Celia P Briscoe, Mohammad Tadayyon, John L Andrews, William G Benson, Jon K Chambers, Michelle M Eilert, Catherine Ellis, Nabil A Elshourbagy, Aaron S Goetz, Dana T Minnick, Paul R Murdock, Howard R Sauls, Usman Shabon, Lisa D Spinage, Jay C Strum, Philip G Szekeres, Kong B Tan, James M Way, Diane M Ignar, Shelagh Wilson, Alison I Muir. J Biol Chem 2003
Times Cited: 818
Times Cited: 818
Times Cited
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Similarity
Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.
Yasuaki Itoh, Yuji Kawamata, Masataka Harada, Makoto Kobayashi, Ryo Fujii, Shoji Fukusumi, Kazuhiro Ogi, Masaki Hosoya, Yasuhiro Tanaka, Hiroshi Uejima,[...]. Nature 2003
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Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120.
Akira Hirasawa, Keiko Tsumaya, Takeo Awaji, Susumu Katsuma, Tetsuya Adachi, Masateru Yamada, Yukihiko Sugimoto, Shunichi Miyazaki, Gozoh Tsujimoto. Nat Med 2005
Akira Hirasawa, Keiko Tsumaya, Takeo Awaji, Susumu Katsuma, Tetsuya Adachi, Masateru Yamada, Yukihiko Sugimoto, Shunichi Miyazaki, Gozoh Tsujimoto. Nat Med 2005
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GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects.
Da Young Oh, Saswata Talukdar, Eun Ju Bae, Takeshi Imamura, Hidetaka Morinaga, WuQiang Fan, Pingping Li, Wendell J Lu, Steven M Watkins, Jerrold M Olefsky. Cell 2010
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Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.
Celia P Briscoe, Andrew J Peat, Stephen C McKeown, David F Corbett, Aaron S Goetz, Thomas R Littleton, David C McCoy, Terry P Kenakin, John L Andrews, Carina Ammala,[...]. Br J Pharmacol 2006
Celia P Briscoe, Andrew J Peat, Stephen C McKeown, David F Corbett, Aaron S Goetz, Thomas R Littleton, David C McCoy, Terry P Kenakin, John L Andrews, Carina Ammala,[...]. Br J Pharmacol 2006
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Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion.
Sara Edfalk, Pär Steneberg, Helena Edlund. Diabetes 2008
Sara Edfalk, Pär Steneberg, Helena Edlund. Diabetes 2008
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Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial.
K Kaku, K Enya, R Nakaya, T Ohira, R Matsuno. Diabetes Obes Metab 2015
K Kaku, K Enya, R Nakaya, T Ohira, R Matsuno. Diabetes Obes Metab 2015
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GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivo.
Maria Hauge, Marie A Vestmar, Anna S Husted, Jeppe P Ekberg, Michael J Wright, Jerry Di Salvo, Adam B Weinglass, Maja S Engelstoft, Andreas N Madsen, Michael Lückmann,[...]. Mol Metab 2014
Maria Hauge, Marie A Vestmar, Anna S Husted, Jeppe P Ekberg, Michael J Wright, Jerry Di Salvo, Adam B Weinglass, Maja S Engelstoft, Andreas N Madsen, Michael Lückmann,[...]. Mol Metab 2014
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The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.
Andrew J Brown, Susan M Goldsworthy, Ashley A Barnes, Michelle M Eilert, Lili Tcheang, Dion Daniels, Alison I Muir, Mark J Wigglesworth, Ian Kinghorn, Neil J Fraser,[...]. J Biol Chem 2003
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A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.
Knut Kotarsky, Niclas E Nilsson, Erik Flodgren, Christer Owman, Björn Olde. Biochem Biophys Res Commun 2003
Knut Kotarsky, Niclas E Nilsson, Erik Flodgren, Christer Owman, Björn Olde. Biochem Biophys Res Commun 2003
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Role of GPR40 in fatty acid action on the beta cell line INS-1E.
Hagit Shapiro, Sigal Shachar, Israel Sekler, Michal Hershfinkel, Michael D Walker. Biochem Biophys Res Commun 2005
Hagit Shapiro, Sigal Shachar, Israel Sekler, Michal Hershfinkel, Michael D Walker. Biochem Biophys Res Commun 2005
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The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse.
Pär Steneberg, Nir Rubins, Reut Bartoov-Shifman, Michael D Walker, Helena Edlund. Cell Metab 2005
Pär Steneberg, Nir Rubins, Reut Bartoov-Shifman, Michael D Walker, Helena Edlund. Cell Metab 2005
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Complex Pharmacology of Free Fatty Acid Receptors.
