FFA4 receptor (GPR120): A hot target for the development of anti-diabetic therapies

European Journal of Pharmacology

Volumn 763, Issue , 2015, Pages 160-168

  Liu, Hong Da ^a,b,c   Wang, Wen Bo ^a,c   Xu, Zhi Gang ^a   Liu, Chang Hong ^d   He, Dong Fang ^a,c   Du, Lv Pei ^a   Li, Min Yong ^a   Yu, Xiao ^b,c   Sun, Jin Peng ^a,c  

^a SHANDONG UNIVERSITY   (China)

^b SHANDONG UNIVERSITY   (China)

^c Shandong Provincial Pharmaceutical Co   (China)

^d THE FIRST AFFILIATED HOSPITAL OF SHANDONG FIRST MEDICAL UNIVERSITY   (China)

Author keywords

Arrestin; Biased signaling; Glucose metabolism; GPR120; Lipid

Indexed keywords

ANTIDIABETIC AGENT; ANTIINFLAMMATORY AGENT; BETA ARRESTIN; BETA ARRESTIN 2; COMPLEMENTARY DNA; CPDA; G PROTEIN COUPLED RECEPTOR 120; GSK 137647A; GW 9508; LIGAND; NCG 21; TUG 891; UNCLASSIFIED DRUG; G PROTEIN COUPLED RECEPTOR; RETINA S ANTIGEN;

ADIPOGENESIS; AMINO ACID SEQUENCE; AMINO TERMINAL SEQUENCE; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CALCIUM TRANSPORT; CARBOXY TERMINAL SEQUENCE; DIABETES MELLITUS; DRUG MECHANISM; DRUG STRUCTURE; DRUG TARGETING; FFA4 RECEPTOR GENE; GENE LOCATION; GLUCOSE METABOLISM; GLUCOSE TRANSPORT; HUMAN; INSULIN RELEASE; INTRACELLULAR SIGNALING; LIGAND BINDING; METABOLIC BALANCE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN PHOSPHORYLATION; PROTEIN PROCESSING; PROTEIN PROTEIN INTERACTION; RECEPTOR GENE; ANIMAL; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; GENETICS; METABOLISM; MOLECULAR GENETICS; MOLECULARLY TARGETED THERAPY; PROCEDURES; SIGNAL TRANSDUCTION;

AMINO ACID SEQUENCE; ANIMALS; ARRESTIN; DRUG DISCOVERY; HUMANS; HYPOGLYCEMIC AGENTS; MOLECULAR SEQUENCE DATA; MOLECULAR TARGETED THERAPY; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION;

EID: 84942373362     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2015.06.028     Document Type: Article

References (65)

