Free Fatty Acid Receptors in Health and Disease

Colonic Gene Expression in Conventional and Germ-Free Mice with a Focus on the Butyrate Receptor GPR109A and the Butyrate Transporter SLC5A8

Cresci, G. A., Thangaraju, M., Mellinger, J. D., Liu, K., & Ganapathy, V. (2010) · Journal of Gastrointestinal Surgery · doi:10.1007/s11605-009-1045-x · Cited by 164

Discovery of a Potent and Selective GPR120 Agonist

Shimpukade, B., Hudson, B. D., Hovgaard, C. K., Milligan, G., & Ulven, T. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm300215x · Cited by 162

Identification of a Novel Human Eicosanoid Receptor Coupled to Gi/o

Hosoi, T., Koguchi, Y., Sugikawa, E., Chikada, A., Ogawa, K., Tsuda, N., Suto, N., Tsunoda, S., Taniguchi, T., & Ohnuki, T. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m203194200 · Cited by 162

Microbial metabolite sensor GPR43 controls severity of experimental GVHD

Fujiwara, H., Docampo, M. D., Riwes, M., Peltier, D., Toubai, T., Henig, I., Wu, S. J., Kim, S., Taylor, A., Brabbs, S., et al. (2018) · Nature Communications · doi:10.1038/s41467-018-06048-w · Cited by 161

Free Fatty Acid Receptors and Their Role in Regulation of Energy Metabolism

Hara, T., Kimura, I., Inoue, D., Ichimura, A., & Hirasawa, A. (2013) · Reviews of physiology, biochemistry and pharmacology · doi:10.1007/112_2013_13 · Cited by 160

The short chain fatty acid receptor GPR43 regulates inflammatory signals in adipose tissue M2-type macrophages

Nakajima, A., Nakatani, A., Hasegawa, S., Irie, J., Ozawa, K., Tsujimoto, G., Suganami, T., Itoh, H., & Kimura, I. (2017) · PLoS ONE · doi:10.1371/journal.pone.0179696 · Cited by 159

A place for dietary fibre in the management of the metabolic syndrome

Delzenne, N. M., & Cani, P. D. (2005) · Current Opinion in Clinical Nutrition & Metabolic Care · doi:10.1097/01.mco.0000171124.06408.71 · Cited by 158

Impaired Islet Function in Commonly Used Transgenic Mouse Lines due to Human Growth Hormone Minigene Expression

Brouwers, B., de Faudeur, G., Osipovich, A. B., Goyvaerts, L., Lemaire, K., Boesmans, L., Cauwelier, E. J. G., Granvik, M., Pruniau, V. P. E. G., Lommel, L. V., et al. (2014) · Cell Metabolism · doi:10.1016/j.cmet.2014.11.004 · Cited by 158

Evolutionary Aspects of Diet and Essential Fatty Acids

Simopoulos, A. P. (2000) · KARGER eBooks · doi:10.1159/000059742 · Cited by 156

Fermentation of polysaccharides and absorption of short chain fatty acids in the mammalian hindgut

Rechkemmer, G., Rönnau, K., & Engelhardt, W. V. (1988) · Comparative Biochemistry and Physiology Part A Physiology · doi:10.1016/0300-9629(88)90668-8 · Cited by 152

A Gut Feeling for Obesity: 7TM Sensors on Enteroendocrine Cells

Engelstoft, M. S., Egerod, K. L., Holst, B., & Schwartz, T. W. (2008) · Cell Metabolism · doi:10.1016/j.cmet.2008.11.004 · Cited by 151

Identification and Functional Characterization of Allosteric Agonists for the G Protein-Coupled Receptor FFA2

Lee, T. W., Schwandner, R., Swaminath, G., Weiszmann, J., Cardozo, M. G., Greenberg, J., Jaeckel, P., Ge, H., Wang, Y., Jiao, X., et al. (2008) · Molecular Pharmacology · doi:10.1124/mol.108.049536 · Cited by 150

The Glutamate Receptors

Mc, A., Daw, M. I., & Isaac, J. (2008) · Humana Press eBooks · doi:10.1007/978-1-59745-055-3 · Cited by 150

Lower Prevalence of Impaired Glucose Tolerance and Diabetes Associated With Daily Seal Oil or Salmon Consumption among Alaska Natives

Adler, A., Boyko, E. J., Schraer, C. D., & Murphy, N. J. (1994) · Diabetes Care · doi:10.2337/diacare.17.12.1498 · Cited by 147

Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation

Dragano, N. R. V., Solon, C., Ramalho, A. F. S., de Moura, R. F., Razolli, D. S., Christiansen, E., Azevedo, C., Ulven, T., & Velloso, L. A. (2017) · Journal of Neuroinflammation · doi:10.1186/s12974-017-0869-7 · Cited by 147

