| First Author | Kogure R | Year | 2011 |
| Journal | Biochem Biophys Res Commun | Volume | 416 |
| Issue | 1-2 | Pages | 58-63 |
| PubMed ID | 22079287 | Mgi Jnum | J:179210 |
| Mgi Id | MGI:5301464 | Doi | 10.1016/j.bbrc.2011.10.141 |
| Citation | Kogure R, et al. (2011) 5-Hydroxy-eicosapentaenoic acid is an endogenous GPR119 agonist and enhances glucose-dependent insulin secretion. Biochem Biophys Res Commun 416(1-2):58-63 |
| abstractText | GPR119 is one of the G-protein-coupled receptors expressed in pancreatic beta-cells and intestinal endocrine cells. Since agonists to GPR119 stimulate glucose-dependent insulin secretion, GPR119 agonists are anticipated to promote anti-diabetic effects and control of glucose homeostasis. Here, we reported that an omega-3 unsaturated fatty acid metabolite, 5-hydroxy-eicosapentaenoic acid (5-HEPE), was a potent agonist for GPR119 and enhanced glucose-dependent insulin secretion. 5-HEPE stimulated cAMP accumulation in mouse MIN6 insulinoma cells and human HuTu80 intestinal adenocarcinoma cells. These effects were blunted by GPR119-specific siRNA. Recombinant GPR119 also responded to 5-HEPE as well as authentic agonists. Several previous reports have indicated the beneficial biological effects of omega-3 unsaturated fatty acids, and epidemiological studies have suggested that these fatty acids plays a protective role against diabetes. However, the molecular pharmacology and receptor identifications of omega-3 unsaturated fatty acids and their metabolites have not yet been well investigated. It is hoped that our findings will encourage novel investigations into the molecular relationships between omega-3 fatty acids and diabetes. |