1. B. Ahren Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes Nat. Rev. Drug Discov. 8 2009 369 385
2. D. Ancel, A. Bernard, S. Subramaniam, A. Hirasawa, G. Tsujimoto, T. Hashimoto, P. Passilly-Degrace, N.A. Khan, and P. Besnard The oral lipid sensor GPR120 is not indispensable for the orosensory detection of dietary lipids in mice J. Lipid Res. 56 2015 369 378
3. R.N. Burns, M. Singh, I.S. Senatorov, and N.H. Moniri Mechanisms of homologous and heterologous phosphorylation of FFA receptor 4 (GPR120): GRK6 and PKC mediate phosphorylation of Thr(3)(4)(7), Ser(3)(5)(0), and Ser(3)(5)(7) in the C-terminal tail Biochem. Pharmacol. 87 2014 650 659
4. A.J. Butcher, B.D. Hudson, B. Shimpukade, E. Alvarez-Curto, R. Prihandoko, T. Ulven, G. Milligan, and A.B. Tobin Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4 J. Biol. Chem. 289 2014 18451 18465
5. C. Cartoni, K. Yasumatsu, T. Ohkuri, N. Shigemura, R. Yoshida, N. Godinot, J. le Coutre, Y. Ninomiya, and S. Damak Taste preference for fatty acids is mediated by GPR40 and GPR120 J. Neurosci. 30 2010 8376 8382
6. C.Y. Chao, C.K. Lii, S.Y. Ye, C.C. Li, C.Y. Lu, A.H. Lin, K.L. Liu, and H.W. Chen Docosahexaenoic acid inhibits vascular endothelial growth factor (VEGF)-induced cell migration via the GPR120/PP2A/ERK1/2/eNOS signaling pathway in human umbilical vein endothelial cells J. Agric. Food Chem. 62 2014 4152 4158
7. L.M. Cornall, M.L. Mathai, D.H. Hryciw, and A.J. McAinch GPR120 agonism as a countermeasure against metabolic diseases Drug Discov. Today 19 2014 670 679
8. R. Fredriksson, P.J. Hoglund, D.E. Gloriam, M.C. Lagerstrom, and H.B. Schioth Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives FEBS Lett. 554 2003 381 388
9. B. Gao, Q. Huang, Q. Jie, H.Y. Zhang, L. Wang, Y.S. Guo, Z. Sun, B.Y. Wei, Y.H. Han, J. Liu, L. Yang, and Z.J. Luo Ginsenoside-Rb2 inhibits dexamethasone-induced apoptosis through promotion of GPR120 induction in bone marrow-derived mesenchymal stem cells Stem Cells Dev. 24 2015 781 790
10. Z. Gong, M. Yoshimura, S. Aizawa, R. Kurotani, J.M. Zigman, T. Sakai, and I. Sakata G protein-coupled receptor 120 signaling regulates ghrelin secretion in vivo and in vitro Am. J. Physiol. Endocrinol. Metab. 306 2014 E28 E35
11. C. Gotoh, Y.H. Hong, T. Iga, D. Hishikawa, Y. Suzuki, S.H. Song, K.C. Choi, T. Adachi, A. Hirasawa, G. Tsujimoto, S. Sasaki, and S.G. Roh The regulation of adipogenesis through GPR120 Biochem. Biophys. Res. Commun. 354 2007 591 597
12. T. Hara, A. Hirasawa, Q. Sun, K. Sadakane, C. Itsubo, T. Iga, T. Adachi, T.A. Koshimizu, T. Hashimoto, Y. Asakawa, and G. Tsujimoto Novel selective ligands for free fatty acid receptors GPR120 and GPR40 Naunyn Schmiedebergs Arch. Pharmacol. 380 2009 247 255
13. A.U. Hasan, K. Ohmori, K. Konishi, J. Igarashi, T. Hashimoto, K. Kamitori, F. Yamaguchi, I. Tsukamoto, T. Uyama, Y. Ishihara, T. Noma, M. Tokuda, and M. Kohno Eicosapentaenoic acid upregulates VEGF-A through both GPR120 and PPARgamma mediated pathways in 3T3-L1 adipocytes Mol. Cell. Endocrinol. 406 2015 10 18
14. B.C. Heng, D. Aubel, and M. Fussenegger An overview of the diverse roles of G-protein coupled receptors (GPCRs) in the pathophysiology of various human diseases Biotechnol. Adv. 31 2013 1676 1694
15. A. Hirasawa, T. Hara, A. Ichimura, and G. Tsujimoto Free fatty acid receptors and their physiological role in metabolic regulation Yakugaku Zasshi 131 2011 1683 1689
16. A. Hirasawa, K. Tsumaya, T. Awaji, S. Katsuma, T. Adachi, M. Yamada, Y. Sugimoto, S. Miyazaki, and G. Tsujimoto Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120 Nat. Med. 11 2005 90 94
17. F.B. Hu Globalization of diabetes: the role of diet, lifestyle, and genes Diabetes Care 34 2011 1249 1257