Dietary Omega-3 Fatty Acid Deficiency and High Fructose Intake in the Development of Metabolic Syndrome, Brain Metabolic Abnormalities, and Non-Alcoholic Fatty Liver Disease

Simopoulos, A. P. (2013) · Nutrients · doi:10.3390/nu5082901 · Cited by 146

TAK-875, an Orally Available G Protein-Coupled Receptor 40/Free Fatty Acid Receptor 1 Agonist, Enhances Glucose-Dependent Insulin Secretion and Improves Both Postprandial and Fasting Hyperglycemia in Type 2 Diabetic Rats

Tsujihata, Y., Ito, R., Suzuki, M., Harada, A., Negoro, N., Yasuma, T., Momose, Y., & Takeuchi, K. (2011) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.183772 · Cited by 146

Branched Fatty Acid Esters of Hydroxy Fatty Acids (FAHFAs) Protect against Colitis by Regulating Gut Innate and Adaptive Immune Responses

Lee, J., Moraes‐Vieira, P. M., Castoldi, Â., Aryal, P., Yee, E. U., Vickers, C., Parnas, O., Donaldson, C. J., Saghatelian, A., & Kahn, B. B. (2016) · Journal of Biological Chemistry · doi:10.1074/jbc.m115.703835 · Cited by 145

Trans Fat Intake and Its Dietary Sources in General Populations Worldwide: A Systematic Review

Wanders, A. J., Zock, P. L., & Brouwer, I. A. (2017) · Nutrients · doi:10.3390/nu9080840 · Cited by 144

Differential Signaling by Splice Variants of the Human Free Fatty Acid Receptor GPR120

Watson, S., Brown, A., & Holliday, N. D. (2012) · Molecular Pharmacology · doi:10.1124/mol.111.077388 · Cited by 142

Omega-3 Polyunsaturated Fatty Acids in Prevention of Mood and Anxiety Disorders

Su, K., Matsuoka, Y., & Pae, C. (2015) · Clinical Psychopharmacology and Neuroscience · doi:10.9758/cpn.2015.13.2.129 · Cited by 141

A Potent Class of GPR40 Full Agonists Engages the EnteroInsular Axis to Promote Glucose Control in Rodents

Luo, J., Swaminath, G., Brown, S. P., Zhang, J., Guo, Q., Chen, M., Nguyen, K., Tran, T., MIAO, L. N., Dransfield, P. J., et al. (2012) · PLoS ONE · doi:10.1371/journal.pone.0046300 · Cited by 140

Novel selective ligands for free fatty acid receptors GPR120 and GPR40

Hara, T., Hirasawa, A., Sun, Q. L., Sadakane, K., Itsubo, C., Iga, T., Adachi, T., Koshimizu, T., Hashimoto, T., Asakawa, Y., et al. (2009) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-009-0425-9 · Cited by 140

Free Fatty Acid Receptor GPR120 Is Highly Expressed in Enteroendocrine K Cells of the Upper Small Intestine and Has a Critical Role in GIP Secretion After Fat Ingestion

Iwasaki, K., Harada, N., Sasaki, K., Yamane, S., Iida, K., Suzuki, K., Hamasaki, A., Nasteska, D., Shibue, K., Joo, E., et al. (2014) · Endocrinology · doi:10.1210/en.2014-1653 · Cited by 139

Extracellular Ionic Locks Determine Variation in Constitutive Activity and Ligand Potency between Species Orthologs of the Free Fatty Acid Receptors FFA2 and FFA3

Hudson, B. D., Tikhonova, I. G., Pandey, S. K., Ulven, T., & Milligan, G. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.396259 · Cited by 136

Efficacy and safety of fasiglifam ( TAK ‐875), a G protein‐coupled receptor 40 agonist, in J apanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double‐blind, placebo‐controlled, phase III trial

Kaku, K., Enya, K., Nakaya, R., Ohira, T., & Matsuno, R. (2015) · Diabetes Obesity and Metabolism · doi:10.1111/dom.12467 · Cited by 135

Male mice that lack the G-protein-coupled receptor GPR41 have low energy expenditure and increased body fat content

Bellahcene, M., O’Dowd, J. F., Wargent, E. T., Zaibi, M. S., Hislop, D. C., Ngala, R. A., Smith, D. M., Cawthorne, M. A., Stocker, C. J., & Arch, J. R. S. (2012) · British Journal Of Nutrition · doi:10.1017/s0007114512003923 · Cited by 135

Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system

Nakamoto, K., Nishinaka, T., Matsumoto, K., Kasuya, F., Mankura, M., Kōyama, Y., & Tokuyama, S. (2011) · Brain Research · doi:10.1016/j.brainres.2011.11.012 · Cited by 134

GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans

Stone, V. M., Dhayal, S., Brocklehurst, K. J., Lenaghan, C., Winzell, M. S., Hammar, M., Xu, X., Smith, D. M., & Morgan, N. G. (2014) · Diabetologia · doi:10.1007/s00125-014-3213-0 · Cited by 133