Graeme Milligan, Bharat Shimpukade, Trond Ulven, Brian D Hudson. Chem Rev 2017
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Free Fatty Acid Receptor 1 (FFAR1) as an Emerging Therapeutic Target for Type 2 Diabetes Mellitus: Recent Progress and Prevailing Challenges.
Zheng Li, Xue Xu, Wenlong Huang, Hai Qian. Med Res Rev 2018
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Free Fatty Acid Receptors in Health and Disease.
Ikuo Kimura, Atsuhiko Ichimura, Ryuji Ohue-Kitano, Miki Igarashi. Physiol Rev 2020
Ikuo Kimura, Atsuhiko Ichimura, Ryuji Ohue-Kitano, Miki Igarashi. Physiol Rev 2020
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TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial.
Charles F Burant, Prabhakar Viswanathan, John Marcinak, Charlie Cao, Majid Vakilynejad, Benhuai Xie, Eckhard Leifke. Lancet 2012
Charles F Burant, Prabhakar Viswanathan, John Marcinak, Charlie Cao, Majid Vakilynejad, Benhuai Xie, Eckhard Leifke. Lancet 2012
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A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice.
Da Young Oh, Evelyn Walenta, Taro E Akiyama, William S Lagakos, Denise Lackey, Ariane R Pessentheiner, Roman Sasik, Nasun Hah, Tyler J Chi, Jason M Cox,[...]. Nat Med 2014
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Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development.
Zheng Li, Qianqian Qiu, Xinqian Geng, Jianyong Yang, Wenlong Huang, Hai Qian. Expert Opin Investig Drugs 2016
Zheng Li, Qianqian Qiu, Xinqian Geng, Jianyong Yang, Wenlong Huang, Hai Qian. Expert Opin Investig Drugs 2016
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A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents.
Jian Luo, Gayathri Swaminath, Sean P Brown, Jane Zhang, Qi Guo, Michael Chen, Kathy Nguyen, Thanhvien Tran, Lynn Miao, Paul J Dransfield,[...]. PLoS One 2012
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Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human.
Atsuhiko Ichimura, Akira Hirasawa, Odile Poulain-Godefroy, Amélie Bonnefond, Takafumi Hara, Loïc Yengo, Ikuo Kimura, Audrey Leloire, Ning Liu, Keiko Iida,[...]. Nature 2012
Atsuhiko Ichimura, Akira Hirasawa, Odile Poulain-Godefroy, Amélie Bonnefond, Takafumi Hara, Loïc Yengo, Ikuo Kimura, Audrey Leloire, Ning Liu, Keiko Iida,[...]. Nature 2012
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The fatty acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding.
Melkam Kebede, Thierry Alquier, Martin G Latour, Meriem Semache, Caroline Tremblay, Vincent Poitout. Diabetes 2008
Melkam Kebede, Thierry Alquier, Martin G Latour, Meriem Semache, Caroline Tremblay, Vincent Poitout. Diabetes 2008
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Lack of FFAR1/GPR40 does not protect mice from high-fat diet-induced metabolic disease.
Hong Lan, Lizbeth M Hoos, Li Liu, Glen Tetzloff, Weiwen Hu, Susan J Abbondanzo, Galya Vassileva, Eric L Gustafson, Joseph A Hedrick, Harry R Davis. Diabetes 2008
Hong Lan, Lizbeth M Hoos, Li Liu, Glen Tetzloff, Weiwen Hu, Susan J Abbondanzo, Galya Vassileva, Eric L Gustafson, Joseph A Hedrick, Harry R Davis. Diabetes 2008
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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.
Yoshiyuki Tsujihata, Ryo Ito, Masami Suzuki, Ayako Harada, Nobuyuki Negoro, Tsuneo Yasuma, Yu Momose, Koji Takeuchi. J Pharmacol Exp Ther 2011
Yoshiyuki Tsujihata, Ryo Ito, Masami Suzuki, Ayako Harada, Nobuyuki Negoro, Tsuneo Yasuma, Yu Momose, Koji Takeuchi. J Pharmacol Exp Ther 2011
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The regulation of adipogenesis through GPR120.
