Free Fatty Acid Receptors in Health and Disease

From Dietary Fiber to Host Physiology: Short-Chain Fatty Acids as Key Bacterial Metabolites

Koh, A., De Vadder, F., Kovatcheva-Datchary, P., & Bäckhed, F. (2016) · Cell · doi:10.1016/j.cell.2016.05.041 · Cited by 7,070

A metagenome-wide association study of gut microbiota in type 2 diabetes

Qin, J., Li, Y., Cai, Z., Li, S., Zhu, J., Zhang, F., Liang, S., Zhang, W., Guan, Y., Shen, D., et al. (2012) · Nature · doi:10.1038/nature11450 · Cited by 6,762

Commensal microbe-derived butyrate induces the differentiation of colonic regulatory T cells

Furusawa, Y., Obata, Y., Fukuda, S., Endo, T. A., Nakato, G., Takahashi, D., Nakanishi, Y., Uetake, C., Kato, K., Kato, T., et al. (2013) · Nature · doi:10.1038/nature12721 · Cited by 5,549

Mechanisms linking obesity to insulin resistance and type 2 diabetes

Kahn, S. E., Hull, R. L., & Utzschneider, K. M. (2006) · Nature · doi:10.1038/nature05482 · Cited by 5,448

The Microbial Metabolites, Short-Chain Fatty Acids, Regulate Colonic T reg Cell Homeostasis

Smith, P. M., Howitt, M. R., Panikov, N., Michaud, M., Gallini, C. A., Bohlooly-Y, M., Glickman, J. N., & Garrett, W. S. (2013) · Science · doi:10.1126/science.1241165 · Cited by 5,413

The role of short-chain fatty acids in the interplay between diet, gut microbiota, and host energy metabolism

den Besten, G., van Eunen, K., Groen, A. K., Venema, K., Reijngoud, D.-J., & Bakker, B. M. (2013) · Journal of Lipid Research · doi:10.1194/jlr.r036012 · Cited by 5,048

Metabolites produced by commensal bacteria promote peripheral regulatory T-cell generation

Arpaia, N., Campbell, C., Fan, X., Dikiy, S., van der Veeken, J., deRoos, P., Liu, H., Cross, J. R., Pfeffer, K., Coffer, P. J., et al. (2013) · Nature · doi:10.1038/nature12726 · Cited by 4,838

Host-gut microbiota metabolic interactions

Nicholson, J. K., Holmes, E., Kinross, J., Burcelin, R., Gibson, G., Jia, W., & Pettersson, S. (2012) · Science · doi:10.1126/science.1223813 · Cited by 4,760

Host microbiota constantly control maturation and function of microglia in the CNS

Erny, D., Hrabě de Angelis, A. L., Jaitin, D., Wieghofer, P., Staszewski, O., David, E., Keren-Shaul, H., Mahlakoiv, T., Jakobshagen, K., Buch, T., et al. (2015) · Nature Neuroscience · doi:10.1038/nn.4030 · Cited by 3,569

Gut microbiota, metabolites and host immunity

Rooks, M. G., & Garrett, W. S. (2016) · Nature reviews. Immunology · doi:10.1038/nri.2016.42 · Cited by 3,409

Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43

Maslowski, K. M., Vieira, A. T., Ng, A., Kranich, J., Sierro, F., Yu, D., Schilter, H. C., Rolph, M. S., Mackay, F., Artis, D., et al. (2009) · Nature · doi:10.1038/nature08530 · Cited by 3,241

Short chain fatty acids in human large intestine, portal, hepatic and venous blood

Cummings, J. H., Pomare, E. W., Branch, W. J., Naylor, C. P., & Macfarlane, G. T. (1987) · Gut · doi:10.1136/gut.28.10.1221 · Cited by 3,119

Gut metagenome in European women with normal, impaired and diabetic glucose control

Karlsson, F. H., Tremaroli, V., Nookaew, I., Bergström, G., Behre, C. J., Fagerberg, B., Nielsen, J., & Bäckhed, F. (2013) · Nature · doi:10.1038/nature12198 · Cited by 3,115

Short-Chain Fatty Acids and Human Colonic Function: Roles of Resistant Starch and Nonstarch Polysaccharides

Topping, D. L., & Clifton, P. M. (2001) · Physiological Reviews · doi:10.1152/physrev.2001.81.3.1031 · Cited by 3,091

The G-Protein-Coupled Receptors in the Human Genome Form Five Main Families. Phylogenetic Analysis, Paralogon Groups, and Fingerprints

Fredriksson, R., Lagerström, M. C., Lundin, L.-G., & Schiöth, H. B. (2003) · Molecular Pharmacology · doi:10.1124/mol.63.6.1256 · Cited by 2,941