The Role of Short-Chain Fatty Acids, Produced by Anaerobic Bacteria, in the Cystic Fibrosis Airway

Mirković, B., Murray, M., Lavelle, G., Molloy, K., Azim, A. A., Gunaratnam, C., Healy, F. M., Slattery, D. M., McNally, P., Hatch, J. E., et al. (2015) · American Journal of Respiratory and Critical Care Medicine · doi:10.1164/rccm.201505-0943oc · Cited by 133

Modulation of Osteoclastogenesis by Fatty Acids

Cornish, J., MacGibbon, A. K. H., Lin, J., Watson, M., Callon, K. E., Tong, P. C., Dunford, J. E., van der Does, Y., Williams, G. A., Grey, A. B., et al. (2008) · Endocrinology · doi:10.1210/en.2008-0111 · Cited by 132

The Role of the Gastrointestinal Microbiota in Colorectal Cancer

Rowland, I. R. (2009) · Current Pharmaceutical Design · doi:10.2174/138161209788168191 · Cited by 131

Redox balance is key to explaining full vs. partial switching to low-yield metabolism

van Hoek, M. J., & Merks, R. M. (2012) · BMC Systems Biology · doi:10.1186/1752-0509-6-22 · Cited by 131

The Gut-Microglia Connection: Implications for Central Nervous System Diseases

Wang, Y., Wang, Z., Wang, Y., Li, F., Jia, J., Song, X., Qin, S., Wang, R., Jin, F., Kitazato, K., et al. (2018) · Frontiers in Immunology · doi:10.3389/fimmu.2018.02325 · Cited by 130

Selective Orthosteric Free Fatty Acid Receptor 2 (FFA2) Agonists

Schmidt, J., Smith, N. J., Christiansen, E., Tikhonova, I. G., Grundmann, M., Hudson, B. D., Ward, R. J., Drewke, C., Milligan, G., Kostenis, E., et al. (2011) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.210872 · Cited by 127

N-Oleoyldopamine Enhances Glucose Homeostasis through the Activation of GPR119

Chu, Z., Carroll, C., Chen, R., Alfonso, J., Gutierrez, V., He, H., Lucman, A., Xing, C., Sebring, K., Zhou, J., et al. (2009) · Molecular Endocrinology · doi:10.1210/me.2009-0239 · Cited by 127

Identification of Residues Important for Agonist Recognition and Activation in GPR40

Sum, C. S., Tikhonova, I. G., Neumann, S., Engel, S., Raaka, B. M., Costanzi, S., & Gershengorn, M. C. (2007) · Journal of Biological Chemistry · doi:10.1074/jbc.m705077200 · Cited by 125

Inulin and fructo-oligosaccharides have divergent effects on colitis and commensal microbiota in HLA-B27 transgenic rats

Koleva, P. T., Valcheva, R. S., Sun, X., Gänzle, M. G., & Dieleman, L. A. (2012) · British Journal Of Nutrition · doi:10.1017/s0007114511007203 · Cited by 124

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

Christiansen, E., Urban, C., Merten, N., Liebscher, K., Karlsen, K. K., Hamacher, A., Spinrath, A., Bond, A. D., Drewke, C., Ullrich, S., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm8010178 · Cited by 124

Reduction in Voltage-Gated K+ Currents in Primary Cultured Rat Pancreatic β-Cells by Linoleic Acids

Feng, D. D., Luo, Z., Roh, S.-G., Hernandez, M., Tawadros, N., Keating, D. J., & Chen, C. (2006) · Endocrinology · doi:10.1210/en.2005-0225 · Cited by 124

Short-chain fatty acid receptors inhibit invasive phenotypes in breast cancer cells

Thirunavukkarasan, M., Wang, C., Rao, A., Hind, T., Teo, Y. L., Siddiquee, A. A.-M., Goghari, M. A. I., Kumar, A. P., & Herr, D. R. (2017) · PLoS ONE · doi:10.1371/journal.pone.0186334 · Cited by 124

Peptide YY Is Secreted after Oral Glucose Administration in a Gender-Specific Manner

Kim, B.-J., Carlson, O. D., Jang, H.-J., Elahi, D., Berry, C., & Egan, J. M. (2005) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2005-0409 · Cited by 122

Maternal High Fiber Diet during Pregnancy and Lactation Influences Regulatory T Cell Differentiation in Offspring in Mice

Nakajima, A., Kaga, N., Nakanishi, Y., Ohno, H., Miyamoto, J., Kimura, I., Hori, S., Sasaki, T., Hiramatsu, K., Okumura, K., et al. (2017) · The Journal of Immunology · doi:10.4049/jimmunol.1700248 · Cited by 120

Short-chain fatty acids induce acute phosphorylation of the p38 mitogen-activated protein kinase/heat shock protein 27 pathway via GPR43 in the MCF-7 human breast cancer cell line

