockout (GPR40-/-) mice. Oil-induced GIP secretion was reduced by 50% and 80% in GPR120-/- and GPR40-/- mice compared to that in wild-type (WT) mice, respectively...
March 15, 2017: Endocrinology
https://www.readbyqxmd.com/read/28317734/aroma-compound-diacetyl-suppresses-glucagon-like-peptide-1-production-and-secretion-in-stc-1-cells
#10
Triona McCarthy, Christine Bruen, Fiona O'Halloran, Harriet Schellekens, Kieran Kilcawley, John F Cryan, Linda Giblin
Diacetyl is a volatile flavour compound that has a characteristic buttery aroma and is widely used in the flavour industry. The aroma of a food plays an important role in food palatability and thus intake. This study investigates the effect of diacetyl on the satiety hormone, glucagon-like peptide (GLP-1), using the enteroendocrine cell line, STC-1. Diacetyl decreased proglucagon mRNA and total GLP-1 from glucose stimulated STC-1 cells. This dampening effect on GLP-1 appears to be mediated by increasing intracellular cAMP levels, increasing synthesis of the G protein coupled receptor, GPR120, and its recruitment to the cell surface...
August 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28314803/omega-3-polyunsaturated-fatty-acids-accelerate-airway-repair-by-activating-ffa4-in-club-cells
#11
Kyoung-Pil Lee, Soo-Jin Park, Saeromi Kang, Jung-Min Koh, Koichi Sato, Hae Young Chung, Fumikazu Okajima, Dong-Soon Im
A GPCR named FFA4 (also known as GPR120) was found to act as a GPCR for omega-3 polyunsaturated fatty acids. Its expression has been reported in lung epithelial club cells. The authors investigated whether supplementation of the omega-3 fatty acids benefits lung health. Omacor® (7.75 mg kg-1), clinically prescribed preparation of omega-3 fatty acids and FFA4-knockout mice were utilized in a naphthalene-induced mouse model of acute airway injury (one injection of 30 mg kg-1, i.p.). Naphthalene injection induced complete destruction of bronchiolar epithelial cells within a day...
March 17, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28285320/gpr120-a-critical-role-in-adipogenesis-inflammation-and-energy-metabolism-in-adipose-tissue
#12
REVIEW
Tongxing Song, Yang Yang, Yuanfei Zhou, Hongkui Wei, Jian Peng
It is well known that adipose tissue has a critical role in the development of obesity and metabolic diseases and that adipose tissue acts as an endocrine organ to regulate lipid and glucose metabolism. Accumulating in the adipose tissue, fatty acids serve as a primary source of essential nutrients and act on intracellular and cell surface receptors to regulate biological events. G protein-coupled receptor 120 (GPR120) represents a promising target for the treatment of obesity-related metabolic disorders for its involvement in the regulation of adipogenesis, inflammation, glucose uptake, and insulin resistance...
March 11, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/28277660/discovery-of-potent-and-orally-bioavailable-gpr40-full-agonists-bearing-thiophen-2-ylpropanoic-acid-scaffold
#13
He Li, Qi Huang, Cheng Chen, Bin Xu, He-Yao Wang, Ya-Qiu Long
The free fatty acid receptor GPR40 is predominantly expressed in pancreatic β-cells and enhances insulin secretion in a glucose dependent manner. Therefore, GPR40 agonists are possible novel insulin secretagogues with reduced or no risk of hypoglycemia for the treatment of type 2 diabetes mellitus (T2DM). Chemically and structurally diverse GPR40 agonists with high safety are pursued for the clinical development of GPR40-based pharmacotherapeutics. Herein we report our design and discovery of a new chemotype of GPR40 agonists free of the typical phenylpropanoic acid scaffold...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28263744/gpr120-in-adipocytes-has-differential-roles-in-the-production-of-pro-inflammatory-adipocytokines
#14
Arif Ul Hasan, Koji Ohmori, Takeshi Hashimoto, Kazuyo Kamitori, Fuminori Yamaguchi, Takahisa Noma, Junsuke Igarashi, Kazuhito Tsuboi, Masaaki Tokuda, Akira Nishiyama, Masakazu Kohno
How nutritional excess leads to inflammatory responses in metabolic syndrome is not well characterized. Here, we evaluated the effects of ω-3 polyunsaturated fatty acid specific G-protein coupled receptor 120 (GPR120) activation on inflammatory pathways in adipocytes, and the influence of this process on macrophage migration. Using 3T3-L1 adipocytes, we found that agonizing GPR120 using its synthetic ligand, GSK137647, attenuated both basal and lipopolysaccharide-induced production of interleukin-6 (IL-6) and C-C motif chemokine ligand 2 (CCL2)...
April 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28261474/expression-of-fatty-acid-sensing-g-protein-coupled-receptors-in-peripartal-holstein-cows
#15
Alea Agrawal, Abdulrahman Alharthi, Mario Vailati-Riboni, Zheng Zhou, Juan J Loor
BACKGROUND: G-protein coupled receptors (GPCR), also referred as Free Fatty Acid Receptors (FFAR), are widely studied within human medicine as drug targets for metabolic disorders. To combat metabolic disorders prevalent in dairy cows during the transition period, which co-occur with negative energy balance and changes to lipid and glucose metabolism, it may be helpful to identify locations and roles of FFAR and other members of the GPCR family in bovine tissues. RESULTS: Quantitative RT-PCR (qPCR) of subcutaneous adipose, liver, and PMNL samples during the transition period (-10, +7, and +20 or +30 d) were used for expression profiling of medium- (MCFA) and long-chain fatty acid (LCFA) receptors GPR120 and GPR40, MCFA receptor GPR84, and niacin receptor HCAR2/3...