18. B.D. Hudson, B. Shimpukade, A.E. Mackenzie, A.J. Butcher, J.D. Pediani, E. Christiansen, H. Heathcote, A.B. Tobin, T. Ulven, and G. Milligan 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 Mol. Pharmacol. 84 2013 710 725
19. B.D. Hudson, B. Shimpukade, G. Milligan, and T. Ulven The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120) J. Biol. Chem. 289 2014 20345 20358
20. A. Ichimura, A. Hirasawa, T. Hara, and G. Tsujimoto Free fatty acid receptors act as nutrient sensors to regulate energy homeostasis Prostagland. Other Lipid Mediat. 89 2009 82 88
21. A. Ichimura, A. Hirasawa, O. Poulain-Godefroy, A. Bonnefond, T. Hara, L. Yengo, I. Kimura, A. Leloire, N. Liu, K. Iida, H. Choquet, P. Besnard, C. Lecoeur, S. Vivequin, K. Ayukawa, M. Takeuchi, K. Ozawa, M. Tauber, C. Maffeis, A. Morandi, R. Buzzetti, P. Elliott, A. Pouta, M.R. Jarvelin, A. Korner, W. Kiess, M. Pigeyre, R. Caiazzo, W. Van Hul, L. Van Gaal, F. Horber, B. Balkau, C. Levy-Marchal, K. Rouskas, A. Kouvatsi, J. Hebebrand, A. Hinney, A. Scherag, F. Pattou, D. Meyre, T.A. Koshimizu, I. Wolowczuk, G. Tsujimoto, and P. Froguel Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human Nature 483 2012 350 354
22. S. Ishii, M. Hirane, Y. Kitamura, S. Mori, N. Fukushima, K. Honoki, and T. Tsujiuchi Role of GPR120 in cell motile activity induced by 12-O-tetradecanoylphorbol-13-acetate in liver epithelial WB-F344 cells Mol. Cell. Biochem. 400 2015 145 151
23. S. Janssen, J. Laermans, H. Iwakura, J. Tack, and I. Depoortere Sensing of fatty acids for octanoylation of ghrelin involves a gustatory G-protein PloS One 7 2012 e40168
24. S. Katsuma, N. Hatae, T. Yano, Y. Ruike, M. Kimura, A. Hirasawa, and G. Tsujimoto Free fatty acids inhibit serum deprivation-induced apoptosis through GPR120 in a murine enteroendocrine cell line STC-1 J. Biol. Chem. 280 2005 19507 19515
25. N. Koren, S. Simsa-Maziel, R. Shahar, B. Schwartz, and E. Monsonego-Ornan Exposure to omega-3 fatty acids at early age accelerate bone growth and improve bone quality J. Nutr. Biochem. 25 2014 623 633
26. Y. Li, H. Zhang, C. Jiang, M. Xu, Y. Pang, J. Feng, X. Xiang, W. Kong, G. Xu, Y. Li, and X. Wang Hyperhomocysteinemia promotes insulin resistance by inducing endoplasmic reticulum stress in adipose tissue J. Biol. Chem. 288 2013 9583 9592
27. T. Lieu, G. Jayaweera, and N.W. Bunnett GPBA: a GPCR for bile acids and an emerging therapeutic target for disorders of digestion and sensation Br. J. Pharmacol. 171 2014 1156 1166
28. D. Liu, L. Wang, Q. Meng, H. Kuang, and X. Liu G-protein coupled receptor 120 is involved in glucose metabolism in fat cells Cell. Mol. Biol. (Noisy-le-grand) Suppl. 58 2012 OL1757 OL1762
29. Y. Liu, L.Y. Chen, M. Sokolowska, M. Eberlein, S. Alsaaty, A. Martinez-Anton, C. Logun, H.Y. Qi, and J.H. Shelhamer The fish oil ingredient, docosahexaenoic acid, activates cytosolic phospholipase A(2) via GPR120 receptor to produce prostaglandin E(2) and plays an anti-inflammatory role in macrophages Immunology 143 2014 81 95
30. X. Lu, X. Zhao, J. Feng, A.P. Liou, S. Anthony, S. Pechhold, Y. Sun, H. Lu, and S. Wank Postprandial inhibition of gastric ghrelin secretion by long-chain fatty acid through GPR120 in isolated gastric ghrelin cells and mice Am. J. Physiol. Gastrointest. Liver Physiol. 303 2012 G367 G376
31. S. Miyauchi, A. Hirasawa, T. Iga, N. Liu, C. Itsubo, K. Sadakane, T. Hara, and G. Tsujimoto Distribution and regulation of protein expression of the free fatty acid receptor GPR120 Naunyn Schmiedebergs Arch. Pharmacol. 379 2009 427 434
32. K. Moore, Q. Zhang, N. Murgolo, T. Hosted, and R. Duffy Cloning, expression, and pharmacological characterization of the GPR120 free fatty acid receptor from cynomolgus monkey: comparison with human GPR120 splice variants Comp. Biochem. Physiol. B: Biochem. Mol. Biol. 154 2009 419 426