Yonezawa, T., Kobayashi, Y., & Obara, Y. (2006) · Cellular Signalling · doi:10.1016/j.cellsig.2006.06.004 · Cited by 118

Lack of FFAR1/GPR40 Does Not Protect Mice From High-Fat Diet–Induced Metabolic Disease

Hong, L., Hoos, L. M., Liu, L., Tetzloff, G. G., Hu, W., Abbondanzo, S. J., Vassileva, G., Gustafson, E. L., Hedrick, J. A., & Davis, H. R. (2008) · Diabetes · doi:10.2337/db08-0596 · Cited by 118

Conserved Polar Residues in Transmembrane Domains V, VI, and VII of Free Fatty Acid Receptor 2 and Free Fatty Acid Receptor 3 Are Required for the Binding and Function of Short Chain Fatty Acids

Stoddart, L. A., Smith, N. J., Jenkins, L., Brown, A. J., & Milligan, G. (2008) · Journal of Biological Chemistry · doi:10.1074/jbc.m805601200 · Cited by 117

The G-protein coupled receptor, GPR84 regulates IL-4 production by T lymphocytes in response to CD3 crosslinking

Venkataraman, C., & Kuo, F. (2005) · Immunology Letters · doi:10.1016/j.imlet.2005.05.010 · Cited by 115

Expression of free fatty acid receptor GPR40 in the central nervous system of adult monkeys

Ma, D., Tao, B., Warashina, S., Kotani, S., Lu, L., Kaplamadzhiev, D. B., Mori, Y., Tonchev, A. B., & Yamashima, T. (2007) · Neuroscience Research · doi:10.1016/j.neures.2007.05.001 · Cited by 112

Defining the Molecular Basis for the First Potent and Selective Orthosteric Agonists of the FFA2 Free Fatty Acid Receptor

Hudson, B. D., Due‐Hansen, M. E., Christiansen, E., Hansen, A. M., Mackenzie, A. E., Murdoch, H., Pandey, S. K., Ward, R. J., Márquez, R., Tikhonova, I. G., et al. (2013) · Journal of Biological Chemistry · doi:10.1074/jbc.m113.455337 · Cited by 111

Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity

Martin, C., Passilly‐Degrace, P., Chevrot, M., Ancel, D., Sparks, S. M., Drucker, D. J., & Besnard, P. (2012) · Journal of Lipid Research · doi:10.1194/jlr.m025874 · Cited by 111

G protein-coupled receptors as targets for anti-diabetic therapeutics

Oh, D. Y., & Olefsky, J. M. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2015.4 · Cited by 111

β-Arrestin 2 Mediates G Protein-Coupled Receptor 43 Signals to Nuclear Factor-κB

Lee, S. U., In, H. J., Kwon, M. S., Park, B.-O., Jo, M., Kim, M.-O., Cho, S., Lee, S., Lee, H., Kwak, Y. S., et al. (2013) · Biological and Pharmaceutical Bulletin · doi:10.1248/bpb.b13-00312 · Cited by 110

G Protein-Coupled Receptors: Functional and Mechanistic Insights Through Altered Gene Expression

Rohrer, D. K., & Kobilka, B. K. (1998) · Physiological Reviews · doi:10.1152/physrev.1998.78.1.35 · Cited by 109

SCFA Receptors in Pancreatic β Cells: Novel Diabetes Targets?

Priyadarshini, M., Wicksteed, B. L., Schiltz, G. E., Gilchrist, A., & Layden, B. T. (2016) · Trends in Endocrinology and Metabolism · doi:10.1016/j.tem.2016.03.011 · Cited by 109

FFAR2‐FFAR3 receptor heteromerization modulates short‐chain fatty acid sensing

Ang, Z., Xiong, D., Wu, M., & Ding, J. L. (2017) · The FASEB Journal · doi:10.1096/fj.201700252rr · Cited by 109

Activation of the omega-3 fatty acid receptor GPR120 mediates anti-inflammatory actions in immortalized hypothalamic neurons

Wellhauser, L., & Belsham, D. D. (2014) · Journal of Neuroinflammation · doi:10.1186/1742-2094-11-60 · Cited by 108

Expression and Characterization of a 5-oxo-6E,8Z,11Z,14Z-Eicosatetraenoic Acid Receptor Highly Expressed on Human Eosinophils and Neutrophils

Jones, C. E., Holden, S., Tenaillon, L., Bhatia, U., Seuwen, K., TRANTER, P. R., Turner, J., Kettle, R., Bouhelal, R., Charlton, S. J., et al. (2003) · Molecular Pharmacology · doi:10.1124/mol.63.3.471 · Cited by 108

GPR40 is expressed in glucagon producing cells and affects glucagon secretion

Flodgren, E., Olde, B., Abaraviciene, S. M., Winzell, M. S., Åhrén, B., & Salehi, A. A. (2007) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2006.12.193 · Cited by 106