Chizu Gotoh, Yeon-Hee Hong, Tomoyo Iga, Daisuke Hishikawa, Yasuki Suzuki, Sang-Houn Song, Ki-Choon Choi, Tetsuya Adachi, Akira Hirasawa, Gozoh Tsujimoto,[...]. Biochem Biophys Res Commun 2007
Chizu Gotoh, Yeon-Hee Hong, Tomoyo Iga, Daisuke Hishikawa, Yasuki Suzuki, Sang-Houn Song, Ki-Choon Choi, Tetsuya Adachi, Akira Hirasawa, Gozoh Tsujimoto,[...]. Biochem Biophys Res Commun 2007
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Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.
Nobuyuki Negoro, Shinobu Sasaki, Satoshi Mikami, Masahiro Ito, Masami Suzuki, Yoshiyuki Tsujihata, Ryo Ito, Ayako Harada, Koji Takeuchi, Nobuhiro Suzuki,[...]. ACS Med Chem Lett 2010
Nobuyuki Negoro, Shinobu Sasaki, Satoshi Mikami, Masahiro Ito, Masami Suzuki, Yoshiyuki Tsujihata, Ryo Ito, Ayako Harada, Koji Takeuchi, Nobuhiro Suzuki,[...]. ACS Med Chem Lett 2010
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Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet beta-cells: mediation by PLC and L-type Ca2+ channel and link to insulin release.
Ken Fujiwara, Fumihiko Maekawa, Toshihiko Yada. Am J Physiol Endocrinol Metab 2005
Ken Fujiwara, Fumihiko Maekawa, Toshihiko Yada. Am J Physiol Endocrinol Metab 2005
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Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation.
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. J Neuroinflammation 2017
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. J Neuroinflammation 2017
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Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
Sean P Brown, Paul J Dransfield, Marc Vimolratana, XianYun Jiao, Liusheng Zhu, Vatee Pattaropong, Ying Sun, Jinqian Liu, Jian Luo, Jane Zhang,[...]. ACS Med Chem Lett 2012
Sean P Brown, Paul J Dransfield, Marc Vimolratana, XianYun Jiao, Liusheng Zhu, Vatee Pattaropong, Ying Sun, Jinqian Liu, Jian Luo, Jane Zhang,[...]. ACS Med Chem Lett 2012
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Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.
Emmanuel Le Poul, Cecile Loison, Sofie Struyf, Jean-Yves Springael, Vincent Lannoy, Marie-Eve Decobecq, Stephane Brezillon, Vincent Dupriez, Gilbert Vassart, Jo Van Damme,[...]. J Biol Chem 2003
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A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1.
Chiori Yabuki, Hidetoshi Komatsu, Yoshiyuki Tsujihata, Risa Maeda, Ryo Ito, Kae Matsuda-Nagasumi, Kensuke Sakuma, Kazumasa Miyawaki, Naoya Kikuchi, Koji Takeuchi,[...]. PLoS One 2013
Chiori Yabuki, Hidetoshi Komatsu, Yoshiyuki Tsujihata, Risa Maeda, Ryo Ito, Kae Matsuda-Nagasumi, Kensuke Sakuma, Kazumasa Miyawaki, Naoya Kikuchi, Koji Takeuchi,[...]. PLoS One 2013
15
GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo.
Martin G Latour, Thierry Alquier, Elizabeth Oseid, Caroline Tremblay, Thomas L Jetton, Jian Luo, Daniel C-H Lin, Vincent Poitout. Diabetes 2007
Martin G Latour, Thierry Alquier, Elizabeth Oseid, Caroline Tremblay, Thomas L Jetton, Jian Luo, Daniel C-H Lin, Vincent Poitout. Diabetes 2007
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Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
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Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from beta-cells through activation of GPR40.
Susanne Schnell, Michael Schaefer, Christof Schöfl. Mol Cell Endocrinol 2007
Susanne Schnell, Michael Schaefer, Christof Schöfl. Mol Cell Endocrinol 2007
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Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor.
Daniel C-H Lin, Qi Guo, Jian Luo, Jane Zhang, Kathy Nguyen, Michael Chen, Thanh Tran, Paul J Dransfield, Sean P Brown, Jonathan Houze,[...]. Mol Pharmacol 2012
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Short-chain fatty acids stimulate glucagon-like peptide-1 secretion via the G-protein-coupled receptor FFAR2.
Gwen Tolhurst, Helen Heffron, Yu Shan Lam, Helen E Parker, Abdella M Habib, Eleftheria Diakogiannaki, Jennifer Cameron, Johannes Grosse, Frank Reimann, Fiona M Gribble. Diabetes 2012
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Loss of FFA2 and FFA3 increases insulin secretion and improves glucose tolerance in type 2 diabetes.