33. Y. Oh da, E. Walenta, T.E. Akiyama, W.S. Lagakos, D. Lackey, A.R. Pessentheiner, R. Sasik, N. Hah, T.J. Chi, J.M. Cox, M.A. Powels, J. Di Salvo, C. Sinz, S.M. Watkins, A.M. Armando, H. Chung, R.M. Evans, O. Quehenberger, J. McNelis, J.G. Bogner-Strauss, and J.M. Olefsky A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice Nat. Med. 20 2014 942 947
34. D.Y. Oh, S. Talukdar, E.J. Bae, T. Imamura, H. Morinaga, W. Fan, P. Li, W.J. Lu, S.M. Watkins, and J.M. Olefsky GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects Cell 142 2010 687 698
35. H.E. Parker, A.M. Habib, G.J. Rogers, F.M. Gribble, and F. Reimann Nutrient-dependent secretion of glucose-dependent insulinotropic polypeptide from primary murine K cells Diabetologia 52 2009 289 298
36. S.J. Paulsen, L.K. Larsen, G. Hansen, S. Chelur, P.J. Larsen, and N. Vrang Expression of the fatty acid receptor GPR120 in the gut of diet-induced-obese rats and its role in GLP-1 secretion PLoS One 9 2014 e88227
37. D.A. Raptis, P. Limani, J.H. Jang, U. Ungethum, C. Tschuor, R. Graf, B. Humar, and P.A. Clavien GPR120 on Kupffer cells mediates hepatoprotective effects of omega3-fatty acids J. Hepatol. 60 2014 625 632
38. A. Rohwedder, Q. Zhang, S.A. Rudge, and M.J. Wakelam Lipid droplet formation in response to oleic acid in Huh-7 cells is mediated by the fatty acid receptor FFAR4 J. Cell Sci. 127 2014 3104 3115
39. O.B. Sanchez-Reyes, M.T. Romero-Avila, J.A. Castillo-Badillo, Y. Takei, A. Hirasawa, G. Tsujimoto, R. Villalobos-Molina, and J.A. Garcia-Sainz Free fatty acids and protein kinase C activation induce GPR120 (free fatty acid receptor 4) phosphorylation Eur. J. Pharmacol. 723 2014 368 374
40. A. Sclafani, S. Zukerman, and K. Ackroff GPR40 and GPR120 fatty acid sensors are critical for postoral but not oral mediation of fat preferences in the mouse Am. J. Physiol. Regul. Integr. Comp. Physiol. 305 2013 R1490 R1497
41. B.P. Shah, P. Liu, T. Yu, D.R. Hansen, and T.A. Gilbertson TRPM5 is critical for linoleic acid-induced CCK secretion from the enteroendocrine cell line, STC-1 Am. J. Physiol. Cell Physiol. 302 2012 C210 C219
42. S.K. Shenoy, and R.J. Lefkowitz beta-Arrestin-mediated receptor trafficking and signal transduction Trends Pharmacol. Sci. 32 2011 521 533
43. B. Shimpukade, B.D. Hudson, C.K. Hovgaard, G. Milligan, and T. Ulven Discovery of a potent and selective GPR120 agonist J. Med. Chem. 55 2012 4511 4515
44. A.K. Shukla, G.H. Westfield, K. Xiao, R.I. Reis, L.Y. Huang, P. Tripathi-Shukla, J. Qian, S. Li, A. Blanc, A.N. Oleskie, A.M. Dosey, M. Su, C.R. Liang, L.L. Gu, J.M. Shan, X. Chen, R. Hanna, M. Choi, X.J. Yao, B.U. Klink, A.W. Kahsai, S.S. Sidhu, S. Koide, P.A. Penczek, A.A. Kossiakoff, V.L. Woods Jr., B.K. Kobilka, G. Skiniotis, and R.J. Lefkowitz Visualization of arrestin recruitment by a G-protein-coupled receptor Nature 512 2014 218 222
45. A. Soto-Guzman, N. Navarro-Tito, L. Castro-Sanchez, R. Martinez-Orozco, and E.P. Salazar Oleic acid promotes MMP-9 secretion and invasion in breast cancer cells Clin. Exp. Metastasis 27 2010 505 515
46. A. Soto-Guzman, T. Robledo, M. Lopez-Perez, and E.P. Salazar Oleic acid induces ERK1/2 activation and AP-1 DNA binding activity through a mechanism involving Src kinase and EGFR transactivation in breast cancer cells Mol. Cell. Endocrinol. 294 2008 81 91
47. S.M. Sparks, G. Chen, J.L. Collins, D. Danger, S.T. Dock, C. Jayawickreme, S. Jenkinson, C. Laudeman, M.A. Leesnitzer, X. Liang, P. Maloney, D.C. McCoy, D. Moncol, V. Rash, T. Rimele, P. Vulimiri, J.M. Way, and S. Ross Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120) Bioorg. Med. Chem. Lett. 24 2014 3100 3103
48. V.M. Stone, S. Dhayal, K.J. Brocklehurst, C. Lenaghan, M. Sorhede Winzell, M. Hammar, X. Xu, D.M. Smith, and N.G. Morgan GPR120 (FFAR4) is preferentially expressed in pancreatic delta cells and regulates somatostatin secretion from murine islets of Langerhans Diabetologia 57 2014 1182 1191