Medium chain length fatty acid esters and their medical and nutritional applications

Babayan, V. K. (1981) · Journal of the American Oil Chemists Society · doi:10.1007/bf02666072 · Cited by 106

α‐Linolenic acid‐derived metabolites from gut lactic acid bacteria induce differentiation of anti‐inflammatory M2 macrophages through G protein‐coupled receptor 40

Ohue‐Kitano, R., Watanabe‐Yasuoka, Y., Goto, T., Kitamura, N., Park, S., Kishino, S., Kimura, I., Kasubuchi, M., Takahashi, H., Li, Y., et al. (2017) · The FASEB Journal · doi:10.1096/fj.201700273r · Cited by 105

Colocalization of GPR120 with phospholipase-Cβ2 and α-gustducin in the taste bud cells in mice

Matsumura, S., Eguchi, A., Mizushige, T., et al. (2008) · Neuroscience Letters · doi:10.1016/j.neulet.2008.11.056 · Cited by 104

Free Fatty Acids-Sensing G Protein-Coupled Receptors in Drug Targeting and Therapeutics

Yonezawa, T., Kurata, R., Yoshida, K., Murayama, M. A., Cui, X., & Hasegawa, A. (2013) · Current Medicinal Chemistry · doi:10.2174/09298673113209990168 · Cited by 104

Update on cardiometabolic health effects of ω-3 fatty acids

Kromhout, D., & de Goede, J. (2013) · Current Opinion in Lipidology · doi:10.1097/mol.0000000000000041 · Cited by 104

Decreased intestinal nutrient response in diet-induced obese rats: role of gut peptides and nutrient receptors

Duca, F. A., Swartz, T. D., Sakar, Y., & Covașă, M. (2012) · International Journal of Obesity · doi:10.1038/ijo.2012.45 · Cited by 102

Omega 3 Fatty Acids and GPR120

Oh, D. Y., & Olefsky, J. M. (2012) · Cell Metabolism · doi:10.1016/j.cmet.2012.04.009 · Cited by 102

Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity

Azevedo, C. M. G., Watterson, K. R., Wargent, E. T., Hansen, S. V. F., Hudson, B. D., Kępczyńska, M. A., Dunlop, J., Shimpukade, B., Christiansen, E., Milligan, G., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00685 · Cited by 102

Human and mouse monocytes display distinct signalling and cytokine profiles upon stimulation with FFAR2/FFAR3 short-chain fatty acid receptor agonists

Ang, Z., Er, J. Z., Tan, N. S., Lu, J., Liou, Y., Grosse, J., & Ding, J. L. (2016) · Scientific Reports · doi:10.1038/srep34145 · Cited by 102

Absorption of Short Chain Fatty Acids in Man.

Dawson, A. M., Holdsworth, C. D., & Webb, J. (1964) · Experimental Biology and Medicine · doi:10.3181/00379727-117-29505 · Cited by 101

The GPR120 agonist TUG‐891 promotes metabolic health by stimulating mitochondrial respiration in brown fat

Schilperoort, M., van Dam, A. D., Hoeke, G., Shabalina, I. G., Okolo, A., Hanyaloglu, A. C., Dib, L. H., Mol, I. M., Caengprasath, N., Chan, Y., et al. (2018) · EMBO Molecular Medicine · doi:10.15252/emmm.201708047 · Cited by 101

Identification and characterization of the bovine G protein-coupled receptor GPR41 and GPR43 genes

Wang, A., Gu, Z., Heid, B., Akers, R. M., & Jiang, H. (2009) · Journal of Dairy Science · doi:10.3168/jds.2009-2037 · Cited by 100

Inflammatory changes in adipose tissue enhance expression of GPR84, a medium‐chain fatty acid receptor

Nagasaki, H., Kondo, T., Fuchigami, M., Hashimoto, H., Sugimura, Y., Ozaki, N., Arima, H., Ota, A., Oiso, Y., & Hamada, Y. (2012) · FEBS Letters · doi:10.1016/j.febslet.2012.01.001 · Cited by 99

Short‐chain fatty acid receptor GPR41‐mediated activation of sympathetic neurons involves synapsin 2b phosphorylation

Inoue, D., Kimura, I., Wakabayashi, M., Tsumoto, H., Ozawa, K., Hara, T., Takei, Y., Hirasawa, A., Ishihama, Y., & Tsujimoto, G. (2012) · FEBS Letters · doi:10.1016/j.febslet.2012.04.021 · Cited by 99

FFAR1 Is Involved in Both the Acute and Chronic Effects of Palmitate on Insulin Secretion

Kristinsson, H., Smith, D. M., Bergsten, P., & Sargsyan, E. (2013) · Endocrinology · doi:10.1210/en.2013-1352 · Cited by 98

Omega-3 fatty acids and the treatment of depression: a review of scientific evidence