2017: Journal of Animal Science and Biotechnology
https://www.readbyqxmd.com/read/28183801/fatty-acid-16-4-n-3-stimulates-a-gpr120-induced-signaling-cascade-in-splenic-macrophages-to-promote-chemotherapy-resistance
#16
Julia M Houthuijzen, Ilse Oosterom, Brian D Hudson, Akira Hirasawa, Laura G M Daenen, Chelsea M McLean, Steffen V F Hansen, Marijn T M van Jaarsveld, Daniel S Peeper, Sahar Jafari Sadatmand, Jeanine M L Roodhart, Chris H A van de Lest, Trond Ulven, Kenji Ishihara, Graeme Milligan, Emile E Voest
Although chemotherapy is designed to eradicate tumor cells, it also has significant effects on normal tissues. The platinum-induced fatty acid 16:4(n-3) (hexadeca-4,7,10,13-tetraenoic acid) induces systemic resistance to a broad range of DNA-damaging chemotherapeutics. We show that 16:4(n-3) exerts its effect by activating splenic F4/80(+)/CD11b(low) macrophages, which results in production of chemoprotective lysophosphatidylcholines (LPCs). Pharmacologic studies, together with analysis of expression patterns, identified GPR120 on F4/80(+)/CD11b(low) macrophages as the relevant receptor for 16:4(n-3)...
February 9, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28169160/corrigendum-to-discovery-of-benzofuran-propanoic-acid-gpr120-agonists-from-uhts-hit-to-mechanism-based-pharmacodynamic-effects-bioorg-med-chem-lett-26-2016-5724-5728
#17
Matthew Lombardo, Kate Bender, Clare London, Michael A Plotkin, 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
No abstract text is available yet for this article.
February 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28159555/different-effects-of-g-protein-coupled-receptor-120-gpr120-and-gpr40-on-cell-motile-activity-of-highly-migratory-osteosarcoma-cells
#18
Kaede Takahashi, Kaori Fukushima, Yuka Onishi, Yusuke Node, Karin Inui, Nobuyuki Fukushima, Kanya Honoki, Toshifumi Tsujiuchi
G-protein-coupled receptor 120 (GPR120) and GPR40 are members of free fatty acid (FFA) receptors and mediate a variety of biological responses through binding of medium- and long-chain FFAs. Recently, it has been reported that GPR120 and GPR40 regulated cellular functions of cancer cells. In the present study, to assess whether GPR120 and GPR40 are involved in the enhancement of cell motile activity of osteosarcoma cells, we established highly migratory (MG63-R7) cells from osteosarcoma MG-63 cells. The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells, while no change of GPR40 expression was observed...
March 11, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28148462/exploration-of-phenylpropanoic-acids-as-agonists-of-the-free-fatty-acid-receptor-4-ffa4-identification-of-an-orally-efficacious-ffa4-agonist
#19
Steven M Sparks, Christopher Aquino, Pierette Banker, Jon L Collins, David Cowan, Caroline Diaz, Steven T Dock, Donald L Hertzog, Xi Liang, Erin D Swiger, Josephine Yuen, Grace Chen, Channa Jayawickreme, David Moncol, Christopher Nystrom, Vincent Rash, Thomas Rimele, Shane Roller, Sean Ross
The long chain free fatty acid receptor 4 (FFA4/GPR120) has recently been recognized as lipid sensor playing important roles in nutrient sensing and inflammation and thus holds potential as a therapeutic target for type 2 diabetes and metabolic syndrome. To explore the effects of stimulating this receptor in animal models of metabolic disease, we initiated work to identify agonists with appropriate pharmacokinetic properties to support progression into in vivo studies. Extensive SAR studies of a series of phenylpropanoic acids led to the identification of compound 29, a FFA4 agonist which lowers plasma glucose in two preclinical models of type 2 diabetes...
January 17, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28105282/discovery-of-chromane-propionic-acid-analogues-as-selective-agonists-of-gpr120-with-in-vivo-activity-in-rodents
#20
Gregory L Adams, Francisco Velazquez, Charles Jayne, Unmesh Shah, Shouwu Miao, Eric R Ashley, Maria Madeira, Taro E Akiyama, Jerry Di Salvo, Takao Suzuki, Nengxue Wang, Quang Truong, Eric Gilbert, Dan Zhou, Andreas Verras, Melissa Kirkland, Michele Pachanski, Maryann Powles, Wu Yin, Feroze Ujjainwalla, Srikanth Venkatraman, Scott D Edmondson
GPR120 (FFAR4) is a fatty acid sensing G protein coupled receptor (GPCR) that has been identified as a target for possible treatment of type 2 diabetes. A selective activator of GPR120 containing a chromane scaffold has been designed, synthesized, and evaluated in vivo. Results of these efforts suggest that chromane propionic acid 18 is a suitable tool molecule for further animal studies. Compound 18 is selective over the closely related target GPR40 (FFAR1), has a clean off-target profile, demonstrates suitable pharmacokinetic properties, and has been evaluated in wild-type/knockout GPR120 mouse oGTT studies...
January 12, 2017: ACS Medicinal Chemistry Letters
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