Gut Microbiota Metabolism of Dietary Fiber Influences Allergic Airway Disease and Hematopoiesis

Trompette, A., Gollwitzer, E. S., Yadava, K., Sichelstiel, A. K., Sprenger, N., Ngom-Bru, C., Blanchard, C., Junt, T., Nicod, L. P., Harris, N. L., et al. (2014) · Nature Medicine · doi:10.1038/nm.3444 · Cited by 2,862

Human nutrition, the gut microbiome and the immune system

Kau, A. L., Ahern, P. P., Griffin, N. W., Goodman, A. L., & Gordon, J. I. (2011) · Nature · doi:10.1038/nature10213 · Cited by 2,588

Changes in gut microbiota control inflammation in obese mice through a mechanism involving GLP-2-driven improvement of gut permeability

Cani, P. D., Possemiers, S., Van de Wiele, T., Guiot, Y., Everard, A., Rottier, O., Geurts, L., Naslain, D., Neyrinck, A., Lambert, D. M., et al. (2009) · Gut · doi:10.1136/gut.2008.165886 · Cited by 2,518

The impact of dietary fiber on gut microbiota in host health and disease

Makki, K., Deehan, E. C., Walter, J., & Bäckhed, F. (2018) · Cell Host & Microbe · doi:10.1016/j.chom.2018.05.012 · Cited by 2,517

GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects

Oh, D. Y., Talukdar, S., Bae, E. J., Imamura, T., Morinaga, H., Fan, W., Li, P., Lu, W. J., Watkins, S. M., & Olefsky, J. M. (2010) · Cell · doi:10.1016/j.cell.2010.07.041 · Cited by 2,428

The Orphan G Protein-coupled Receptors GPR41 and GPR43 Are Activated by Propionate and Other Short Chain Carboxylic Acids

Brown, A. J., Goldsworthy, S. M., Barnes, A. A., Eilert, M. M., Tcheang, L., Daniels, D., Muir, A. I., Wigglesworth, M. J., Kinghorn, I., Fraser, N. J., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m211609200 · Cited by 2,409

Short-chain fatty acids stimulate glucagon-like peptide-1 secretion via the G-protein-coupled receptor FFAR2

Tolhurst, G., Heffron, H., Lam, Y. S., Parker, H. E., Habib, A. M., Diakogiannaki, E., Cameron, J., Grosse, J., Reimann, F., & Gribble, F. M. (2012) · Diabetes · doi:10.2337/db11-1019 · Cited by 2,404

Activation of Gpr109a, receptor for niacin and the commensal metabolite butyrate, suppresses colonic inflammation and carcinogenesis

Singh, N., Gurav, A., Sivaprakasam, S., Brady, E., Padia, R., Shi, H., Thangaraju, M., Prasad, P. D., Manicassamy, S., Munn, D. H., et al. (2014) · Immunity · doi:10.1016/j.immuni.2013.12.007 · Cited by 2,368

Gut hormone PYY3-36 physiologically inhibits food intake

Batterham, R. L., Cowley, M. A., Small, C. J., Herzog, H., Cohen, M. A., Dakin, C. L., Wren, A. M., Brynes, A. E., Low, M. J., Ghatei, M. A., et al. (2002) · Nature · doi:10.1038/nature00887 · Cited by 2,351

Microbiota-Generated Metabolites Promote Metabolic Benefits via Gut-Brain Neural Circuits

De Vadder, F., Kovatcheva-Datchary, P., Goncalves, D., Vinera, J., Zitoun, C., Duchampt, A., Bäckhed, F., & Mithieux, G. (2014) · Cell · doi:10.1016/j.cell.2013.12.016 · Cited by 2,200

Nuclear Receptors and Lipid Physiology: Opening the X-Files

Chawla, A., Repa, J. J., Evans, R. M., & Mangelsdorf, D. J. (2001) · Science · doi:10.1126/science.294.5548.1866 · Cited by 2,085

The microbiome and butyrate regulate energy metabolism and autophagy in the mammalian colon

Donohoe, D. R., Garge, N., Zhang, X., Sun, W., O'Connell, T. M., Bunger, M. K., & Bultman, S. J. (2011) · Cell Metabolism · doi:10.1016/j.cmet.2011.02.018 · Cited by 2,003 · cited 6×

A role for glucagon-like peptide-1 in the central regulation of feeding

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Fatty acid-binding proteins: role in metabolic diseases and potential as drug targets

Furuhashi, M., & Hotamisligil, G. S. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2589 · Cited by 1,785

Selective increases of bifidobacteria in gut microflora improve high-fat-diet-induced diabetes in mice through a mechanism associated with endotoxaemia