Wani, A. L., Bhat, S. A., & Ara, A. (2015) · Integrative Medicine Research · doi:10.1016/j.imr.2015.07.003 · Cited by 97

Regulation of Energy Homeostasis by GPR41

Inoue, D., Tsujimoto, G., & Kimura, I. (2014) · Frontiers in Endocrinology · doi:10.3389/fendo.2014.00081 · Cited by 97

AMG 837: A Novel GPR40/FFA1 Agonist that Enhances Insulin Secretion and Lowers Glucose Levels in Rodents

Lin, D. C.-H., Zhang, J., Zhuang, R., Li, F., Nguyen, K., Chen, M., Tran, T., Lopez, E., Lu, J. Y. L., Li, X. N., et al. (2011) · PLoS ONE · doi:10.1371/journal.pone.0027270 · Cited by 95

A Novel Antidiabetic Drug, Fasiglifam/TAK-875, Acts as an Ago-Allosteric Modulator of FFAR1

Yabuki, C., Komatsu, H., Tsujihata, Y., Risa, M., Ito, R., Kae, M.-N., Sakuma, K., Miyawaki, K., Kikuchi, N., Takeuchi, K., et al. (2013) · PLoS ONE · doi:10.1371/journal.pone.0076280 · Cited by 95

Butyrate and other short-chain fatty acids increase the rate of lipolysis in 3T3-L1 adipocytes

Rumberger, J. M., Arch, J. R. S., & Green, A. (2014) · PeerJ · doi:10.7717/peerj.611 · Cited by 95

Agonists at GPR119 mediate secretion of GLP‐1 from mouse enteroendocrine cells through glucose‐independent pathways

Lan, H., Lin, H. V., Cf, W., Wright, M. J., Xu, S. S., Kang, L., Juhl, K., Hedrick, J., & Kowalski, T. J. (2011) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2011.01754.x · Cited by 93

Inflammation stimulates niacin receptor (GPR109A/HCA2) expression in adipose tissue and macrophages

Feingold, K. R., Moser, A. H., Shigenaga, J. K., & Grünfeld, C. (2014) · Journal of Lipid Research · doi:10.1194/jlr.m050955 · Cited by 93

Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist

Brown, S. P., Dransfield, P. J., Vimolratana, M., Jiao, X., Zhu, L., Pattaropong, V., Sun, Y., Liu, J., Luo, J., Zhang, J., et al. (2012) · ACS Medicinal Chemistry Letters · doi:10.1021/ml300133f · Cited by 93

The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators

Wang, Y., Jiao, X., Kayser, F., Liu, J., Wang, Z., Wanska, M., Greenberg, J., Weiszmann, J., Ge, H., Tian, H., et al. (2009) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2009.11.112 · Cited by 92

Structure-Activity Relationships of GPR120 Agonists Based on a Docking Simulation

Sun, Q. L., Hirasawa, A., Hara, T., Kimura, I., Adachi, T., Awaji, T., Ishiguro, M., Suzuki, T., Miyata, N., & Tsujimoto, G. (2010) · Molecular Pharmacology · doi:10.1124/mol.110.066324 · Cited by 92

Thiazolidinediones Induce Osteocyte Apoptosis by a G Protein-coupled Receptor 40-dependent Mechanism

Mieczkowska, A., Baslé, M. F., Chappard, D., & Mabilleau, G. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.324814 · Cited by 91

Bidirectional, Iterative Approach to the Structural Delineation of the Functional “Chemoprint” in GPR40 for Agonist Recognition

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Identifying ligands at orphan GPCRs: current status using structure‐based approaches

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Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs

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Fatty acid‐induced cholecystokinin secretion and changes in intracellular Ca2+ in two enteroendocrine cell lines, STC‐1 and GLUTag

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GPR41 modulates insulin secretion and gene expression in pancreatic β‐cells and modifies metabolic homeostasis in fed and fasting states

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Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles

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Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development

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Expression of odorant receptor Olfr78 in enteroendocrine cells of the colon

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Uncovering the Pharmacology of the G Protein-Coupled Receptor GPR40: High Apparent Constitutive Activity in Guanosine 5′-O-(3-[35S]thio)triphosphate Binding Studies Reflects Binding of an Endogenous Agonist

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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

Yashiro, H., Tsujihata, Y., Takeuchi, K., Hazama, M., Johnson, P. R. V., & Rorsman, P. (2012) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.187708 · Cited by 84

G2A as a receptor for oxidized free fatty acids

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The Free Fatty Acid Receptor G Protein-coupled Receptor 40 (GPR40) Protects from Bone Loss through Inhibition of Osteoclast Differentiation*

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Structural basis for GPR40 allosteric agonism and incretin stimulation

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Long-Chain Free Fatty Acid Receptor GPR120 Mediates Oil-Induced GIP Secretion Through CCK in Male Mice