Cong Tang, Kashan Ahmed, Andreas Gille, Shun Lu, Hermann-Josef Gröne, Sorin Tunaru, Stefan Offermanns. Nat Med 2015
Cong Tang, Kashan Ahmed, Andreas Gille, Shun Lu, Hermann-Josef Gröne, Sorin Tunaru, Stefan Offermanns. Nat Med 2015
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Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice.
Kae Nagasumi, Ritsuko Esaki, Kimihiko Iwachidow, Yoshitaka Yasuhara, Kazuhiro Ogi, Hideyuki Tanaka, Mitsugu Nakata, Takashi Yano, Kozo Shimakawa, Shigehisa Taketomi,[...]. Diabetes 2009
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Activation of G protein-coupled receptor 43 in adipocytes leads to inhibition of lipolysis and suppression of plasma free fatty acids.
Hongfei Ge, Xiaofan Li, Jennifer Weiszmann, Ping Wang, Helene Baribault, Jin-Long Chen, Hui Tian, Yang Li. Endocrinology 2008
Hongfei Ge, Xiaofan Li, Jennifer Weiszmann, Ping Wang, Helene Baribault, Jin-Long Chen, Hui Tian, Yang Li. Endocrinology 2008
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β-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1.
Arturo D Mancini, Gyslaine Bertrand, Kevin Vivot, Éric Carpentier, Caroline Tremblay, Julien Ghislain, Michel Bouvier, Vincent Poitout. J Biol Chem 2015
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Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus.
Elisabeth Defossa, Michael Wagner. Bioorg Med Chem Lett 2014
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Current status of GPR40/FFAR1 modulators in medicinal chemistry (2016-2019): a patent review.
Zheng Li, Zongtao Zhou, Luyong Zhang. Expert Opin Ther Pat 2020
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SCO-267, a GPR40 Full Agonist, Improves Glycemic and Body Weight Control in Rat Models of Diabetes and Obesity.
Hikaru Ueno, Ryo Ito, Shin-Ichi Abe, Mitsugi Ookawara, Hirohisa Miyashita, Hitomi Ogino, Yasufumi Miyamoto, Tomoki Yoshihara, Akihiro Kobayashi, Yoshiyuki Tsujihata,[...]. J Pharmacol Exp Ther 2019
Hikaru Ueno, Ryo Ito, Shin-Ichi Abe, Mitsugi Ookawara, Hirohisa Miyashita, Hitomi Ogino, Yasufumi Miyamoto, Tomoki Yoshihara, Akihiro Kobayashi, Yoshiyuki Tsujihata,[...]. J Pharmacol Exp Ther 2019
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Differential signaling by splice variants of the human free fatty acid receptor GPR120.
Sarah-Jane Watson, Alastair J H Brown, Nicholas D Holliday. Mol Pharmacol 2012
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The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism.
Brian D Hudson, Bharat Shimpukade, Amanda E Mackenzie, Adrian J Butcher, John D Pediani, Elisabeth Christiansen, Helen Heathcote, Andrew B Tobin, Trond Ulven, Graeme Milligan. Mol Pharmacol 2013
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GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans.
Virginia M Stone, Shalinee Dhayal, Katy J Brocklehurst, Carol Lenaghan, Maria Sörhede Winzell, Mårten Hammar, Xiufeng Xu, David M Smith, Noel G Morgan. Diabetologia 2014
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Free fatty acid (FFA) and hydroxy carboxylic acid (HCA) receptors.
Stefan Offermanns. Annu Rev Pharmacol Toxicol 2014
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Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases.
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A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1.
M Sawzdargo, S R George, T Nguyen, S Xu, L F Kolakowski, B F O'Dowd. Biochem Biophys Res Commun 1997
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High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.
Ankita Srivastava, Jason Yano, Yoshihiko Hirozane, Georgia Kefala, Franz Gruswitz, Gyorgy Snell, Weston Lane, Anthony Ivetac, Kathleen Aertgeerts, Jasmine Nguyen,[...]. Nature 2014
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Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders.
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The fatty acid receptor FFA1/GPR40 a decade later: how much do we know?
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Co-cited is the co-citation frequency, indicating how many articles cite the article together with the query article. Similarity is the co-citation as percentage of the times cited of the query article or the article in the search results, whichever is the lowest. These numbers are calculated for the last 100 citations when articles are cited more than 100 times.