Cani, P. D., Neyrinck, A. M., Fava, F., Knauf, C., Burcelin, R. G., Tuohy, K. M., Gibson, G. R., & Delzenne, N. M. (2007) · Diabetologia · doi:10.1007/s00125-007-0791-0 · Cited by 1,774

An Increase in the Omega-6/Omega-3 Fatty Acid Ratio Increases the Risk for Obesity

Simopoulos, A. (2016) · Nutrients · doi:10.3390/nu8030128 · Cited by 1,668

Functional Characterization of Human Receptors for Short Chain Fatty Acids and Their Role in Polymorphonuclear Cell Activation

Le Poul, E., Loison, C., Struyf, S., Springael, J.-Y., Lannoy, V., Decobecq, M.-E., Brezillon, S., Dupriez, V., Vassart, G., Van Damme, J., et al. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m301403200 · Cited by 1,651

Effects of the gut microbiota on host adiposity are modulated by the short-chain fatty-acid binding G protein-coupled receptor, Gpr41

Samuel, B. S., Shaito, A., Motoike, T., Rey, F. E., Backhed, F., Manchester, J. K., Hammer, R. E., Williams, S. C., Crowley, J., Yanagisawa, M., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0808567105 · Cited by 1,564

Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120

Hirasawa, A., Tsumaya, K., Awaji, T., Katsuma, S., Adachi, T., Yamada, M., Sugimoto, Y., Miyazaki, S., & Tsujimoto, G. (2005) · Nature Medicine · doi:10.1038/nm1168 · Cited by 1,545

Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40

Itoh, Y., Kawamata, Y., Harada, M., Kobayashi, M., Fujii, R., Fukusumi, S., Ogi, K., Hosoya, M., Tanaka, Y., Uejima, H., et al. (2003) · Nature · doi:10.1038/nature01478 · Cited by 1,538

The gut microbiota suppresses insulin-mediated fat accumulation via the short-chain fatty acid receptor GPR43

Kimura, I., Ozawa, K., Inoue, D., Imamura, T., Kimura, K., Maeda, T., Terasawa, K., Kashihara, D., Hirano, K., Tani, T., et al. (2013) · Nature Communications · doi:10.1038/ncomms2852 · Cited by 1,512

Gut microbial metabolites in obesity, NAFLD and T2DM

Canfora, E. E., Meex, R. C. R., Venema, K., & Blaak, E. E. (2019) · Nature Reviews Endocrinology · doi:10.1038/s41574-019-0156-z · Cited by 1,493

Structural diversity of G protein-coupled receptors and significance for drug discovery

Lagerström, M. C., & Schiöth, H. B. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2518 · Cited by 1,492

Regulation of hepatic fatty acid oxidation and ketone body production

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Metabolite-sensing receptors GPR43 and GPR109A facilitate dietary fibre-induced gut homeostasis through regulation of the inflammasome

Macia, L., Tan, J., Vieira, A. T., Leach, K., Stanley, D., Luong, S., Maruya, M., Ian McKenzie, C., Hijikata, A., Wong, C., et al. (2015) · Nature Communications · doi:10.1038/ncomms7734 · Cited by 1,439

Effects of targeted delivery of propionate to the human colon on appetite regulation, body weight maintenance and adiposity in overweight adults

Chambers, E. S., Viardot, A., Psichas, A., Morrison, D. J., Murphy, K. G., Zac-Varghese, S. E. K., MacDougall, K., Preston, T., Tedford, C., Finlayson, G. S., et al. (2015) · Gut · doi:10.1136/gutjnl-2014-307913 · Cited by 1,424

Butyrate and Propionate Protect against Diet-Induced Obesity and Regulate Gut Hormones via Free Fatty Acid Receptor 3-Independent Mechanisms

Lin, H. V., Frassetto, A., Kowalik Jr, E. J., Nawrocki, A. R., Lu, M. M., Kosinski, J. R., Hubert, J. A., Szeto, D., Yao, X., Forrest, G., et al. (2012) · PLoS ONE · doi:10.1371/journal.pone.0035240 · Cited by 1,378

Regulation of immune cell function by short‐chain fatty acids

Corrêa‐Oliveira, R., Fachi, J. L., Vieira, A., Sato, F. T., & Vinolo, M. A. R. (2016) · Clinical & Translational Immunology · doi:10.1038/cti.2016.17 · Cited by 1,346

Short-chain fatty acids induce both effector and regulatory T cells by suppression of histone deacetylases and regulation of the mTOR–S6K pathway

Park, J., Kim, M., Kang, S. G., Jannasch, A. H., Cooper, B., Patterson, J., & Kim, C. H. (2015) · Mucosal Immunology · doi:10.1038/mi.2014.44 · Cited by 1,307