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The Importance of Omega-6/Omega-3 Fatty Acid Ratio in Cell Function

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Transition period-related changes in the abundance of the mRNAs of adiponectin and its receptors, of visfatin, and of fatty acid binding receptors in adipose tissue of high-yielding dairy cows

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Extracellular Loop 2 of the Free Fatty Acid Receptor 2 Mediates Allosterism of a Phenylacetamide Ago-Allosteric Modulator

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FFAR3 modulates insulin secretion and global gene expression in mouse islets

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DHA promotes the neuronal differentiation of rat neural stem cells transfected with GPR40 gene

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The 17,18-epoxyeicosatetraenoic acid–G protein–coupled receptor 40 axis ameliorates contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques

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GPR40 is a low-affinity epoxyeicosatrienoic acid receptor in vascular cells

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A GPR40 Agonist GW9508 Suppresses CCL5, CCL17, and CXCL10 Induction in Keratinocytes and Attenuates Cutaneous Immune Inflammation

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Swimming Endurance Capacity of Mice is Increased by Chronic Consumption of Medium-Chain Triglycerides

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Chemogenetics defines receptor-mediated functions of short chain free fatty acids

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The Molecular Basis of Ligand Interaction at Free Fatty Acid Receptor 4 (FFA4/GPR120)

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Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes

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Complex Pharmacology of Novel Allosteric Free Fatty Acid 3 Receptor Ligands

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A novel anti-inflammatory role of GPR120 in intestinal epithelial cells

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Exendin-4 protects pancreatic beta cells from palmitate-induced apoptosis by interfering with GPR40 and the MKK4/7 stress kinase signalling pathway

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Glucose activates free fatty acid receptor 1 gene transcription via phosphatidylinositol-3-kinase-dependent O -GlcNAcylation of pancreas-duodenum homeobox-1

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G Protein-Coupled Receptor 43 Modulates Neutrophil Recruitment during Acute Inflammation

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GPR120: a critical role in adipogenesis, inflammation, and energy metabolism in adipose tissue

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Medium‐Chain Triglyceride‐Based Fat Emulsions: An Alternative Energy Supply in Stress and Sepsis

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Expression of the Fatty Acid Receptor GPR120 in the Gut of Diet-Induced-Obese Rats and Its Role in GLP-1 Secretion

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GPR40 activation leads to CREB and ERK phosphorylation in primary cultures of neurons from the mouse CNS and in human neuroblastoma cells

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Eicosapentaenoic acid shows anti-inflammatory effect via GPR120 in 3T3-L1 adipocytes and attenuates adipose tissue inflammation in diet-induced obese mice

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GPR119 expression in normal human tissues and islet cell tumors: evidence for its islet-gastrointestinal distribution, expression in pancreatic beta and alpha cells, and involvement in islet function

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Central agonism of GPR120 acutely inhibits food intake and food reward and chronically suppresses anxiety-like behavior in mice

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Discovery of a Potent and Selective Free Fatty Acid Receptor 1 Agonist with Low Lipophilicity and High Oral Bioavailability

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Oleic acid induces intracellular calcium mobilization, MAPK phosphorylation, superoxide production and granule release in bovine neutrophils

Hidalgo, M. A., Nahuelpan, C., Manosalva, C., Jara, E. L., Carretta, M. D., Conejeros, I., Loaiza, A., Chihuailaf, R. H., & Burgos, R. A. (2011) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2011.04.144 · Cited by 54

FFAR4 (GPR120) Signaling Is Not Required for Anti-Inflammatory and Insulin-Sensitizing Effects of Omega-3 Fatty Acids

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The acute glucose lowering effect of specific GPR120 activation in mice is mainly driven by glucagon-like peptide 1

Sundström, L., Myhre, S., Sundqvist, M., Ahnmark, A., McCoull, W., Raubo, P., Groombridge, S. D., Polla, M., Nyström, A.-C., Kristensson, L., et al. (2017) · PLOS ONE · doi:10.1371/journal.pone.0189060 · Cited by 53

Acute stimulation of glucagon secretion by linoleic acid results from GPR40 activation and [Ca2+]i increase in pancreatic islet α-cells

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The short-chain fatty acid receptor GPR43 is transcriptionally regulated by XBP1 in human monocytes

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Decrease of Food Intake in Rats after Ingestion of Medium-Chain Triacylglycerol

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Selective novel inverse agonists for human GPR43 augment GLP-1 secretion

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Peptides and Their Potential Role in the Treatment of Diabetes and Obesity

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The activation of supraspinal GPR 40/ FFA 1 receptor signalling regulates the descending pain control system

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Effect of GPR84 deletion on obesity and diabetes development in mice fed long chain or medium chain fatty acid rich diets

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Experimental Challenges to Targeting Poorly Characterized GPCRs: Uncovering the Therapeutic Potential for Free Fatty Acid Receptors

