Free fatty acid receptor 1

Free fatty acid receptor 1 (FFAR1), also known as G protein-coupled receptor 40 (GPR40), is a protein that in humans is encoded by the FFAR1 gene. It is a member of the G protein-coupled receptor family and plays a significant role in the regulation of glucose homeostasis and insulin secretion.

Function

FFAR1 is a receptor for medium and long chain free fatty acids (FFAs). It is mainly expressed in pancreatic beta cells and to a lesser extent in the brain, where it mediates the potentiation of glucose-stimulated insulin secretion. FFAR1 is involved in the taste perception of fatty acids, and it also mediates the taste of fat.

Clinical significance

FFAR1 has been identified as a potential therapeutic target for the treatment of type 2 diabetes. Activation of FFAR1 by FFAs enhances insulin secretion from pancreatic beta cells only in the presence of elevated glucose levels. This glucose-dependent insulinotropic effect has led to the development of synthetic FFAR1 agonists for the treatment of type 2 diabetes.

Pharmacology

Several synthetic FFAR1 agonists have been developed for the treatment of type 2 diabetes. These include TAK-875 (Fasiglifam), a selective FFAR1 agonist that has been shown in clinical trials to improve glycemic control in patients with type 2 diabetes.

See also

• Free fatty acid receptor
• G protein-coupled receptor
• Type 2 diabetes
• Insulin
• Glucose

References

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