The G protein-coupled receptor, GPR40, is a specific receptor for free fatty acids. Singnaling pathways are activated in islet β-cells by fatty acids as binding to GPR40. Fatty acids regulate insulin secretion and cause β-cell hyperplasia through GPR40. GPR40 also mediates responses to antidiabetic drugs like thiazolidinediones. GPR40 agonists and/or antagonists show potential effect in the development of new anti-diabetic drugs.