49. R.T. Strachan, J.P. Sun, D.H. Rominger, J.D. Violin, S. Ahn, A. Rojas Bie Thomsen, X. Zhu, A. Kleist, T. Costa, and R.J. Lefkowitz Divergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR) J. Biol. Chem. 289 2014 14211 14224
50. Q. Sun, A. Hirasawa, T. Hara, I. Kimura, T. Adachi, T. Awaji, M. Ishiguro, T. Suzuki, N. Miyata, and G. Tsujimoto Structure-activity relationships of GPR120 agonists based on a docking simulation Mol. Pharmacol. 78 2010 804 810
51. T. Suzuki, S. Igari, A. Hirasawa, M. Hata, M. Ishiguro, H. Fujieda, Y. Itoh, T. Hirano, H. Nakagawa, M. Ogura, M. Makishima, G. Tsujimoto, and N. Miyata Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists J. Med. Chem. 51 2008 7640 7644
52. T. Tanaka, S. Katsuma, T. Adachi, T.A. Koshimizu, A. Hirasawa, and G. Tsujimoto Free fatty acids induce cholecystokinin secretion through GPR120 Naunyn-Schmiedeberg's Arch. Pharmacol. 377 2008 523 527
53. T. Tanaka, T. Yano, T. Adachi, T.A. Koshimizu, A. Hirasawa, and G. Tsujimoto Cloning and characterization of the rat free fatty acid receptor GPR120: in vivo effect of the natural ligand on GLP-1 secretion and proliferation of pancreatic beta cells Naunyn Schmiedebergs Arch. Pharmacol. 377 2008 515 522
54. A. Tiwari GPR43: an emerging target for the potential treatment of type 2 diabetes, obesity and insulin resistance Curr. Opin. Investig. Drugs 11 2010 385 393
55. T. Tsukahara, K. Watanabe, T. Watanabe, H. Yamagami, M. Sogawa, T. Tanigawa, M. Shiba, K. Tominaga, Y. Fujiwara, K. Maeda, K. Hirakawa, and T. Arakawa Tumor necrosis factor alpha decreases glucagon-like peptide-2 expression by up-regulating G-protein-coupled receptor 120 in Crohn disease Am. J. Pathol. 185 2015 185 196
56. S. Ussar, and M.H. Tschop [Br]eaking FAt Cell 159 2014 238 240
57. H.M. Wang, J.H. Dong, Q. Li, Q. Hu, S.L. Ning, W. Zheng, M. Cui, T.S. Chen, X. Xie, J.P. Sun, and X. Yu A stress response pathway in mice upregulates somatostatin level and transcription in pancreatic delta cells through Gs and beta-arrestin 1 Diabetologia 57 2014 1899 1910
58. S.J. Watson, A.J. Brown, and N.D. Holliday Differential signaling by splice variants of the human free fatty acid receptor GPR120 Mol. Pharmacol. 81 2012 631 642
59. P. Wellendorph, L.D. Johansen, and H. Brauner-Osborne Molecular pharmacology of promiscuous seven transmembrane receptors sensing organic nutrients Mol. Pharmacol. 76 2009 453 465
60. L. Wellhauser, and D.D. Belsham Activation of the omega-3 fatty acid receptor GPR120 mediates anti-inflammatory actions in immortalized hypothalamic neurons J. Neuroinflammation 11 2014 60
61. E.J. Whalen, S. Rajagopal, and R.J. Lefkowitz Therapeutic potential of beta-arrestin- and G protein-biased agonists Trends Mol. Med. 17 2011 126 139
62. Q. Wu, H. Wang, X. Zhao, Y. Shi, M. Jin, B. Wan, H. Xu, Y. Cheng, H. Ge, and Y. Zhang Identification of G-protein-coupled receptor 120 as a tumor-promoting receptor that induces angiogenesis and migration in human colorectal carcinoma Oncogene 32 2013 5541 5550
63. Y. Yan, W. Jiang, T. Spinetti, A. Tardivel, R. Castillo, C. Bourquin, G. Guarda, Z. Tian, J. Tschopp, and R. Zhou Omega-3 fatty acids prevent inflammation and metabolic disorder through inhibition of NLRP3 inflammasome activation Immunity 38 2013 1154 1163
64. M.M. Yore, I. Syed, P.M. Moraes-Vieira, T. Zhang, M.A. Herman, E.A. Homan, R.T. Patel, J. Lee, S. Chen, O.D. Peroni, A.S. Dhaneshwar, A. Hammarstedt, U. Smith, T.E. McGraw, A. Saghatelian, and B.B. Kahn Discovery of a class of endogenous mammalian lipids with anti-diabetic and anti-inflammatory effects Cell 159 2014 318 332
65. D. Zhang, and P.S. Leung Potential roles of GPR120 and its agonists in the management of diabetes Drug Des. Dev. Ther. 8 2014 1013 1027