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Increased Postprandial GIP and Glucagon Responses, But Unaltered GLP-1 Response after Intervention with Steroid Hormone, Relative Physical Inactivity, And High-Calorie Diet in Healthy Subjects

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Free Fatty Acid Receptor 4 (GPR120) Stimulates Bone Formation and Suppresses Bone Resorption in the Presence of Elevated n-3 Fatty Acid Levels

Ahn, S. H., Park, S., Baek, J., Lee, S.-Y., Baek, W., Lee, S.-Y., Lee, Y., Yoo, H. J., Kim, H., Lee, S. H., et al. (2016) · Endocrinology · doi:10.1210/en.2015-1855 · Cited by 48

Activation of tongue-expressed GPR40 and GPR120 by non caloric agonists is not sufficient to drive preference in mice

Godinot, N., Yasumatsu, K., Barcos, M. E., Pineau, N., Ledda, M., Viton, F., Ninomiya, Y., le Coutre, J., & Damak, S. (2013) · Neuroscience · doi:10.1016/j.neuroscience.2013.06.043 · Cited by 45

Low fasting insulin levels in Eskimos compared to American Indians: are Eskimos less insulin resistant?

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G Protein‐Coupled Receptor 120 Signaling Negatively Regulates Osteoclast Differentiation, Survival, and Function

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AKR1B7 Is Induced by the Farnesoid X Receptor and Metabolizes Bile Acids

Schmidt, D. R., Schmidt, S., Holmstrom, S. R., Makishima, M., Yu, R. T., Cummins, C. L., Mangelsdorf, D. J., & Kliewer, S. A. (2010) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.181230 · Cited by 41

The oral lipid sensor GPR120 is not indispensable for the orosensory detection of dietary lipids in mice

Ancel, D., Bernard, A., Selvakumar, S., Hirasawa, A., Tsujimoto, G., Hashimoto, T., Passilly‐Degrace, P., Khan, N.-A., & Besnard, P. (2014) · Journal of Lipid Research · doi:10.1194/jlr.m055202 · Cited by 41

Gustducin couples fatty acid receptors to GLP-1 release in colon

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Effects of Obesity and Gastric Bypass Surgery on Nutrient Sensors, Endocrine Cells, and Mucosal Innervation of the Mouse Colon

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Gut carbohydrate inhibits GIP secretion via a microbiota/SCFA/FFAR3 pathway

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Anti-Inflammatory and Insulin-Sensitizing Effects of Free Fatty Acid Receptors

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Identification of transforming activity of free fatty acid receptor 2 by retroviral expression screening

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Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist

Takano, R., Yoshida, M., Inoue, M., Honda, T., Nakashima, R., Matsumoto, K., Yano, T., Ogata, T., Watanabe, N., Hirouchi, M., et al. (2015) · ACS Medicinal Chemistry Letters · doi:10.1021/ml500391n · Cited by 35

Oxidized Lipids and Lysophosphatidylcholine Induce the Chemotaxis, Up-Regulate the Expression of CCR9 and CXCR4 and Abrogate the Release of IL-6 in Human Monocytes

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Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4

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Dysfunctional GPR40/FFAR1 signaling exacerbates pain behavior in mice

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Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists

Cox, J. M., Chu, H. D., Chelliah, M. V., Debenham, J. S., Eagen, K. A., Lan, P., Lombardo, M., London, C., Plotkin, M. A., Shah, U., et al. (2016) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6b00360 · Cited by 34

Phytosphingosine is a novel activator of GPR120

Nagasawa, T., Nakamichi, H., Hama, Y., Higashiyama, S., Igarashi, Y., & Mitsutake, S. (2018) · The Journal of Biochemistry · doi:10.1093/jb/mvy017 · Cited by 34

Design and Synthesis of Novel, Selective GPR40 AgoPAMs

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Functional Analysis of Free Fatty Acid Receptor GPR120 in Human Eosinophils: Implications in Metabolic Homeostasis

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GPR40/FFAR1 deficient mice increase noradrenaline levels in the brain and exhibit abnormal behavior

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Insulinotropic effects of GPR120 agonists are altered in obese diabetic and obese non-diabetic states

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Production and characterization of a monoclonal antibody against GPR40 (FFAR1; free fatty acid receptor 1)

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Functional Consequences of GPCR Heterodimerization: GPCRs as Allosteric Modulators

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Novel Mechanism of Fatty Acid Sensing in Enteroendocrine Cells: Specific Structures in Oxo‐Fatty Acids Produced by Gut Bacteria Are Responsible for CCK Secretion in STC‐1 Cells via GPR40

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Involvement of the Long-Chain Fatty Acid Receptor GPR40 in Depression-Related Behavior

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FFA3 Activation Stimulates Duodenal Bicarbonate Secretion and Prevents NSAID-Induced Enteropathy via the GLP-2 Pathway in Rats

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Free fatty acid receptor 3 is a key target of short chain fatty acid

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