Acetate mediates a microbiome–brain–β-cell axis to promote metabolic syndrome

Perry, R. J., Peng, L., Barry, N. A., Cline, G. W., Zhang, D., Cardone, R. L., Petersen, K. F., Kibbey, R. G., Goodman, A. L., & Shulman, G. I. (2016) · Nature · doi:10.1038/nature18309 · Cited by 1,299

Olfactory receptor responding to gut microbiota-derived signals plays a role in renin secretion and blood pressure regulation

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Resolvin E1 and protectin D1 activate inflammation-resolution programmes

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Consumption of a Fat-Rich Diet Activates a Proinflammatory Response and Induces Insulin Resistance in the Hypothalamus

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Medium-chain triglycerides: an update

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Short-Chain Fatty Acids Activate GPR41 and GPR43 on Intestinal Epithelial Cells to Promote Inflammatory Responses in Mice

Kim, M. H., Kang, S. G., Park, J. H., Yanagisawa, M., & Kim, C. H. (2013) · Gastroenterology · doi:10.1053/j.gastro.2013.04.056 · Cited by 1,127

Saturated fatty acids produce an inflammatory response predominantly through the activation of TLR4 signaling in hypothalamus: implications for the pathogenesis of obesity

Milanski, M., Degasperi, G., Coope, A., Morari, J., Denis, R., Cintra, D. E., Tsukumo, D. M. L., Anhe, G., Amaral, M. E., Takahashi, H. K., et al. (2009) · The Journal of Neuroscience · doi:10.1523/jneurosci.2760-08.2009 · Cited by 1,125

Short-chain fatty acids and ketones directly regulate sympathetic nervous system via G protein-coupled receptor 41 (GPR41)

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The Orphan G Protein-coupled Receptor GPR40 Is Activated by Medium and Long Chain Fatty Acids

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Microbiota and neurodevelopmental windows: implications for brain disorders

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G-protein-coupled receptors and signaling networks: emerging paradigms

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FATTY ACID SYNTHESIS AND ITS REGULATION

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Conserved shifts in the gut microbiota due to gastric bypass reduce host weight and adiposity

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Dietary gut microbial metabolites, short-chain fatty acids, and host metabolic regulation

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Epidemiological studies in the Upernavik district, Greenland. Incidence of some chronic diseases 1950-1974.

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Commensal bacteria protect against food allergen sensitization

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Dietary metabolism, the gut microbiome, and heart failure

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Targeting gut microbiota in obesity: effects of prebiotics and probiotics

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Treatment of Diversion Colitis with Short-Chain-Fatty Acid Irrigation

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Absorption of Short-Chain Fatty Acids by the Colon

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Short-chain fatty acids stimulate leptin production in adipocytes through the G protein-coupled receptor GPR41

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Bariatric Surgery and Long-term Durability of Weight Loss

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Epidemiological Studies in the Upernavik District, Greenland: Incidence of Some Chronic Diseases 1950–1974

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Anatomical Profiling of G Protein-Coupled Receptor Expression

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Gut microbial metabolites limit the frequency of autoimmune T cells and protect against type 1 diabetes

Mariño, E., Richards, J. L., McLeod, K. H., Stanley, D., Yap, Y. A., Knight, J., McKenzie, C., Kranich, J., Oliveira, A. C., Rossello, F. J., et al. (2017) · Nature Immunology · doi:10.1038/ni.3713 · Cited by 686

Dietary Fiber Confers Protection Against Flu by Shaping Ly6c Patrolling Monocyte Hematopoiesis and CD8 T Cell Metabolism

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Dietary Fiber and Bacterial SCFA Enhance Oral Tolerance and Protect against Food Allergy through Diverse Cellular Pathways

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Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human

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Microbiota-derived short-chain fatty acids promote Th1 cell IL-10 production to maintain intestinal homeostasis

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Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents

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(d)-β-Hydroxybutyrate Inhibits Adipocyte Lipolysis via the Nicotinic Acid Receptor PUMA-G

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Inhibition of histone-deacetylase activity by short-chain fatty acids and some polyphenol metabolites formed in the colon

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Acetate and Propionate Short Chain Fatty Acids Stimulate Adipogenesis via GPCR43

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Dietary intakes and food sources of omega‐6 and omega‐3 polyunsaturated fatty acids

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Microbiome–host systems interactions: protective effects of propionate upon the blood–brain barrier

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Gpr40 Is Expressed in Enteroendocrine Cells and Mediates Free Fatty Acid Stimulation of Incretin Secretion

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Transport of Fatty Acids

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GPR41/FFAR3 and GPR43/FFAR2 as Cosensors for Short-Chain Fatty Acids in Enteroendocrine Cells vs FFAR3 in Enteric Neurons and FFAR2 in Enteric Leukocytes

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G Protein–Coupled Receptor Oligomerization Revisited: Functional and Pharmacological Perspectives

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