Potentiation of Glucose-stimulated Insulin Secretion by the GPR40-PLC-TRPC Pathway in Pancreatic β-Cells

Scientific Reports

Volumn 6, Issue , 2016, Pages

  Yamada, Hodaka ^a   Yoshida, Masashi ^a   Ito, Kiyonori ^a   Dezaki, Katsuya ^a   Yada, Toshihiko ^a   Ishikawa, San E ^a   Kakei, Masafumi ^a  

^a JICHI MEDICAL UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

BENZOFURAN DERIVATIVE; G PROTEIN COUPLED RECEPTOR; G-PROTEIN-COUPLED RECEPTOR 40, RAT; GLUCOSE; INSULIN; PHOSPHOLIPASE C; SULFONE; TAK-875; TOLBUTAMIDE; TRANSIENT RECEPTOR POTENTIAL CHANNEL C;

ANIMAL; DRUG EFFECTS; DRUG POTENTIATION; MALE; METABOLISM; PANCREAS ISLET BETA CELL; RAT; SECRETION (PROCESS); SIGNAL TRANSDUCTION;

ANIMALS; BENZOFURANS; DRUG SYNERGISM; GLUCOSE; INSULIN; INSULIN-SECRETING CELLS; MALE; RATS; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION; SULFONES; TOLBUTAMIDE; TRPC CATION CHANNELS; TYPE C PHOSPHOLIPASES;

EID: 84968876611     PISSN: None     EISSN: 20452322     Source Type: Journal    
DOI: 10.1038/srep25912     Document Type: Article

References (34)

1. Ahren, B. Islet G protein-coupled receptors as potential targets for treatment of type 2 diabetes. Nat Rev Drug Discov 8, 369-385 (2009).
2. Tomita, T. et al. Expression of the gene for a membrane-bound fatty acid receptor in the pancreas and islet cell tumours in humans: evidence for GPR40 expression in pancreatic beta cells and implications for insulin secretion. Diabetologia 49, 962-968 (2006).
3. Itoh, Y. et al. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 422, 173-176 (2003).
4. Araki, T., Hirayama, M., Hiroi, S. & Kaku, K. GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Diabetes Obes Metab 14, 271-278 (2012).
5. Kaku, K., Araki, T. & Yoshinaka, R. Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes. Diabetes Care 36, 245-250 (2013).
6. Burant, C. F. et al. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet 379, 1403-1411 (2012).
7. Nolan, C. J., Madiraju, M. S., Delghingaro-Augusto, V., Peyot, M. L. & Prentki, M. Fatty acid signaling in the beta-cell and insulin secretion. Diabetes 55 Suppl 2, S16-23 (2006).
8. Briscoe, C. P. et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 278, 11303-11311 (2003).
9. 2+ channel and link to insulin release. Am J Physiol Endocrinol Metab 289, E670-677 (2005).
10. Latour, M. G. et al. GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo. Diabetes 56, 1087-1094 (2007).
11. Leech, C. A. et al. Molecular physiology of glucagon-like peptide-1 insulin secretagogue action in pancreatic beta cells. Progress in biophysics and molecular biology 107, 236-247 (2011).
12. Ferdaoussi, M. et al. G protein-coupled receptor (GPR)40-dependent potentiation of insulin secretion in mouse islets is mediated by protein kinase D1. Diabetologia 55, 2682-2692 (2012).
13. Drucker, D. J. The biology of incretin hormones. Cell Metab 3, 153-165 (2006).
14. Yosida, M. et al. Involvement of cAMP/EPAC/TRPM2 activation in glucose- and incretin-induced insulin secretion. Diabetes 63, 3394-3403 (2014).
15. Togashi, K. et al. TRPM2 activation by cyclic ADP-ribose at body temperature is involved in insulin secretion. The EMBO journal 25, 1804-1815 (2006).
16. Uchida, K. et al. Lack of TRPM2 impaired insulin secretion and glucose metabolisms in mice. Diabetes 60, 119-126 (2011).
17. Negoro, N. et al. Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent. J Med Chem 55, 3960-3974 (2012).
18. 2+-sensitive nonselective cation channels in regulating the membrane potential of pancreatic beta-cells. Diabetes 47, 1066-1073 (1998).
19. Shapiro, H., Shachar, S., Sekler, I., Hershfinkel, M. & Walker, M. D. Role of GPR40 in fatty acid action on the beta cell line INS-1E. Biochem Biophys Res Commun 335, 97-104 (2005).
20. Uchida, K. & Tominaga, M. The role of TRPM2 in pancreatic beta-cells and the development of diabetes. Cell Calcium 56, 332-339 (2014).
21. Liu, D., Zhu, Z. & Tepel, M. The role of transient receptor potential channels in metabolic syndrome. Hypertens Res 31, 1989-1995 (2008).
22. Putney, J. W. Capacitative calcium entry: from concept to molecules. Immunol Rev 231, 10-22 (2009).
23. 2+ entry by inositol lipids in mammalian cells by multiple mechanisms. Cell Calcium 45, 527-534 (2009).
24. + currents in primary cultured rat pancreatic beta-cells by linoleic acids. Endocrinology 147, 674-682 (2006).
25. Song, W. J., Mondal, P., Li, Y., Lee, S. E. & Hussain, M. A. Pancreatic beta-cell response to increased metabolic demand and to pharmacologic secretagogues requires EPAC2A. Diabetes 62, 2796-2807 (2013).
26. Welters, H. J. et al. Differential protective effects of palmitoleic acid and cAMP on caspase activation and cell viability in pancreatic beta-cells exposed to palmitate. Apoptosis : an international journal on programmed cell death 11, 1231-1238 (2006).
27. Yang, M., Chisholm, J. W., Soelaiman, S. & Shryock, J. C. Sulfonylureas uncouple glucose-dependence for GPR40-mediated enhancement of insulin secretion from INS-1E cells. Mol Cell Endocrinol 315, 308-313 (2010).
28. + channels via membrane phospholipid metabolism. Curr Med Chem 10, 235-243 (2003).
29. Mancini, A. D. & Poitout, V. The fatty acid receptor FFA1/GPR40 a decade later: how much do we know? Trends Endocrinol Metab 24, 398-407 (2013).
30. Schmitz-Peiffer, C. & Biden, T. J. Protein kinase C function in muscle, liver, and beta-cells and its therapeutic implications for type 2 diabetes. Diabetes 57, 1774-1783 (2008).
31. Shigeto, M. et al. GLP-1 stimulates insulin secretion by PKC-dependent TRPM4 and TRPM5 activation. J Clin Invest 125, 4714-4728 (2015).
32. + channels in free radical-mediated inhibition of insulin secretion in rat pancreatic beta-cells. Diabetes 44, 878-883 (1995).
33. Dezaki, K. et al. Ghrelin attenuates cAMP-PKA signaling to evoke insulinostatic cascade in islet beta-cells. Diabetes 60, 2315-2324 (2011).
34. Damdindorj, B. et al. Exogenous and endogenous ghrelin counteracts GLP-1 action to stimulate cAMP signaling and insulin secretion in islet beta-cells. FEBS Lett 586, 2555-2562 (2012).